Title of Invention

'THE COMPOUND N-(2-BROMOPHENYL)-N'-[((R)-1-(5-TRIFLUOROMETHYL-2-PYRIDYL)PYRROLIDIN-3-YL)UREA"

Abstract The compound N-(2-Bromophenyl)-N-[((R)-l-(5-trifluoromethyl-2-pyridyl)pyrrolidin-3-yl)]urea, having the formula: or a pharmaceutically acceptable salt or solvate thereof.
Full Text NOVEL COMPOUNDS
This invention relates to novel compounds, especially urea derivatives, having pharmacological activity, processes for their preparation, to compositions containing them and to their use in medicine, especially in the treatment of various disorders.
Vanilloids are a class of natural and synthetic compounds that are characterised by the presence of a vanillyl (4-hydroxy 3-methoxybenzyl) group or a functionally equivalent group. Vanilloid Receptor (VR-1), whose function is modulated by such compounds, has been widely studied and is extensively reviewed by Szallasi and Blumberg (The American Society for Pharmacology and Experimental Therapeutics, 1999, Vol. 51, No. 2.).
A wide variety of Vanilloid compounds of different structures are known in the art, for example those disclosed in European Patent Application Numbers, EP 0 347 000 and EP 0 401 903, UK Patent Application Number GB 2226313 and International Patent Application, Publication Number WO 92/09285. Particularly notable examples of vanilloid compounds or vanilloid receptor modulators are capsaicin or trans 8-methyl-N-vaniHyl-6-nonenamide which is isolated from the pepper plant, capsazepine (Tetrahedron, 53,1997, 4791) and olvanil or- N-(4-hydroxy-3-methoxybenzyl)oleamide (J. Med. Chem., 36,1993, 2595).
US Patent Numbers, US 3,424,760 and US 3,424,761 both describe a series of 3-Ureidopyrrolidines that are said to exhibit analgesic, central nervous system, and pyschopharmacologic activities. These patents specifically disclose the compounds 1-(1-phenyl-3-pyrrolidinyl)-3-phenyl urea and 1-(1-phenyl-3-pyrrolidinyl)-3-(4-methoxyphenyl)urea respectively.
International Patent Applications, Publication Numