Title of Invention	NOVEL AMINO SUBSTITUTED PYRIMIDINONE DERIVATIVES
Abstract	The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polyrnorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I). X The present invention also provides a process for the preparation of the above said novel amino substituted pyrimidinone derivatives of the formula (I) pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polyrnorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel amino substituted pyrimidinone derivatives of the present invention are useful for the treatment of inflammation and immunological diseases. Particularly the compounds of the present invention are useful for the .1 treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-I, IL-6, IL-I~, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteophorosis; multiple myeloma; uveititis;

Title of Invention

NOVEL AMINO SUBSTITUTED PYRIMIDINONE DERIVATIVES

Abstract

The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polyrnorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I). X The present invention also provides a process for the preparation of the above said novel amino substituted pyrimidinone derivatives of the formula (I) pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polyrnorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel amino substituted pyrimidinone derivatives of the present invention are useful for the treatment of inflammation and immunological diseases. Particularly the compounds of the present invention are useful for the .1 treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-I, IL-6, IL-I~, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteophorosis; multiple myeloma; uveititis;

Full Text	Field of the Invention The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I). The present invention also provides a process for the preparation of the above said novel amino substituted pyrimidinone derivatives of the formula (I) pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel amino substituted pyrimidinone derivatives of the present invention are useful for the treatment of inflammation and immunological diseases. Particularly the compounds of the present invention are useful for the treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-ip, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteophorosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic p cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes; bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection; and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster vimses. Background of Invention It has been reported that Cyclooxygenase enzyme exists in three isoforms, namely, COX-1, COX-2 and COX-3. COX-1 enzyme is essential and primarily responsible for the regulation of gastric fluids whereas COX-2 enzyme is present at the basal levels and is reported to have a major role in the prostaglandin synthesis for inflammatory response. These prostaglandins are known to cause inflammation in the body. Hence, if the synthesis of these prostaglandins is stopped by way of inhibiting COX-2 enzyme, inflammation and its related disorders can be treated. COX-3 possesses glycosylation-dependent cyclooxygenase activity. Comparison of canine COX-3 activity with murine COX-1 and COX-2 demonstrated that this enzyme is selectively inhibited by analgesic/antipyretic drugs such as acetaminophen, phenacetin, antipyrine, and dipyrone, and is potently inhibited by some nonsteroidal antiinflammatory drugs. Thus, inhibition of COX-3 could represent a primary central mechanism by which these drugs decrease pain and possibly fever. Recent reports show that inhibitors of COX-1 enzyme causes gastric ulcers, where as selective COX-2 and COX-3 enzyme inhibitors are devoid of this function and hence are found to be safe. The present invention is concerned with treatment of immunological diseases or inflammation, notably such diseases are mediated by cytokines or cyclooxygenase. The principal elements of the immune system are macrophages or antigen-presenting cells, T cells and B cells. The role of other immune cells such as NK cells, basophils, mast cells and dendritic cells are known, but their role in primary immunologic disorders is uncertain. Macrophages are important mediators of both inflammation and providing the necessary "help" for T cell stimulation and proUferation. Most importantly macrophages make IL-1, IL-12 and TNF-a all of which are potent pro-inflammatory molecules and also provide help for T cells. In addition, activation of macrophages results in the induction of enzymes, such as cyclooxygenase-2 (COX-2) and cyclooxygenase-3 (COX-3), inducible nitric oxide synthase (iNOS) and production of free radicals capable of damaging normal cells. Many factors activate macrophages, including bacterial products, superantigens and interferon gamma (IFN y). It is believed that phosphotyrosine kinases (PTKs) and other undefined cellular kinases are involved in the activation process. Cytokines are molecules secreted by immune cells that are important in mediating immune responses. Cytokine production may lead to the secretion of other cytokines, altered cellular function, cell division or differentiation. Inflammation is the body's normal response to injury or infection. However, in inflammatory diseases such as rheumatoid arthritis, pathologic inflammatory processes can lead to morbidity and mortality. The cytokine tumor necrosis factor-alpha (TNF-a) plays a central role in the inflammatory response and has been targeted as a point of intervention in inflammatory disease. TNF-a is a polypeptide hormone released by activated macrophages and other cells. At low concentrations, TNF-a participates in the protective inflammatory response by activating leukocytes and promoting their migration to extravascular sites of inflammation (Moser et al, J Clin Invest, 83, 444-55,1989). At higher concentrations, TNF-a can act as a potent hydrogen and induce the production of other pro-inflammatory cytokines (Haworth et al., Eur J Immunol, 21, 2575-79, 1991; Brennan et a/.. Lancet, 2, 244-7, 1989). TNF-a also stimulates the synthesis of acute-phase proteins. In rheumatoid arthritis, a chronic and progressive inflammatory disease affecting about 1 % of the adult U.S. population, TNF-a mediates the cytokine cascade that leads to joint damage and destmction (Arend et al., Arthritis Rheum, 38, 151-60,1995), Inhibitors of TNF-a, including soluble TNF receptors (etanercept) (Goldenberg, Clin Ther, 21, 75-87, 1999) and anti-TNF-a antibody (infliximab) (Luong et aL, Ann Pharmacother, 34, 743-60, 2000), have recently been approved by the U.S. Food and Drug Administration (FDA) as agents for the treatment of rheumatoid arthritis. Elevated levels of TNF-a have also been implicated in many other disorders and disease conditions, including cachexia, septic shock syndrome, osteoarthritis, inflammatory bowel disease such as Crohn's disease and ulcerative colitis etc. Elevated levels of TNF-a and/or IL-1 over basal levels have been implicated in mediating or exacerbating a number of disease states including rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; pancreatic (5 cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes; bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection. HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses (including HSV-1, HSV-2), and herpes zoster are also exacerbated by TNF-a. It can be seen that inhibitors of TNF-a are potentially useful in the treatment of a wide variety of diseases. Compounds that inhibit TNF-a have been described in several patents. Excessive production of IL-6 is implicated in several disease states, it is highly desirable to develop compounds that inhibit IL-6 secretion. Compounds that inhibit IL-6 have been described in U.S. Pat. Nos. 6,004,813; 5,527,546 and 5,166,137. The cytokine IL-lp also participates in the inflammatory response. It stimulates thymocyte proliferation, fibroblast growth factor activity, and the release of prostaglandin from synovial cells. Elevated or unregulated levels of the cytokine IL-ip have been associated with a number of inflammatory diseases and other disease states, including but not limited to adult respiratory distress syndrome, allergy, Alzheimer's disease etc. Since overproduction of IL-lp is associated with numerous disease conditions, it is desirable to develop compounds that inhibit the production or activity of IL-ip. In rheumatoid arthritis models in animals, multiple intra-articular injections of IL-1 have led to an acute and destructive form of arthritis (Chandrasekhar et al.. Clinical Immunol Immunopathol. 55, 382, 1990). In studies using cultured rheumatoid synovial cells, IL-1 is a more potent inducer of stromelysin than TNF-a. (Firestein, Am. J. Pathol. 140, 1309, 1992). At sites of local injection, neutrophil, lymphocyte, and monocyte emigration has been observed. The emigration is attributed to the induction of chemokines (e.g., IL-8), and the up-regulation of adhesion molecules (Dinarello, Eur. Cytokine Netw. 5, 517-531, 1994). In rheumatoid arthritis, both IL-1 and TNF-a induce synoviocytes and chondrocytes to produce coUagenase and neutral proteases, which leads to tissue destruction within the arthritic joints. In a model of arthritis (collagen-induced arthritis (CIA) in rats and mice) intra-articular administration of TNF-a either prior to or after the induction of CIA led to an accelerated onset of arthritis and a more severe course of the disease (Brahn et al., Lymphokine Cytokine Res. 11, 253, 1992; and Cooper, Clin. Exp. Immunol. 898, 244, 1992). IL-8 has been implicated in exacerbating and/or causing many disease states in which massive neutrophil in filtration into sites of inlammation or injury (e.g., ischemia) is mediated chemotactic nature of IL-8, including, but not limited to, the following: asthma, inflammatory bowl disease, psoriasis, adult respiratory distress syndrome, cardiac and renal reperfusion injury, thrombosis and glomerulonephritis. In addition to the chemotaxis effect on neutrophils, IL-8 has also has ability to activate neutrophils. Thus, reduction in IL-8 levels may lead to diminished neutrophil infiltration. Few prior art reference which disclose the closest pyrimidine compounds are given here: i) US patent Nos. 6,420,385 and 6,410,729 disclose novel compounds of formula (Ila) X is O, S or NR”; R” represents -Y or -Z--Y, and R"“ represents -Z-Y; provided that R"“ is other than a substituted-aryl, (substituted-aryl)methyl or (substituted-aryl)ethyl radical; wherein each Z is independently optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, aryl or heteroaryl; Y is independently a hydrogen; halo, cyano, nitro, etc., R” is independently a hydrogen, optionally substituted alkyl, alkenyl, alkynyl etc., R”“ and R”“ are each independently represent optionally substituted aryl or heteroaryl. An example of these compounds is shown in formula (lib) R is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaromatic group (e.g. a heteroaromatic ring structure having four to five carbon atoms and one heteroatom selected from the group consisting of nitrogen, sulfur and oxygen); R is an alkyl, haloalkyl, polyhaloalkyl, haloalkenyl, polyhaloalkenyl, alkenyl, alkynyl, haloalkynyl, polyhaloalkynyl, alkenynyl, alkoxyalkyl, dialkoxyalkyl, haloalkoxyalkyl, oxoalkyl, trimethylsilylalkynyl, cyanoalkyl or aryl group; R” is a hydrogen, halo, acyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxyalkyl, alkoxyimino, alkoxycarbonylalkyl, dialkoxyalkyl, formyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, hydroxyalkyl, hydroxyimino, polyhaloalkyl, polyhaloalkenyl, polyhaloalkynyl, polyhaloalkoxy, trimethylsilylalkynyl, alkoxyalkoxy, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, cyanoalkyl, hydroxy or cyano group; and R” is a hydrogen, halo, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkylthio, polyhaloalkyl, polyhaloalkenyl, polyhaloalkynyl, polyhaloalkoxy, polyhaloalkylthio, cycloalkyl, aryl, aryloxy, heterocyclyl, aralkyl, alkylamino, dialkylamino, dialkylaminocarbonyl, or cyano group; and X is oxygen or sulfiir. An example of these compounds is shown in formula (Ilf) Objective of the Invention We have focused our research to identify selective COX-2 and COX-3 inhibitors which are devoid of any side effects, normally associated with antiinflammatory agents. Our sustained efforts have resulted in novel substituted pyrimidinone derivatives. The derivatives may be useful in the treatment of inflammation and immunological diseases. Particularly the compound of the present invention are useful for the treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-lp, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic p cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes; bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection; and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses. Summary of the Invention The present invention relates to novel amino substituted pyrimidinone derivatives of the formula (I) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; Y represents a bond or NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent ft fi n n hydrogen, SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2, Yet another embodiment of the present invention there is provided a novel pyrimidone derivatives of the formula (II) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R represents SR , or S(0)pR ; R represents hydrogen, SR , or R 7 S S(0)pR , wherein R represents alkyl or aryl; R represents alkyl, amino or aryl T A group; and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylslfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, aryl, aralkyl, haloalkyl, acyl, alkoxy, aryloxy, aralkoxy, heteroaryl, heterocyclyl, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2. Yet another embodiment of the present invention there is provided a novel pyrimidinedione derivatives of the formula (III) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, SR”, wherein R” represents alkyl or aryl; S(0)pR”, wherein R” represents alkyl, O A amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR , wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2. Yet another embodiment of the present invention there is provided a novel diaryl pyrimidinedione derivatives of the formula (IV) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R' and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl, sulfamoyl; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl. haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, haloalkyl, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, arylalkyl, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups or R” together with R form a double bond; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, amino, alkyl, haloalkyl, acyl, monoalkylamino, dialkylamino, arylamino or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups or R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; R” represents hydrogen, haloalkyl, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, arylalkyl, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2. Detailed Description of the Invention Suitable ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl, benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like. The term alkyl refer to linear or branched (Ci-Ci2)alkyl group, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, n-pentyl, isopentyl, hexyl and the like. The term aryl refer to phenyl or naphthyl. The term halogen refer to fluorine, chlorine, bromine or iodine. The term haloalkyl refer to chloromethyl, chloroethyl, trifluoromethyl, trifluoroethyl, dichloromethyl, dichloroethyl and the like. The term acyl refer to -C(=0)CH3, -C(=0)C2H5, -C(=0)C3H7, -CeO)C6Hi3, -CeS)CH3, -G(=S)C2H5, -C(=S)C3H7, -C(=S)C6Hi3, benzoyl; The term alkoxy refer to linear or branched (CpCe) alkoxy group, such as methoxy, ethoxy, n-propoxy, isopropoxy and the like. The term haloalkyl refer to; monoalkylamino group such as -NHCH3, -NHC2H5, -NHC3H7, -NHCfiHu, and the like. The term alkoxy refer to dialkylamino group such as -N(CH3)2, -NCH3(C2H5), -N(C2H5)2 and the like. The term alkoxy refer to acylamino group such as -NHC(=0)CH3, -NHC(=0)C2H5, -NHC(=0)C3H7, -NHC(=0)C6Hi3, and the like. The term alkoxy refer to alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl and the like. The term alkylsulfonyl refer to methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, iso-propylsulfonyl and the like. The term alkylsulfinyl refer to methylsulfinyl, ethylsulfmyl, n-propylsulfmyl, iso-propylsulfmyl and the like. The term alkylthio refer to methylthio, ethylthio, n-propyhhio, iso-propyhhio and the Uke. The term alkoxyalkyl refer to methoxymethyl, ethoxymethyl, methoxyethyl, ethoxyethyl and the Uke. The term carboxyUc acid or its derivatives refer to esters, amides and acid haUdes. The term arylamino refer to phenyl amino, naphthyl amino* The term alkoxyamino refer to methoxyamino, ethoxyamino, propoxy amino and the like. m and n are integers ranging from 0-2. Pharmaceutically acceptable salts of the present invention include alkali metal salts like Li, Na, and K salts, alkaline earth metal salts like Ca and Mg salts, salts of organic bases such as diethanolamine, a-phenylethylamine, benzylamine, piperidine, morpholine, pyridine, hydroxyethylpyrrolidine, hydroxyethylpipendine, guanidine, choline and the like, ammonium or substituted ammonium salts, aluminum salts. Salts also include amino acid salts such as glycine, alanine, cystine, cysteine, lysine, arginine, phenylalanine etc. Salts may include acid addition salts where appropriate which are, sulphates, nitrates, phosphates, perchlorates, borates, hydrohalides, acetates, tartrates, maleates, citrates, succinates, palmoates, methanesulphonates, tosylates, benzoates, salicylates, hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, ketoglutarates and the like. Pharmaceutically acceptable solvates may be hydrates or comprising other solvents of crystallization such as alcohols. Representative compounds of fomiula (I) according to the present invention include: 6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one; 6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-bromophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylthiophenyl)-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methylphenyl)-2-(4-methylthio-phenylamino)-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylsulfonyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylphenyl)-1 H-pyrimidin-4-one; 4-(6-Amino-4-oxo-1 -phenyl-1,4-dihydro-pyrimidin-2-ylamino)- benzenesulfonamide; 4-(6-Amino-4-oxo-1 -(4-methyl-phenyl)-1,4-dihydro-pyrimidin-2-ylainino)- benzenesulfonamide; 6-Amino-2-phenylamino-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-2- phenylamino-1 -(4-chloropyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2- phenylamino-1 -(4-bromopyridin-2-yl)-1 H-pyrimidin-4-one; Representative compounds of fomiula (II) according to the present invention include: 5-Cyano-4-methylthio-1 -(4-methylthio-phenyl)-2-phenyl-1,6-dihydro-pyrimidin-6-one; 5-Cyano-4-methylthio-1 -(4-methylthiO"phenyl)-2-(4-trifluoromethylphenyl)-1,6-dihydro-pyrimidin-6-one; 5-Cyano-1 -(4-fluorophenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one; 5-Cyano-1 -(4-methylphenyl)-2-(4-methylsulfonyl-phenyl)-4-methylthio-1,6-dihydro-pyrimidin-6-one; 5-Carboxy-4-methylthio-1 -(4-methylthio-phenyl)-2-phenyl-1,6-dihydro- pyrimidin-6-one; 5-Carbamoyl-2-(4-fluorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6- dihydro-pyrimidin-6-one; 5-Chloro-2-(4-chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro- pyrimidin-6-one; 2-(4-Chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro- pyrimidin-6-one; 2-(4-Chlorophenyl)-1 -(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one; 1 -(4-Methylphenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro- pyrimidin-6-one; 1 -(4-Methylphenyl)-2-(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one; 4-(5-Cyano-4-methylthio-6-oxo-2-phenyl-6H-pyrimidin-1 -yl)- benzenesulfonamide; 4-(5-Cyano-4-methylthio-6-oxo-2-(4-methylphenyl)-6H-pyrimidin-l-yl)- benzenesulfonamide and 4-(5-Carboxy-4-methylthio-6-oxo-2-phenyl-6H-pyrimidin-1 -yl)- benzenesulfonamide. Representative compounds of fomiula (III) according to the present invention include: 1-(4-Methylsulfanyl-phenyl)-6-phenyl-pyrimidin-2,4-( 1 H)-dione; 6-(4-Methylphenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Ethylphenyl)-l-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione; l-(4-Methylphenyl)-6-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione; 1 -(4-Bromophenyl)-6-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 5-Cyano-1 "(4-fluorophenyl)-2-(4-methylsulfonyl-phenyl)-4-methylthio-1,6- dihydro-pyrimidin-6-one; 5-Cyano-1 -(4-methylphenyl)-4-methylsulfonyl-2-(4-methylsulfonyl-phenyl)" 1,6- dihydro-pyrimidin-6-one; 5-Cyano-1 -(4-methylphenyl)-4-methylsulfonyl-2-(4-methylthio-phenyl)-1,6- dihydro-pyrimidin-6-one; 5-Cyano-1 -(4-methylphenyl)-4-methylthio-2-(4-sulfamoyl-phenyl)-1,6-dihydro- pyrimidin-6-one; 5-Cyano-2-(4-fluorophenyl)-1 -(4-methylthio-phenyl)-4-methylthio-1,6-dihydro- pyrimidin-6-one; 5-Cyano-2-(4-fluorophenyl)-1 -(4-methylsulfonyl-phenyl)-4-methylthio-1,6- dihydro-pyrimidin-6-one; 5-Cyano-2-(4-fluorophenyl)-4-methylthio-1 -(4-sulfamoyl-phenyl)-1,6-dihydro- pyrimidin-6-one; 5-Cyano-2-(4-chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro- pyrimidin-6-one; 5-Cyano-1 -(4-methylphenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro- pyrimidin-6-one; 2-(4-Methanesulfonyl-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6- dihydro-pyrimidine-5-carboxylic acid; 2-(4-Methanesulfanyl-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6- dihydro-pyrimidine-5-carboxylic acid; 2-(4-Fluroro-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6-dihydro- pyrimidine-5-carboxylic acid; 6-(4-Chlorophenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chloro-3-methylphenyl)4-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(m dione; 6-(3 -Chloro-4-methylphenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1H)- dione; 6-(4-FluoroO-methylphenyl)4-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)- dione; 6-(4-Fluorophenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Methylsulfanyl-phenyl)-1 -phenyl"pyrimidin-2,4-( 1 H)-dione; 6-(4-Methylphenyl)-l-(3-chloro-4-methylsulfonyl-phenyl)-pyrimidin-2,4-(lH)- dione; 6-(4-Methoxy-3 -methylphenyl)-1 -(4-methylsulfonyl-phenyl)-p3nimidin-2,4-( 1H)- dione; 6-(4-Methylphenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Ethylphenyl)-1 -(4"methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chlorophenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chloro-3-methylphenyl)-1 -(4-methylsulfonyl-phenyl)-p)nimidin-2,4-( 1H)- dione; 6-(4-Chlorophenyl)-1 -(3 -inethoxy-4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1H)- dione; 6-(3-Chloro-4-methylphenyl)-l-(4-methylsulfonyl-phenyl)-pyrimidin-2,4-(lH)- dione; 6-(4-Fluorophenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; l-(4-Methylsulfonyl-phenyl)-6-phenyl-pyrimidin-2,4-(lH)-dione; l-(4-Methylsulfanyl-phenyl)-6-(pyridin-2-yl)-pyrimidin-2,4-(lH)-dione; 6-(4-Methylpyridin-2-yl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chloropyridin-2-yl)-l-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione; 6-(4-Methylsulfanyl-phenyl)-1 -(pyridin-2-yl)-pyrimidin-2,4-( 1 H)-dione; l-(4"Methylsulfonyl-phenyl)-6-(pyridin-2-yl)-pyrimidin-2,4-(lH)-dione; 6-(4-Methylpyridin-2-yl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chloropyridin-2-yl)-1-(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)--dione; 4-(2,4-Dioxo-6-(4-methylphenyl)-3,4-dihydro-2H-pyrimidin-l-yl)- benzenesulfonamide; 4-(2,4-Dioxo-6-phenyl-3,4-dihydro-2H-pyrimidin-l-yl)-benzenesulfonamide; 4-[6-(4-Bromo-phenyl)-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-yl]- benzenesulfonamide; 4-(2,6-Dioxo-3-phenyl-1,2,3,6-tetrahydro-pyrimidin-4-yl)-benzenesulfonamide; 4-(2,6-Dioxo-3-(4-methylsulfanyl-phenyl)-l,2,3,6-tetrahydro-pyrimidin-4-yl)- benzenesulfonamide and 4-[3-(4-Chloro-phenyl)-2,6-dioxo-1,253,6-tetrahydro-pyrimidin- 4-yl]-benzenesulfonamide. Representative compounds of formula (IV) according to the present invention include: 5,6-Diphenyl-2-trifluoromethyl-pyrimidin-4-one; 5-Phenyl-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one; 5-(4-Chlorophenyl)-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one; 5-(4-Fluorophenyl)-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one; 4-[5-(4-Fluorophenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]-benzenesulfonamide; 4-[5-(4-Methylsulfonylphenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]- benzenesulfonamide; 4-[5-(4-Methylthiophenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]- benzenesulfonamide; 6-(4-Methylsulfonylphenyl)-5-phenyl-2-thiouracil; 6"(4-Chlorophenyl)-5-phenyl-2-thiouracil; 6-(4-Methylphenyl)-5-phenyl-2-thiouracil; 5"Phenyl-6-(4-trifluoromethylphenyl)-2-thiouracil; 5-(4-Chlorophenyl)-6-phenyl-2-thiouracil; 5"(4-Methylthiophenyl)-6-phenyl-2-thiouracil; 5-(4-Methoxyphenyl)-6-phenyl-2-thiouracil; 5"(4-Chlorophenyl)-6-(4"methylphenyl)-2-thiouracil; 4"(5-Phenyl-2-thio-4-oxo-pyrimidin"6-yl)benzenesulfonamide; 4'"(6-Phenyl-2-thio-4-oxo-pyrimidin-5-yl)benzenesulfonamide; 6"(4-Chlorophenyl)-5-phenyl-uracil; 6-(4-Methylphenyl)-5-phenyl-uracil; 5"Phenyl-6-(4-trifluoromethylphenyl)-uracil; 5-(4-Chlorophenyl)-6-phenyl-uracil; 5"(4-Methylthiophenyl)-6-phenyl-uracil; 5"(4-Methoxyphenyl)-6-phenyl-uracil; 5-(4-Chlorophenyl)-6-(4-methylphenyl)-uracil; l,3-Dimethyl-6-(4-chlorophenyl)-5-phenyl-uracil; l,3-Diniethyl-6-(4-methylphenyl)-5"phenyl-uracil; 4-[ {6-(4-chlorophenyl)-2,4-dioxo-pyrimidin-5-yl} Jbenzenesulfonamide and 4"[5-(4-chlorophenyl)-2,4-dioxo-pyrimidin-6-yl}]benzenesulfonamide. According to yet another embodiment of the present invention, there is provided a process for the preparation of novel amino substituted pyrimidinone Q Q derivatives of the formula (I) wherein Y represents NR , where R and all other symbols are as defined above, which comprises, reacting compound of formula (la) where all symbols are as defined above. The reaction of compound of formula (la) with (lb) to produce compound of formula (I) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, pyridine, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, diphenylether, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof or by neat reaction. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 36 h. According to yet another embodiment of the present invention there is provided a process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) wherein any of the groups R or R represent SR , wherein R” represents alkyl or aryl to novel amino substituted pyrimidinone derivatives of the formula (I) wherein any of the groups R or R represent S(0)pR 5 where p represents 1 or 2 and R represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, an alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions. According to yet another embodiment of the present invention there is provided a process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) wherein R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl may be converted to novel amino substituted pyrimidinone derivatives of the formula (I) wherein R or R represent S(0)pR , where p is 1 or 2, R represents amino by using the procedure described in the literature (Huang etMl Tetrahedron Lett. 39, 7201, 1994). In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (I) wherein either of R” or R” represent S(0)pR” wherein R” represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Ic) wherein all symbols are as defined earlier wherein either of R” or R"“ represents hydrogen with chlorosulfonic acid and ammonia. The reaction of compound of formula (Ic) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the rangeof 2 to 12 h. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (la) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, amino, acyl, alkyl, alkoxy, aryl group; the ring represented by A is selected from aryl or heteroaryl; R” represents hydrogen, SR”, wherein R” represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R represents hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2. In yet another embodiment of the present invention, the compounds of formula (la) are prepared by methylating the compound of formula (Ia-1) where all symbols are as defined above. The methylation of compound of formula (Ia-1) to produce compound of formula (la) may be carried out by treating with methylating agent like methyliodide, dimethylsulphate and diazomethane etc., in the presence of base such as sodium hydroxide, potassium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol, water and the like or mixture thereof. According to another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein all symbols are as defined earlier, which comprises reacting a compound of the formula (Ila) wherein all symbols are as defined above, to produce a compound of formula (II). The reaction of compound of formula (Ila) with compound of formula (lib) may be carried out using appropriate solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o- dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert- butylalchol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The condensation reaction may be carried out under acidic conditions using mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction is usually carried out under cooling to refluxing conditions. The final product purified by using chromatographic techniques or by recrystallization. The reaction may be carried out for period in the range of 2 to 20 h. According to another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein all symbols are as defined earlier, which comprises reacting a compound of the formula (lie) wherein all symbols are as defined above, to produce a compound of formula (II). The reaction of compound of formula (lie) with compound of formula (lid) may be carried out using appropriate solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The condensation reaction may be carried out under acidic conditions using mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction is usually carried out under cooling to refluxing conditions. The final product purified by using chromatographic techniques or by recrystallization. The reaction may be carried out for period in the range of 30 min. to 10 hours. According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidone derivatives of the formula (II) wherein any of the groups R” or R” represent SR', wherein R” represents alkyl or aryl to novel pyrimidone derivatives of the formula (II) wherein any of the groups R or R represent S(0)pR , where p represents 1 or 2 and R” represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, an alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions. According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidone derivatives of the formula (II) wherein R” or R” represent S(0)pR”, where p is 1 or 2, R” represents alkyl or aryl may be converted to novel pyrimidone derivatives of the formula (II) wherein R” or R” represent S(0)pR” where p is 1 or 2, R” represents amino by using the procedure described in the literature (Huang et.al Tetrahedron Lett., 39, 7201, 1994). In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein either of R” or R” represent S(0)pR”, wherein R” represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (He) where R” represents hydrogen with chlorosulfonic acid and ammonia. The reaction of compound of formula (He) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (lib) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl, or S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an T A integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2. In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (lib), which comprises, methylating the compound of formula (IIb-2) The methylation of (IIb-2) may be carried out by treating with methylating agent like methyliodide, dimethylsulphate and diazomethane etc., in the presence of base such as sodium hydroxide, potassium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol, water etc. In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (IIb-2), which comprises, reacting compound of formula (IIb-3) The reaction of compound of formula (IIb-3) with compound of formula (IIb-4) may be carried out in solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The reaction may be carried out at a temperature in the range of 0 to 200 °C for period in the range of 30 min. to 5 hours. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (lid) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl, or S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R” and R"* may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2. In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (lid), which comprises, reacting compound of formula (IIb-3) The reaction of compound of formula (IIb-3) with compound of formula (IId-1) may be carried out in the presence of catalysts like aluminium chloride, triethyl aluminium, sodium hydride, sodium methoxide, butyl lithium, lithium diisopropylamine, sodium bis trimethyl silylamide, lithium bis trimethyl silylamide, using solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The reaction may be carried out at a temperature in the range of 50 to 200 °C for period in the range of 30 min. to 10 hours. According to yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (III) wherein all symbols are as defined above, as shown in scheme I below: Scheme-l The reaction of compound of formula (Ilia) with (Illb) to produce compound of formula (IIIc) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof. The condensation may be carried out under acidic conditions using mineral or organic acids or basic conditions using carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h. The cyclization of compound of formula (IIIc) to obtain compound of formula (III) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof The cyclization is carried out under acidic conditions using mineral or organic acids or basic conditions using carbonates, bicarbonates, hydrides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h. In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (III) wherein either of R” and R” represent S(0)pR”, wherein R” represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Illd) wherein all symbols are as defined earlier 1 "i wherein any one of R and R represent hydrogen with chlorosulfonic acid and ammonia. The reaction of compound of formula (Illd) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12h. According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidinedione derivatives of the formula (III) wherein any of the groups R” or R” represent SR”, wherein R” represents alkyl or aryl to novel pyrimidinedione derivatives of the formula (III) wherein any of the groups R or R represent S(0)pR , where p represents 1 or 2 Q and R represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions. According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidinedione derivatives of the formula (III) wherein R” or R” represent S(0)pR” where p is 1 or 2, R” represents alkyl or aryl to novel pyrimidinedione derivatives of the formula (III) wherein R or R"“ represent S(0)pR”, where p is 1 or 2, R” represents amino by using the procedure described in the literature (Huang et al Tetrahedron Lett. 39, 7201, 1994). In yet another embodiment of the present invention, there is provided a novel intermediate of formula (Ilia) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the ring represented by B is selected from aryl or heteroaryl; R represents SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R” represents hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylthio, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy. aryloxy, monoalkylamino, dialkylamino, arylamino, groups; n is an integer and represents 0 to 2. In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (Ilia) as shown in scheme 2 below. The reaction of compound of formula (Ille) wherein R' represents alkyl group and all other symbols are as defined above with (Illf) to produce compound of formula (Illg) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof. The reaction may be carried out in the presence of base such as sodium hydroxide, potassium hydroxide, sodium bicarbonate, sodium carbonate and the like. The reaction may be carried out at a temperature in the range of 10 to 80 °C for period in the range of 4 to 24 h. The conversion of compound of formula (Illg) to obtain compound of formula (Ilia) may be carried out in the presence of acids such as hydrochloric acid, sulfuric acid, acetic acid, nitrous acid and the like. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IIIc) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl; O Q S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an T A integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylthio, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxy, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2. According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” together with R” form a double bond; R” represents trifluoromethyl and R” represents hydrogen and all other symbols are as defined above, as shown in scheme 2 below : where R' represent (C1-C3) alkyl group and all other symbols are as defined earlier. The compound of formula (IVb) may be prepared using trifluoro acetic anhydride in the presence of solvents such as acetic anhydride, toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof or by neat reaction. The reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals; organic bases such as pyridine, triethyl amine and the like. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 24 h. The compound of formula (IV) is prepared by reacting the compound of formula (IVb) with ammonia after refluxing with acetic anhydride, in the solvents such as selected from acetic anhydride, toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol and the like. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 1 to 12 h. According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) where R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR and all other symbols are as defined above, which comprises reacting a compound of the formula (IVa) where R' represent (C1-C3) alkyl group and all other symbols are as defined earlier, with a compound of the formula (IVc) where R' represent (CpCa) alkyl group and all other symbols are as defined earlier, with a compound of the formula (IVc) where R” and R” are as defined above to produce a compound of formula (IV) defined above. The reaction of compound of formula (IVd) with compound of formula (IVc) may be carried out in neat or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 20 h. In yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) wherein either of R or R represent sulfamoyl and all other symbols are as defined earlier, which comprises reacting compound of formula (IV) wherein all symbols are as defined earlier where R” and R” are as defined above to produce a compound of formula (IV) defined above. The reaction of compound of formula (IVa) with compound of formula (IVc) may be carried out in neat or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h. According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) where R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR and all other symbols are as defined above, which comprises reacting a compound of the formula (IVd) wherein either of R” or R” represent hydrogen with chlorosulfonic acid and ammonia. The reaction of compound of formula (IV) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction is carried out under cooling to reflux temperature for period in the range of 2 to 12 h. In yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein any of the groups R or R represent alkylthio to novel diaryl pyrimidinone derivatives of the formula (IV) wherein any of the groups R or R represent alkylsuflinyl or alkylsulfonyl by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions. According to yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R or R represent alkylsulfonyl or alkylsulfinyl to novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” or R” represent sulfamoyl by using the procedure described in the hterature (Huang et.al. Tetrahedron Lett. 1994, 39, 7201). In yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” and R” together with the carbon atom to which they are attached represent thioxo to and all other symbols are as defined above to novel ft 7 diaryl pyrimidinone derivatives of the formula (IV) wherein R and R together with the carbon atom to which they are attached represent oxo. The conversion may be carried using hydrogen peroxide in the presence or absence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The reaction may be carried out under basic conditions using bases such as carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IVa) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl, sulfamoyl; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2; R' represent (CpCs) alkyl group. In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (IVa), which comprises reacting compound of formula (IVa-1) The reaction of compound of formula (IVa-1) with compound of formula (IVa-2) may be carried out using cupric acetate, zinc dust in the presence or absence of solvents such as toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h,. In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IVd) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxy!, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl, sulfamoyl; R” and R"* may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2; R' represent (CpCs) alkyl group. In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (Id), which comprises reacting compound of formula (IVd-1) wherein all symbols are as defined above. The reaction of compound of formula (IVd-1) with compound of formula (IVd-2) may be carried out using lithium bis(trimethylsilyl)amide, sodium trimethylsilyl)amide, Sodium hydride, Sodim methoxide, sodium ethoxide, Butyl lithium, Lithiumdiisopropylamine etc., in ne”t or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropanol, tert-butyl alcohol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 10 hours. It is appreciated that in any of the above-mentioned reactions, any reactive group in the substrate molecule may be protected according to conventional chemical practice. Suitable protecting groups in any of the above-mentioned reactions are those used conventionally in the art. The methods of formation and removal of such protecting groups are those conventional methods appropriate to the molecule being protected. The pharmaceutically acceptable salts are prepared by reacting the compound of formulae (I) or (II) or (III) or (IV) with 1 to 4 equivalents of a base such as sodium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol etc. Mixture of solvents may be used. Organic bases such as diethanolamine, a-phenylethylamine, benzylamine, piperidine, morpholine, pyridine, hydroxyethylpyrrolidine, hydroxyethylpiperidine, guanidine, choline and the like, ammonium or substituted ammonium salts, aluminum salts. Amino acid such as glycine, alanine, cystine, cysteine, lysine, arginine, phenylalanine, etc may be used for the preparation of amino acid salts. Alternatively, acid addition salts wherever applicable are prepared by the treatment with acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, p-toluenesulphonic acid, methanesulfonic acid, acetic acid, citric acid, maleic acid, salicylic acid, hydroxynaphthoic acid, ascorbic acid, palmitic acid, succinic acid. benzoic acid, benzenesulfonic acid, tartaric acid and in solvents like ethyl acetate, ether, alcohols, acetone, tetrahydrofliran, dioxane etc. Mixture of solvents may also be used. The stereoisomers of the compounds forming part of this invention may be prepared by using reactants in their single enantiomeric form in the process wherever possible or by conducting the reaction in the presence of reagents or catalysts in their single enantiomer form or by resolving the mixture of stereoisomers by conventional methods. Some of the preferred methods include use of microbial resolution, resolving the diastereomeric salts formed with chiral acids such as mandelic acid, camphorsulfonic acid, tartaric acid, lactic acid, and the like wherever applicable or chiral bases such as brucine, cinchona alkaloids and their derivatives and the like. Commonly used methods are compiled by Jaques et al in "Enantiomers, Racemates and Resolution" (Wiley Interscience, 1981). More specifically the compound of formula (I) may be converted to a 1:1 mixture of diastereomeric amides by treating with chiral amines, aminoacids, aminoalcohols derived from aminoacids; conventional reaction conditions may be employed to convert acid into an amide; the diastereomers may be separated either by fractional crystallization or chromatography and the stereoisomers of compound of formula (I) may be prepared by hydrolysing the pure diastereomeric amide. Various polymorphs of compound of formulae (I) or (II) or (III) or (IV) forming part of this invention may be prepared by crystallization of compound of formulae (I) or (II) or (III) or (IV) under different conditions. For example, using different solvents commonly used or their mixtures for recrystallization; crystallizations at different temperatures; various modes of cooling, ranging from very fast to very slow cooling during crystallizations. Polymorphs may also be obtained by heating or melting the compound followed by gradual or fast cooling. The presence of polymorphs may be determined by solid probe NMR spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques. Pharmaceutically acceptable solvates of the compounds of formulae (I) or (II) or (III) or (IV) forming part of this invention may be prepared by conventional methods such as dissolving the compounds of formulae (I) or (II) or (III) or (IV) in solvents such as water, methanol, ethanol, mixture of solvents such as acetone:water, dioxane:water, N,N"dimethylformamide:water and the like, preferably water and recrystallizing by using different crystallization techniques. The present invention provides a pharmaceutical composition, containing the compounds of the general formulae (I) or (II) or (III) or (IV) as defined above, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable hydrates and solvates in combination with the usual pharmaceutically employed carriers, diluents and the like, useful for the treatment of arthritis, pain, fever, psoriasis, allergic diseases, asthma, inflammatory bowel syndrome, gastro-intestinal ulcers, cardiovascular disorders including ischemic heart disease, atherosclerosis, cancer, ischemic-induced cell damage, particularly brain damage caused by stroke, other pathological disorders associated with free radicals. The pharmaceutical composition of the present invention are effective in the treatment of inflammation and immunological diseases, particularly those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-8 and cyclooxygenase such as COX-2 andCOX-3. The pharmaceutical composition may be in the forms normally employed, such as tablets, capsules, powders, syrups, solutions, aerosols, suspensions and the like, may contain flavoring agents, sweeteners etc., in suitable solid or liquid carriers or diluents, or in suitable sterile media to form injectable solutions or suspensions. Such compositions typically contain from 1 to 20 %, preferably 1 to 10 % by weight of active compound, the remainder of the composition being pharmaceutically acceptable carriers, diluents or solvents. The present invention is provided by the examples given below, which are provided by way of illustration only and should not be considered to limit the scope of the invention. Dry hydrogen chloride gas was passed through a mixture of ethyl cyanoacetate (17.3g, 153mmol) and 4-ethoxyphenylthiourea (lOg, Slmmol) in dioxane (60ml) for 20 hours at 0 - 5 °C. The reaction mixture was refluxed for 6 hours, poured onto ice-water mixture and neutralized with saturated sodium bicarbonate solution. The precipitate thus separated was filtered, washed with water and dried in vacuum to yield the title compound (9.32g, 69.5%, purity 94.1% by HPLC) mp 222 - 225 °C. “H-NMR (DMSO - da): 5 1.34 - 1.37 (t, 3H), 4.04 - 4.09 (q, 2H), 4.93 (s, IH), 6.2 (bs, 2H, D2O exchangeable), 7.01 - 7.03 (d, 2H), 7.15 - 7.17 (d, 2H), 11.92 (s, IH, D2O exchangeable). MS m/z: 264.1 (M”). 6-Amino-l-phenyl"2-thiouracil (5.5g. 25mmol) (synthesized according to the procedure given in CJ.Shishoo et aL, Indian J. Chem., 35B, pp 662, 1996) was added to the stirred potassium hydroxide (IN, 50ml) solution and filtered. Methyl iodide (6.26g, 44mmol) was added to the vigorous stirred filtrate at 20 °C and stirring was continued at room temperature for 2 hours. The reaction mixture was poured onto ice-water, separated solid was filtered, washed with water and dried to furnish the title compound (4.80g, 82.1%) mp 213 - 216 °C. “H-NMR (CDCI3): 5 2.40 (s, 3H), 4.93 (bs, 2H, D2O exchangeable), 5.38 (s, IH), 7.33 -7.35 (m, 2H), 7.59 - 7.60 (s, 3H). MS m/z: 234.1 (M”). The title compound was prepared from 6-amino-l-(4-methylphenyl)-2-thiouracil (7g, 30mmol) (synthesized according to the procedure given in CJ.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) by following the procedure described in preparation 2, (6.0g, 80.9%) mpl30 - 132 °C. MS m/z: 248.2 (M”). The title compound was prepared from 6-amino-l-(4-methoxyphenyl)-2-thiouracil (lOg, 40mmol) (synthesized according to the procedure given in C.J.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) by following the procedure described in preparation 2, (9.64g, 91.3%, purity 99%) by HPLC) mpl82 - 186 °C. “H-NMR (DMSO-de): 5 2.25 (s, 3H), 3.83 (s, 3H), 4.96 (s, IH), 5.94 (s, 2H, D2O exchangeable), 7.09 - 7.11 (d, 2H), 7.33 - 7.35 (d, 2H). MS m/z: 264.1 (M”). The title compound was prepared from 6-amino-l-(4-ethoxyphenyl)-2-thiouracil (8g, 30.4mmol) (obtained in preparation 1) according to the procedure described in preparation 2, (6.88g, 81.7%, purity 90.8% by HPLC) mp 177 - 181 X. “H-NMR (CDCI3): 5 1.45 - 1.49 (t, 3H), 2.42 (s, 3H), 4.10 - 4.12 (q, 2H), 5.31 (s, IH), 7.05 - 7.07 (m, 2H), 7.23 - 7.25 (m, 2H), MS m/z: 278.1(M”). The title compound was prepared by following the procedure described in preparation 2 from 6-amino-1 -(4-chlorophenyl)-2-thiouracil (8g, 31.5mmol) (synthesized according to the procedure given in C.J.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) (7.34g, 86.9%), mpl80 - 182 °C. “H-NMR (DMSO-d6): 5 2.27 (s, 3H), 4.96 (s, IH), 6.09 (s, 2H), 7.50 -7.52 (d, 2H), 7.64 - 7.66 (d, 2H).MS m/z: 268.1 (M”). Preparation 7 Synthesis of 6-amino-2-methylthio-l-(4-bromophenyl)-lH-pyrimidin-4-one The title compound was prepared by following the procedure described in preparation 2 from 6-amino-l-(4-bromophenyl)-2-thiouracil (Ig, 3.35mmol) (synthesized according to the procedure given in CJ.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) (0.55g, 52.5%), mp 138 - 140 °C. MS m/z: 312.0/313.9 (M”). Sodium hydroxide solution (33%, 32.5ml) was added to ethyl acetoacetate (97.5g, 750mmol) in a mixture of water (250ml) and toluene (12ml) at 0-5 ”C under stirring (pH 11). After 30 minutes 4-methylbenzoylchloride (127.46g, 825mmol) and sodium hydroxide solution (33%, 135ml) was added simultaneously over a period two hours. The reaction mixture was stirred for 15 minutes at 0 °C and for 1 hour at 35 °C. Aqueous layer was separated, ammonium chloride (40g) was added and stirred slowly over night. The reaction mixture was saturated with sodium chloride and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness in vacuum. The crude product thus obtained was purified by column chromatography to yield the title compound as viscous oil (54g, 35%). MS m/z: 207.1 (M”). Ethyl acetoacetate (51.25g, 390 mmol) was added dropwise to the stirred suspension of anhydrous magnesium chloride (37.54g, 390mmol) in dried dichloromethane (200ml) over a period of 1 hour under argon atmosphere at 0 °C followed by pyridine (62.5g, 788mmol). After 15 minutes, 4-chlorobenzoylchloride (68.95g, 394 mmol) was added dropwise and stirring was continued for 15 minutes at 0 °C and further stirred for 1.5 hours at 30 °C. The resulting reaction mixture was neutralized with hydrochloric acid (6N, 235ml) at 0-5 °C, filtered and washed with water. The filtrate was extracted with diethylether (3X100 ml). The ether extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness in vacuum. The obtained oil was taken in ammonium chloride (21g in 200ml water) solution containing ammonia (2ml) and stirred at 30 °C for 20 minutes. The resulting solution was extracted with ethyl acetate (3X200ml). Ethyl acetate extract was dried over anhydrous sodium sulphate, concentrated to yield the crude product, which was purified by column chromatography to yield the title compound as viscous oil (43g, 48.2%). H-NMR (DMSO - d6): 8 1.15 - 1.18 (t, 3H), 4.08 - 4.13 (q, 2H), 4.20 (s, 2H), 7.61 - 7.64 (d, 2H), 7.94 - 7.97 (d, 2H). MS m/z: 227.1 (M”). Lithium bis(triniethylsilyl)amide (20% in tetrahydrofuran, 203.6ml, 217mmol) was added dropwise to a stirred solution of 4-methylthioacetophenone (20.2g, 121 mmol) in dried tetrahydrofuran (300ml) at - 20 °C and stirring was continued for 1 hour at -20 °C. Ethylchloroformate (19.8g, 182mmol) was added dropwise to the stirred reaction mixture at -20 °C and stirring was continued for 3 hours. The reaction was quenched with saturated ammonium chloride solution and extracted with ethylacetate. The organic extract was washed with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness in vacuum. The crude product thus obtained was purified by column chromatography to yield the title compound as viscous oil (16.45g, 56.8%). “H-NMR (DMSO - de): 8 1.15 - 1.19 (t, 3H), 2.54 (s, 3H), 4.07 - 4.11 (q, 2H), 4.13 (s, 2H), 7.36 - 7.39 (d, 2H), 7.85 - 7.88 (d, 2H). MS m/z: 239 (M”). Potassium hydroxide (12.55g, 224mmol) was added to the vigorously stirred solution of methylthiopseudourea.H2S04 (14.57g, 52mmol) in water (80ml). Ethyl (4-methyl)benzoylacetate (20.0g, 97mmol) (obtained in preparation 8) was added to it and stirred at room temperature for 18 hours. The solid thus obtained was filtered, washed with water, ether and dried at 60 °C in vacuum to yield the title compound (1.85g, 9.5%). “H-NMR (DMSO - d6): 5 2.37 (s, 3H), 6.46 (s, IH), 7.33 - 7.35 (d, 2H), 7.76 - 7.78 (d, 2H), 7.91 (bs, 2H, D2O exchangeable). MS m/z: 203.1 (M'). The title compound was prepared from ethyl (4-chloro)benzoylacetate (5.0g, 22mmol) (obtained in preparation 9) and methylthiopseudourea.H2S04 (3.3Ig, 12mmol) by following the procedure described in preparation 4, (0.573g, 11.6%). MS m/z: 223 (M”). The title compound was prepared from ethyl (4-methylthiobenzoyl)acetate (16.447g, 69mmol) (obtained in preparation 10) and methylthiopseudourea.H2S04 (10.56g, 38mmol) according to the procedure described in preparation 4, (1.82g, 11.5%, mp 266 - 267 °C). “H-NMR (DMSO -d6): 8 2.53 (s, 3H), 6.48 (s, IH), 7.37 - 7.39 (d, 2H), 7.79 - 7.81 (d, 2H), 7.92 (bs, 2H). MS m/z: 235 (M”). A suspension of 2-amino-6-(4-methylphenyl)-l,3-oxazin-4-one (l.Og, 5mmol) (obtained in preparation 11) in 10% hydrochloric acid (60ml) was refluxed for Ihr. The resulting suspension was cooled, filtered, washed with water and dried at 60 °C in vacuum for 8 hours to yield the title compound (0.32g, 32%). “H-NMR (DMSO - d6): 8 2.38 (s, 3H), 6.65 (s, IH), 7.35 - 7.37 (d, 2H), 7.79 - 7.81 (d, 2H), 11.89 (bs, IH, D2O exchangeable). MS m/z: 203.1 (M”), The title compound was prepared from 2-amino-6-(4-chlorophenyl)-l,3-oxazin-4-one (0.573g, 2.6mmol) (obtained in preparation 12) according to the procedure described in preparation 14 (0.57g, 99%, mp 254 - 256 °C). H-NMR (DMSO -d6): 5 6.65 (s, IH), 7.58 - 7.60 (d, 2H), 7.86 - 7.89 (d, 2H), 11.90 (bs, IH, D2O exchangeable). The title compound was prepared from 2-amino-6-(4-methylsulfanyl-phenyl)-l,3-oxazin-4-one (1.82g, 7.8mmol) (obtained in preparation 20) by following the procedure described in preparation 14 (0.78g, 42.7%). “H-NMR (DMSO - d”): 8 2.53 (s, 3H), 6.67 (s, IH), 7.37 - 7.40 (d, 2H), 7.81 - 7.83 (d, 2H), 11,89 (bs, IH). MS m/z: 235 (M”). Preparation 17 Synthesis of N-(4-methylsulfanyl-phenyl)-[N'-l-(3-phenyl)-l,3-diketone]urea 4-Methylthioaniline (3.36g, 24mmol) was added to a stirred suspension of 6-phenyl-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.189g, Immol) (synthesized according to the procedure given in Harvey I. Skulnick, Heterocylces, 23 (7), ppl685, 1985) in ethanol (5ml). The reaction mixture was refluxed for 4 hours, cooled at room temperature, filtered, washed with ethanol, ether, dried in vacuum at 60 “C for 5 hours to yield the title compound (O.lg, 30.5%, mp 143 - 145 °C). “H-NMR (DMSO - dg): 8 2.45 (s, 3H), 4.28 (s, IH), 7.23 - 7.27 (d, 2H), 7.47 -7.59 (m, 4H), 7.67 - 7.69 (d, IH), 7.96 - 7.98 (d, 2H). MS m/z: 329.2 (M”). Preparation 18 Synthesis of N-(4-methyIsulfanyl-phenyl)-{N'-l-[3-(4-methyl)phenyl]-l,3- diketone}urea 4"Methylthioaniline (0.636g, 4. 6mmol) was added to the stirred suspension of 6-(4-methylphenyl)-2H-3,4-dihydro-l,3-oxazine-2,4-dione (0.310g, 1.5mmol) (obtained in preparation 14) in ethanol (10ml). The reaction mixture was refluxed with stirring for 6 hours, cooled at room temperature, filtered, washed with ethanol followed by ether and dried in vacuum at 60 °C for five hours to yield the title compound (0.24g, 46%, mp 234 - 237 °C). “H-NMR (DMSO - Preparation 19 Synthesis of N-(4-metliylsulfanyl-phenyI)-{N'-l-[3-(4-clilorophenyl)]-l,3- dil”etone}urea The title compound was prepared from 6-(4-chlorophenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.57g, 2.5mmol) (obtained in preparation 15) and 4-methylthioaniline (2.48g, 17.8mmol) according to the procedure described in preparation 11 (0.33g, 35.7%). “H-NMR (DMSO - dg): 8 2.41 (s, 3H), 6.64 (s, IH), 7.10 - 7.19 (m, 4H), 7.25 - 7.33 (m, 4H), 11.59 (bs, IH). MS m/z: 363 (M”). Preparation 20 Syntiiesis of N-(4-metliylp!ienyl)-{N'-l-[3-(4-metliylsuIfanyl-piienyl)]-l,3- dil(etone}urea The title compound was prepared from 6-(4-methylsulfanyl-phenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.35g, l.Smmol) (obtained in preparation 16) and 4-methylaniline (1.12g, 10.4mmol) according to the procedure described in preparation 11 (0. 24g, 47%). H-NMR (DMSO - d6): 8 2.26 (s, 3H), 2.53 (s, 3H), 4.22 (s, IH), 7.12 - 7.14 (d, 2H), 7.38 - 7.42 (d, 4H), 7.87 - 7.89 (d, 2H). MS m/z: 343.1 (M”). Preparation 21 Synthesis of N-(4-bromoplienyl)-{N'-l-[3-(4-metiiylsulfanyl-plienyl)]-l,3-dilcetone}urea The title compound was prepared from 6-(4-methylsulfanyl-phenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.7g, 2.99mmol) (obtained in preparation 9) and 4-bromoaniline (3.6g, 20mmol) by following the procedure described in preparation 11 (0. 445g, 36.8%). “H-NMR (DMSO - de): 8 2.55 (s, 3H), 6.68 (s, IH), 7.37 - 7.39 (d, 4H), 7.49 (s, 2H), 7.81 - 7.83 (d, 4H), 11.8 (bs, IH). MS m/z: 407.2 (M"). Finely powdered anhydrous aluminium chloride (0.83g, 6mmol) was added to a stirred mixture of 4-chlorobenzonitrile (0.6875g, 5mmol) and 4-methylthioaniline (0.695g, 5mmol) over a period of 30 min. The reaction mixture was heated at 180 -190 °C for 3 hours with stirring and allowed to cool to 50 °C, The resultant mixture was triturated with ethyl acetate and basified with sodium hydroxide (20%) solution. The ethyl acetate layer was washed with water, dried over anhydrous sodium sulphate and concentrated to give the crude product, which was purified by column chromatography to yield the title compound (0.6g, 43.4%, purity 98.8% by HPLC), mp 148 - 150 °C. “H-NMR (CDCI3): 6 2.48 (s, 3H), 6.90-6.97(m, 2H), 7.11-7.41(m, 4H), 7.74 (bs, 2H). MS m/z: 277.0 (M”) described in preparation 22, (0.495g, 44.4%, purity 98.3% by HPLC), mp 144 -146 °C. 'H-NMR (CDCI3): 5 2.49 (s, 3H), 4.8 (bs, 2H), 6.93-6.95 (d, 2H), 7.26-7.32 (m, 2H), 7.70-7.72 (d, 2H), 7.99-8.01 (d, 2H). MS m/z: 311.1(M”). The title compound was prepared from 4-methylthiobenzonitrile (0.50g, 33.6mmol) and 4-fluoroaniline (0.372g, 33.6mmol) by following the procedure described in preparation 22, (0.43g, 49.3%, mp 145 - 147 °C, purity 94.7% by HPLC). 'H-NMR (CDCI3): 5 2.52 (s, 3H), 6.93-6.94 (m, 3H), 7.17-7.32 (m, 5H). MSm/z:261.1(M”) The title compound was prepared from 4-methylthiobenzonitrile (2.50g, 16.78mmol) and 4-methylaniline (1.789g, 16.78mmol) by following the procedure described in preparation 22, (2.05g, 47.6%, purity 79%) by HPLC), mp The title compound was prepared from 4-fluorobenzonitrile (2.176g, 17.98mmol) and 4-methylthioaniline (2.5g, 17.98mmol) by following the procedure described in preparation 22, (2.06g, 44.1%, purity 98.8% by HPLC), mpl21 - 124 °C. “H-NMR (CDCI3): 5 2.48 (s, 3H), 4.82 (bs, 2H, DjO exchangeable), 6.91-6.93 (d, 2H), 7.1-7.14 (m, 2H), 7.26-7.30 (m, 2H), 7.86 (bs, 2H). MS m/z: 261.1(M”) The title compound was prepared from benzonitrile (3.705g, 35.97mmol) and 4-methylthioaniline (5.0g, 35.97mmol) by following the procedure described in preparation 22, (3.66g, 42.1%, purity 99.8% by HPLC), mp 129 - 131 °C. 'H-NMR (CDCI3): 6 2.49 (s, 3H), 4.84 (bs, 2H), 6.94-6.96 (d, 2H), 7.26-7.31 (m, 2H), 7.45-7.49 (m, 3H), 7.87-7.88 (d, 2H). MS m/z: 243.2 (M”) The title compound was prepared from 4-trifluoromethylbenzonitrile (0.62g, 3.6mmol) and 4-methylthioaniline (0.5g, 3.6mmol) by following the procedure 143 - 145 X. “H-NMR (CDCI3): 5 2.33 (s, 3H), 2.52 (s, 3H), 4.75 (bs, 2H, D2O exchangeable), 6.87 - 6.89 (d, 2H), 7.14 -7.16 (d, 2H), 7.27 - 7.29 (d, 2H), 7.7 -7.79 (d, 2H). MS m/z: 257.1(M”). A solution of oxone (18.42g, 0.03mol) in water (70nil) was added dropwise to the vigorous stirred solution of 4-methylthiobenzonitrile (1.49g, 0.01 mol) in methanol (50ml) at 20 °C and stirring was continued for three hours. The reaction mixture was diluted with water (50ml) and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to fumish the title compound (1.3g, 72.2%), mp 145 - 149 °C. The compound was used with out any purification for the next step. “H-NMR (CDCI3): 5 3.1 (s, 3H), 7.8 - 7.9 (d, 2H), 8.08 - 8,1 (d, 2H). The title compound was obtained from 4-methylsulphonylbenzonitrile (2.00g, llmmol) (obtained according to the procedure described in preparation 28) and 4-methylaniline (1.18g, llmmol) according to the procedure described in preparation 1, (1.25g, 39.3%, purity 90.7% by HPLC), mp 187 - 189 °C. “H-NMR (CDCI3): 5 2.34 (s, 3H), 3.07(s, 3H), 4.92 (bs, 2H, D2O exchangeable), 6.87 - 6.89 (d, 2H), 7.18-7.20 (d, 2H), 8.01- 8.03 (d, 2H), 8.08 - 8.1 (d, 2H). MS mix: 289.1(M”). A solution of oxone (18.42g, 30mmol) in water (70ml) was added dropwise to the vigorous stirred solution of 4-methylthiobenzonitrile (1.49g, 1 Ommol) in methanol (50ml) at 20 °C and stirring was continued for three hours. The reaction mixture was diluted with water (50ml) and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to fumish the title compound (1.3g, 72.2%), mp 145 - 149 °C. The compound was used with out any purification for the next step. “H-NMR (CDCI3): 5 3.1 (s, 3H), 7.8 - 7.9 (d, 2H), 8.08 - 8.1 (d, 2H). Preparation 31 Synthesis of ethyl 3-amino-3-(4-methylsulfonylphenyl)-2-phenyI-2- propenoate Cu(OCOCH3)2.H20 (0.06g, 0.3mmol) and zinc dust (0.718g, llmmol) was added sequentially to the stirred glacial acetic acid (10ml) at 90 °C. The reaction mixture was stirred for 2 min., filtered, washed with glacial acetic acid (5ml) and dried tetrahydrofuran (10ml). The obtained activated zinc was added to dried tetrahydrofuran (30ml) under nitrogen atmosphere with stirring. Ethyl 2-bromo-2-phenyl acetate (0.134g, 0.55mmol) was added together with a crystal of sublimed iodine under reflux. 4-Methylsulfonylbenzonitrile (l.Og, 5.5mmol) (obtained according to the procedure given in preparation 30) in dried tetrahydrofuran (20ml) was added dropwise followed by slow addition of ethyl 2-bromo-2-phenyl acetate (1.21g, 5mmol) and the reaction mixture was refluxed with stirring for 20 hours. The residual zinc was filtered off and the resultant filtrate poured into saturated ammonium chloride solution and extracted with ethylacetate. The ethyl acetate extract was washed with water, dried, and concentrated under reduced pressure to yield the title compound (1.3g, 67.4%) which was used in the next step with out any purification. “H-NMR (CDCI3): 8 1.19 - 1.27 (t, 3H), 3.09 (s, 3H), 4.12 - 4.21 (q, 2H), 7.12 - 7.33 (m, 5H), 7,88 - 7.90 (m, 2H), 8.08 - 8.10 (m, 2H). MS m/z: 346 (M”). Preparation 32 Synthesis of ethyl 3-aminO"2-(4-chlorophenyl)-3-(4-methylsulfonyIphenyl)-2- propenoate The title compound was prepared from ethyl 2-bromo-2-(4-chlorophenyl)acetate (4.2g, ISmmol) and 4-methylsulfonylbenzonitrile (2.72g, ISmmol) (obtained according to the procedure given in preparation 30) by a similar procedure as described in preparation 2 (3.6g, 63%). It was used without further purification in the next step. MS m/z: 380.1(M”). The title compound was prepared from ethyl 2-bromo-2-(4-fluorophenyl)acetate (7g, 27mmol) and 4-methylsulfonylbenzonitrile (4.85g, 27mmol) (obtained according to the procedure given in preparation 30) by following the procedure described in preparation 2 (6.3g, 64.7%). It was used without further purification in the next step. MS m/z: 364 (M"“). Preparation 34 Trifluoroacetic anhydride (3.3g, 15.5mmol) was added to ethyl 3-amino-3-(4-methylsulfonylphenyl)-2-phenyl-2-propenoate (3.45g, lOmmol) (obtained according to the preparation 31) in pyridine (10ml) at 20 °C temperature under stirring. The temperature was raised to 35 °C and stirred for 12 hours. The reaction mixture was poured onto ice-water mixture and acidified with concentrated hydrochloric acid (pH 1) and extracted with ether. The ether extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness in vaccum. The viscous oily residue thus obtained was triturated with the saturated sodium bicarbonate solution and extracted with ether. The ether extract was washed with water, and the combined aqueous phases were acidified with concentrated hydrochloric acid (pH 1). The precipitate thus seperated was extracted with ether. The ether extract was washed with water, dried and concentrated under reduced pressure to yield the title compound (1.5g, 36%), which was used in the next step without further purification. Preparation 35 Synthesis of 2-(4-chloropiienyl)-3-(4-metliylsuIfonylpiienyl)-3- [(trifluoroacetyl)amino]propenoic acid The title compound was prepared from ethyl 3-amino-2-(4-chlorophenyl)-3-(4-methylsulfonylphenyl)-2-propenoate (6.5g, 170mmol) (obtained according to the preparation 32)and trifluoro acetic anhydride by following the procedure described in preparation 34, (1.7g, 22.2%). The compound was used in the next step without further purification. Preparation 36 Synthesis of 2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-3- [(trifluoroacetyl)amino]propenoic acid The title compound was prepared from ethyl 3-amino-2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-2-propenoate (5.7g, 15.7mmol) (obtained according to the preparation 33) and trifluoro acetic anhydride by following the procedure described in preparation 35, (2.5g, 37.3%). The compound was used in the next step without further purification. Preparation 37 Synthesis of ethyl 3-(4-chlorophenyl)-2-phenyl-3-oxopropanoate Lithium bis(trimethylsilyl)amide (20% in tetrahydrofuran, 4L3ml, 45mmol) was added dropwise to a stirred solution of ethyl phenylacetate (7.0g, 42.7mmol) in dried tetrahydrofuran (30ml) at -78 °C. After 15 minutes, the mixture was treated with 4-chlorobenzoyl chloride (7.85g, 44.8mmol) dropwise at -78 °C and the stirring was continued for 2 hours. The reaction was quenched with saturated ammonium chloride solution and extracted with ethyl acetate. The ethyl acetate extract was washed thoroughly with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness in vaccum to furnish the title compound (lO.Og, 78%, purity 84.85% by HPLC), mp 68 - 71 °C. The compound was used in the next step without further purification. “H-NMR (CDCI3): 5 1.23 - 1.26 (t, 3H), 4.21 - 4.23 (q, 2H), 5.53 (s, IH), 7.33 - 7.44 (m, 7H), 7.88 - 7.90 (m, 2H). MS m/z: 303.4 (M”). Preparation 38 Synthesis of ethyl 3-(4-methylpheny!)-2-phenyl-3-oxopropanoate The title compound was prepared from ethyl phenylacetate (7.0g, 42.7mmol) and p-toluoyl chloride (6.93g, 44.8mmol) by following the procedure described in preparation 37 (9.3g, 77%, purity 93.77% by HPLC), mp 53 - 55 “C, The compound was used in the next step without further purification. H-NMR (CDCI3): 5 1.22 - 1.26 (t, 3H), 2.37 (s, 3H), 4.19 - 4.24 (q, 2H), 5.58 (s, IH), 7.20 - 7.41 (m, 7H), 7.85 - 7.87 (m, 2H). MS m/z: 283.2 (M”). Preparation 39 Synthesis of ethyl 2-phenyl-3-(4-trifluoromethylphenyl)-3-oxopropanoate The title compound was prepared from ethyl phenylacetate (7.0g, 42.7mmol) and 4-(trifluoromethyl)benzoylchloride (9.4g, 44.8mmol) by following the procedure described in preparation 37 (4.8g, 33.4%, purity 56.58% by HPLC), mp 151 -155 °C. The compound was used in the next step without further purification. MS m/z: 337.2 (M”). Preparation 40 Synthesis of ethyl 2-(4-chlorophenyl)-3-phenyl-3-oxopropanoate The title compound was prepared from ethyl (4-chlorophenyl)acetate (5.0g, 25mmol) and benzoylchloride (3.65g, 26mmol) by following the procedure described in preparation 37 (6.7g, 88%, purity 98.51% by HPLC). The compound was used in the next step without further purification. “H-NMR (DMSO -de): 8 1.13 - 1.16 (t, 3H), 4.13 - 4.14 (q, 2H), 6.24 (s, IH), 7.43 (s, 4H), 7.53 - 7.6 (m, 3H), 8.01 - 8.04 (m, 2H). MS m/z: 303.1(M”). Preparation 41 Synthesis of ethyl 2-(4-methylthiophenyl)-3-phenyl-3-oxopropanoate The title compound was prepared from ethyl (4-methylthiophenyl)acetate (5.04g, 24mmol) and benzoylchloride (3.38g, 24mmol) by following the procedure described in preparation 37 (6.5g, 86.3%, purity 99.2% by HPLC). The compound was used in the next step without further purification. “H-NMR (CDCI3): 8 1.22 - 1.25 (t, 3H), 2.45 (s, 3H), 4.19 - 4.24 (q, 2H), 5.55 (s, IH), 7.21 - 7.26 (m, 2H), 7.31 - 7.33 (m, 2H), 7.41 - 7.44 (m, 2H), 7.52 - 7.54 (m, IH), 7.94 " 7,96 (m, 2H). MS m/z: 315 (M”). Preparation 42 Synthesis of ethyl 2-(4-methoxyphenyl)-3-phenyl-3-oxopropanoate The title compound was prepared from ethyl (4-methoxyphenyl)acetate (9.5g, 49mmol) and benzoylchloride (7.2 Ig, 51mmol) by following the procedure described in preparation 37 (1 l.Og, 75.4%, purity 89.33% by HPLC), mp 66 - 68 °C. The compound was used in the next step without further purification. H-NMR (CDCI3): 5 1.22 - 1.25 (t, 3H), 3.79 (s, 3H), 4.19 - 4.24 (q, 2H), 5.5 (s, IH), 6.87 - 6.9 (m, 3H), 7.51 - 7.55 (m, 4H), 7.94 - 7.96 (d, 2H).MS m/z: 299.2 (M"). The title compound was prepared from ethyl (4-chlorophenyl)acetate (6.2g, 31mmol) and 4-methyl benzoyl chloride (5,02g, 32.5mmol) by following the procedure described in preparation 37 (7.9g, 80%, purity 94.93% by HPLC). The compound was used in the next step without further purification. “H-NMR (CDCI3): 5 1.22 - 1.25 (t, 3H) 2.38 (s, 3H), 4.18 - 4.24 (q, 2H), 5.5 (s, IH), 7.22 ~ 7.26 (m, 2H), 7.31 - 7.36 (m, 4H), 7.83 - 7.85 (d, 2H). MS m/z: 317.1 (M""). A mixture of 6-amino-2-methylthio-l-phenyl-lH-pyrimidin-4-one (2.33g, lOmmol) (obtained in preparation 2) and aniline (4.6g, SOmmol) in presence of catalytic amount of concentrated hydrochloric acid was heated at 120 -130 °C for 7 hours. The reaction mixture was cooled, filtered and washed with hexane. The obtained crude product was recrystallised from ethanol to provide the title compound (1.13g, 40.6%, purity 99.5% by HPLC), mp 202 - 206 °C. 'H-NMR (DMSO-de): 8 5.09 (s, IH), 6.96 - 7.03 (m, 2H), 7.24 - 7.30 (m, 4H), 7.40 - 7.42 (m, 2H), 7.59 - 7.61 (m, 2H), 8.74 (s, IH, DjO exchangeable), 8.94 (s, IH, D2O exchangeable), 10.0 (s, IH, D2O exchangeable). IR (KBr) cm': 3302, 3152 (-NH-), 1666 (-C=0). MS m/z: 279.2 (M”). Example 2 Synthesis of 6-amino-2-(4-methoxy-phenylamino)-l-phenyl-lH-pyrimidin-4- one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (1.5g, 6.5mmol) (obtained in preparation 2) and 4-methoxyaniline (3.96g, 32mmol) by following the procedure described in example 1 (0.8g, 40.3%, purity 98.4% by HPLC), mp 213 - 216 °C. H-NMR (CDCI3): 5 3.73 (s, 3H), 4.9 (s, IH), 6.87 - 6.89 (m, 2H), 7.00 (m, IH), 7.25 -7.29 (m, 4H), 7.60 - 7.62 (m, 2H), 8.73 (bs, 2H, D2O exchangeable), 10.0 (bs, IH, D2O exchangeable). IR (KBr) cm-” 3305, 3152 (-NH-), 1678 (-C=0). MS m/z: 309.2 (M”). Example 3 Synthesis of 6-amino-2-(4-ethoxy-phenylamino)-l-phenyl-lH-pyrimidin-4- one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (l.Og, 4mmol) (obtained in preparation 2) and 4-ethoxyaniline (2.94g, 21mmol) by following the procedure described in example 1 (0.49g, 35.2%, purity 97.1% by HPLC), mp 111 - 113 ”C. “H-NMR (DMSO-da): 5 1.30 - 1.33 (t, 3H), 3.97 - 4.02 (q, 2H), 4.92 (s, IH), 6.85 - 6.87 (m, 2H), 6.99 - 7.02 (m, IH), 7.24 - 7.29 (m, 4H), 7.60 -7.62 (m, 2H), 8.72 (bs, 2H, D2O exchangeable), 9.9 (s, IH, D2O exchangeable). IR (KBr) cm': 3308, 2976, 1674(-C=0). MS m/z: 323.3 (M”). Example 4 Synthesis of 6-amino-2-(4-methylthio-phenylamliio)-l-phenyl-lH-pyriinidin-4-one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (3.Og, 12.8mmol) (obtained in preparation 2) and 4-methylthioaniline (8.85g, 64mmol) by following the procedure described in example 1 (2.26g, 54.1%, purity 92.7% by HPLC), mp 133 - 135 °C. “H-NMR (DMSO-dfi): 5 2.45 (s, 3H), 5,06 (s, IH), 7.00 - 7.04 (m, IH), 7.18-7.21 (m, 2H), 7.25 - 7.31 (m, 2H), 7.37 - 7.42 (m, 2H), 7.58 -7.61 (m, 2H), 8.87 - 8.95 (bs, 2H, D2O exchangeable), 10.2 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3421, 1627 (-C=0). MS m/z: 325.2 (M”). Example 5 Synthesis of 6-amino-2-(4-methyl-phenylamino)-l-phenyl-lH-pyrimidin-4- one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-methylaniline (4.59g, 42.9mmol) by following the procedure described in example 1 (1.33g, 53%), purity 98.4% by HPLC), mp 207 - 210 °C. 'H-NMR (DMSO-dfi): 6 2.25 (s, 3H), 5.02 (s, IH), 6.98 - 7.10 (m, 3H), 7.23 -7.30 (m, 3H), 7.39 - 7.60 (m, 3H), 8.63 - 8.90 (m, 2H, D2O exchangeable), 9.93 (bs, IH, D2O exchangeable). IR (KBr) cm-': 3306, 1630 (-C=0). MS m/z: 293.1 (M”). Example 6 Synthesis of 6-amino-2-(4-chloro-phenyIamino)-l-phenyl-lH-pyrimidin-4- one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-chloroaniline (5.47g, 42.9mmol) by following the procedure described in example 1 (1.2g, 45%, purity 98.9% by HPLC), mp 233 - 237 °C. 'H-NMR (DMSO-de): 8 5.07 (s, IH), 7.0 - 7.06 (m, IH), 7.24 -7.34 (m, 5H), 7.40 - 7.42 (m, 2H), 7.52 - 7.54 (m, 2H), 8.8 - 9.01 (bs, 2H, D2O exchangeable). IR (KBr) cm-': 3424, 1627 (-C=0). MS m/z: 313 (M”). Example 7 Synthesis of 6-amino-2-(4-fluoro-phenylaiiiino)-l-phenyl-lH-pyrimidin-4-one The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-fluoroaniline (4.76g, 42.9mmol) by following the procedure described in example 1 (0.8g, 31%, purity 98.3% by HPLC), mp 225 - 227 “C. “H-NMR (DMSO-de): 8 4.95 (s, IH), 6.99 - 7.56 (m, 9H), 8.73 (bs, IH, D2O exchangeable), 8.92 (bs, IH, D2O exchangeable), 10 (bs, D2O exchangeable). IR (KBr) cm"“ 3295, 1637 (-C=0). MS m/z: 297.3 (M”). Example 8 Synthesis of 6-amino-l-(4-methylphenyl)-2-(4-methylthio-phenylamino)-lH- pyrimidin-4-one The title compound was prepared from 6-amino-2-methylthio-1 -(4-methylphenyl)-lH-pyrimidin-4-one (Ig, 4mmol) (obtained in preparation 3) and 4-methylthioaniline (1.112g, 8mmol) by following the procedure described in example 1 (0.45g, 32.8%, purity 94.8% by HPLC), mp 231 - 234 °C. 'H-NMR (DMSO-dfi): 5 2.26 (s, 3H), 2.45 (s, 3H), 5.0 (s, IH), 7.08 - 7.12 (m, 2H), 7.18 -7.22 (m, 3H), 7.36 - 7.56 (m, 4H), 8.93 - 8.96 (m, 2H, D2O exchangeable). IR (KBr) cm-': 3303, 1627 (-C=0). MS m/z: 339.1 (M”). Example 9 Synthesis of 6-amino-l-(4-methoxyphenyl)-2-phenylamino-lH-pyrimidin-4- one The title compound was prepared from 6-amino-2-methylthio-l-(4-methoxyphenyl)-lH-pyrimidin-4-one (1.5g, 5.7mmol) (obtained in preparation 4) and aniline (2.65g, 28.5mmol) by following the procedure described in example 1 (0.41g, 23%, purity 97.1% by HPLC), mp 180 - 190 °C. H-NMR (DMSO-dg): 8 3.72 (s, 3H), 4.95 (s, IH), 6.85 - 6.87 (m, 3H), 7.2 - 7.30 (m, 3H), 7.5 - 7.6 (m, 3H), 8.4 (bs, IH, D2O exchangeable), 8.8 (bs, IH, D2O exchangeable), 9.8 (bs, IH, D2O exchangeable). IR (KBr) cm"': 3401 (NH), 1630 (-C=0). MS m/z: 309.2 (M"). Example 10 Synthesis of 6-amino-l-(4-etlioxyphenyl)-2-plienylamino-lH-pyrimidin-4-one The title compound was prepared from 6-amino-2-methylthio-1 -(4-ethoxyphenyl)-lH-pyrimidin-4-one (2.0g, 7.2mmol) (obtained in preparation 5) and aniline (3.2g, 35mmol) by following the procedure described in example 1 (0.71g, 30%, purity 98% by HPLC), mp 114 - 118 °C. “H-NMR (DMS0-d6): 6 1.30 - 1.33 (t, 3H), 3.97 - 4.02 (q, 2H), 5.01 (s, IH), 6.85 - 7.60 (m, 9H), 8.45 (bs, IH, D2O exchangeable), 8.88 (bs, IH, D2O exchangeable), 10.0 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3309(-NH-), 1628 (-C=0). MS m/z: 323.2 (M”). Example 11 Synthesis of 6-amino-l-(4-chlorophenyl)-2-phenylamino-lH-pyrimidin-4-one The title compound was prepared from 6-amino-2-methylthio-1 -(4-chlorophenyl)-lH-pyrimidin-4-one (2.0g, 7.48mmol) (obtained in preparation 6) and aniline (3.48g, 37.4mmol) by following the procedure described in example 1 (1.21g, 52%, purity 95.7% by HPLC), mp 216 - 222 °C. “H-NMR (DMS0-d6): 6 5.15 (s, IH), 6.97 - 7.02 (m, IH), 7.26 - 7.32 (m, 4H), 7.40 - 7,71 (m, 5H), 8.94 (s, IH, D2O exchangeable), 10.4 (bs, IH, DjO exchangeable). IR (KBr) cm': 3306, 1678 (-C-0). MS m/z: 313.1 (M”). Example 12 Synthesis of 6-amino-l-(4-bromophenyl)-2-phenylammo-lH-pyrimidiii-4-one The title compound was prepared from 6-amino-2-methylthio-l-(4-bromophenyl)-lH-pyrimidin-4-one (l.Og, 3.2mmol) (obtained in preparation 7) and aniline (0.57g, 6mmol) by following the procedure described in example 1 (0.6g, 52.5%, purity 92.1% by HPLC), mp 211 - 213 °C. 'H-NMR (DMSO-d”): d 5.1 (bs, IH), 6.9 - 7.0 (m, IH), 7.29 - 7.43 (m, 8H), 8.92 - 9.0 (bm, 2H, D2O exchangeable). IR (KBr) cm"“ 3320, 1633 (-C=0). MS m/z: 357/358.9 (M”). Example 13 Synthesis of l-(4-methylsulfanyl-phenyl)-6-phenyl-lH-pyrimidin-2,4-(lH)-dione A mixture of N-(4-methylsulfanyl-phenyl)-[N'-l-(3-phenyl)-l,3-diketone]urea (O.lg, 0,3mmol) (obtained in preparation 17) and p-toluenesulfonic acid (0.057g, O.Bmmol) in toluene (10ml) was refluxed with stirring for 4 hours. The reaction mixture was allowed to cool at room temperature, poured into water and extracted with ethylacetate. The ethylacetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was purified by column chromatography to yield the title compound (0.09g, 95.2%, mp 239 - 242 °C (decomposed), purity 98.10% by HPLC). 'H-NMR (DMSO - dg): 6 2.39 (s, 3H), 5.63 (s, IH), 7.07 - 7.10 (d, 2H), 7.14-7.17 (d, 2H), 7.22 - 7.24 (s, 5H), 11.54 (s, IH). IR (KBr) cm"': 3188, 3040 (-NH-), 1720, 1681 (-C=0). MS m/z: 311. KM""). Example 14 Synthesis of l-(4-methylsulfanyl-phenyl)-6-(4-methylphenyl)-lH-pyrimidin- 2,4-(lH)-dione The title compound was prepared from N-(4-methylsulfanyl-phenyl)-{N'-l-[3-(4-methylphenyl)]-l,3-diketone}urea (0.24g, 0.7mmol) (obtained in preparation 18) and p-toluenesulfonic acid (0.134g, 0.7mmol) in toluene (10ml) by refluxing for 2 hours and following the procedure described in example 13 (0.17g, 74.9%, mp 235 - 238 °C, purity 98.9% by HPLC). 'H-NMR (DMSO - dg): 5 2.20 (s, 3H), 2.40 (s, 3H), 5.59 (s, IH), 7.02 -7.17 (m, 8H), 11.53 (bs, IH). IR (KBr) cm"': 3180, 3051 (-NH-), 1693 (-C=0). MS m/z: 325.3 (M”). Example 15 Synthesis of 1 -(4-methylsulfanyI-phenyl)-6-(4-chlorophenyl)-l H-pyrimidin- 2,4-(lH)-dione The title compound was prepared from N-(4-methylsulfanyl-phenyl)-{N'-l-[3-(4-chlorophenyl)]-l,3-diketone}urea (0.33g, 0.91mmol) (obtained in preparation 19) in toluene (30ml) containing p-toluenesulfonic acid (0.294g, 1.6mmol) was refluxed for 9 hours by following the procedure described in example 13 (0.289g, 92.2%, mp 249 - 251 °C, purity 99.6% by HPLC). 'H-NMR (DMSO - dg): 5 2.41 (s, 3H), 5.67 (s, IH), 7.10 - 7.19 (m, 4H), 7.25 -7.33 (m, 4H), 11.5 (bs, IH). IR (KBr) cm-” 3178, 3054 (-NH-), 1691 (-C=0). MS m/z: 345 (M”). Example 16 Synthesis of l-(4-methylphenyl)-6-(4-methylsulfanyl-phenyi)-lH-pyrimidin- 2,4-(lH)-dione The title compound was prepared from N-(4-methylphenyl)-{N'-l-[3-(4-methylsulfanyl-phenyl)]-l,3-diketone}urea (0.24g, 0.7mmol) (obtained in preparation 13) and p-toluenesulfonic acid (0,134g, OJmmol) in toluene (10ml) by refluxing for 4 hours and following the procedure described in example 13 (0.186g, 82%, mp 266 - 268 “C, purity 99.8 % by HPLC). “H-NMR (DMSO -de): 8 2.20 (s, 3H), 2.38 (s, 3H), 5.60 (s, IH), 7.03 - 7.13 (m, 8H), 11.59 (bs, IH, D2O exchangeable). IR (KBr) cm-”: 3335 (-NH-), 1683 (-C=0). MS m/z: 325.2 (M"). Example 17 Synthesis of l-(4-bromophenyl)-6-(4-methylsulfanyl-phenyl)-lH-pyrimidin- 2,4-(lH)-dione The title compound was prepared from N-(4-bromophenyl)- {N' -1 - [3 -(4-methylsulfanyl-phenyl)]-l,3-diketone}urea (0.430g, 1.05mmol) (obtained in preparation 21) in toluene (10ml) containing p-toluenesulfonic acid (0.602g, 3mmol) was refluxed for 8 hours and following the procedure described in example 13 (0.151g, 36.8%, mp 282 - 285 °C, purity 97.8% by HPLC). “H-NMR (DMSO - de): 5 2.55 (s, 3H), 5.68 (s, IH), 7.08 - 7,01 (d, 2H), 7.15 - 7.17 (d, 2H), 7.20 - 7.22 (d, 2H), 7.48 - 7.50 (d, 2H), 11,58 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3155 (-NH-), 3022, 1712 (-C=0). MS m/z: 389 (M”). Example 18 Synthesis of l-(4-methylsulfonyl-phenyl)-6-phenyl-pyrimidin-lH-pyrimidin- 2,4-(lH)-dione Oxone (1.189g, 1.93mmol) in water (5ml) was added dropwise to a stirred suspension of 1 -(4-methylsulfanyl-phenyl)-6-phenyl-1 H-pyrimidin-2,4-( 1H)-dione (0.2g, 0.64mmol) (obtained according to the procedure described in example 13) in methanol (10ml) and stirring was continued for 3 hours at room temperature. Saturated sodium bicarbonate solution (20ml) was added to the reaction mixture and extracted with ethylacetate. The ethylacetate extract was washed with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was purified by column chromatography to yield the title compound (0.117g, 53.2%, mp 283 -287 °C (decompose), purity 96.5% by HPLC). “H-NMR (DMSO - d6): 8 3.18 (s, 3H), 5.72 (s, IH), 7.21 - 7.25 (s, 5H), 7.53 - 7.55 (d, 2H), 7.78 -7.8 (d, 2H), 11.68 (bs, IH). IR (KBr) cm"': 3033 (-NH-), 1719, 1684 (-C=0). MS m/z: 343.1 (M"). Example 19 Synthesis of 6-(4-methylphenyl)-l-(4-methylsulfonyl-phenyl)-lH-pyrimidin- 2,4-(lH)-dione The title compound was prepared from l-(4-methylsulfanyl-phenyl)-6-(4-methylphenyl)-lH-pyrimidin-2,4-(lH)-dione (0.3g, 0.92mmol) (obtained according to the procedure described in example 18) by following the procedure described in example 6 (0.244g, 74.2%, mp 285 - 288 °C, purity 99.4% by HPLC). 'H-NMR (DMSO - dfi): 5 2.19 (s, 3H), 3.20 (s, 3H), 5.68 (s, IH), 7.03 -7.05 (d, 2H), 7.05 - 7.09 (d, 2H), 7.53 - 7.55 (d, 2H), 7.80 - 7.82 (d, 2H), 11.65 (bs, IH, D2O exchangeable). IR (KBr) cm': 3008 (-NH-), 1716, 1681 (-C=0). MS m/z: 357.1 (M""). Example 20 Synthesis of 6-(4-chlorophenyl)-l-(4-methylsulfonyl-phenyl)-lH-pyrimidin- 2,4-(lH)-dione The title compound was prepared from l-(4-methylsulfanyl-phenyl)-6-(4-chlorophenyl)-lH-pyrimidin-2,4-(lH)-dione (0.5g, 1.4mmol) (obtained according to the procedure described in example 18) by following the procedure described in example 6 (0.326g, 59.3%, mp 294 - 298 °C, purity 97.6% by HPLC). “H-NMR (DMSO - de): 8 3.20 (s, 3H), 5.76 (s, IH), 7.24 - 7.26 (d, 2H), 7.32 - 7.34 (d, 2H), 7.55 - 7.57 (d, 2H), 7.82 -7.84 (d, IH), 11.71 (bs, IH, D2O exchangeable). IR (KBr) cm”“: 3437, 3170, 3049 (-NH-), 1690 (-C=0). MS m/z: 377.1 (M”). Example 21 Synthesis of 4-(2,6-dioxO"'3-phenyl-l,2,3,6-tetrahydro-pyrimidin-4-yl)- benzenesulfonamide The chlorosulfonic acid (1.18g, lOmmol) was added to a solution of 1,6-diphenyluracil (0.2g, 0.75mmol) (synthesized according to the procedure given in Harvey I. Skulnick, Heterocycles, 23, (7), ppl685, 1985) in chloroform (20ml) and refluxed for 2 hours. The reaction mixture was poured onto ice-water mixture and extracted with ethylacetate. The ethylacetate extract was washed with brine, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was taken in tetrahydrofuran (20ml) and treated with ammonia solution (1ml) under stirring. The reaction mixture was stirred for 1 hour and concentrated to dryness in vacuum. The product thus obtained was dissolved in ethylacetate, washed with water, brine and dried over anhydrous sodium sulphate. The ethylacetate extract was concentrated to dryness under reduced pressure and purified by column chromatography to yield the title compound (O.lg, 18.3%). mp : , “H-NMR (DMSO - de): 8 5.69 (s, IH), 7.21 - 7.26 (m, 5H), 7.36 - 7.46 (m, 4H), 7.65 - 7.72 (m, 2H), 11.63 (bs, IH). MS m/z: 344.1 (M”). Example22 Synthesis of 5-cyano-2-(4-chlorophenyl)-4-methylthio-l-(4-methylthio- phenyl)-l,6-dihydro-pyrimidin-6-one A mixture of ethyl 2-cyano-3,3-dimethylthioacrylate (1.345g, 6.2mmol) and N-(4-methylthio-phenyl)-4-chlorobenzamidine (1.7g, 6.2mmol) (obtained according to the procedure described in preparation 22) was heated at 110 -120 °C for 2 hours. The gummy mass thus obtained was purified by column chromatography to give the title compound (l.lg, yield 44.4%, purity 94.6% by HPLC), mp 206- 207 °C.'H-NMR (CDCI3): 5 2.47 (s, 3H), 2.66 (s, 3H), 6.99 -7.01 (d, 2H), 7.18-7.30 (m, 6H). IR (KBr) cm-': 2218(-CN), 1672 (-C=0). MS m/z: 400.1(M”). Example 23 Synthesis of 5-cyano-2-(4-fluorophenyl)-4-methylthio-l-(4-methylthio- phenyl)-l,6-dihydro-pyrimidin-6-one The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (1.25g, 5.76mmol) and N-(4-methylthio-phenyl)-4-fluorobenzamidine (1.50g, 5.76mmol) (obtained in preparation 23) according to the procedure described in example 22, (l.Sg, 81.8%, purity 99.4% by HPLC), mp 204-207 °C. 'H-NMR (CDCI3): 5 2.46 (s, 3H), 2.67 (s, 3H), 6.94 -7.01 (m, 4H), 7.17-7.26 (m, 2H), 7.35-7.38 (m, 2H). IR (KBr) cm-': 2218(-CN), 1678 (-C=0). MS m/z: 384 (M”) Example 24 Synthesis of 5-cyano-4-methylthio-l-(4-methylthio-phenyl)-2-phenyl-l,6-dihydro-pyrimidin-6-one The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (1.345g, 6.2mmol) and N-(4-methylthio-phenyl)benzamidine (1.50g, 6.2mmol) (obtained in preparation 24) by following the procedure described in example 22, (1.28g, yield 56.6%, purity 98.8% by HPLC), mp 204 - 205 °C. 'H-NMR (CDCI3): 8 2.45 (s, 3H), 2.67 (s, 3H), 6.99 - 7.01 (m, 2H), 7.15 -7.17 (m, 2H), 7.26 - 7.37 (m, 5H). IR (KBr) cm"': 2218 (-CN), 1682 (-C=0). MS m/z: 366 Example 25 Synthesis of 5-cyano-4-methylthio-l-(4-methylthio-phenyl)-2-(4- trifluoromethylphenyl)-l,6-dihy(lro-pyrimidiii-6-one The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (l.Og, 4.6mmol) and the N-(4-methylthio-phenyl)-4-trifluoromethylbenzamidine (1.50g, 4.8mmol) (obtained according to the procedure described in preparation 25) by following the procedure described in example 22, (1.6g, 80.1%, purity 99.3% by HPLC), mp 228 - 229 °C. 'H-NMR (CDCI3): 8 2.46 (s, 3H), 2.66 (s, 3H), 6.99 - 7.01 (d, 2H), 7.17-7.19 (d, 2H), 7.46 - 7.48 (d, 2H), 7.54 - 7.56 (d, 2H). IR (KBr) cm'“ 2215 (-CN), 1680 (-C=0). MS m/z: 434.2 (M”). Example 26 Synthesis of 5-cyano-l-(4-fluorophenyI)-4-methylthio-2-(4-methylthio- phenyI)-l,6-dihydro-pyrimidin-6-one The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (0.334g, 1.54mmol) and N-(4-fluorophenyl)-4-methylthiobenzamidine (0.40g, l,54mmol) (obtained in preparation 26) by following the procedure described in example 22, (0.32g, 54.3%, purity 99.2% by HPLC), mp 219 - 221 °C. “H-NMR (CDCI3): 5 2.46 (s, 3H), 2.68 (s, 3H), 7.05 - 7.12 (m, 6H), 7.23 -7.27 (m, 2H). IR (KBr) cm-”: 2218 (-CN), 1667 (-C=0). MS m/z: 384 (M”). Example 27 Synthesis of 5-cyano-l-(4-methylphenyl)-4-methylthio-2-(4-methylthio- phenyl)-l,6-dihydro-pyrimidin-6-one The title compound was prepared from ethyl 2-cyano-3,3"dimethylthioacrylate (0.848g, 3.9mmol) and N-(4-methylphenyl)-4-methylthiobenzamidine (l.Og, 3.9mmol) (obtained in preparation 27) by following the procedure described in example 22, (0.68g, 46%, purity 99.3% by HPLC), mp 196 - 198 “C. “H-NMR (CDCI3): 5 2.34 (s, 3H), 2.45 (s, 3H), 2,67 (s, 3H), 6.99 - 7.01 (m, 2H), 7.04 -7.06 (m, 2H), 7.14 - 7.18 (m, 2H), 7.26-7.28 (m, 2H). IR (KBr) cm'“ 2215 (-CN), 1688 (-C=0). MS m/z: 380.4 (M""). Example 28 Synthesis of 5-cyano-l-(4--inethylpheiiyl)-2-(4-methylsulphonyl-phenyl)-4- methylthio-l,6-dihydro-pyriinidin-6-one The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (0.378g, 1.74mmol) and N-(4-methylphenyl)-4-methylsulphonylbenzamidine (0.5g, 1.74mmol) (obtained in preparation 29) according to the procedure described in example 22, (0.43g, 59.6%, purity 99.1% by HPLC), mp 242 - 244 °C. “H-NMR (CDCI3): 6 2.34 (s, 3H), 2.65 (s, 3H), 3.04 (s, 3H), 6.95 - 6.97 (d, 2H), 7.15 - 7.17 (d, 2H), 7.51 - 7.54 (d, 2H), 7.82 -7.84 (d, 2H). IR (KBr) cm'“ 2217 (-CN), 1696 (-C=0). MS m/z: 412 (M”). Example 29 Synthesis of 5-carboxy-l-(4-methyIphenyl)-4-methylthio-2-(4-methylthio- phenyl)-l,6-dihydro-pyrimidin-6-one A mixture of 5-cyano-l-(4-methylphenyl)"4-methylthio-2-(4-methylthio-phenyl)-l,6"dihydro-pyrimidin-6-one (2.5g, 6.59mmol) (obtained according to the procedure described in example 6) and potassium hydroxide (40%, 25ml) solution was refluxed for 2 hours. The reaction mixture was poured onto ice- water, neutralised with dilute hydrochloric acid and filtered. The solid thus obtained was washed with water and dried to yield title compound (2.12g, 80.8%, purity 91.6% by HPLC), mp 173 • 175 °C. “H-NMR (CDCI3): 8 2.34 (s, 3H), 2.53 (s, 3H), 2.69 (s, 3H), 7.16 - 7.18 (d, 2H), 7.26 - 7.37 (m, 4H), 7.92 - 7.94 (d, 2H), 14.0 (s, IH, D2O exchangeable). IR (KBr) cm'“ 3311(-COOH), 1702(-C-O). MS m/z: 398.5 (M""). Example 30 Synthesis of 5,6-diphenyl-2-trifluoromethyl-pyrimidin-4-one 2,3-Diphenyl-3-[(trifluoromethyl)-amino]propenoic acid (2.0g, 5.9mol) (synthesized according to the procedure given in US 4987140) was refluxed in acetic anhydride (5ml) for 2 hours and allowed to cool to room temperature. The reaction mixture was cooled to -50 "“C to -60 °C then ammonia gas was passed until the solid separated out. The reaction mass was poured into water and extracted with ethyl acetate. The organic extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to give crude product, which was purified by column chromatography to afford the title compound (0.28g, 15 %, purity 99.58% by HPLC), mp 194 - 197 “C. “H-NMR (CDCI3): 5 7.23 - 7.39 (m, lOH). MS m/z: 317.2 (M”). Example 31 Synthesis of 5-phenyl-6-(4-methylsulfoiiylphenyl)-2-trifluoromethyl- pyrimidin-4-one The title compound was prepared from 2-phenyl-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (1.48g, 3,6mmol) (obtained according to the preparation 34) by following the procedure described in example 1 (0.22g, 15.6%, purity 92.11% by HPLC), mp 231 - 238 °C. H-NMR (DMSO-d”): 5 3.16 (s, 3H), 7.16 - 7.17 (m, 2H), 7.25 - 7.26 (m, 3H), 7.46 - 7.48 (m, 2H), 7.55 -7.77 (m, 2H). MS m/z: 395.2 (M”). Example 32 Synthesis of 5-(4-chlorophenyl)-6-(4-methylsulfonyIphenyl)-2- trifluoromethyl-pyrimidin-4-one The title compound was prepared from 2-(4-chlorophenyl)-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (1.5g, 3.4mmol) (obtained according to the procedure given in preparation 35) by following the procedure described in example 1 (0.24g, 17%, purity 95.45% by HPLC), mp 227 - 230 “C. “H-NMR (DMS0-d6): 5 3.20 (s, 3H), 7.27 - 7.30 (d, 2H), 7.40 - 7.42 (d, 2H), 7.54 - 7.56 (d, 2H), 7.86 - 7.88 (d, 2H), 13.9 (bs, IH, D2O exchangeable). MS m/z: 429.2 (M”). The title compound was prepared from 2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (2.52g, 6mmol) (obtained according to the procedure given in preparation 36) by following the procedure described in example 1 (0.7g, 29.1%, purity 99.64% by HPLC), mp 271 - 274 °C. H-NMR (DMS0-d6): 5 3.21 (s, 3H), 7.16 - 7.28 (m, 2H), 7.29 -7.32 (m, 2H), 7.53 - 7.55 (d, 2H), 7.86 - 7.87 (d, 2H), 13.9 (bs, IH, D2O exchangeable). MS m/z: 413 (M"“). A stirred mixture of ethyl-3-amino-2,3-diphenyl-2-propenoate (4.0g, 15mmol) (synthesized according to the procedure given in US 4987140) and thiourea (1.14g, ISmmol) was heated at 180 - 190 "“C for 2 hours. The reaction mixture was allowed to cool to room temperature, poured into water, filtered and dried. The soUd thus obtained was purified by washing with ether and finally by methanol to give the title compounds (0.25g, 6 %, purity 98.25% by HPLC),.mp 276 - 278 °C. “H-NMR (DMSO-de): 8 7.00 - 7.31 (m, lOH), 12.54 (s, IH, D2O exchangeable), 12.68 (s, IH, D2O exchangeable). MS m/z: 281.2 (M”). Example 35 Synthesis of 6-(4-methylsulfonylphenyl)-5-phenyI-2-thiouracil The title compound was prepared fi'om ethyl-3 -amino-3 -(4-methylsulfonylphenyl)-2-phenyl-2"propenoate (1.12g, 3.25mmol) (obtained according to the preparation 31) and thiourea (0,5g, 6.5mmol) by following the procedure described in example 5 (O.lg, 9%, purity 97. 42 % by HPLC), mp 122 - 125 °C. “H-NMR (DMS0-d6): 6 3.2 (s, 3H), 7.03 - 7.04 (m, 2H), 7.17 (bs, 3H), 7.51 ■ 7.53 (d, 2H), 7.81 - 7.83 (d, 2H), 12.64 (s, IH, D2O exchangeable), 12.76 (s, IH, D2O exchangeable). MS m/z: 359 (M”), Example 36 Synthesis of 6-(4-chlorophenyI)-5-phenyl-2-thiouracil A stirred mixture of ethyl 3-(4-chlorophenyl)-2-phenyl-3-oxopropanoate (7.5g, 24.8mol) (obtained according to the procedure given in preparation 37) and thiourea (1.88g, 24.8mol) was heated at 180 - 190 °C for 2 hours. The reaction mixture was allowed to cool to room temperature and triturated with acetone. The resultant mixture was poured onto ice-water mixture with vigorous stirring and filtered. The solid was treated with 10% aqueous potassium hydroxide solution under vigorous stirring and filtered. The clear filtrate was cooled to 0- 5 °C and acidified to pH 6 by dilute hydrochloric acid. The precipitate thus obtained was filtered, washed thoroughly with water and dried to furnish the title compound (2.2g, 28.1%, purity 96.82% by HPLC), mp 262 - 265 °C. “H-NMR (DMSO-da): 8 7.00 - 7.03 (d, 2H), 7.15 - 7.18 (m, 3H), 7.22 - 7.25 (d, 2H), 7.32 - 7.34 (d, 2H), 12.57 (s, IH, D2O exchangeable), 12.70 (s, IH, D2O exchangeable). MS m/z:315(M”). The title compound was prepared from ethyl 3-(4-methylphenyl)-2-phenyl-3-oxopropanoate (7.0g, 24.8mmol) (obtained according to the procedure given in preparation 38) and thiourea (1.89g, 24,8mmol) by following the similar procedure described in example 7 (3.3g, 44.6%, purity 93.64% by HPLC), mp 248 - 251 °C. “H-NMR (DMS0-d6): 5 2.27 (s, 3H), 6.99 - 7.14 (m, 9H), 12.30 (s, IH, D2O exchangeable), 12.55 (s, IH, D2O exchangeable). MS m/z: 295.2 (M”). The title compound was prepared from ethyl 2-phenyl-3-(4-trifluoromethylphenyl)-3-oxopropanoate (4.5g, 13.4mmol) (obtained according to the preparation 39) and thiourea (1.02g, 13.4mmol) by following similar procedure as described in example 7, (0.7g, 15 %, purity 98.53% by HPLC), mp 281 - 284 °C. “H-NMR (DMSO-dg): 5 7.02 - 7.04 (d, 2H), 7.14 - 7.19 (m, 3H), 7.45 - 7.47 (d, 2H), 7.63 - 7.65 (d, 2H), 12.63 (s, IH, D2O exchangeable), 12.75 (s, IH, D2O exchangeable). MS m/z: 349.1 (M”). The title compound was prepared from ethyl 2-(4"Chlorophenyl)-3-phenyl-3-oxopropanoate (6.5g, 21.5mol) (obtained according to the procedure given in preparation 40) and thiourea (1.64g, 21.5mmol) by following the procedure described in example 7 (2.0g, 30%, purity 95.81% by HPLC), mp 307 - 310 °C. “H-NMR (DMS0-d6): 5 7.02 - 7.04 (d, 2H), 7.21 - 7,28 (m, 7H), 12.59 (s, IH, D2O exchangeable), 12.72 (s, IH, D2O exchangeable). MS m/z: 315 (M”). The title compound was prepared from ethyl 2-(4-methylthiophenyl)-3-phenyl"3-oxopropanoate (5.5g, 17.5mmol) (obtained according to the procedure given in preparation 41) and thiourea (1.33g, 17.5mmol) by following the procedure described in example 7 (1.5g, 26.3%, purity 96.8% respectively by HPLC), mp 286 - 290 °C. “H-NMR (DMS0-d6): 5 2.40 (s, 3H), 6.93 - 6.95 (d, 2H), 7.0 -7.02 (d, 2H), 7.20 - 7.33 (m, 5H), 12.46 (s, IH, D2O exchangeable), 12.62 (s, IH, D2O exchangeable). MS m/z: 327.2 (M”). Example 41 Synthesis of 5-(4-methoxyphenyl)-6-phenyl-2-thiouracil The title compound was prepared from ethyl 2-(4-methoxyphenyl)-3-phenyl-3-oxopropanoate (2.0g, 67mmol) (obtained according to the procedure given in preparation 42) and thiourea (0.5Ig, 67mmol) by following the procedure described in example 7 (0.5 g, 24 %, purity 91.74% by HPLC), mp 279 -282 °C. “H-NMR (DMS0-d6): 8 3.66 (s, 3H), 6.70 - 6.73 (m, 2H), 6.91 - 6.93 (m, 2H), 7.20 - 7.32 (m, 5H), 12.48 (s, IH, D2O exchangeable), 12.64 (s, IH, D2O exchangeable). MS m/z: 311.1 (M"“). The title compound was prepared from ethyl 2-(4-chlorophenyl)-3-(4-methylphenyl)-3-oxopropanoate (7.5g, 23.7mmol) (obtained according to the procedure given in preparation 43) and thiourea (1.8g, 23.7mmol) by following the procedure described in example 7 (4.5g, 58%, purity 93.06% by HPLC), mp 265 - 268 °C. “H-NMR (DMSO-dg): 8 3.16 (s, 3H), 7.02 - 7.04 (d, 2H), 7.09 (s, 4H), 7.23 - 7.25 (d, 2H), 12.51 (s, IH, D2O exchangeable), 12.70 (s, IH, D2O exchangeable). MS m/z: 329.2 (M”). A solution of hydrogen peroxide (30% v/v, 20nil) was added dropwise to a stirred solution of 6-(4-chlorophenyl)-5-phenyl-2-thiouracil (2.0g, 6.35mmol) (obtained according to procedure described in example 7) in ethanolic potassium hydroxide (10%w/v, 40ml) at 50 °C. The reaction mixture was stirred for 3 hours at 60 °C, allowed to cool to 0-5 °C and filtered. The solid obtained was dissolved in water and acidified with dilute hydrochloric acid to pH 6 under cold condition. The precipitate thus separated was filtered, washed thoroughly with water and dried. The crude product was purified by column chromatography to yield the title compound (0.73g, 38.2%, purity 95.65% by HPLC), mp 305 - 306 “C. H-NMR (DMS0-d6): 5 6.97 - 6.99 (d, 2H), 7.14 - 7.20 (m, 5H), 7.31 - 7.33 (d, 2H), 11.14 (s, IH, D2O exchangeable), 11.2 (s, IH, D2O exchangeable). MS m/z: 299.1 (M”), The title compound was prepared from 6-(4-methylphenyl)-5-phenyl-2-thiouracil (2.9g, 9.8mmol) (obtained according to the procedure described in example 8) in ethanolic potassium hydroxide solution (10% w/v, 100ml) by following the procedure described in example 14 (1.2g, 44 %, purity 98.71% by HPLC), mp 246 - 249 °C. “H-NMR (DMS0-d6): 6 2.23 (s, 3H), 6.97 - 7.10 (m, 9H), 11.03 (s, IH, D2O exchangeable), 11.30 (s, IH, D2O exchangeable). MS m/z: 279.1 (M”). The title compound was prepared from 6-(4-trifluoromethylphenyl)-5-phenyl-2-thiouracil (0.4g, ll.Smol) (obtained according to the procedure described in example 9) in ethanolic potassium hydroxide solution (10% w/v, 15ml) by following the procedure described in example 14 (O.lg, 26.2%, purity 97.66% by HPLC), mp 258 - 264 °C. “H-NMR (DMS0-d6): 8 6.99 - 7.01 (d, 2H), 7.13 -7.18 (m, 3H), 7.43 - 7.45 (d, 2H), 7.64 - 7.66 (d, 2H), 11.22 (s, IH, D2O exchangeable), 11.42 (s, IH, D2O exchangeable). MS m/z: 333.1 (M”). Example 46 Synthesis of 5-(4-chlorophenyl)-6-phenyl-uracil The title compound was prepared from 5-(4-chlorophenyl)-6-phenyl-2-thiouracil (5.0g, 15.9mmol) (obtained according to the procedure described in example 10) in ethanolic potassium hydroxide solution (10% w/v, 50ml) by following the procedure described in example 14 (1.7g, 35.5%, purity 96.47% by HPLC), mp 326 - 330 °C. “H-NMR (DMSO-de): 8 6.98 - 7.01 (d, 2H), 7.19 - 7.33 (m, 7H), 11.18 (s, IH, D2O exchangeable), 11.39 (s, IH, D2O exchangeable). MS m/z: 299.2 (M”). The title compound was prepared from 5-(4-methylthiophenyl)-6-phenyl-2-thiouracil (1.5g, 4.6mmol) (obtained according to the procedure described in example 11) in ethanohc potassium hydroxide solution (10% w/v, 20ml) by following the procedure described in example 14 (0.48g, 33.7%, purity 94.98% by HPLC), mp 275 - 278 °C. “H-NMR (DMS0-d6): 5 2.39 (s, 3H), 6.91 - 6.93 (d, 2H), 7.02 -7.04 (d, 2H), 7.20 - 7.22 (m, 2H), 7.27 - 7.32 (m, 3H), 11,12 (s, IH, D2O exchangeable), 11.33 (s, IH, D2O exchangeable). MS m/z: 311.1 (M”). The title compound was prepared from 5-(4-methoxyphenyl)-6-phenyl-2-thiouracil (0.8g, 2.3mmol) (obtained according to the procedure described in example 12) in ethanolic potassium hydroxide solution (10% w/v, 30ml) by following the procedure described in example 14 (0.54g, 71.2%, purity 97.85% by HPLC), mp 276 - 279 °C. “H-NMR (DMSO-dfi): 8 3.66 (s, 3H), 6.70 - 6.72 (d, 2H), 6,88 - 6.90 (d, 2H), 7.18 - 7.31 (m, 5H), 11.06 (s, IH, D2O exchangeable), 11.30 (s, IH, D2O exchangeable). MS m/z: 295.2 (M”). The title compound was prepared from 5-(4-chlorophenyl)-6-(4-methylphenyl)-2-thiouracil (4,5g, 13.7mmol) (obtained according to the procedure described in example 13) in ethanoUc potassium hydroxide solution (10% w/v, 50ml) by following the procedure described in example 14 (0.59g, 14%, purity 99.86% by HPLC), mp 281 - 283 °C. “H-NMR (DMS0-d6): 5 2.25 (s, 3H), 6.99 - 7.01 (m, 2H), 7.06 - 7.09 (m, 4H), 7.21 - 7.24 (m, 2H), 11.12 (s, IH, D2O exchangeable), 11.36 (s, IH, D2O exchangeable). MS m/z: 313 (M”). Described below are the examples of pharmacological assays used for finding out the efficacy of the compounds of the present invention wherein their protocols and results are provided. Rat Carrageenan Paw Edema Test The carrageenan paw edema test was performed as described by Winter et al (Proc.Soc. Exp Biol Me., Ill, 544, 1962). Male Wistar rats were selected and the body weight were equivalent within each group. The rats were fasted for eighteen hours with free access to water. The rats were dosed orally with the test compound suspended in vehicle containing 0.5% methylcellulose. The control rats were administered the vehicle alone. After one hour the rats were injected with 0.1 ml of 1% Carrageenan solution in 0.9% saline into the sub plantar surface of the right hind paw. Paw thickness was measured using vemier calipers at 0 time, after 2 and 3 hours. The average of foot swelling in drug treated animals was compared with that of control animals. Anti-inflammatory activity was expressed as the percentage inhibition of edema compared with control group [Arzneim-Forsch/Drug Res 43(1), 1, 44-50,1993; Ottemess and Bliven, Laboratory Models for Testing NSAIDs, In Non-Steroidal Anti-Inflammatory Drugs, (J. Lombardino, ed.l985)]. The data of the selected compounds in this invention are summarized in Table I. In order to evaluate their role on the ulcer formation, the animals were sacrificed by cervical dislocation, the stomach removed and flushed with 1% formalin (10ml). The stomach was opened along the greater curvature. The haemorrhagic puncta and sulci were identified macroscopically. The presence or absence of stomach lesions was scored. The incidence of ulceration was calculated from the number of rats that showed atleast one gastric ulcer or haemorrhagic erosion. In vitro gvaluation of Cycloxvgenase-2 (COX-2) inhibition activity The compounds of this invention exhibited in vitro inhibition of COX-2. The COX-2 inhibition activity of the compounds illustrated in the examples was determined by the following method. Human Whole Blood Assay Human whole blood provides a protein and cell rich milieu appropriate for the study of biochemical efficacy of anti-inflammatory compounds such as selective COX-2 inhibitors. Studies have shown that normal human blood does not contain COX-2 enzyme. This is correlating with the observation that COX-2 inhibitors have no effect on prostaglandin E2 (PGE2) production in normal blood. These inhibitors are active only after incubation of human blood with lipopolysaccharide (LPS), which induces COX-2 production in the blood. Method Fresh blood was collected in tubes containing potassium EDTA by vein puncture from male volunteers. The subjects should have no apparent inflammatory conditions and not taken NSAIDs for atleast 7 days prior to blood collection. Blood was treated with aspirin in vitro (lO”g/ml, at time zero) to inactivate COX-1, and then with LPS (10”g/ml) along with test agents or vehicle. The blood was incubated for 24 h at 37 “C, after which the tubes were centrifuged, the plasma was separated and stored at -80 °C (J Pharmacol Exp Ther 271, 1705, 1994; Proc Natl Acad Sci USA 96, 7563, 1999). The plasma was assayed for PGE2 using Cayman ELISA kit as per the procedure outlined by the manufacturer (Cayman Chemicals, Ann Arbor, USA). The plasma was also tested for TNF-a, IL-ljS, and IL-6 using appropriate human ELISA kit as per the procedure of manufacturer (Cayman Chemicals, Ann Arbor, USA). Representative results of COX-2 inhibition are shown in Table IL Tumor Necrosis Factor Alpha (TNF-a) This assay determines the effect of test compounds on the production of TNF-a from human monocytes. Compounds were tested for their ability to downregulate the production of TNF-a in activated monocytes. Test compounds were incubated for three, six and twenty four hours with human monocytes, Lipopolysaccharide was used to stimulate the monocytes. The level of TNF-a was quantitated using Enzyme-Linked Immunosorbent assay performed in a 96 well format. Representative results of TNF-a inhibition are shown in Table III. InterIeukin-6(IL-6) This assay determines the effect of test compounds on the production of IL-6 from human monocytes. Compounds are tested for their abiUty to downregulate the production of IL-6 in activated monocytes. Test compounds were incubated for three, six and twenty four hours with human monocytes. Lipopolysaccharide was used to stimulate the monocytes. The level of Interleukin-6 is quantitated using Enzyme-Linked Immunosorbent assay performed in a 96 well format. Representative results of IL-6 inhibition are shown in Table IV. Inhibitory Action on Adjuvant Arthritis Compounds were assayed for their activity on rat adjuvant induced arthritis according to Theisen-Popp et al., (Agents Actions 42, 50-55,1994). Six - seven weeks old, Wistar rats were weighed, marked and assigned to groups [a negative control group in which arthritis was not induced (non-adjuvant control), a vehicle-treated arthritis control group, test substance treated arthritis group]. Adjuvant induced arthritis was induced by an injection of Mycobacterium butyricum (Difco) suspended in liquid paraffin into the sub-plantar region of the right hind paw (J Pharmacol Exp Ther, 284, 714, 1998). Body weight, contralateral paw volumes were determined at various days (0, 4, 14, 21) for all the groups. The test compound or vehicle was administered orally beginning post injection of adjuvant and continued for 21 days. On day 21, body weight and paw volume of both right and left hind paw, spleen, and thymus weights were determined. In addition, the radiograph of both hind paws was taken to assess the tibio-tarsal joint integrity. Hind limb below the stifle joint was removed and fixed in 1% formalin saline. At the end of the experiment, plasma samples were analysed for cytokines, interleukins and prostaglandins. The presence or absence of lesions in the stomachs was also observed. Two-factor ('treatment' and 'time') Analysis of Variance with repeated measures on 'time' were applied to the % changes for body weight and foot volumes. A post hoc Dunnetf s test was conducted to compare the effect of treatments to vehicle. A one-way Analysis of Variance was applied to the thymus and spleen weights followed by the Dunnett's test to compare the effect of treatments to vehicle. Dose-response curves for % inhibition in foot volumes on days 4, 14 and 21 were fitted by a 4-parameter logistic function using a nonlinear Least Squares* regression. ID50 was defined as the dose corresponding to a 50% reduction from the vehicle and was derived by interpolation from the fitted 4-parameter equation In-vitro Anti-Cancer activity The compounds of the present invention were also tested for anticancer activity. Each test compound was screened against a battery of 60 human cell lines obtained from eight organs. The cell suspensions were diluted according to the particular cell type and the target cell density (5000-40,000 cells per well based on cell growth characteristics) was added into 96-well micro titer plates. Inoculates were allowed a pre-incubation period of 24 h at 37 °C for stabilization. Dilutions at twice the intended test concentrations were added at time zero in 100 \|il aliquots to micro titer plate wells. Usually test compounds were evaluated at five 10-fold dilutions. The highest well concentration used in the test is 10""* M. The cells were then incubated in the presence of the test compound for further 48 h in 5% CO2 atmosphere and 100% humidity. After completion of the incubation period the adherent cells were fixed to the plate by means of trichloroacetic acid. After three to five times washing, the cell layer was treated with the protein stain Sulforhodamine B. The optical density, which is proportional to protein mass, was then read by spectrophotometer plate readers at a wavelength of 515 nm. The anticancer activity is shown in figures 1-4. Brief description of the figures Figures 1 and 2 : Inhibition of cell proliferation in MCF-7 breast cancer cells Figures 3 and 4 : Inhibition of cell proliferation in MDA-MB-231 breast cancer cells We Claim: 1. Novel amino substituted pyrimidinone derivatives of the formula (I) their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; Y represents a bond or NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent hydrogen, SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, subfamily, alkoxyalkyl groups or carboxylic acids or its derivatives; R’ represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR’, wherein R’ represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2. 2. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, wherein the ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl, benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like. 3. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, which are selected from : 6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one; 6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-bromophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Ainino-2-(4-methylthio-phenylamino)-1 -(4-methylthiophenyl)-1 H-pyrimidin-4- one; 6-Amino-1 -(4-methylphenyl)-2-(4-methylthio-phenylamino)-1 H-pyrimidin-4- one; 6-Amino-2-(4-methylsulfonyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylphenyl)-1 H-pyrimidin-4- one; 4-(6-Amino-4-oxo-1 -phenyl-1,4-dihydro-pyrimidin-2-ylamino)- benzenesulfonamide; 4-(6-Amino-4-oxo-1 -(4-methyl-phenyl)-1,4-dihydro-pyrimidin-2-ylamino)- benzenesulfonamide; 6-Amino-2-phenylamino-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-2- phenylamino-1 -(4-chloropyridin-2-yl)-1 H-pyrimidin-4-one and 6-Amino-2-phenylamino-1-(4-bromopyridin-2-yl)-1 H-pyrimidin-4-one; 4. A process for the preparation of novel amino substituted pyrimidinone derivatives of the formula (I) groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2. 2. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, wherein the ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl, benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like. 3. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, which are selected from : 6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one; 6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-bromophenyl)"2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or Q Q heteroaryl; Y represents NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent hydrogen, SR’, wherein R’ represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R’ represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR’, wherein R’ represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2, which comprises, reacting compound of formula (la) wherein any one of R’ or R’ represent SR’, wherein R’ represents alkyl or aryl and the other R or R may be same or different and independently represent hydrogen or S(0)pR , where p is 1 or 2, R represents alkyl, amino or aryl and all other symbols are as defined in claim 1, to novel amino substituted pyrimidinone derivatives of the formula (I) wherein any one of R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl group using an oxidizing agent 6. A process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) as claimed in claim 1, wherein any one of the group R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl and the other R or R represent hydrogen or SR , wherein R’ represents alkyl or aryl and all other symbols are as defined in claim 1, to novel amino substituted pyrimidinone derivatives of the formula (I) wherein any one of R’ or R’ represent S(0)pR’ where p is 1 or 2, R’ represents amino group. 7. A process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) as claimed in claim 1, V wherein either of R and R represent S(0)pR , where R represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Ic) wherein all symbols are as defined in claim 1 wherein either of R and R represents hydrogen; with chlorosulfonic acid followed by ammonia. 8.A pharmaceutical composition, which comprises a compound of formula (I) as defined in claim 1 together with a pharmaceutically acceptable carrier, diluent, excipient or solvate.

Full Text

Field of the Invention
The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I).

The present invention also provides a process for the preparation of the above said novel amino substituted pyrimidinone derivatives of the formula (I) pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them.
The novel amino substituted pyrimidinone derivatives of the present invention are useful for the treatment of inflammation and immunological diseases. Particularly the compounds of the present invention are useful for the treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-ip, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteophorosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis;

cancer; ischemic-induced cell damage; pancreatic p cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes; bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection; and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster vimses.
Background of Invention
It has been reported that Cyclooxygenase enzyme exists in three isoforms, namely, COX-1, COX-2 and COX-3. COX-1 enzyme is essential and primarily responsible for the regulation of gastric fluids whereas COX-2 enzyme is present at the basal levels and is reported to have a major role in the prostaglandin synthesis for inflammatory response. These prostaglandins are known to cause inflammation in the body. Hence, if the synthesis of these prostaglandins is stopped by way of inhibiting COX-2 enzyme, inflammation and its related disorders can be treated. COX-3 possesses glycosylation-dependent cyclooxygenase activity. Comparison of canine COX-3 activity with murine COX-1 and COX-2 demonstrated that this enzyme is selectively inhibited by analgesic/antipyretic drugs such as acetaminophen, phenacetin, antipyrine, and dipyrone, and is potently inhibited by some nonsteroidal antiinflammatory drugs. Thus, inhibition of COX-3 could represent a primary central mechanism by which these drugs decrease pain and possibly fever. Recent reports show that inhibitors

of COX-1 enzyme causes gastric ulcers, where as selective COX-2 and COX-3 enzyme inhibitors are devoid of this function and hence are found to be safe.
The present invention is concerned with treatment of immunological diseases or inflammation, notably such diseases are mediated by cytokines or cyclooxygenase. The principal elements of the immune system are macrophages or antigen-presenting cells, T cells and B cells. The role of other immune cells such as NK cells, basophils, mast cells and dendritic cells are known, but their role in primary immunologic disorders is uncertain. Macrophages are important mediators of both inflammation and providing the necessary "help" for T cell stimulation and proUferation. Most importantly macrophages make IL-1, IL-12 and TNF-a all of which are potent pro-inflammatory molecules and also provide help for T cells. In addition, activation of macrophages results in the induction of enzymes, such as cyclooxygenase-2 (COX-2) and cyclooxygenase-3 (COX-3), inducible nitric oxide synthase (iNOS) and production of free radicals capable of damaging normal cells. Many factors activate macrophages, including bacterial products, superantigens and interferon gamma (IFN y). It is believed that phosphotyrosine kinases (PTKs) and other undefined cellular kinases are involved in the activation process.
Cytokines are molecules secreted by immune cells that are important in mediating immune responses. Cytokine production may lead to the secretion of other cytokines, altered cellular function, cell division or differentiation. Inflammation is the body's normal response to injury or infection. However, in inflammatory diseases such as rheumatoid arthritis, pathologic inflammatory processes can lead to morbidity and mortality. The cytokine tumor necrosis factor-alpha (TNF-a) plays a central role in the inflammatory response and has been targeted as a point of intervention in inflammatory disease. TNF-a is a

polypeptide hormone released by activated macrophages and other cells. At low concentrations, TNF-a participates in the protective inflammatory response by activating leukocytes and promoting their migration to extravascular sites of inflammation (Moser et al, J Clin Invest, 83, 444-55,1989). At higher concentrations, TNF-a can act as a potent hydrogen and induce the production of other pro-inflammatory cytokines (Haworth et al., Eur J Immunol, 21, 2575-79, 1991; Brennan et a/.. Lancet, 2, 244-7, 1989). TNF-a also stimulates the synthesis of acute-phase proteins. In rheumatoid arthritis, a chronic and progressive inflammatory disease affecting about 1 % of the adult U.S. population, TNF-a mediates the cytokine cascade that leads to joint damage and destmction (Arend et al., Arthritis Rheum, 38, 151-60,1995), Inhibitors of TNF-a, including soluble TNF receptors (etanercept) (Goldenberg, Clin Ther, 21, 75-87, 1999) and anti-TNF-a antibody (infliximab) (Luong et aL, Ann Pharmacother, 34, 743-60, 2000), have recently been approved by the U.S. Food and Drug Administration (FDA) as agents for the treatment of rheumatoid arthritis.
Elevated levels of TNF-a have also been implicated in many other disorders and disease conditions, including cachexia, septic shock syndrome, osteoarthritis, inflammatory bowel disease such as Crohn's disease and ulcerative colitis etc.
Elevated levels of TNF-a and/or IL-1 over basal levels have been implicated in mediating or exacerbating a number of disease states including rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; pancreatic (5 cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis;

anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes; bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection. HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses (including HSV-1, HSV-2), and herpes zoster are also exacerbated by TNF-a.
It can be seen that inhibitors of TNF-a are potentially useful in the treatment of a wide variety of diseases. Compounds that inhibit TNF-a have been described in several patents.
Excessive production of IL-6 is implicated in several disease states, it is highly desirable to develop compounds that inhibit IL-6 secretion. Compounds that inhibit IL-6 have been described in U.S. Pat. Nos. 6,004,813; 5,527,546 and 5,166,137.
The cytokine IL-lp also participates in the inflammatory response. It stimulates thymocyte proliferation, fibroblast growth factor activity, and the release of prostaglandin from synovial cells. Elevated or unregulated levels of the cytokine IL-ip have been associated with a number of inflammatory diseases and other disease states, including but not limited to adult respiratory distress syndrome, allergy, Alzheimer's disease etc. Since overproduction of IL-lp is associated with numerous disease conditions, it is desirable to develop compounds that inhibit the production or activity of IL-ip.
In rheumatoid arthritis models in animals, multiple intra-articular injections of IL-1 have led to an acute and destructive form of arthritis (Chandrasekhar et al.. Clinical Immunol Immunopathol. 55, 382, 1990). In studies using cultured rheumatoid synovial cells, IL-1 is a more potent inducer of stromelysin than TNF-a. (Firestein, Am. J. Pathol. 140, 1309, 1992). At sites of

local injection, neutrophil, lymphocyte, and monocyte emigration has been observed. The emigration is attributed to the induction of chemokines (e.g., IL-8), and the up-regulation of adhesion molecules (Dinarello, Eur. Cytokine Netw. 5, 517-531, 1994).
In rheumatoid arthritis, both IL-1 and TNF-a induce synoviocytes and chondrocytes to produce coUagenase and neutral proteases, which leads to tissue destruction within the arthritic joints. In a model of arthritis (collagen-induced arthritis (CIA) in rats and mice) intra-articular administration of TNF-a either prior to or after the induction of CIA led to an accelerated onset of arthritis and a more severe course of the disease (Brahn et al., Lymphokine Cytokine Res. 11, 253, 1992; and Cooper, Clin. Exp. Immunol. 898, 244, 1992).
IL-8 has been implicated in exacerbating and/or causing many disease states in which massive neutrophil in filtration into sites of inlammation or injury (e.g., ischemia) is mediated chemotactic nature of IL-8, including, but not limited to, the following: asthma, inflammatory bowl disease, psoriasis, adult respiratory distress syndrome, cardiac and renal reperfusion injury, thrombosis and glomerulonephritis. In addition to the chemotaxis effect on neutrophils, IL-8 has also has ability to activate neutrophils. Thus, reduction in IL-8 levels may lead to diminished neutrophil infiltration.
Few prior art reference which disclose the closest pyrimidine compounds are given here:
i) US patent Nos. 6,420,385 and 6,410,729 disclose novel compounds of formula (Ila)

X is O, S or NR”; R” represents -Y or -Z--Y, and R"“ represents -Z-Y; provided that R"“ is other than a substituted-aryl, (substituted-aryl)methyl or (substituted-aryl)ethyl radical; wherein each Z is independently optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, aryl or heteroaryl; Y is independently a hydrogen; halo, cyano, nitro, etc., R” is independently a hydrogen, optionally substituted alkyl, alkenyl, alkynyl etc., R”“ and R”“ are each independently represent optionally substituted aryl or heteroaryl. An example of these compounds is shown in formula (lib)

R is a substituted or unsubstituted aryl group or a substituted or unsubstituted
heteroaromatic group (e.g. a heteroaromatic ring structure having four to five
carbon atoms and one heteroatom selected from the group consisting of nitrogen,
sulfur and oxygen); R is an alkyl, haloalkyl, polyhaloalkyl, haloalkenyl,
polyhaloalkenyl, alkenyl, alkynyl, haloalkynyl, polyhaloalkynyl, alkenynyl,
alkoxyalkyl, dialkoxyalkyl, haloalkoxyalkyl, oxoalkyl, trimethylsilylalkynyl,
cyanoalkyl or aryl group; R” is a hydrogen, halo, acyl, alkyl, alkenyl, alkynyl,
alkoxy, alkylthio, alkoxyalkyl, alkoxyimino, alkoxycarbonylalkyl, dialkoxyalkyl,
formyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, hydroxyalkyl,
hydroxyimino, polyhaloalkyl, polyhaloalkenyl, polyhaloalkynyl, polyhaloalkoxy,
trimethylsilylalkynyl, alkoxyalkoxy, aminocarbonylalkyl,
alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, cyanoalkyl, hydroxy or cyano group; and R” is a hydrogen, halo, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkylthio, polyhaloalkyl,

polyhaloalkenyl, polyhaloalkynyl, polyhaloalkoxy, polyhaloalkylthio, cycloalkyl, aryl, aryloxy, heterocyclyl, aralkyl, alkylamino, dialkylamino, dialkylaminocarbonyl, or cyano group; and X is oxygen or sulfiir. An example of these compounds is shown in formula (Ilf)

Objective of the Invention
We have focused our research to identify selective COX-2 and COX-3 inhibitors which are devoid of any side effects, normally associated with antiinflammatory agents. Our sustained efforts have resulted in novel substituted pyrimidinone derivatives. The derivatives may be useful in the treatment of inflammation and immunological diseases. Particularly the compound of the present invention are useful for the treatment of inflammation and immunological diseases those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-lp, IL-8 and cyclooxygenase such as COX-2 and COX-3. The compounds of the present invention are also useful in the treatment of rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic p cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; asthma; muscle degeneration; cachexia; type I and type II diabetes;

bone resorption diseases; ischemia reperfusion injury; atherosclerosis; brain trauma; multiple sclerosis; cerebral malaria; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection; and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses.
Summary of the Invention
The present invention relates to novel amino substituted pyrimidinone derivatives of the formula (I)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; Y represents a bond or NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent
ft fi n n
hydrogen, SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl,

alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2,
Yet another embodiment of the present invention there is provided a novel pyrimidone derivatives of the formula (II)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R represents SR , or S(0)pR ; R represents hydrogen, SR , or
R 7 S
S(0)pR , wherein R represents alkyl or aryl; R represents alkyl, amino or aryl
T A
group; and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylslfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives;

R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, aryl, aralkyl, haloalkyl, acyl, alkoxy, aryloxy, aralkoxy, heteroaryl, heterocyclyl, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2.
Yet another embodiment of the present invention there is provided a novel pyrimidinedione derivatives of the formula (III)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, SR”, wherein R” represents alkyl or aryl; S(0)pR”, wherein R” represents alkyl,
O A
amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro,

cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR , wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2.
Yet another embodiment of the present invention there is provided a novel diaryl pyrimidinedione derivatives of the formula (IV)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R' and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl, sulfamoyl; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl.

haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, haloalkyl, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, arylalkyl, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups or R” together with R form a double bond; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, amino, alkyl, haloalkyl, acyl, monoalkylamino, dialkylamino, arylamino or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups or R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; R” represents hydrogen, haloalkyl, hydroxyl, formyl, cyano, nitro, nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, arylalkyl, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2.
Detailed Description of the Invention Suitable ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl,

benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like.
The term alkyl refer to linear or branched (Ci-Ci2)alkyl group, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, n-pentyl, isopentyl, hexyl and the like.
The term aryl refer to phenyl or naphthyl.
The term halogen refer to fluorine, chlorine, bromine or iodine.
The term haloalkyl refer to chloromethyl, chloroethyl, trifluoromethyl, trifluoroethyl, dichloromethyl, dichloroethyl and the like.
The term acyl refer to -C(=0)CH3, -C(=0)C2H5, -C(=0)C3H7, -CeO)C6Hi3, -CeS)CH3, -G(=S)C2H5, -C(=S)C3H7, -C(=S)C6Hi3, benzoyl;
The term alkoxy refer to linear or branched (CpCe) alkoxy group, such as methoxy, ethoxy, n-propoxy, isopropoxy and the like.
The term haloalkyl refer to; monoalkylamino group such as -NHCH3, -NHC2H5, -NHC3H7, -NHCfiHu, and the like.
The term alkoxy refer to dialkylamino group such as -N(CH3)2, -NCH3(C2H5), -N(C2H5)2 and the like.
The term alkoxy refer to acylamino group such as -NHC(=0)CH3, -NHC(=0)C2H5, -NHC(=0)C3H7, -NHC(=0)C6Hi3, and the like.
The term alkoxy refer to alkoxycarbonyl group such as methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl and the like.
The term alkylsulfonyl refer to methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, iso-propylsulfonyl and the like.
The term alkylsulfinyl refer to methylsulfinyl, ethylsulfmyl, n-propylsulfmyl, iso-propylsulfmyl and the like.

The term alkylthio refer to methylthio, ethylthio, n-propyhhio, iso-propyhhio and the Uke.
The term alkoxyalkyl refer to methoxymethyl, ethoxymethyl, methoxyethyl, ethoxyethyl and the Uke.
The term carboxyUc acid or its derivatives refer to esters, amides and acid haUdes.
The term arylamino refer to phenyl amino, naphthyl amino*
The term alkoxyamino refer to methoxyamino, ethoxyamino, propoxy amino and the like.
m and n are integers ranging from 0-2.
Pharmaceutically acceptable salts of the present invention include alkali
metal salts like Li, Na, and K salts, alkaline earth metal salts like Ca and Mg salts,
salts of organic bases such as diethanolamine, a-phenylethylamine, benzylamine,
piperidine, morpholine, pyridine, hydroxyethylpyrrolidine,
hydroxyethylpipendine, guanidine, choline and the like, ammonium or substituted ammonium salts, aluminum salts. Salts also include amino acid salts such as glycine, alanine, cystine, cysteine, lysine, arginine, phenylalanine etc. Salts may include acid addition salts where appropriate which are, sulphates, nitrates, phosphates, perchlorates, borates, hydrohalides, acetates, tartrates, maleates, citrates, succinates, palmoates, methanesulphonates, tosylates, benzoates, salicylates, hydroxynaphthoates, benzenesulfonates, ascorbates, glycerophosphates, ketoglutarates and the like. Pharmaceutically acceptable solvates may be hydrates or comprising other solvents of crystallization such as alcohols.

Representative compounds of fomiula (I) according to the present invention include:
6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one; 6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-bromophenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one; 6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylthiophenyl)-1 H-pyrimidin-4-one;
6-Amino-1 -(4-methylphenyl)-2-(4-methylthio-phenylamino)-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylsulfonyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one; 6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylphenyl)-1 H-pyrimidin-4-one;

4-(6-Amino-4-oxo-1 -phenyl-1,4-dihydro-pyrimidin-2-ylamino)-
benzenesulfonamide;
4-(6-Amino-4-oxo-1 -(4-methyl-phenyl)-1,4-dihydro-pyrimidin-2-ylainino)-
benzenesulfonamide;
6-Amino-2-phenylamino-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-methoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylthio-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-ethoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-1 -(4-methoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-ethoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-2- phenylamino-1 -(4-chloropyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2- phenylamino-1 -(4-bromopyridin-2-yl)-1 H-pyrimidin-4-one;
Representative compounds of fomiula (II) according to the present invention include:
5-Cyano-4-methylthio-1 -(4-methylthio-phenyl)-2-phenyl-1,6-dihydro-pyrimidin-6-one;
5-Cyano-4-methylthio-1 -(4-methylthiO"phenyl)-2-(4-trifluoromethylphenyl)-1,6-dihydro-pyrimidin-6-one;
5-Cyano-1 -(4-fluorophenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one;
5-Cyano-1 -(4-methylphenyl)-2-(4-methylsulfonyl-phenyl)-4-methylthio-1,6-dihydro-pyrimidin-6-one;

5-Carboxy-4-methylthio-1 -(4-methylthio-phenyl)-2-phenyl-1,6-dihydro-
pyrimidin-6-one;
5-Carbamoyl-2-(4-fluorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-
dihydro-pyrimidin-6-one;
5-Chloro-2-(4-chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro-
pyrimidin-6-one;
2-(4-Chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro-
pyrimidin-6-one;
2-(4-Chlorophenyl)-1 -(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one;
1 -(4-Methylphenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro-
pyrimidin-6-one;
1 -(4-Methylphenyl)-2-(4-methylthio-phenyl)-1,6-dihydro-pyrimidin-6-one;
4-(5-Cyano-4-methylthio-6-oxo-2-phenyl-6H-pyrimidin-1 -yl)-
benzenesulfonamide;
4-(5-Cyano-4-methylthio-6-oxo-2-(4-methylphenyl)-6H-pyrimidin-l-yl)-
benzenesulfonamide and
4-(5-Carboxy-4-methylthio-6-oxo-2-phenyl-6H-pyrimidin-1 -yl)-
benzenesulfonamide.
Representative compounds of fomiula (III) according to the present invention include:
1-(4-Methylsulfanyl-phenyl)-6-phenyl-pyrimidin-2,4-( 1 H)-dione; 6-(4-Methylphenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Ethylphenyl)-l-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione; l-(4-Methylphenyl)-6-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione; 1 -(4-Bromophenyl)-6-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;

5-Cyano-1 "(4-fluorophenyl)-2-(4-methylsulfonyl-phenyl)-4-methylthio-1,6-
dihydro-pyrimidin-6-one;
5-Cyano-1 -(4-methylphenyl)-4-methylsulfonyl-2-(4-methylsulfonyl-phenyl)" 1,6-
dihydro-pyrimidin-6-one;
5-Cyano-1 -(4-methylphenyl)-4-methylsulfonyl-2-(4-methylthio-phenyl)-1,6-
dihydro-pyrimidin-6-one;
5-Cyano-1 -(4-methylphenyl)-4-methylthio-2-(4-sulfamoyl-phenyl)-1,6-dihydro-
pyrimidin-6-one;
5-Cyano-2-(4-fluorophenyl)-1 -(4-methylthio-phenyl)-4-methylthio-1,6-dihydro-
pyrimidin-6-one;
5-Cyano-2-(4-fluorophenyl)-1 -(4-methylsulfonyl-phenyl)-4-methylthio-1,6-
dihydro-pyrimidin-6-one;
5-Cyano-2-(4-fluorophenyl)-4-methylthio-1 -(4-sulfamoyl-phenyl)-1,6-dihydro-
pyrimidin-6-one;
5-Cyano-2-(4-chlorophenyl)-4-methylthio-1 -(4-methylthio-phenyl)-1,6-dihydro-
pyrimidin-6-one;
5-Cyano-1 -(4-methylphenyl)-4-methylthio-2-(4-methylthio-phenyl)-1,6-dihydro-
pyrimidin-6-one;
2-(4-Methanesulfonyl-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6-
dihydro-pyrimidine-5-carboxylic acid;
2-(4-Methanesulfanyl-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6-
dihydro-pyrimidine-5-carboxylic acid;
2-(4-Fluroro-phenyl)-4-methylsulfanyl-6-oxo-1 -(4-methylphenyl)-1,6-dihydro-
pyrimidine-5-carboxylic acid;

6-(4-Chlorophenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione; 6-(4-Chloro-3-methylphenyl)4-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(m
dione;
6-(3 -Chloro-4-methylphenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1H)-
dione; 6-(4-FluoroO-methylphenyl)4-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-
dione;
6-(4-Fluorophenyl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
6-(4-Methylsulfanyl-phenyl)-1 -phenyl"pyrimidin-2,4-( 1 H)-dione;
6-(4-Methylphenyl)-l-(3-chloro-4-methylsulfonyl-phenyl)-pyrimidin-2,4-(lH)-
dione;
6-(4-Methoxy-3 -methylphenyl)-1 -(4-methylsulfonyl-phenyl)-p3nimidin-2,4-( 1H)-
dione;
6-(4-Methylphenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
6-(4-Ethylphenyl)-1 -(4"methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
6-(4-Chlorophenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
6-(4-Chloro-3-methylphenyl)-1 -(4-methylsulfonyl-phenyl)-p)nimidin-2,4-( 1H)-
dione;
6-(4-Chlorophenyl)-1 -(3 -inethoxy-4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1H)-
dione;
6-(3-Chloro-4-methylphenyl)-l-(4-methylsulfonyl-phenyl)-pyrimidin-2,4-(lH)-
dione;
6-(4-Fluorophenyl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
l-(4-Methylsulfonyl-phenyl)-6-phenyl-pyrimidin-2,4-(lH)-dione;
l-(4-Methylsulfanyl-phenyl)-6-(pyridin-2-yl)-pyrimidin-2,4-(lH)-dione;
6-(4-Methylpyridin-2-yl)-1 -(4-methylsulfanyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;

6-(4-Chloropyridin-2-yl)-l-(4-methylsulfanyl-phenyl)-pyrimidin-2,4-(lH)-dione;
6-(4-Methylsulfanyl-phenyl)-1 -(pyridin-2-yl)-pyrimidin-2,4-( 1 H)-dione;
l-(4"Methylsulfonyl-phenyl)-6-(pyridin-2-yl)-pyrimidin-2,4-(lH)-dione;
6-(4-Methylpyridin-2-yl)-1 -(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)-dione;
6-(4-Chloropyridin-2-yl)-1-(4-methylsulfonyl-phenyl)-pyrimidin-2,4-( 1 H)--dione;
4-(2,4-Dioxo-6-(4-methylphenyl)-3,4-dihydro-2H-pyrimidin-l-yl)-
benzenesulfonamide;
4-(2,4-Dioxo-6-phenyl-3,4-dihydro-2H-pyrimidin-l-yl)-benzenesulfonamide;
4-[6-(4-Bromo-phenyl)-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-yl]-
benzenesulfonamide;
4-(2,6-Dioxo-3-phenyl-1,2,3,6-tetrahydro-pyrimidin-4-yl)-benzenesulfonamide;
4-(2,6-Dioxo-3-(4-methylsulfanyl-phenyl)-l,2,3,6-tetrahydro-pyrimidin-4-yl)-
benzenesulfonamide and
4-[3-(4-Chloro-phenyl)-2,6-dioxo-1,253,6-tetrahydro-pyrimidin-
4-yl]-benzenesulfonamide.
Representative compounds of formula (IV) according to the present invention include:
5,6-Diphenyl-2-trifluoromethyl-pyrimidin-4-one;
5-Phenyl-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one; 5-(4-Chlorophenyl)-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one;
5-(4-Fluorophenyl)-6-(4-methylsulfonylphenyl)-2-trifluoromethyl-pyrimidin-4-one;
4-[5-(4-Fluorophenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]-benzenesulfonamide;

4-[5-(4-Methylsulfonylphenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]-
benzenesulfonamide;
4-[5-(4-Methylthiophenyl)-2-trifluoromethyl-4-oxo-pyrimidin-6-yl]-
benzenesulfonamide;
6-(4-Methylsulfonylphenyl)-5-phenyl-2-thiouracil;
6"(4-Chlorophenyl)-5-phenyl-2-thiouracil;
6-(4-Methylphenyl)-5-phenyl-2-thiouracil;
5"Phenyl-6-(4-trifluoromethylphenyl)-2-thiouracil;
5-(4-Chlorophenyl)-6-phenyl-2-thiouracil;
5"(4-Methylthiophenyl)-6-phenyl-2-thiouracil;
5-(4-Methoxyphenyl)-6-phenyl-2-thiouracil;
5"(4-Chlorophenyl)-6-(4"methylphenyl)-2-thiouracil;
4"(5-Phenyl-2-thio-4-oxo-pyrimidin"6-yl)benzenesulfonamide;
4'"(6-Phenyl-2-thio-4-oxo-pyrimidin-5-yl)benzenesulfonamide;
6"(4-Chlorophenyl)-5-phenyl-uracil;
6-(4-Methylphenyl)-5-phenyl-uracil;
5"Phenyl-6-(4-trifluoromethylphenyl)-uracil;
5-(4-Chlorophenyl)-6-phenyl-uracil;
5"(4-Methylthiophenyl)-6-phenyl-uracil;
5"(4-Methoxyphenyl)-6-phenyl-uracil;
5-(4-Chlorophenyl)-6-(4-methylphenyl)-uracil;
l,3-Dimethyl-6-(4-chlorophenyl)-5-phenyl-uracil;
l,3-Diniethyl-6-(4-methylphenyl)-5"phenyl-uracil;
4-[ {6-(4-chlorophenyl)-2,4-dioxo-pyrimidin-5-yl} Jbenzenesulfonamide and
4"[5-(4-chlorophenyl)-2,4-dioxo-pyrimidin-6-yl}]benzenesulfonamide.

According to yet another embodiment of the present invention, there is provided a process for the preparation of novel amino substituted pyrimidinone
Q Q
derivatives of the formula (I) wherein Y represents NR , where R and all other symbols are as defined above, which comprises, reacting compound of formula (la)

where all symbols are as defined above.
The reaction of compound of formula (la) with (lb) to produce compound of formula (I) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, pyridine, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, diphenylether, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof or by neat reaction. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may

be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 36 h.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) wherein any of the groups R or R represent SR , wherein R” represents alkyl or aryl to novel amino substituted pyrimidinone derivatives of the formula (I) wherein any of the groups R or R represent S(0)pR 5 where p represents 1 or 2 and R represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, an alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) wherein R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl may be converted to novel amino substituted pyrimidinone derivatives of the formula (I) wherein R or R represent S(0)pR , where p is 1 or 2, R represents amino by using the procedure described in the literature (Huang etMl Tetrahedron Lett. 39, 7201, 1994).

In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (I) wherein either of R” or R” represent S(0)pR” wherein R” represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Ic) wherein all symbols are as defined earlier

wherein either of R” or R"“ represents hydrogen with chlorosulfonic acid and ammonia.
The reaction of compound of formula (Ic) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the rangeof 2 to 12 h.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (la)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, amino, acyl, alkyl, alkoxy, aryl group; the ring represented by A is selected from aryl or heteroaryl; R” represents hydrogen, SR”, wherein R” represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R represents hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino groups; m is an integer and is in the range of 0 to 2.
In yet another embodiment of the present invention, the compounds of formula (la) are prepared by methylating the compound of formula (Ia-1)

where all symbols are as defined above.
The methylation of compound of formula (Ia-1) to produce compound of formula (la) may be carried out by treating with methylating agent like methyliodide, dimethylsulphate and diazomethane etc., in the presence of base such as sodium hydroxide, potassium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol, water and the like or mixture thereof.
According to another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein all symbols are as defined earlier, which comprises reacting a compound of the formula (Ila)

wherein all symbols are as defined above, to produce a compound of formula (II).
The reaction of compound of formula (Ila) with compound of formula
(lib) may be carried out using appropriate solvents like toluene, xylene,
tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-
dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide,
dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert-
butylalchol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat
reactions. The condensation reaction may be carried out under acidic conditions
using mineral or organic acids, or basic conditions viz. carbonates, bicarbonates,
hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth
metals. The reaction may be carried out by using phase transfer catalysts viz.
triethylbenzylammonium chloride, tetrabutylammonium bromide,
tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction is usually carried out under cooling to refluxing conditions. The final product purified by using chromatographic techniques or by recrystallization. The reaction may be carried out for period in the range of 2 to 20 h.
According to another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein all symbols are as defined earlier, which comprises reacting a compound of the formula (lie)

wherein all symbols are as defined above, to produce a compound of formula (II). The reaction of compound of formula (lie) with compound of formula (lid) may be carried out using appropriate solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The condensation reaction may be carried out under acidic conditions using mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction is usually carried out under cooling to refluxing conditions. The final product purified by using chromatographic techniques or by recrystallization. The reaction may be carried out for period in the range of 30 min. to 10 hours.

According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidone derivatives of the formula (II) wherein any of the groups R” or R” represent SR', wherein R” represents alkyl or aryl to novel pyrimidone derivatives of the formula (II) wherein any of the groups R or R represent S(0)pR , where p represents 1 or 2 and R” represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, an alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidone derivatives of the formula (II) wherein R” or R” represent S(0)pR”, where p is 1 or 2, R” represents alkyl or aryl may be converted to novel pyrimidone derivatives of the formula (II) wherein R” or R” represent S(0)pR” where p is 1 or 2, R” represents amino by using the procedure described in the literature (Huang et.al Tetrahedron Lett., 39, 7201, 1994).
In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidone derivatives of the formula (II) wherein either of R” or R” represent S(0)pR”, wherein R” represents amino group

and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (He)

where R” represents hydrogen with chlorosulfonic acid and ammonia.
The reaction of compound of formula (He) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (lib)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl, or S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an
T A
integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl,

haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2.
In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (lib), which comprises, methylating the compound of formula (IIb-2)

The methylation of (IIb-2) may be carried out by treating with methylating agent like methyliodide, dimethylsulphate and diazomethane etc., in the presence of base such as sodium hydroxide, potassium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol, water etc.
In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (IIb-2), which comprises, reacting compound of formula (IIb-3)

The reaction of compound of formula (IIb-3) with compound of formula (IIb-4) may be carried out in solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, pyridine, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The reaction may be carried out at a temperature in the range of 0 to 200 °C for period in the range of 30 min. to 5 hours.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (lid)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl, or S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R” and R"* may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2.

In yet another embodiment of the present invention, there is provided a process for the preparation of novel intermediate of formula (lid), which comprises, reacting compound of formula (IIb-3)

The reaction of compound of formula (IIb-3) with compound of formula (IId-1) may be carried out in the presence of catalysts like aluminium chloride, triethyl aluminium, sodium hydride, sodium methoxide, butyl lithium, lithium diisopropylamine, sodium bis trimethyl silylamide, lithium bis trimethyl silylamide, using solvents like toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethyl acetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid etc, a mixture thereof or the like or by neat reactions. The reaction may be carried out at a temperature in the range of 50 to 200 °C for period in the range of 30 min. to 10 hours.
According to yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (III) wherein all symbols are as defined above, as shown in scheme I below:

Scheme-l
The reaction of compound of formula (Ilia) with (Illb) to produce compound of formula (IIIc) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof. The condensation may be carried out under acidic conditions using mineral or organic acids or basic conditions using carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out by using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h.

The cyclization of compound of formula (IIIc) to obtain compound of formula (III) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof The cyclization is carried out under acidic conditions using mineral or organic acids or basic conditions using carbonates, bicarbonates, hydrides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction may be carried out using phase transfer catalysts viz. triethylbenzylammonium chloride, tetrabutylammonium bromide, tetrabutylammonium hydrogensulphate, tricaprylylmethylammonium chloride (aliquat 336) and the like. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12 h.
In yet another embodiment of the present invention, there is provided a process for the preparation of novel pyrimidinedione derivatives of the formula (III) wherein either of R” and R” represent S(0)pR”, wherein R” represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Illd) wherein all symbols are as defined earlier

1 "i
wherein any one of R and R represent hydrogen with chlorosulfonic acid and ammonia.
The reaction of compound of formula (Illd) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction may be carried out at a temperature in the range of 50 °C to reflux temperature for period in the range of 2 to 12h.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidinedione derivatives of the formula (III) wherein any of the groups R” or R” represent SR”, wherein R” represents alkyl or aryl to novel pyrimidinedione derivatives of the formula (III) wherein any of the groups R or R represent S(0)pR , where p represents 1 or 2
Q
and R represents alkyl or aryl; by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel pyrimidinedione derivatives of the

formula (III) wherein R” or R” represent S(0)pR” where p is 1 or 2, R” represents alkyl or aryl to novel pyrimidinedione derivatives of the formula (III) wherein R or R"“ represent S(0)pR”, where p is 1 or 2, R” represents amino by using the procedure described in the literature (Huang et al Tetrahedron Lett. 39, 7201, 1994).
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (Ilia)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the ring represented by B is selected from aryl or heteroaryl; R represents SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R” represents hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylthio, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxyl, amino, halogen, alkoxy.

aryloxy, monoalkylamino, dialkylamino, arylamino, groups; n is an integer and represents 0 to 2.
In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (Ilia) as shown in scheme 2 below.

The reaction of compound of formula (Ille) wherein R' represents alkyl group and all other symbols are as defined above with (Illf) to produce compound of formula (Illg) may be carried out in the presence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, o-dichlorobenzene, acetone, ethylacetate, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalcohol, acetic acid, propionic acid and the like or a mixture thereof. The reaction may be carried out in the presence of base such as sodium hydroxide, potassium hydroxide, sodium bicarbonate, sodium carbonate and the like. The reaction may be carried

out at a temperature in the range of 10 to 80 °C for period in the range of 4 to 24 h.
The conversion of compound of formula (Illg) to obtain compound of formula (Ilia) may be carried out in the presence of acids such as hydrochloric acid, sulfuric acid, acetic acid, nitrous acid and the like.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IIIc)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X and Y may be same or different and independently represent oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R and R are different and represent hydrogen, SR , wherein R represents alkyl or aryl;
O Q
S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an
T A
integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylthio, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R” and R” may be same or different and independently represent hydrogen, halogen, hydroxyl, formyl, cyano, nitro,

nitroso, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR”, wherein R” represents hydroxy, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer and is in the range of 0 to 2; n is an integer and is in the range of 0 to 2.
According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” together with R*” form a double bond; R” represents trifluoromethyl and R” represents hydrogen and all other symbols are as defined above, as shown in scheme 2 below :

where R' represent (C1-C3) alkyl group and all other symbols are as defined earlier.
The compound of formula (IVb) may be prepared using trifluoro acetic anhydride in the presence of solvents such as acetic anhydride, toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof or by neat reaction. The reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and

alkoxides of alkali metals and alkaline earth metals; organic bases such as pyridine, triethyl amine and the like. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 24 h.
The compound of formula (IV) is prepared by reacting the compound of formula (IVb) with ammonia after refluxing with acetic anhydride, in the solvents such as selected from acetic anhydride, toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol and the like. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 1 to 12 h.
According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) where R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR and all other symbols are as defined above, which comprises reacting a compound of the formula (IVa)

where R' represent (C1-C3) alkyl group and all other symbols are as defined earlier, with a compound of the formula (IVc)

where R' represent (CpCa) alkyl group and all other symbols are as defined earlier, with a compound of the formula (IVc)

where R” and R” are as defined above to produce a compound of formula (IV) defined above.
The reaction of compound of formula (IVd) with compound of formula (IVc) may be carried out in neat or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 20 h.
In yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) wherein either of R or R represent sulfamoyl and all other symbols are as defined earlier, which comprises reacting compound of formula (IV) wherein all symbols are as defined earlier

where R” and R” are as defined above to produce a compound of formula (IV) defined above.
The reaction of compound of formula (IVa) with compound of formula (IVc) may be carried out in neat or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h.
According to yet another embodiment of the present invention, there is provided a process for the preparation of novel diaryl pyrimidinone derivatives of the formula (IV) where R and R together with the carbon atom to which they are attached form oxo, thioxo or =NR and all other symbols are as defined above, which comprises reacting a compound of the formula (IVd)

wherein either of R” or R” represent hydrogen with chlorosulfonic acid and ammonia.
The reaction of compound of formula (IV) with chlorosulfonic acid and ammonia may be carried out in the presence of solvents such as acetic acid, dichloromethane, acetone, tetrahydrofuran, dioxane, ethyl acetate, chloroform, water, an alcohol and the like or a mixture thereof. The reaction is carried out under cooling to reflux temperature for period in the range of 2 to 12 h.
In yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein any of the groups R or R represent alkylthio to novel diaryl pyrimidinone derivatives of the formula (IV) wherein any of the groups R* or R represent alkylsuflinyl or alkylsulfonyl by using suitable oxidizing agent. The oxidizing agent may be selected from potassium peroxymonosulfate (Oxone), hydrogen peroxide, tert-butylperoxide, Jones reagent, peracid [e.g peracetic acid, perbenzoic acid, m-chloroperbenzoic acid etc], chromic acid, potassium permanganate, alkali metal periodate [e.g sodium periodate, etc], magnesium mono peroxypthalate, osmium tetroxide/N-methylmorpholine-N-oxide, sodium tungstate, and the like. The oxidation is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, alcohol [eg. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is usually carried out under cooling to refluxing conditions.
According to yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R or R represent alkylsulfonyl or alkylsulfinyl to novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” or R” represent

sulfamoyl by using the procedure described in the hterature (Huang et.al. Tetrahedron Lett. 1994, 39, 7201).
In yet another embodiment of the present invention there is provided a process for the conversion of novel diaryl pyrimidinone derivatives of the formula (IV) wherein R” and R” together with the carbon atom to which they are attached represent thioxo to and all other symbols are as defined above to novel
ft 7
diaryl pyrimidinone derivatives of the formula (IV) wherein R and R together with the carbon atom to which they are attached represent oxo.
The conversion may be carried using hydrogen peroxide in the presence or absence of solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The reaction may be carried out under basic conditions using bases such as carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IVa)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl, sulfamoyl; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2; R' represent (CpCs) alkyl group.
In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (IVa), which comprises reacting compound of formula (IVa-1)

The reaction of compound of formula (IVa-1) with compound of formula (IVa-2) may be carried out using cupric acetate, zinc dust in the presence or absence of solvents such as toluene, xylene, tetrahydrofiiran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropylalcohol, tert-butylalchol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may be carried out by using acidic condition: mineral or organic acids, or basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 16 h,.
In yet another embodiment of the present invention, there is provided a novel intermediate of formula (IVd)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts and their pharmaceutically acceptable compositions, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxy!, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or heteroaryl; R” and R” are different and represent hydrogen, halogen, cyano, azido, hydroxy, amino, nitro, formyl, alkyl, haloalkyl, alkoxy, thioalkyl, alkylsulfinyl, alkylsulfonyl,

sulfamoyl; R” and R"* may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2; R' represent (CpCs) alkyl group.
In yet another embodiment of the present invention, there is provided a process for the preparation of compound of formula (Id), which comprises reacting compound of formula (IVd-1)

wherein all symbols are as defined above.
The reaction of compound of formula (IVd-1) with compound of formula (IVd-2) may be carried out using lithium bis(trimethylsilyl)amide, sodium trimethylsilyl)amide, Sodium hydride, Sodim methoxide, sodium ethoxide, Butyl lithium, Lithiumdiisopropylamine etc., in ne”t or using solvents such as toluene, xylene, tetrahydrofuran, dioxane, chloroform, dichloromethane, dichloroethane, acetone, ethylacetate, o-dichlorobenzene, acetonitrile, N,N-dimethylformamide, dimethylsulfoxide, ethanol, methanol, isopropanol, tert-butyl alcohol, acetic acid, propionic acid and the like or a mixture thereof. The condensation reaction may

be carried out by using basic conditions viz. carbonates, bicarbonates, hydrides, hydroxides, alkyls and alkoxides of alkali metals and alkaline earth metals. The reaction is usually carried out under cooling to refluxing conditions. The reaction may be carried out for period in the range of 2 to 10 hours.
It is appreciated that in any of the above-mentioned reactions, any reactive group in the substrate molecule may be protected according to conventional chemical practice. Suitable protecting groups in any of the above-mentioned reactions are those used conventionally in the art. The methods of formation and removal of such protecting groups are those conventional methods appropriate to the molecule being protected.
The pharmaceutically acceptable salts are prepared by reacting the compound of formulae (I) or (II) or (III) or (IV) with 1 to 4 equivalents of a base such as sodium hydroxide, sodium methoxide, sodium hydride, potassium t-butoxide, calcium hydroxide, magnesium hydroxide and the like, in solvents like ether, tetrahydrofuran, methanol, t-butanol, dioxane, isopropanol, ethanol etc. Mixture of solvents may be used. Organic bases such as diethanolamine, a-phenylethylamine, benzylamine, piperidine, morpholine, pyridine, hydroxyethylpyrrolidine, hydroxyethylpiperidine, guanidine, choline and the like, ammonium or substituted ammonium salts, aluminum salts. Amino acid such as glycine, alanine, cystine, cysteine, lysine, arginine, phenylalanine, etc may be used for the preparation of amino acid salts. Alternatively, acid addition salts wherever applicable are prepared by the treatment with acids such as hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid, p-toluenesulphonic acid, methanesulfonic acid, acetic acid, citric acid, maleic acid, salicylic acid, hydroxynaphthoic acid, ascorbic acid, palmitic acid, succinic acid.

benzoic acid, benzenesulfonic acid, tartaric acid and in solvents like ethyl acetate, ether, alcohols, acetone, tetrahydrofliran, dioxane etc. Mixture of solvents may also be used.
The stereoisomers of the compounds forming part of this invention may be prepared by using reactants in their single enantiomeric form in the process wherever possible or by conducting the reaction in the presence of reagents or catalysts in their single enantiomer form or by resolving the mixture of stereoisomers by conventional methods. Some of the preferred methods include use of microbial resolution, resolving the diastereomeric salts formed with chiral acids such as mandelic acid, camphorsulfonic acid, tartaric acid, lactic acid, and the like wherever applicable or chiral bases such as brucine, cinchona alkaloids and their derivatives and the like. Commonly used methods are compiled by Jaques et al in "Enantiomers, Racemates and Resolution" (Wiley Interscience, 1981). More specifically the compound of formula (I) may be converted to a 1:1 mixture of diastereomeric amides by treating with chiral amines, aminoacids, aminoalcohols derived from aminoacids; conventional reaction conditions may be employed to convert acid into an amide; the diastereomers may be separated either by fractional crystallization or chromatography and the stereoisomers of compound of formula (I) may be prepared by hydrolysing the pure diastereomeric amide.
Various polymorphs of compound of formulae (I) or (II) or (III) or (IV) forming part of this invention may be prepared by crystallization of compound of formulae (I) or (II) or (III) or (IV) under different conditions. For example, using different solvents commonly used or their mixtures for recrystallization; crystallizations at different temperatures; various modes of cooling, ranging from very fast to very slow cooling during crystallizations. Polymorphs may also be

obtained by heating or melting the compound followed by gradual or fast cooling. The presence of polymorphs may be determined by solid probe NMR spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques.
Pharmaceutically acceptable solvates of the compounds of formulae (I) or (II) or (III) or (IV) forming part of this invention may be prepared by conventional methods such as dissolving the compounds of formulae (I) or (II) or (III) or (IV) in solvents such as water, methanol, ethanol, mixture of solvents such as acetone:water, dioxane:water, N,N"dimethylformamide:water and the like, preferably water and recrystallizing by using different crystallization techniques. The present invention provides a pharmaceutical composition, containing the compounds of the general formulae (I) or (II) or (III) or (IV) as defined above, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable hydrates and solvates in combination with the usual pharmaceutically employed carriers, diluents and the like, useful for the treatment of arthritis, pain, fever, psoriasis, allergic diseases, asthma, inflammatory bowel syndrome, gastro-intestinal ulcers, cardiovascular disorders including ischemic heart disease, atherosclerosis, cancer, ischemic-induced cell damage, particularly brain damage caused by stroke, other pathological disorders associated with free radicals. The pharmaceutical composition of the present invention are effective in the treatment of inflammation and immunological diseases, particularly those mediated by cytokines such as TNF-a, IL-1, IL-6, IL-8 and cyclooxygenase such as COX-2 andCOX-3.
The pharmaceutical composition may be in the forms normally employed, such as tablets, capsules, powders, syrups, solutions, aerosols, suspensions and

the like, may contain flavoring agents, sweeteners etc., in suitable solid or liquid carriers or diluents, or in suitable sterile media to form injectable solutions or suspensions. Such compositions typically contain from 1 to 20 %, preferably 1 to 10 % by weight of active compound, the remainder of the composition being pharmaceutically acceptable carriers, diluents or solvents.
The present invention is provided by the examples given below, which are provided by way of illustration only and should not be considered to limit the scope of the invention.

Dry hydrogen chloride gas was passed through a mixture of ethyl cyanoacetate (17.3g, 153mmol) and 4-ethoxyphenylthiourea (lOg, Slmmol) in dioxane (60ml) for 20 hours at 0 - 5 °C. The reaction mixture was refluxed for 6 hours, poured onto ice-water mixture and neutralized with saturated sodium bicarbonate solution. The precipitate thus separated was filtered, washed with water and dried in vacuum to yield the title compound (9.32g, 69.5%, purity 94.1% by HPLC) mp 222 - 225 °C. “H-NMR (DMSO - da): 5 1.34 - 1.37 (t, 3H), 4.04 - 4.09 (q, 2H), 4.93 (s, IH), 6.2 (bs, 2H, D2O exchangeable), 7.01 - 7.03 (d, 2H), 7.15 - 7.17 (d, 2H), 11.92 (s, IH, D2O exchangeable). MS m/z: 264.1 (M”).

6-Amino-l-phenyl"2-thiouracil (5.5g. 25mmol) (synthesized according to the procedure given in CJ.Shishoo et aL, Indian J. Chem., 35B, pp 662, 1996) was added to the stirred potassium hydroxide (IN, 50ml) solution and filtered. Methyl iodide (6.26g, 44mmol) was added to the vigorous stirred filtrate at 20 °C and stirring was continued at room temperature for 2 hours. The reaction mixture was poured onto ice-water, separated solid was filtered, washed with water and dried to furnish the title compound (4.80g, 82.1%) mp 213 - 216 °C. “H-NMR (CDCI3): 5 2.40 (s, 3H), 4.93 (bs, 2H, D2O exchangeable), 5.38 (s, IH), 7.33 -7.35 (m, 2H), 7.59 - 7.60 (s, 3H). MS m/z: 234.1 (M”).

The title compound was prepared from 6-amino-l-(4-methylphenyl)-2-thiouracil (7g, 30mmol) (synthesized according to the procedure given in CJ.Shishoo et al,

Indian J. Chem., 35B, pp 662, 1996) by following the procedure described in preparation 2, (6.0g, 80.9%) mpl30 - 132 °C. MS m/z: 248.2 (M”).

The title compound was prepared from 6-amino-l-(4-methoxyphenyl)-2-thiouracil (lOg, 40mmol) (synthesized according to the procedure given in C.J.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) by following the procedure described in preparation 2, (9.64g, 91.3%, purity 99%) by HPLC) mpl82 - 186 °C. “H-NMR (DMSO-de): 5 2.25 (s, 3H), 3.83 (s, 3H), 4.96 (s, IH), 5.94 (s, 2H, D2O exchangeable), 7.09 - 7.11 (d, 2H), 7.33 - 7.35 (d, 2H). MS m/z: 264.1 (M”).

The title compound was prepared from 6-amino-l-(4-ethoxyphenyl)-2-thiouracil (8g, 30.4mmol) (obtained in preparation 1) according to the procedure described in preparation 2, (6.88g, 81.7%, purity 90.8% by HPLC) mp 177 - 181 X. “H-NMR (CDCI3): 5 1.45 - 1.49 (t, 3H), 2.42 (s, 3H), 4.10 - 4.12 (q, 2H), 5.31 (s, IH), 7.05 - 7.07 (m, 2H), 7.23 - 7.25 (m, 2H), MS m/z: 278.1(M”).

The title compound was prepared by following the procedure described in preparation 2 from 6-amino-1 -(4-chlorophenyl)-2-thiouracil (8g, 31.5mmol) (synthesized according to the procedure given in C.J.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) (7.34g, 86.9%), mpl80 - 182 °C. “H-NMR (DMSO-d6): 5 2.27 (s, 3H), 4.96 (s, IH), 6.09 (s, 2H), 7.50 -7.52 (d, 2H), 7.64 - 7.66 (d, 2H).MS m/z: 268.1 (M”).
Preparation 7
Synthesis of 6-amino-2-methylthio-l-(4-bromophenyl)-lH-pyrimidin-4-one

The title compound was prepared by following the procedure described in preparation 2 from 6-amino-l-(4-bromophenyl)-2-thiouracil (Ig, 3.35mmol) (synthesized according to the procedure given in CJ.Shishoo et al, Indian J. Chem., 35B, pp 662, 1996) (0.55g, 52.5%), mp 138 - 140 °C. MS m/z: 312.0/313.9 (M”).

Sodium hydroxide solution (33%, 32.5ml) was added to ethyl acetoacetate (97.5g, 750mmol) in a mixture of water (250ml) and toluene (12ml) at 0-5 *”C under stirring (pH 11). After 30 minutes 4-methylbenzoylchloride (127.46g, 825mmol) and sodium hydroxide solution (33%, 135ml) was added simultaneously over a period two hours. The reaction mixture was stirred for 15 minutes at 0 °C and for 1 hour at 35 °C. Aqueous layer was separated, ammonium chloride (40g) was added and stirred slowly over night. The reaction mixture was saturated with sodium chloride and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated to

dryness in vacuum. The crude product thus obtained was purified by column chromatography to yield the title compound as viscous oil (54g, 35%). MS m/z: 207.1 (M”).

Ethyl acetoacetate (51.25g, 390 mmol) was added dropwise to the stirred suspension of anhydrous magnesium chloride (37.54g, 390mmol) in dried dichloromethane (200ml) over a period of 1 hour under argon atmosphere at 0 °C followed by pyridine (62.5g, 788mmol). After 15 minutes, 4-chlorobenzoylchloride (68.95g, 394 mmol) was added dropwise and stirring was continued for 15 minutes at 0 °C and further stirred for 1.5 hours at 30 °C. The resulting reaction mixture was neutralized with hydrochloric acid (6N, 235ml) at 0-5 °C, filtered and washed with water. The filtrate was extracted with diethylether (3X100 ml). The ether extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness in vacuum. The obtained oil was taken in ammonium chloride (21g in 200ml water) solution containing ammonia (2ml) and stirred at 30 °C for 20 minutes. The resulting solution was extracted with ethyl acetate (3X200ml). Ethyl acetate extract was dried over anhydrous sodium sulphate, concentrated to yield the crude product, which was purified by column chromatography to yield the title compound as viscous oil (43g, 48.2%). *H-NMR (DMSO - d6): 8 1.15 - 1.18 (t, 3H), 4.08 - 4.13 (q, 2H), 4.20 (s, 2H), 7.61 - 7.64 (d, 2H), 7.94 - 7.97 (d, 2H). MS m/z: 227.1 (M”).

Lithium bis(triniethylsilyl)amide (20% in tetrahydrofuran, 203.6ml, 217mmol) was added dropwise to a stirred solution of 4-methylthioacetophenone (20.2g, 121 mmol) in dried tetrahydrofuran (300ml) at - 20 °C and stirring was continued for 1 hour at -20 °C. Ethylchloroformate (19.8g, 182mmol) was added dropwise to the stirred reaction mixture at -20 °C and stirring was continued for 3 hours. The reaction was quenched with saturated ammonium chloride solution and extracted with ethylacetate. The organic extract was washed with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness in vacuum. The crude product thus obtained was purified by column chromatography to yield the title compound as viscous oil (16.45g, 56.8%). “H-NMR (DMSO - de): 8 1.15 - 1.19 (t, 3H), 2.54 (s, 3H), 4.07 - 4.11 (q, 2H), 4.13 (s, 2H), 7.36 - 7.39 (d, 2H), 7.85 - 7.88 (d, 2H). MS m/z: 239 (M”).

Potassium hydroxide (12.55g, 224mmol) was added to the vigorously stirred solution of methylthiopseudourea.H2S04 (14.57g, 52mmol) in water (80ml). Ethyl (4-methyl)benzoylacetate (20.0g, 97mmol) (obtained in preparation 8) was added to it and stirred at room temperature for 18 hours. The solid thus obtained
was filtered, washed with water, ether and dried at 60 °C in vacuum to yield the title compound (1.85g, 9.5%). “H-NMR (DMSO - d6): 5 2.37 (s, 3H), 6.46 (s, IH), 7.33 - 7.35 (d, 2H), 7.76 - 7.78 (d, 2H), 7.91 (bs, 2H, D2O exchangeable). MS m/z: 203.1 (M').

The title compound was prepared from ethyl (4-chloro)benzoylacetate (5.0g, 22mmol) (obtained in preparation 9) and methylthiopseudourea.H2S04 (3.3Ig, 12mmol) by following the procedure described in preparation 4, (0.573g, 11.6%). MS m/z: 223 (M”).

The title compound was prepared from ethyl (4-methylthiobenzoyl)acetate
(16.447g, 69mmol) (obtained in preparation 10) and
methylthiopseudourea.H2S04 (10.56g, 38mmol) according to the procedure described in preparation 4, (1.82g, 11.5%, mp 266 - 267 °C). “H-NMR (DMSO -d6): 8 2.53 (s, 3H), 6.48 (s, IH), 7.37 - 7.39 (d, 2H), 7.79 - 7.81 (d, 2H), 7.92 (bs, 2H). MS m/z: 235 (M”).

A suspension of 2-amino-6-(4-methylphenyl)-l,3-oxazin-4-one (l.Og, 5mmol) (obtained in preparation 11) in 10% hydrochloric acid (60ml) was refluxed for Ihr. The resulting suspension was cooled, filtered, washed with water and dried at 60 °C in vacuum for 8 hours to yield the title compound (0.32g, 32%). “H-NMR (DMSO - d6): 8 2.38 (s, 3H), 6.65 (s, IH), 7.35 - 7.37 (d, 2H), 7.79 - 7.81 (d, 2H), 11.89 (bs, IH, D2O exchangeable). MS m/z: 203.1 (M”),

The title compound was prepared from 2-amino-6-(4-chlorophenyl)-l,3-oxazin-4-one (0.573g, 2.6mmol) (obtained in preparation 12) according to the procedure described in preparation 14 (0.57g, 99%, mp 254 - 256 °C). *H-NMR (DMSO -d6): 5 6.65 (s, IH), 7.58 - 7.60 (d, 2H), 7.86 - 7.89 (d, 2H), 11.90 (bs, IH, D2O exchangeable).

The title compound was prepared from 2-amino-6-(4-methylsulfanyl-phenyl)-l,3-oxazin-4-one (1.82g, 7.8mmol) (obtained in preparation 20) by following the procedure described in preparation 14 (0.78g, 42.7%). “H-NMR (DMSO - d”): 8 2.53 (s, 3H), 6.67 (s, IH), 7.37 - 7.40 (d, 2H), 7.81 - 7.83 (d, 2H), 11,89 (bs, IH). MS m/z: 235 (M”).
Preparation 17
Synthesis of N-(4-methylsulfanyl-phenyl)-[N'-l-(3-phenyl)-l,3-diketone]urea

4-Methylthioaniline (3.36g, 24mmol) was added to a stirred suspension of 6-phenyl-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.189g, Immol) (synthesized according to the procedure given in Harvey I. Skulnick, Heterocylces, 23 (7), ppl685, 1985) in ethanol (5ml). The reaction mixture was refluxed for 4 hours, cooled at room temperature, filtered, washed with ethanol, ether, dried in vacuum at 60 “C for 5 hours to yield the title compound (O.lg, 30.5%, mp 143 - 145 °C). “H-NMR (DMSO - dg): 8 2.45 (s, 3H), 4.28 (s, IH), 7.23 - 7.27 (d, 2H), 7.47 -7.59 (m, 4H), 7.67 - 7.69 (d, IH), 7.96 - 7.98 (d, 2H). MS m/z: 329.2 (M”).
Preparation 18
Synthesis of N-(4-methyIsulfanyl-phenyl)-{N'-l-[3-(4-methyl)phenyl]-l,3-
diketone}urea

4"Methylthioaniline (0.636g, 4. 6mmol) was added to the stirred suspension of 6-(4-methylphenyl)-2H-3,4-dihydro-l,3-oxazine-2,4-dione (0.310g, 1.5mmol) (obtained in preparation 14) in ethanol (10ml). The reaction mixture was refluxed

with stirring for 6 hours, cooled at room temperature, filtered, washed with ethanol followed by ether and dried in vacuum at 60 °C for five hours to yield the title compound (0.24g, 46%, mp 234 - 237 °C). “H-NMR (DMSO - Preparation 19
Synthesis of N-(4-metliylsulfanyl-phenyI)-{N'-l-[3-(4-clilorophenyl)]-l,3-
dil”etone}urea

The title compound was prepared from 6-(4-chlorophenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.57g, 2.5mmol) (obtained in preparation 15) and 4-methylthioaniline (2.48g, 17.8mmol) according to the procedure described in preparation 11 (0.33g, 35.7%). “H-NMR (DMSO - dg): 8 2.41 (s, 3H), 6.64 (s, IH), 7.10 - 7.19 (m, 4H), 7.25 - 7.33 (m, 4H), 11.59 (bs, IH). MS m/z: 363 (M”).
Preparation 20
Syntiiesis of N-(4-metliylp!ienyl)-{N'-l-[3-(4-metliylsuIfanyl-piienyl)]-l,3-
dil(etone}urea

The title compound was prepared from 6-(4-methylsulfanyl-phenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.35g, l.Smmol) (obtained in preparation 16) and 4-methylaniline (1.12g, 10.4mmol) according to the procedure described in preparation 11 (0. 24g, 47%). *H-NMR (DMSO - d6): 8 2.26 (s, 3H), 2.53 (s, 3H), 4.22 (s, IH), 7.12 - 7.14 (d, 2H), 7.38 - 7.42 (d, 4H), 7.87 - 7.89 (d, 2H). MS m/z: 343.1 (M”).
Preparation 21
Synthesis of N-(4-bromoplienyl)-{N'-l-[3-(4-metiiylsulfanyl-plienyl)]-l,3-dilcetone}urea

The title compound was prepared from 6-(4-methylsulfanyl-phenyl)-2H-3,4-dihydro-l,3-oxazin-2,4-dione (0.7g, 2.99mmol) (obtained in preparation 9) and 4-bromoaniline (3.6g, 20mmol) by following the procedure described in preparation 11 (0. 445g, 36.8%). “H-NMR (DMSO - de): 8 2.55 (s, 3H), 6.68 (s, IH), 7.37 -

7.39 (d, 4H), 7.49 (s, 2H), 7.81 - 7.83 (d, 4H), 11.8 (bs, IH). MS m/z: 407.2 (M").

Finely powdered anhydrous aluminium chloride (0.83g, 6mmol) was added to a stirred mixture of 4-chlorobenzonitrile (0.6875g, 5mmol) and 4-methylthioaniline (0.695g, 5mmol) over a period of 30 min. The reaction mixture was heated at 180 -190 °C for 3 hours with stirring and allowed to cool to 50 °C, The resultant mixture was triturated with ethyl acetate and basified with sodium hydroxide (20%) solution. The ethyl acetate layer was washed with water, dried over anhydrous sodium sulphate and concentrated to give the crude product, which was purified by column chromatography to yield the title compound (0.6g, 43.4%, purity 98.8% by HPLC), mp 148 - 150 °C. “H-NMR (CDCI3): 6 2.48 (s, 3H), 6.90-6.97(m, 2H), 7.11-7.41(m, 4H), 7.74 (bs, 2H). MS m/z: 277.0 (M”)

described in preparation 22, (0.495g, 44.4%, purity 98.3% by HPLC), mp 144 -146 °C. 'H-NMR (CDCI3): 5 2.49 (s, 3H), 4.8 (bs, 2H), 6.93-6.95 (d, 2H), 7.26-7.32 (m, 2H), 7.70-7.72 (d, 2H), 7.99-8.01 (d, 2H). MS m/z: 311.1(M”).

The title compound was prepared from 4-methylthiobenzonitrile (0.50g, 33.6mmol) and 4-fluoroaniline (0.372g, 33.6mmol) by following the procedure described in preparation 22, (0.43g, 49.3%, mp 145 - 147 °C, purity 94.7% by HPLC). 'H-NMR (CDCI3): 5 2.52 (s, 3H), 6.93-6.94 (m, 3H), 7.17-7.32 (m, 5H). MSm/z:261.1(M”)

The title compound was prepared from 4-methylthiobenzonitrile (2.50g, 16.78mmol) and 4-methylaniline (1.789g, 16.78mmol) by following the procedure described in preparation 22, (2.05g, 47.6%, purity 79%) by HPLC), mp

The title compound was prepared from 4-fluorobenzonitrile (2.176g, 17.98mmol) and 4-methylthioaniline (2.5g, 17.98mmol) by following the procedure described in preparation 22, (2.06g, 44.1%, purity 98.8% by HPLC), mpl21 - 124 °C. “H-NMR (CDCI3): 5 2.48 (s, 3H), 4.82 (bs, 2H, DjO exchangeable), 6.91-6.93 (d, 2H), 7.1-7.14 (m, 2H), 7.26-7.30 (m, 2H), 7.86 (bs, 2H). MS m/z: 261.1(M”)

The title compound was prepared from benzonitrile (3.705g, 35.97mmol) and 4-methylthioaniline (5.0g, 35.97mmol) by following the procedure described in preparation 22, (3.66g, 42.1%, purity 99.8% by HPLC), mp 129 - 131 °C. 'H-NMR (CDCI3): 6 2.49 (s, 3H), 4.84 (bs, 2H), 6.94-6.96 (d, 2H), 7.26-7.31 (m, 2H), 7.45-7.49 (m, 3H), 7.87-7.88 (d, 2H). MS m/z: 243.2 (M”)

The title compound was prepared from 4-trifluoromethylbenzonitrile (0.62g, 3.6mmol) and 4-methylthioaniline (0.5g, 3.6mmol) by following the procedure

143 - 145 X. “H-NMR (CDCI3): 5 2.33 (s, 3H), 2.52 (s, 3H), 4.75 (bs, 2H, D2O exchangeable), 6.87 - 6.89 (d, 2H), 7.14 -7.16 (d, 2H), 7.27 - 7.29 (d, 2H), 7.7 -7.79 (d, 2H). MS m/z: 257.1(M”).

A solution of oxone (18.42g, 0.03mol) in water (70nil) was added dropwise to the vigorous stirred solution of 4-methylthiobenzonitrile (1.49g, 0.01 mol) in methanol (50ml) at 20 °C and stirring was continued for three hours. The reaction mixture was diluted with water (50ml) and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to fumish the title compound (1.3g, 72.2%), mp 145 - 149 °C. The compound was used with out any purification for the next step. “H-NMR (CDCI3): 5 3.1 (s, 3H), 7.8 - 7.9 (d, 2H), 8.08 - 8,1 (d, 2H).

The title compound was obtained from 4-methylsulphonylbenzonitrile (2.00g, llmmol) (obtained according to the procedure described in preparation 28) and 4-methylaniline (1.18g, llmmol) according to the procedure described in preparation 1, (1.25g, 39.3%, purity 90.7% by HPLC), mp 187 - 189 °C. “H-NMR (CDCI3): 5 2.34 (s, 3H), 3.07(s, 3H), 4.92 (bs, 2H, D2O exchangeable), 6.87 - 6.89 (d, 2H), 7.18-7.20 (d, 2H), 8.01- 8.03 (d, 2H), 8.08 - 8.1 (d, 2H). MS mix: 289.1(M”).

A solution of oxone (18.42g, 30mmol) in water (70ml) was added dropwise to the vigorous stirred solution of 4-methylthiobenzonitrile (1.49g, 1 Ommol) in methanol (50ml) at 20 °C and stirring was continued for three hours. The reaction mixture was diluted with water (50ml) and extracted with ethyl acetate. The ethyl acetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to fumish the title compound (1.3g, 72.2%), mp 145 - 149 °C. The compound was used with out any purification for the next step. “H-NMR (CDCI3): 5 3.1 (s, 3H), 7.8 - 7.9 (d, 2H), 8.08 - 8.1 (d, 2H).
Preparation 31
Synthesis of ethyl 3-amino-3-(4-methylsulfonylphenyl)-2-phenyI-2-
propenoate

Cu(OCOCH3)2.H20 (0.06g, 0.3mmol) and zinc dust (0.718g, llmmol) was added sequentially to the stirred glacial acetic acid (10ml) at 90 °C. The reaction mixture was stirred for 2 min., filtered, washed with glacial acetic acid (5ml) and dried tetrahydrofuran (10ml). The obtained activated zinc was added to dried tetrahydrofuran (30ml) under nitrogen atmosphere with stirring. Ethyl 2-bromo-2-phenyl acetate (0.134g, 0.55mmol) was added together with a crystal of sublimed iodine under reflux. 4-Methylsulfonylbenzonitrile (l.Og, 5.5mmol) (obtained according to the procedure given in preparation 30) in dried tetrahydrofuran (20ml) was added dropwise followed by slow addition of ethyl 2-bromo-2-phenyl acetate (1.21g, 5mmol) and the reaction mixture was refluxed with stirring for 20 hours. The residual zinc was filtered off and the resultant filtrate poured into saturated ammonium chloride solution and extracted with ethylacetate. The ethyl acetate extract was washed with water, dried, and concentrated under reduced pressure to yield the title compound (1.3g, 67.4%) which was used in the next step with out any purification. “H-NMR (CDCI3): 8 1.19 - 1.27 (t, 3H), 3.09 (s, 3H), 4.12 - 4.21 (q, 2H), 7.12 - 7.33 (m, 5H), 7,88 - 7.90 (m, 2H), 8.08 - 8.10 (m, 2H). MS m/z: 346 (M”).
Preparation 32
Synthesis of ethyl 3-aminO"2-(4-chlorophenyl)-3-(4-methylsulfonyIphenyl)-2-
propenoate

The title compound was prepared from ethyl 2-bromo-2-(4-chlorophenyl)acetate (4.2g, ISmmol) and 4-methylsulfonylbenzonitrile (2.72g, ISmmol) (obtained according to the procedure given in preparation 30) by a similar procedure as described in preparation 2 (3.6g, 63%). It was used without further purification in the next step. MS m/z: 380.1(M”).

The title compound was prepared from ethyl 2-bromo-2-(4-fluorophenyl)acetate (7g, 27mmol) and 4-methylsulfonylbenzonitrile (4.85g, 27mmol) (obtained according to the procedure given in preparation 30) by following the procedure described in preparation 2 (6.3g, 64.7%). It was used without further purification in the next step. MS m/z: 364 (M"“).
Preparation 34

Trifluoroacetic anhydride (3.3g, 15.5mmol) was added to ethyl 3-amino-3-(4-methylsulfonylphenyl)-2-phenyl-2-propenoate (3.45g, lOmmol) (obtained according to the preparation 31) in pyridine (10ml) at 20 °C temperature under stirring. The temperature was raised to 35 °C and stirred for 12 hours. The reaction mixture was poured onto ice-water mixture and acidified with concentrated hydrochloric acid (pH 1) and extracted with ether. The ether extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness in vaccum. The viscous oily residue thus obtained was triturated with the saturated sodium bicarbonate solution and extracted with ether. The ether extract was washed with water, and the combined aqueous phases were acidified with concentrated hydrochloric acid (pH 1). The precipitate thus seperated was extracted with ether. The ether extract was washed with water, dried and concentrated under reduced pressure to yield the title compound (1.5g, 36%), which was used in the next step without further purification.
Preparation 35
Synthesis of 2-(4-chloropiienyl)-3-(4-metliylsuIfonylpiienyl)-3-
[(trifluoroacetyl)amino]propenoic acid

The title compound was prepared from ethyl 3-amino-2-(4-chlorophenyl)-3-(4-methylsulfonylphenyl)-2-propenoate (6.5g, 170mmol) (obtained according to the preparation 32)and trifluoro acetic anhydride by following the procedure described in preparation 34, (1.7g, 22.2%). The compound was used in the next step without further purification.
Preparation 36
Synthesis of 2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-3-
[(trifluoroacetyl)amino]propenoic acid

The title compound was prepared from ethyl 3-amino-2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-2-propenoate (5.7g, 15.7mmol) (obtained according to the preparation 33) and trifluoro acetic anhydride by following the procedure described in preparation 35, (2.5g, 37.3%). The compound was used in the next step without further purification.
Preparation 37
Synthesis of ethyl 3-(4-chlorophenyl)-2-phenyl-3-oxopropanoate

Lithium bis(trimethylsilyl)amide (20% in tetrahydrofuran, 4L3ml, 45mmol) was added dropwise to a stirred solution of ethyl phenylacetate (7.0g, 42.7mmol) in dried tetrahydrofuran (30ml) at -78 °C. After 15 minutes, the mixture was treated with 4-chlorobenzoyl chloride (7.85g, 44.8mmol) dropwise at -78 °C and the stirring was continued for 2 hours. The reaction was quenched with saturated ammonium chloride solution and extracted with ethyl acetate. The ethyl acetate extract was washed thoroughly with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness in vaccum to furnish the title compound (lO.Og, 78%, purity 84.85% by HPLC), mp 68 - 71 °C. The compound was used in the next step without further purification. “H-NMR (CDCI3): 5 1.23 - 1.26 (t, 3H), 4.21 - 4.23 (q, 2H), 5.53 (s, IH), 7.33 - 7.44 (m, 7H), 7.88 - 7.90 (m, 2H). MS m/z: 303.4 (M”).
Preparation 38
Synthesis of ethyl 3-(4-methylpheny!)-2-phenyl-3-oxopropanoate

The title compound was prepared from ethyl phenylacetate (7.0g, 42.7mmol) and p-toluoyl chloride (6.93g, 44.8mmol) by following the procedure described in preparation 37 (9.3g, 77%, purity 93.77% by HPLC), mp 53 - 55 “C, The

compound was used in the next step without further purification. H-NMR (CDCI3): 5 1.22 - 1.26 (t, 3H), 2.37 (s, 3H), 4.19 - 4.24 (q, 2H), 5.58 (s, IH), 7.20 - 7.41 (m, 7H), 7.85 - 7.87 (m, 2H). MS m/z: 283.2 (M”).
Preparation 39
Synthesis of ethyl 2-phenyl-3-(4-trifluoromethylphenyl)-3-oxopropanoate

The title compound was prepared from ethyl phenylacetate (7.0g, 42.7mmol) and 4-(trifluoromethyl)benzoylchloride (9.4g, 44.8mmol) by following the procedure described in preparation 37 (4.8g, 33.4%, purity 56.58% by HPLC), mp 151 -155 °C. The compound was used in the next step without further purification. MS m/z: 337.2 (M”).
Preparation 40
Synthesis of ethyl 2-(4-chlorophenyl)-3-phenyl-3-oxopropanoate

The title compound was prepared from ethyl (4-chlorophenyl)acetate (5.0g, 25mmol) and benzoylchloride (3.65g, 26mmol) by following the procedure described in preparation 37 (6.7g, 88%, purity 98.51% by HPLC). The compound was used in the next step without further purification. “H-NMR (DMSO -de): 8

1.13 - 1.16 (t, 3H), 4.13 - 4.14 (q, 2H), 6.24 (s, IH), 7.43 (s, 4H), 7.53 - 7.6 (m, 3H), 8.01 - 8.04 (m, 2H). MS m/z: 303.1(M”).
Preparation 41
Synthesis of ethyl 2-(4-methylthiophenyl)-3-phenyl-3-oxopropanoate

The title compound was prepared from ethyl (4-methylthiophenyl)acetate (5.04g, 24mmol) and benzoylchloride (3.38g, 24mmol) by following the procedure described in preparation 37 (6.5g, 86.3%, purity 99.2% by HPLC). The compound was used in the next step without further purification. “H-NMR (CDCI3): 8 1.22 - 1.25 (t, 3H), 2.45 (s, 3H), 4.19 - 4.24 (q, 2H), 5.55 (s, IH), 7.21 - 7.26 (m, 2H), 7.31 - 7.33 (m, 2H), 7.41 - 7.44 (m, 2H), 7.52 - 7.54 (m, IH), 7.94 " 7,96 (m, 2H). MS m/z: 315 (M”).
Preparation 42
Synthesis of ethyl 2-(4-methoxyphenyl)-3-phenyl-3-oxopropanoate

The title compound was prepared from ethyl (4-methoxyphenyl)acetate (9.5g, 49mmol) and benzoylchloride (7.2 Ig, 51mmol) by following the procedure described in preparation 37 (1 l.Og, 75.4%, purity 89.33% by HPLC), mp 66 - 68

°C. The compound was used in the next step without further purification. H-NMR (CDCI3): 5 1.22 - 1.25 (t, 3H), 3.79 (s, 3H), 4.19 - 4.24 (q, 2H), 5.5 (s, IH), 6.87 - 6.9 (m, 3H), 7.51 - 7.55 (m, 4H), 7.94 - 7.96 (d, 2H).MS m/z: 299.2 (M").

The title compound was prepared from ethyl (4-chlorophenyl)acetate (6.2g, 31mmol) and 4-methyl benzoyl chloride (5,02g, 32.5mmol) by following the procedure described in preparation 37 (7.9g, 80%, purity 94.93% by HPLC). The compound was used in the next step without further purification. “H-NMR (CDCI3): 5 1.22 - 1.25 (t, 3H) 2.38 (s, 3H), 4.18 - 4.24 (q, 2H), 5.5 (s, IH), 7.22 ~ 7.26 (m, 2H), 7.31 - 7.36 (m, 4H), 7.83 - 7.85 (d, 2H). MS m/z: 317.1 (M"").

A mixture of 6-amino-2-methylthio-l-phenyl-lH-pyrimidin-4-one (2.33g, lOmmol) (obtained in preparation 2) and aniline (4.6g, SOmmol) in presence of catalytic amount of concentrated hydrochloric acid was heated at 120 -130 °C for 7 hours. The reaction mixture was cooled, filtered and washed with hexane. The obtained crude product was recrystallised from ethanol to provide the title compound (1.13g, 40.6%, purity 99.5% by HPLC), mp 202 - 206 °C. 'H-NMR (DMSO-de): 8 5.09 (s, IH), 6.96 - 7.03 (m, 2H), 7.24 - 7.30 (m, 4H), 7.40 - 7.42 (m, 2H), 7.59 - 7.61 (m, 2H), 8.74 (s, IH, DjO exchangeable), 8.94 (s, IH, D2O exchangeable), 10.0 (s, IH, D2O exchangeable). IR (KBr) cm': 3302, 3152 (-NH-), 1666 (-C=0). MS m/z: 279.2 (M”).
Example 2
Synthesis of 6-amino-2-(4-methoxy-phenylamino)-l-phenyl-lH-pyrimidin-4-
one

The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (1.5g, 6.5mmol) (obtained in preparation 2) and 4-methoxyaniline (3.96g, 32mmol) by following the procedure described in example 1 (0.8g, 40.3%, purity 98.4% by HPLC), mp 213 - 216 °C. *H-NMR (CDCI3): 5 3.73 (s, 3H), 4.9 (s, IH), 6.87 - 6.89 (m, 2H), 7.00 (m, IH), 7.25 -7.29 (m, 4H), 7.60 - 7.62 (m, 2H), 8.73 (bs, 2H, D2O exchangeable), 10.0 (bs,

IH, D2O exchangeable). IR (KBr) cm-” 3305, 3152 (-NH-), 1678 (-C=0). MS m/z: 309.2 (M”).
Example 3
Synthesis of 6-amino-2-(4-ethoxy-phenylamino)-l-phenyl-lH-pyrimidin-4-
one

The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (l.Og, 4mmol) (obtained in preparation 2) and 4-ethoxyaniline (2.94g, 21mmol) by following the procedure described in example 1 (0.49g, 35.2%, purity 97.1% by HPLC), mp 111 - 113 *”C. “H-NMR (DMSO-da): 5 1.30 - 1.33 (t, 3H), 3.97 - 4.02 (q, 2H), 4.92 (s, IH), 6.85 - 6.87 (m, 2H), 6.99 - 7.02 (m, IH), 7.24 - 7.29 (m, 4H), 7.60 -7.62 (m, 2H), 8.72 (bs, 2H, D2O exchangeable), 9.9 (s, IH, D2O exchangeable). IR (KBr) cm'*: 3308, 2976, 1674(-C=0). MS m/z: 323.3 (M”).
Example 4

Synthesis of 6-amino-2-(4-methylthio-phenylamliio)-l-phenyl-lH-pyriinidin-4-one

The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (3.Og, 12.8mmol) (obtained in preparation 2) and 4-methylthioaniline (8.85g, 64mmol) by following the procedure described in example 1 (2.26g, 54.1%, purity 92.7% by HPLC), mp 133 - 135 °C. “H-NMR (DMSO-dfi): 5 2.45 (s, 3H), 5,06 (s, IH), 7.00 - 7.04 (m, IH), 7.18-7.21 (m, 2H), 7.25 - 7.31 (m, 2H), 7.37 - 7.42 (m, 2H), 7.58 -7.61 (m, 2H), 8.87 - 8.95 (bs, 2H, D2O exchangeable), 10.2 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3421, 1627 (-C=0). MS m/z: 325.2 (M”).
Example 5
Synthesis of 6-amino-2-(4-methyl-phenylamino)-l-phenyl-lH-pyrimidin-4-
one
The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-methylaniline (4.59g, 42.9mmol) by following the procedure described in

example 1 (1.33g, 53%), purity 98.4% by HPLC), mp 207 - 210 °C. 'H-NMR (DMSO-dfi): 6 2.25 (s, 3H), 5.02 (s, IH), 6.98 - 7.10 (m, 3H), 7.23 -7.30 (m, 3H), 7.39 - 7.60 (m, 3H), 8.63 - 8.90 (m, 2H, D2O exchangeable), 9.93 (bs, IH, D2O exchangeable). IR (KBr) cm-': 3306, 1630 (-C=0). MS m/z: 293.1 (M”).
Example 6
Synthesis of 6-amino-2-(4-chloro-phenyIamino)-l-phenyl-lH-pyrimidin-4-
one

The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-chloroaniline (5.47g, 42.9mmol) by following the procedure described in example 1 (1.2g, 45%, purity 98.9% by HPLC), mp 233 - 237 °C. 'H-NMR (DMSO-de): 8 5.07 (s, IH), 7.0 - 7.06 (m, IH), 7.24 -7.34 (m, 5H), 7.40 - 7.42 (m, 2H), 7.52 - 7.54 (m, 2H), 8.8 - 9.01 (bs, 2H, D2O exchangeable). IR (KBr) cm-': 3424, 1627 (-C=0). MS m/z: 313 (M”).
Example 7

Synthesis of 6-amino-2-(4-fluoro-phenylaiiiino)-l-phenyl-lH-pyrimidin-4-one

The title compound was prepared from 6-amino-2-methylthio-l-phenyl-IH-pyrimidin-4-one (2.0g, 8.58mmol) (obtained in preparation 2) and 4-fluoroaniline (4.76g, 42.9mmol) by following the procedure described in example 1 (0.8g, 31%, purity 98.3% by HPLC), mp 225 - 227 “C. “H-NMR (DMSO-de): 8 4.95 (s, IH), 6.99 - 7.56 (m, 9H), 8.73 (bs, IH, D2O exchangeable), 8.92 (bs, IH, D2O exchangeable), 10 (bs, D2O exchangeable). IR (KBr) cm"“ 3295, 1637 (-C=0). MS m/z: 297.3 (M”).
Example 8
Synthesis of 6-amino-l-(4-methylphenyl)-2-(4-methylthio-phenylamino)-lH-
pyrimidin-4-one

The title compound was prepared from 6-amino-2-methylthio-1 -(4-methylphenyl)-lH-pyrimidin-4-one (Ig, 4mmol) (obtained in preparation 3) and 4-methylthioaniline (1.112g, 8mmol) by following the procedure described in

example 1 (0.45g, 32.8%, purity 94.8% by HPLC), mp 231 - 234 °C. 'H-NMR (DMSO-dfi): 5 2.26 (s, 3H), 2.45 (s, 3H), 5.0 (s, IH), 7.08 - 7.12 (m, 2H), 7.18 -7.22 (m, 3H), 7.36 - 7.56 (m, 4H), 8.93 - 8.96 (m, 2H, D2O exchangeable). IR (KBr) cm-': 3303, 1627 (-C=0). MS m/z: 339.1 (M”).
Example 9
Synthesis of 6-amino-l-(4-methoxyphenyl)-2-phenylamino-lH-pyrimidin-4-
one

The title compound was prepared from 6-amino-2-methylthio-l-(4-methoxyphenyl)-lH-pyrimidin-4-one (1.5g, 5.7mmol) (obtained in preparation 4) and aniline (2.65g, 28.5mmol) by following the procedure described in example 1 (0.41g, 23%, purity 97.1% by HPLC), mp 180 - 190 °C. *H-NMR (DMSO-dg): 8 3.72 (s, 3H), 4.95 (s, IH), 6.85 - 6.87 (m, 3H), 7.2 - 7.30 (m, 3H), 7.5 - 7.6 (m, 3H), 8.4 (bs, IH, D2O exchangeable), 8.8 (bs, IH, D2O exchangeable), 9.8 (bs, IH, D2O exchangeable). IR (KBr) cm"': 3401 (NH), 1630 (-C=0). MS m/z: 309.2 (M").
Example 10
Synthesis of 6-amino-l-(4-etlioxyphenyl)-2-plienylamino-lH-pyrimidin-4-one

The title compound was prepared from 6-amino-2-methylthio-1 -(4-ethoxyphenyl)-lH-pyrimidin-4-one (2.0g, 7.2mmol) (obtained in preparation 5) and aniline (3.2g, 35mmol) by following the procedure described in example 1 (0.71g, 30%, purity 98% by HPLC), mp 114 - 118 °C. “H-NMR (DMS0-d6): 6 1.30 - 1.33 (t, 3H), 3.97 - 4.02 (q, 2H), 5.01 (s, IH), 6.85 - 7.60 (m, 9H), 8.45 (bs, IH, D2O exchangeable), 8.88 (bs, IH, D2O exchangeable), 10.0 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3309(-NH-), 1628 (-C=0). MS m/z: 323.2 (M”).
Example 11
Synthesis of 6-amino-l-(4-chlorophenyl)-2-phenylamino-lH-pyrimidin-4-one

The title compound was prepared from 6-amino-2-methylthio-1 -(4-chlorophenyl)-lH-pyrimidin-4-one (2.0g, 7.48mmol) (obtained in preparation 6) and aniline (3.48g, 37.4mmol) by following the procedure described in example 1 (1.21g, 52%, purity 95.7% by HPLC), mp 216 - 222 °C. “H-NMR (DMS0-d6): 6 5.15 (s, IH), 6.97 - 7.02 (m, IH), 7.26 - 7.32 (m, 4H), 7.40 - 7,71 (m, 5H), 8.94

(s, IH, D2O exchangeable), 10.4 (bs, IH, DjO exchangeable). IR (KBr) cm': 3306, 1678 (-C-0). MS m/z: 313.1 (M”).
Example 12
Synthesis of 6-amino-l-(4-bromophenyl)-2-phenylammo-lH-pyrimidiii-4-one

The title compound was prepared from 6-amino-2-methylthio-l-(4-bromophenyl)-lH-pyrimidin-4-one (l.Og, 3.2mmol) (obtained in preparation 7) and aniline (0.57g, 6mmol) by following the procedure described in example 1 (0.6g, 52.5%, purity 92.1% by HPLC), mp 211 - 213 °C. 'H-NMR (DMSO-d”): d 5.1 (bs, IH), 6.9 - 7.0 (m, IH), 7.29 - 7.43 (m, 8H), 8.92 - 9.0 (bm, 2H, D2O exchangeable). IR (KBr) cm"“ 3320, 1633 (-C=0). MS m/z: 357/358.9 (M”).
Example 13
Synthesis of l-(4-methylsulfanyl-phenyl)-6-phenyl-lH-pyrimidin-2,4-(lH)-dione

A mixture of N-(4-methylsulfanyl-phenyl)-[N'-l-(3-phenyl)-l,3-diketone]urea (O.lg, 0,3mmol) (obtained in preparation 17) and p-toluenesulfonic acid (0.057g, O.Bmmol) in toluene (10ml) was refluxed with stirring for 4 hours. The reaction mixture was allowed to cool at room temperature, poured into water and extracted with ethylacetate. The ethylacetate extract was washed with water, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was purified by column chromatography to yield the title compound (0.09g, 95.2%, mp 239 - 242 °C (decomposed), purity 98.10% by HPLC). 'H-NMR (DMSO - dg): 6 2.39 (s, 3H), 5.63 (s, IH), 7.07 - 7.10 (d, 2H), 7.14-7.17 (d, 2H), 7.22 - 7.24 (s, 5H), 11.54 (s, IH). IR (KBr) cm"': 3188, 3040 (-NH-), 1720, 1681 (-C=0). MS m/z: 311. KM"").
Example 14
Synthesis of l-(4-methylsulfanyl-phenyl)-6-(4-methylphenyl)-lH-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from N-(4-methylsulfanyl-phenyl)-{N'-l-[3-(4-methylphenyl)]-l,3-diketone}urea (0.24g, 0.7mmol) (obtained in preparation 18) and p-toluenesulfonic acid (0.134g, 0.7mmol) in toluene (10ml) by refluxing for 2 hours and following the procedure described in example 13 (0.17g, 74.9%, mp 235 - 238 °C, purity 98.9% by HPLC). 'H-NMR (DMSO - dg): 5 2.20 (s, 3H),

2.40 (s, 3H), 5.59 (s, IH), 7.02 -7.17 (m, 8H), 11.53 (bs, IH). IR (KBr) cm"': 3180, 3051 (-NH-), 1693 (-C=0). MS m/z: 325.3 (M”).
Example 15
Synthesis of 1 -(4-methylsulfanyI-phenyl)-6-(4-chlorophenyl)-l H-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from N-(4-methylsulfanyl-phenyl)-{N'-l-[3-(4-chlorophenyl)]-l,3-diketone}urea (0.33g, 0.91mmol) (obtained in preparation 19) in toluene (30ml) containing p-toluenesulfonic acid (0.294g, 1.6mmol) was refluxed for 9 hours by following the procedure described in example 13 (0.289g, 92.2%, mp 249 - 251 °C, purity 99.6% by HPLC). 'H-NMR (DMSO - dg): 5 2.41 (s, 3H), 5.67 (s, IH), 7.10 - 7.19 (m, 4H), 7.25 -7.33 (m, 4H), 11.5 (bs, IH). IR (KBr) cm-” 3178, 3054 (-NH-), 1691 (-C=0). MS m/z: 345 (M”).
Example 16
Synthesis of l-(4-methylphenyl)-6-(4-methylsulfanyl-phenyi)-lH-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from N-(4-methylphenyl)-{N'-l-[3-(4-methylsulfanyl-phenyl)]-l,3-diketone}urea (0.24g, 0.7mmol) (obtained in preparation 13) and p-toluenesulfonic acid (0,134g, OJmmol) in toluene (10ml) by refluxing for 4 hours and following the procedure described in example 13 (0.186g, 82%, mp 266 - 268 “C, purity 99.8 % by HPLC). “H-NMR (DMSO -de): 8 2.20 (s, 3H), 2.38 (s, 3H), 5.60 (s, IH), 7.03 - 7.13 (m, 8H), 11.59 (bs, IH, D2O exchangeable). IR (KBr) cm-”: 3335 (-NH-), 1683 (-C=0). MS m/z: 325.2 (M").
Example 17
Synthesis of l-(4-bromophenyl)-6-(4-methylsulfanyl-phenyl)-lH-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from N-(4-bromophenyl)- {N' -1 - [3 -(4-methylsulfanyl-phenyl)]-l,3-diketone}urea (0.430g, 1.05mmol) (obtained in preparation 21) in toluene (10ml) containing p-toluenesulfonic acid (0.602g,

3mmol) was refluxed for 8 hours and following the procedure described in example 13 (0.151g, 36.8%, mp 282 - 285 °C, purity 97.8% by HPLC). “H-NMR (DMSO - de): 5 2.55 (s, 3H), 5.68 (s, IH), 7.08 - 7,01 (d, 2H), 7.15 - 7.17 (d, 2H), 7.20 - 7.22 (d, 2H), 7.48 - 7.50 (d, 2H), 11,58 (bs, IH, D2O exchangeable). IR (KBr) cm'“ 3155 (-NH-), 3022, 1712 (-C=0). MS m/z: 389 (M”).
Example 18
Synthesis of l-(4-methylsulfonyl-phenyl)-6-phenyl-pyrimidin-lH-pyrimidin-
2,4-(lH)-dione

Oxone (1.189g, 1.93mmol) in water (5ml) was added dropwise to a stirred suspension of 1 -(4-methylsulfanyl-phenyl)-6-phenyl-1 H-pyrimidin-2,4-( 1H)-dione (0.2g, 0.64mmol) (obtained according to the procedure described in example 13) in methanol (10ml) and stirring was continued for 3 hours at room temperature. Saturated sodium bicarbonate solution (20ml) was added to the reaction mixture and extracted with ethylacetate. The ethylacetate extract was washed with water, brine, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was purified by column chromatography to yield the title compound (0.117g, 53.2%, mp 283 -287 °C (decompose), purity 96.5% by HPLC). “H-NMR (DMSO - d6): 8 3.18 (s, 3H), 5.72 (s, IH), 7.21 - 7.25 (s, 5H), 7.53 - 7.55 (d, 2H), 7.78 -7.8 (d, 2H),

11.68 (bs, IH). IR (KBr) cm"': 3033 (-NH-), 1719, 1684 (-C=0). MS m/z: 343.1 (M").
Example 19
Synthesis of 6-(4-methylphenyl)-l-(4-methylsulfonyl-phenyl)-lH-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from l-(4-methylsulfanyl-phenyl)-6-(4-methylphenyl)-lH-pyrimidin-2,4-(lH)-dione (0.3g, 0.92mmol) (obtained according to the procedure described in example 18) by following the procedure described in example 6 (0.244g, 74.2%, mp 285 - 288 °C, purity 99.4% by HPLC). 'H-NMR (DMSO - dfi): 5 2.19 (s, 3H), 3.20 (s, 3H), 5.68 (s, IH), 7.03 -7.05 (d, 2H), 7.05 - 7.09 (d, 2H), 7.53 - 7.55 (d, 2H), 7.80 - 7.82 (d, 2H), 11.65 (bs, IH, D2O exchangeable). IR (KBr) cm': 3008 (-NH-), 1716, 1681 (-C=0). MS m/z: 357.1 (M"").
Example 20
Synthesis of 6-(4-chlorophenyl)-l-(4-methylsulfonyl-phenyl)-lH-pyrimidin-
2,4-(lH)-dione

The title compound was prepared from l-(4-methylsulfanyl-phenyl)-6-(4-chlorophenyl)-lH-pyrimidin-2,4-(lH)-dione (0.5g, 1.4mmol) (obtained according to the procedure described in example 18) by following the procedure described in example 6 (0.326g, 59.3%, mp 294 - 298 °C, purity 97.6% by HPLC). “H-NMR (DMSO - de): 8 3.20 (s, 3H), 5.76 (s, IH), 7.24 - 7.26 (d, 2H), 7.32 - 7.34 (d, 2H), 7.55 - 7.57 (d, 2H), 7.82 -7.84 (d, IH), 11.71 (bs, IH, D2O exchangeable). IR (KBr) cm”“: 3437, 3170, 3049 (-NH-), 1690 (-C=0). MS m/z: 377.1 (M”).
Example 21
Synthesis of 4-(2,6-dioxO"'3-phenyl-l,2,3,6-tetrahydro-pyrimidin-4-yl)-
benzenesulfonamide

The chlorosulfonic acid (1.18g, lOmmol) was added to a solution of 1,6-diphenyluracil (0.2g, 0.75mmol) (synthesized according to the procedure given in Harvey I. Skulnick, Heterocycles, 23, (7), ppl685, 1985) in chloroform (20ml) and refluxed for 2 hours. The reaction mixture was poured onto ice-water mixture

and extracted with ethylacetate. The ethylacetate extract was washed with brine, dried over anhydrous sodium sulphate and concentrated to dryness under reduced pressure. The crude solid thus obtained was taken in tetrahydrofuran (20ml) and treated with ammonia solution (1ml) under stirring. The reaction mixture was stirred for 1 hour and concentrated to dryness in vacuum. The product thus obtained was dissolved in ethylacetate, washed with water, brine and dried over anhydrous sodium sulphate. The ethylacetate extract was concentrated to dryness under reduced pressure and purified by column chromatography to yield the title compound (O.lg, 18.3%).
mp : ,
“H-NMR (DMSO - de): 8 5.69 (s, IH), 7.21 - 7.26 (m, 5H), 7.36 - 7.46 (m, 4H), 7.65 - 7.72 (m, 2H), 11.63 (bs, IH). MS m/z: 344.1 (M”).
Example22
Synthesis of 5-cyano-2-(4-chlorophenyl)-4-methylthio-l-(4-methylthio-
phenyl)-l,6-dihydro-pyrimidin-6-one

A mixture of ethyl 2-cyano-3,3-dimethylthioacrylate (1.345g, 6.2mmol) and N-(4-methylthio-phenyl)-4-chlorobenzamidine (1.7g, 6.2mmol) (obtained according to the procedure described in preparation 22) was heated at 110 -120 °C for 2 hours. The gummy mass thus obtained was purified by column chromatography to give the title compound (l.lg, yield 44.4%, purity 94.6% by HPLC), mp 206-

207 °C.'H-NMR (CDCI3): 5 2.47 (s, 3H), 2.66 (s, 3H), 6.99 -7.01 (d, 2H), 7.18-7.30 (m, 6H). IR (KBr) cm-': 2218(-CN), 1672 (-C=0). MS m/z: 400.1(M”).
Example 23
Synthesis of 5-cyano-2-(4-fluorophenyl)-4-methylthio-l-(4-methylthio-
phenyl)-l,6-dihydro-pyrimidin-6-one

The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (1.25g, 5.76mmol) and N-(4-methylthio-phenyl)-4-fluorobenzamidine (1.50g, 5.76mmol) (obtained in preparation 23) according to the procedure described in example 22, (l.Sg, 81.8%, purity 99.4% by HPLC), mp 204-207 °C. 'H-NMR (CDCI3): 5 2.46 (s, 3H), 2.67 (s, 3H), 6.94 -7.01 (m, 4H), 7.17-7.26 (m, 2H), 7.35-7.38 (m, 2H). IR (KBr) cm-': 2218(-CN), 1678 (-C=0). MS m/z: 384 (M”)
Example 24
Synthesis of 5-cyano-4-methylthio-l-(4-methylthio-phenyl)-2-phenyl-l,6-dihydro-pyrimidin-6-one

The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (1.345g, 6.2mmol) and N-(4-methylthio-phenyl)benzamidine (1.50g, 6.2mmol) (obtained in preparation 24) by following the procedure described in example 22, (1.28g, yield 56.6%, purity 98.8% by HPLC), mp 204 - 205 °C. 'H-NMR (CDCI3): 8 2.45 (s, 3H), 2.67 (s, 3H), 6.99 - 7.01 (m, 2H), 7.15 -7.17 (m, 2H), 7.26 - 7.37 (m, 5H). IR (KBr) cm"': 2218 (-CN), 1682 (-C=0). MS m/z: 366
Example 25
Synthesis of 5-cyano-4-methylthio-l-(4-methylthio-phenyl)-2-(4-
trifluoromethylphenyl)-l,6-dihy(lro-pyrimidiii-6-one

The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (l.Og, 4.6mmol) and the N-(4-methylthio-phenyl)-4-trifluoromethylbenzamidine (1.50g, 4.8mmol) (obtained according to the procedure described in preparation 25) by following the procedure described in example 22, (1.6g, 80.1%, purity 99.3% by HPLC), mp 228 - 229 °C. 'H-NMR (CDCI3): 8 2.46 (s, 3H), 2.66 (s, 3H), 6.99 - 7.01 (d, 2H), 7.17-7.19 (d, 2H), 7.46 - 7.48 (d, 2H), 7.54 - 7.56 (d, 2H). IR (KBr) cm'“ 2215 (-CN), 1680 (-C=0). MS m/z: 434.2 (M”).
Example 26
Synthesis of 5-cyano-l-(4-fluorophenyI)-4-methylthio-2-(4-methylthio-
phenyI)-l,6-dihydro-pyrimidin-6-one

The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (0.334g, 1.54mmol) and N-(4-fluorophenyl)-4-methylthiobenzamidine (0.40g, l,54mmol) (obtained in preparation 26) by following the procedure described in example 22, (0.32g, 54.3%, purity 99.2% by HPLC), mp 219 - 221 °C. “H-NMR (CDCI3): 5 2.46 (s, 3H), 2.68 (s, 3H), 7.05 - 7.12 (m, 6H), 7.23 -7.27 (m, 2H). IR (KBr) cm-”: 2218 (-CN), 1667 (-C=0). MS m/z: 384 (M”).
Example 27
Synthesis of 5-cyano-l-(4-methylphenyl)-4-methylthio-2-(4-methylthio-
phenyl)-l,6-dihydro-pyrimidin-6-one

The title compound was prepared from ethyl 2-cyano-3,3"dimethylthioacrylate (0.848g, 3.9mmol) and N-(4-methylphenyl)-4-methylthiobenzamidine (l.Og, 3.9mmol) (obtained in preparation 27) by following the procedure described in example 22, (0.68g, 46%, purity 99.3% by HPLC), mp 196 - 198 “C. “H-NMR (CDCI3): 5 2.34 (s, 3H), 2.45 (s, 3H), 2,67 (s, 3H), 6.99 - 7.01 (m, 2H), 7.04 -7.06 (m, 2H), 7.14 - 7.18 (m, 2H), 7.26-7.28 (m, 2H). IR (KBr) cm'“ 2215 (-CN), 1688 (-C=0). MS m/z: 380.4 (M"").

Example 28
Synthesis of 5-cyano-l-(4--inethylpheiiyl)-2-(4-methylsulphonyl-phenyl)-4-
methylthio-l,6-dihydro-pyriinidin-6-one

The title compound was prepared from ethyl 2-cyano-3,3-dimethylthioacrylate (0.378g, 1.74mmol) and N-(4-methylphenyl)-4-methylsulphonylbenzamidine (0.5g, 1.74mmol) (obtained in preparation 29) according to the procedure described in example 22, (0.43g, 59.6%, purity 99.1% by HPLC), mp 242 - 244 °C. “H-NMR (CDCI3): 6 2.34 (s, 3H), 2.65 (s, 3H), 3.04 (s, 3H), 6.95 - 6.97 (d, 2H), 7.15 - 7.17 (d, 2H), 7.51 - 7.54 (d, 2H), 7.82 -7.84 (d, 2H). IR (KBr) cm'“ 2217 (-CN), 1696 (-C=0). MS m/z: 412 (M”).
Example 29
Synthesis of 5-carboxy-l-(4-methyIphenyl)-4-methylthio-2-(4-methylthio-
phenyl)-l,6-dihydro-pyrimidin-6-one

A mixture of 5-cyano-l-(4-methylphenyl)"4-methylthio-2-(4-methylthio-phenyl)-l,6"dihydro-pyrimidin-6-one (2.5g, 6.59mmol) (obtained according to the procedure described in example 6) and potassium hydroxide (40%, 25ml) solution was refluxed for 2 hours. The reaction mixture was poured onto ice-

water, neutralised with dilute hydrochloric acid and filtered. The solid thus obtained was washed with water and dried to yield title compound (2.12g, 80.8%, purity 91.6% by HPLC), mp 173 • 175 °C. “H-NMR (CDCI3): 8 2.34 (s, 3H), 2.53 (s, 3H), 2.69 (s, 3H), 7.16 - 7.18 (d, 2H), 7.26 - 7.37 (m, 4H), 7.92 - 7.94 (d, 2H), 14.0 (s, IH, D2O exchangeable). IR (KBr) cm'“ 3311(-COOH), 1702(-C-O). MS m/z: 398.5 (M"").
Example 30
Synthesis of 5,6-diphenyl-2-trifluoromethyl-pyrimidin-4-one

2,3-Diphenyl-3-[(trifluoromethyl)-amino]propenoic acid (2.0g, 5.9mol) (synthesized according to the procedure given in US 4987140) was refluxed in acetic anhydride (5ml) for 2 hours and allowed to cool to room temperature. The reaction mixture was cooled to -50 "“C to -60 °C then ammonia gas was passed until the solid separated out. The reaction mass was poured into water and extracted with ethyl acetate. The organic extract was washed with water, dried over anhydrous sodium sulphate and concentrated under reduced pressure to give crude product, which was purified by column chromatography to afford the title compound (0.28g, 15 %, purity 99.58% by HPLC), mp 194 - 197 “C. “H-NMR (CDCI3): 5 7.23 - 7.39 (m, lOH). MS m/z: 317.2 (M”).

Example 31
Synthesis of 5-phenyl-6-(4-methylsulfoiiylphenyl)-2-trifluoromethyl-
pyrimidin-4-one

The title compound was prepared from 2-phenyl-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (1.48g, 3,6mmol) (obtained according to the preparation 34) by following the procedure described in example 1 (0.22g, 15.6%, purity 92.11% by HPLC), mp 231 - 238 °C. H-NMR (DMSO-d”): 5 3.16 (s, 3H), 7.16 - 7.17 (m, 2H), 7.25 - 7.26 (m, 3H), 7.46 - 7.48 (m, 2H), 7.55 -7.77 (m, 2H). MS m/z: 395.2 (M”).
Example 32
Synthesis of 5-(4-chlorophenyl)-6-(4-methylsulfonyIphenyl)-2-
trifluoromethyl-pyrimidin-4-one

The title compound was prepared from 2-(4-chlorophenyl)-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (1.5g, 3.4mmol) (obtained according to the procedure given in preparation 35) by following the procedure described in example 1 (0.24g, 17%, purity 95.45% by HPLC), mp 227 - 230 “C. “H-NMR (DMS0-d6): 5 3.20 (s, 3H), 7.27 - 7.30 (d, 2H), 7.40 - 7.42

(d, 2H), 7.54 - 7.56 (d, 2H), 7.86 - 7.88 (d, 2H), 13.9 (bs, IH, D2O exchangeable). MS m/z: 429.2 (M”).

The title compound was prepared from 2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)-3-[(trifluoroacetyl)amino]propenoic acid (2.52g, 6mmol) (obtained according to the procedure given in preparation 36) by following the procedure described in example 1 (0.7g, 29.1%, purity 99.64% by HPLC), mp 271 - 274 °C. *H-NMR (DMS0-d6): 5 3.21 (s, 3H), 7.16 - 7.28 (m, 2H), 7.29 -7.32 (m, 2H), 7.53 - 7.55 (d, 2H), 7.86 - 7.87 (d, 2H), 13.9 (bs, IH, D2O exchangeable). MS m/z: 413 (M"“).

A stirred mixture of ethyl-3-amino-2,3-diphenyl-2-propenoate (4.0g, 15mmol) (synthesized according to the procedure given in US 4987140) and thiourea

(1.14g, ISmmol) was heated at 180 - 190 "“C for 2 hours. The reaction mixture was allowed to cool to room temperature, poured into water, filtered and dried. The soUd thus obtained was purified by washing with ether and finally by methanol to give the title compounds (0.25g, 6 %, purity 98.25% by HPLC),.mp 276 - 278 °C. “H-NMR (DMSO-de): 8 7.00 - 7.31 (m, lOH), 12.54 (s, IH, D2O exchangeable), 12.68 (s, IH, D2O exchangeable). MS m/z: 281.2 (M”).
Example 35
Synthesis of 6-(4-methylsulfonylphenyl)-5-phenyI-2-thiouracil

The title compound was prepared fi'om ethyl-3 -amino-3 -(4-methylsulfonylphenyl)-2-phenyl-2"propenoate (1.12g, 3.25mmol) (obtained according to the preparation 31) and thiourea (0,5g, 6.5mmol) by following the procedure described in example 5 (O.lg, 9%, purity 97. 42 % by HPLC), mp 122 - 125 °C. “H-NMR (DMS0-d6): 6 3.2 (s, 3H), 7.03 - 7.04 (m, 2H), 7.17 (bs, 3H), 7.51 ■ 7.53 (d, 2H), 7.81 - 7.83 (d, 2H), 12.64 (s, IH, D2O exchangeable), 12.76 (s, IH, D2O exchangeable). MS m/z: 359 (M”),
Example 36
Synthesis of 6-(4-chlorophenyI)-5-phenyl-2-thiouracil

A stirred mixture of ethyl 3-(4-chlorophenyl)-2-phenyl-3-oxopropanoate (7.5g, 24.8mol) (obtained according to the procedure given in preparation 37) and thiourea (1.88g, 24.8mol) was heated at 180 - 190 °C for 2 hours. The reaction mixture was allowed to cool to room temperature and triturated with acetone. The resultant mixture was poured onto ice-water mixture with vigorous stirring and filtered. The solid was treated with 10% aqueous potassium hydroxide solution under vigorous stirring and filtered. The clear filtrate was cooled to 0- 5 °C and acidified to pH 6 by dilute hydrochloric acid. The precipitate thus obtained was filtered, washed thoroughly with water and dried to furnish the title compound (2.2g, 28.1%, purity 96.82% by HPLC), mp 262 - 265 °C. “H-NMR (DMSO-da): 8 7.00 - 7.03 (d, 2H), 7.15 - 7.18 (m, 3H), 7.22 - 7.25 (d, 2H), 7.32 - 7.34 (d, 2H), 12.57 (s, IH, D2O exchangeable), 12.70 (s, IH, D2O exchangeable). MS m/z:315(M”).

The title compound was prepared from ethyl 3-(4-methylphenyl)-2-phenyl-3-oxopropanoate (7.0g, 24.8mmol) (obtained according to the procedure given in

preparation 38) and thiourea (1.89g, 24,8mmol) by following the similar procedure described in example 7 (3.3g, 44.6%, purity 93.64% by HPLC), mp 248 - 251 °C. “H-NMR (DMS0-d6): 5 2.27 (s, 3H), 6.99 - 7.14 (m, 9H), 12.30 (s, IH, D2O exchangeable), 12.55 (s, IH, D2O exchangeable). MS m/z: 295.2 (M”).

The title compound was prepared from ethyl 2-phenyl-3-(4-trifluoromethylphenyl)-3-oxopropanoate (4.5g, 13.4mmol) (obtained according to the preparation 39) and thiourea (1.02g, 13.4mmol) by following similar procedure as described in example 7, (0.7g, 15 %, purity 98.53% by HPLC), mp 281 - 284 °C. “H-NMR (DMSO-dg): 5 7.02 - 7.04 (d, 2H), 7.14 - 7.19 (m, 3H), 7.45 - 7.47 (d, 2H), 7.63 - 7.65 (d, 2H), 12.63 (s, IH, D2O exchangeable), 12.75 (s, IH, D2O exchangeable). MS m/z: 349.1 (M”).

The title compound was prepared from ethyl 2-(4"Chlorophenyl)-3-phenyl-3-oxopropanoate (6.5g, 21.5mol) (obtained according to the procedure given in preparation 40) and thiourea (1.64g, 21.5mmol) by following the procedure described in example 7 (2.0g, 30%, purity 95.81% by HPLC), mp 307 - 310 °C. “H-NMR (DMS0-d6): 5 7.02 - 7.04 (d, 2H), 7.21 - 7,28 (m, 7H), 12.59 (s, IH, D2O exchangeable), 12.72 (s, IH, D2O exchangeable). MS m/z: 315 (M”).

The title compound was prepared from ethyl 2-(4-methylthiophenyl)-3-phenyl"3-oxopropanoate (5.5g, 17.5mmol) (obtained according to the procedure given in preparation 41) and thiourea (1.33g, 17.5mmol) by following the procedure described in example 7 (1.5g, 26.3%, purity 96.8% respectively by HPLC), mp 286 - 290 °C. “H-NMR (DMS0-d6): 5 2.40 (s, 3H), 6.93 - 6.95 (d, 2H), 7.0 -7.02 (d, 2H), 7.20 - 7.33 (m, 5H), 12.46 (s, IH, D2O exchangeable), 12.62 (s, IH, D2O exchangeable). MS m/z: 327.2 (M”).
Example 41
Synthesis of 5-(4-methoxyphenyl)-6-phenyl-2-thiouracil

The title compound was prepared from ethyl 2-(4-methoxyphenyl)-3-phenyl-3-oxopropanoate (2.0g, 67mmol) (obtained according to the procedure given in preparation 42) and thiourea (0.5Ig, 67mmol) by following the procedure described in example 7 (0.5 g, 24 %, purity 91.74% by HPLC), mp 279 -282 °C. “H-NMR (DMS0-d6): 8 3.66 (s, 3H), 6.70 - 6.73 (m, 2H), 6.91 - 6.93 (m, 2H), 7.20 - 7.32 (m, 5H), 12.48 (s, IH, D2O exchangeable), 12.64 (s, IH, D2O exchangeable). MS m/z: 311.1 (M"“).

The title compound was prepared from ethyl 2-(4-chlorophenyl)-3-(4-methylphenyl)-3-oxopropanoate (7.5g, 23.7mmol) (obtained according to the procedure given in preparation 43) and thiourea (1.8g, 23.7mmol) by following the procedure described in example 7 (4.5g, 58%, purity 93.06% by HPLC), mp 265 - 268 °C. “H-NMR (DMSO-dg): 8 3.16 (s, 3H), 7.02 - 7.04 (d, 2H), 7.09 (s, 4H), 7.23 - 7.25 (d, 2H), 12.51 (s, IH, D2O exchangeable), 12.70 (s, IH, D2O exchangeable). MS m/z: 329.2 (M”).

A solution of hydrogen peroxide (30% v/v, 20nil) was added dropwise to a stirred solution of 6-(4-chlorophenyl)-5-phenyl-2-thiouracil (2.0g, 6.35mmol) (obtained according to procedure described in example 7) in ethanolic potassium hydroxide (10%w/v, 40ml) at 50 °C. The reaction mixture was stirred for 3 hours at 60 °C, allowed to cool to 0-5 °C and filtered. The solid obtained was dissolved in water and acidified with dilute hydrochloric acid to pH 6 under cold condition. The precipitate thus separated was filtered, washed thoroughly with water and dried. The crude product was purified by column chromatography to yield the title compound (0.73g, 38.2%, purity 95.65% by HPLC), mp 305 - 306 “C. *H-NMR (DMS0-d6): 5 6.97 - 6.99 (d, 2H), 7.14 - 7.20 (m, 5H), 7.31 - 7.33 (d, 2H), 11.14 (s, IH, D2O exchangeable), 11.2 (s, IH, D2O exchangeable). MS m/z: 299.1 (M”),

The title compound was prepared from 6-(4-methylphenyl)-5-phenyl-2-thiouracil (2.9g, 9.8mmol) (obtained according to the procedure described in example 8) in ethanolic potassium hydroxide solution (10% w/v, 100ml) by following the procedure described in example 14 (1.2g, 44 %, purity 98.71% by HPLC), mp 246 - 249 °C. “H-NMR (DMS0-d6): 6 2.23 (s, 3H), 6.97 - 7.10 (m, 9H), 11.03 (s, IH, D2O exchangeable), 11.30 (s, IH, D2O exchangeable). MS m/z: 279.1 (M”).

The title compound was prepared from 6-(4-trifluoromethylphenyl)-5-phenyl-2-thiouracil (0.4g, ll.Smol) (obtained according to the procedure described in example 9) in ethanolic potassium hydroxide solution (10% w/v, 15ml) by following the procedure described in example 14 (O.lg, 26.2%, purity 97.66% by HPLC), mp 258 - 264 °C. “H-NMR (DMS0-d6): 8 6.99 - 7.01 (d, 2H), 7.13 -7.18 (m, 3H), 7.43 - 7.45 (d, 2H), 7.64 - 7.66 (d, 2H), 11.22 (s, IH, D2O exchangeable), 11.42 (s, IH, D2O exchangeable). MS m/z: 333.1 (M”).
Example 46
Synthesis of 5-(4-chlorophenyl)-6-phenyl-uracil

The title compound was prepared from 5-(4-chlorophenyl)-6-phenyl-2-thiouracil (5.0g, 15.9mmol) (obtained according to the procedure described in example 10) in ethanolic potassium hydroxide solution (10% w/v, 50ml) by following the procedure described in example 14 (1.7g, 35.5%, purity 96.47% by HPLC), mp 326 - 330 °C. “H-NMR (DMSO-de): 8 6.98 - 7.01 (d, 2H), 7.19 - 7.33 (m, 7H), 11.18 (s, IH, D2O exchangeable), 11.39 (s, IH, D2O exchangeable). MS m/z: 299.2 (M”).

The title compound was prepared from 5-(4-methylthiophenyl)-6-phenyl-2-thiouracil (1.5g, 4.6mmol) (obtained according to the procedure described in example 11) in ethanohc potassium hydroxide solution (10% w/v, 20ml) by following the procedure described in example 14 (0.48g, 33.7%, purity 94.98% by HPLC), mp 275 - 278 °C. “H-NMR (DMS0-d6): 5 2.39 (s, 3H), 6.91 - 6.93 (d, 2H), 7.02 -7.04 (d, 2H), 7.20 - 7.22 (m, 2H), 7.27 - 7.32 (m, 3H), 11,12 (s, IH, D2O exchangeable), 11.33 (s, IH, D2O exchangeable). MS m/z: 311.1 (M”).

The title compound was prepared from 5-(4-methoxyphenyl)-6-phenyl-2-thiouracil (0.8g, 2.3mmol) (obtained according to the procedure described in example 12) in ethanolic potassium hydroxide solution (10% w/v, 30ml) by following the procedure described in example 14 (0.54g, 71.2%, purity 97.85% by HPLC), mp 276 - 279 °C. “H-NMR (DMSO-dfi): 8 3.66 (s, 3H), 6.70 - 6.72 (d, 2H), 6,88 - 6.90 (d, 2H), 7.18 - 7.31 (m, 5H), 11.06 (s, IH, D2O exchangeable), 11.30 (s, IH, D2O exchangeable). MS m/z: 295.2 (M”).

The title compound was prepared from 5-(4-chlorophenyl)-6-(4-methylphenyl)-2-thiouracil (4,5g, 13.7mmol) (obtained according to the procedure described in example 13) in ethanoUc potassium hydroxide solution (10% w/v, 50ml) by following the procedure described in example 14 (0.59g, 14%, purity 99.86% by HPLC), mp 281 - 283 °C. “H-NMR (DMS0-d6): 5 2.25 (s, 3H), 6.99 - 7.01 (m,

2H), 7.06 - 7.09 (m, 4H), 7.21 - 7.24 (m, 2H), 11.12 (s, IH, D2O exchangeable), 11.36 (s, IH, D2O exchangeable). MS m/z: 313 (M”).
Described below are the examples of pharmacological assays used for finding out the efficacy of the compounds of the present invention wherein their protocols and results are provided. Rat Carrageenan Paw Edema Test
The carrageenan paw edema test was performed as described by Winter et al (Proc.Soc. Exp Biol Me., Ill, 544, 1962). Male Wistar rats were selected and the body weight were equivalent within each group. The rats were fasted for eighteen hours with free access to water. The rats were dosed orally with the test compound suspended in vehicle containing 0.5% methylcellulose. The control rats were administered the vehicle alone. After one hour the rats were injected with 0.1 ml of 1% Carrageenan solution in 0.9% saline into the sub plantar surface of the right hind paw. Paw thickness was measured using vemier calipers at 0 time, after 2 and 3 hours. The average of foot swelling in drug treated animals was compared with that of control animals. Anti-inflammatory activity was expressed as the percentage inhibition of edema compared with control group [Arzneim-Forsch/Drug Res 43(1), 1, 44-50,1993; Ottemess and Bliven, Laboratory Models for Testing NSAIDs, In Non-Steroidal Anti-Inflammatory Drugs, (J. Lombardino, ed.l985)]. The data of the selected compounds in this invention are summarized in Table I. In order to evaluate their role on the ulcer formation, the animals were sacrificed by cervical dislocation, the stomach removed and flushed with 1% formalin (10ml). The stomach was opened along the greater curvature. The haemorrhagic puncta and sulci were identified macroscopically. The presence or absence of stomach lesions was scored. The

incidence of ulceration was calculated from the number of rats that showed atleast one gastric ulcer or haemorrhagic erosion.

In vitro gvaluation of Cycloxvgenase-2 (COX-2) inhibition activity
The compounds of this invention exhibited in vitro inhibition of COX-2. The COX-2 inhibition activity of the compounds illustrated in the examples was determined by the following method.
Human Whole Blood Assay
Human whole blood provides a protein and cell rich milieu appropriate for the study of biochemical efficacy of anti-inflammatory compounds such as selective COX-2 inhibitors. Studies have shown that normal human blood does not contain COX-2 enzyme. This is correlating with the observation that COX-2 inhibitors have no effect on prostaglandin E2 (PGE2) production in normal blood. These inhibitors are active only after incubation of human blood with lipopolysaccharide (LPS), which induces COX-2 production in the blood.

Method
Fresh blood was collected in tubes containing potassium EDTA by vein puncture from male volunteers. The subjects should have no apparent inflammatory conditions and not taken NSAIDs for atleast 7 days prior to blood collection. Blood was treated with aspirin in vitro (lO”g/ml, at time zero) to inactivate COX-1, and then with LPS (10”g/ml) along with test agents or vehicle. The blood was incubated for 24 h at 37 “C, after which the tubes were centrifuged, the plasma was separated and stored at -80 °C (J Pharmacol Exp Ther 271, 1705, 1994; Proc Natl Acad Sci USA 96, 7563, 1999). The plasma was assayed for PGE2 using Cayman ELISA kit as per the procedure outlined by the manufacturer (Cayman Chemicals, Ann Arbor, USA). The plasma was also tested for TNF-a, IL-ljS, and IL-6 using appropriate human ELISA kit as per the procedure of manufacturer (Cayman Chemicals, Ann Arbor, USA). Representative results of COX-2 inhibition are shown in Table IL

Tumor Necrosis Factor Alpha (TNF-a)
This assay determines the effect of test compounds on the production of TNF-a from human monocytes. Compounds were tested for their ability to downregulate the production of TNF-a in activated monocytes. Test compounds were incubated for three, six and twenty four hours with human monocytes, Lipopolysaccharide was used to stimulate the monocytes. The level of TNF-a was quantitated using Enzyme-Linked Immunosorbent assay performed in a 96 well format. Representative results of TNF-a inhibition are shown in Table III.

InterIeukin-6(IL-6)
This assay determines the effect of test compounds on the production of IL-6 from human monocytes. Compounds are tested for their abiUty to downregulate the production of IL-6 in activated monocytes. Test compounds were incubated for three, six and twenty four hours with human monocytes. Lipopolysaccharide was used to stimulate the monocytes. The level of Interleukin-6 is quantitated using Enzyme-Linked Immunosorbent assay performed in a 96 well format. Representative results of IL-6 inhibition are shown in Table IV.

Inhibitory Action on Adjuvant Arthritis
Compounds were assayed for their activity on rat adjuvant induced arthritis according to Theisen-Popp et al., (Agents Actions 42, 50-55,1994). Six - seven weeks old, Wistar rats were weighed, marked and assigned to groups [a negative control group in which arthritis was not induced (non-adjuvant control), a vehicle-treated arthritis control group, test substance treated arthritis group]. Adjuvant induced arthritis was induced by an injection of Mycobacterium butyricum (Difco) suspended in liquid paraffin into the sub-plantar region of the right hind paw (J Pharmacol Exp Ther, 284, 714, 1998). Body weight, contralateral paw volumes were determined at various days (0, 4, 14, 21) for all the groups. The test compound or vehicle was administered orally beginning post injection of adjuvant and continued for 21 days. On day 21, body weight and paw

volume of both right and left hind paw, spleen, and thymus weights were determined. In addition, the radiograph of both hind paws was taken to assess the tibio-tarsal joint integrity. Hind limb below the stifle joint was removed and fixed in 1% formalin saline. At the end of the experiment, plasma samples were analysed for cytokines, interleukins and prostaglandins. The presence or absence of lesions in the stomachs was also observed.
Two-factor ('treatment' and 'time') Analysis of Variance with repeated measures on 'time' were applied to the % changes for body weight and foot volumes. A post hoc Dunnetf s test was conducted to compare the effect of treatments to vehicle. A one-way Analysis of Variance was applied to the thymus and spleen weights followed by the Dunnett's test to compare the effect of treatments to vehicle. Dose-response curves for % inhibition in foot volumes on days 4, 14 and 21 were fitted by a 4-parameter logistic function using a nonlinear Least Squares* regression. ID50 was defined as the dose corresponding to a 50% reduction from the vehicle and was derived by interpolation from the fitted 4-parameter equation
In-vitro Anti-Cancer activity
The compounds of the present invention were also tested for anticancer activity. Each test compound was screened against a battery of 60 human cell lines obtained from eight organs. The cell suspensions were diluted according to the particular cell type and the target cell density (5000-40,000 cells per well based on cell growth characteristics) was added into 96-well micro titer plates. Inoculates were allowed a pre-incubation period of 24 h at 37 °C for stabilization. Dilutions at twice the intended test concentrations were added at time zero in 100 |il aliquots to micro titer plate wells. Usually test compounds were evaluated at five 10-fold dilutions. The highest well concentration used in the test is 10""* M.

The cells were then incubated in the presence of the test compound for further 48 h in 5% CO2 atmosphere and 100% humidity. After completion of the incubation period the adherent cells were fixed to the plate by means of trichloroacetic acid. After three to five times washing, the cell layer was treated with the protein stain Sulforhodamine B. The optical density, which is proportional to protein mass, was then read by spectrophotometer plate readers at a wavelength of 515 nm. The anticancer activity is shown in figures 1-4.
Brief description of the figures
Figures 1 and 2 : Inhibition of cell proliferation in MCF-7 breast cancer cells Figures 3 and 4 : Inhibition of cell proliferation in MDA-MB-231 breast cancer cells

We Claim:
1. Novel amino substituted pyrimidinone derivatives of the formula (I)

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or

heteroaryl; Y represents a bond or NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent

hydrogen, SR , wherein R represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfinyl, alkylsulfanyl, subfamily, alkoxyalkyl groups or carboxylic acids or its derivatives; R’ represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR’, wherein R’ represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino,

groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2.
2. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, wherein the ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl, benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like.
3. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, which are selected from :
6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one;
6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-bromophenyl)-2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;

6-Ainino-2-(4-methylthio-phenylamino)-1 -(4-methylthiophenyl)-1 H-pyrimidin-4-
one;
6-Amino-1 -(4-methylphenyl)-2-(4-methylthio-phenylamino)-1 H-pyrimidin-4-
one;
6-Amino-2-(4-methylsulfonyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylthio-phenylamino)-1 -(4-methylphenyl)-1 H-pyrimidin-4-
one;
4-(6-Amino-4-oxo-1 -phenyl-1,4-dihydro-pyrimidin-2-ylamino)-
benzenesulfonamide;
4-(6-Amino-4-oxo-1 -(4-methyl-phenyl)-1,4-dihydro-pyrimidin-2-ylamino)-
benzenesulfonamide;
6-Amino-2-phenylamino-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-methoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylthio-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-2-(4-ethoxy-phenylamino)-1 -(pyridin-2-yl)-1 H-pyrimidin-4-one;
6-Amino-1 -(4-methoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-ethoxypyridin-2-yl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-2- phenylamino-1 -(4-chloropyridin-2-yl)-1 H-pyrimidin-4-one and
6-Amino-2-phenylamino-1-(4-bromopyridin-2-yl)-1 H-pyrimidin-4-one;
4. A process for the preparation of novel amino substituted pyrimidinone
derivatives of the formula (I)

groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to
2.
2. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, wherein the ring systems represented by A and B are selected from phenyl, naphthyl, pyrrolidinyl, morpholinyl, thiomorpholinyl, piperidinyl, piperazinyl, pyridyl, thienyl, furyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, tetrazolyl, pyrimidinyl, benzopyranyl, benzofuranyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, benzopyrolyl, benzoxadiazolyl, benzothiadiazolyl, quinolinyl, isoquinolinyl, benzothienyl, benzofuranyl, indolyl and the like.
3. Novel amino substituted pyrimidinone derivatives as claimed in claim 1, which are selected from :
6-Amino-1 -phenyl-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-l-(4-methylphenyl)- 2- phenylamino-lH-pyrimidin-4-one;
6-Amino-1 -(4-methoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-ethoxyphenyl)-2-phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-chlorophenyl)-2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-bromophenyl)"2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-1 -(4-methylsulfonyl-phenyl)-2- phenylamino-1 H-pyrimidin-4-one;
6-Amino-2-(4-methyl-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-methoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-ethoxy-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-methylthio-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-chloro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;
6-Amino-2-(4-fluoro-phenylamino)-1 -phenyl-1 H-pyrimidin-4-one;

their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, and their pharmaceutically acceptable salts, wherein X represents oxygen, sulfur or NR, wherein R represents hydrogen, hydroxyl, acyl, alkyl, alkoxy, aryl, amino, hydroxylamino, alkylamino, arylamino, acylamino, alkoxyamino group; the rings represented by A and B are selected from aryl or
Q Q
heteroaryl; Y represents NR , wherein R represents hydrogen, alkyl and the like; the rings represented by A and B are selected from aryl or heteroaryl; R and R may be same or different and independently represent hydrogen, SR’, wherein R’ represents alkyl or aryl; S(0)pR , wherein R represents alkyl, amino or aryl group and p represents an integer of 1 or 2; R and R may be same or different and independently represent hydrogen, halogen, hydroxyl, nitro, cyano, azido, nitroso, amino, formyl, alkyl, haloalkyl, acyl, alkoxy, monoalkylamino, dialkylamino, acylamino, alkoxycarbonyl, alkylsulfonyl, alkylsulfmyl, alkylsulfanyl, sulfamoyl, alkoxyalkyl groups or carboxylic acids or its derivatives; R’ represents hydrogen, halogen, hydroxyl, formyl, cyano, nitroso, nitro, amino, alkyl, acyl, monoalkylamino, dialkylamino, arylamino, acylamino, alkoxyalkyl or COR’, wherein R’ represents hydroxyl, amino, halogen, alkoxy, aryloxy, monoalkylamino, dialkylamino, arylamino, groups; m is an integer in the range of 0 to 2; n is an integer in the range of 0 to 2, which comprises, reacting compound of formula (la)

wherein any one of R’ or R’ represent SR’, wherein R’ represents alkyl or aryl and the other R or R may be same or different and independently represent hydrogen or S(0)pR , where p is 1 or 2, R represents alkyl, amino or aryl and all other symbols are as defined in claim 1, to novel amino substituted pyrimidinone derivatives of the formula (I) wherein any one of R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl group using an oxidizing agent 6. A process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) as claimed in claim 1,

wherein any one of the group R or R represent S(0)pR , where p is 1 or 2, R represents alkyl or aryl and the other R or R represent hydrogen or SR , wherein R’ represents alkyl or aryl and all other symbols are as defined in claim 1, to

novel amino substituted pyrimidinone derivatives of the formula (I) wherein any one of R’ or R’ represent S(0)pR’ where p is 1 or 2, R’ represents amino group. 7. A process for the conversion of novel amino substituted pyrimidinone derivatives of the formula (I) as claimed in claim 1,
V

wherein either of R and R represent S(0)pR , where R represents amino group and p represents an integer of 1 or 2 and all other symbols are as defined earlier, which comprises reacting compound of formula (Ic) wherein all symbols are as defined in claim 1

wherein either of R and R represents hydrogen; with chlorosulfonic acid
followed by ammonia.
8.A pharmaceutical composition, which comprises a compound of formula (I)

as defined in claim 1 together with a pharmaceutically acceptable carrier, diluent, excipient or solvate.

Documents:

266-mas-2002-abstract.pdf

266-mas-2002-assignement.pdf

266-mas-2002-claims filed.pdf

266-mas-2002-claims granted.pdf

266-mas-2002-correspondnece-others.pdf

266-mas-2002-correspondnece-po.pdf

266-mas-2002-description(complete) filed.pdf

266-mas-2002-description(complete) granted.pdf

266-mas-2002-description(provisional).pdf

266-mas-2002-drawings.pdf

266-mas-2002-form 1.pdf

266-mas-2002-form 3.pdf

266-mas-2002-form 5.pdf

266-mas-2002-other documents.pdf

266.jpg

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Patent Number

209022

Indian Patent Application Number

266/MAS/2002

PG Journal Number

38/2007

Publication Date

21-Sep-2007

Grant Date

16-Aug-2007

Date of Filing

10-Apr-2002

Name of Patentee

M/S. ORCHID RESEARCH LABORATORIES LTD

Applicant Address

ORCHID TOWERS 313,VALLUVAR KOTTAM HIGH ROAD, NUNGAMBAKAM,CHENNAI 600 119.

Inventors:

#	Inventor's Name	Inventor's Address
1	SHIV KUMAR AGARWAL	ORCHID TOWERS 313,VALLUVAR KOTTAM HIGH ROAD, NUNGAMBAKAM,CHENNAI 600 119.

PCT International Classification Number

C 07 D 239/00

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA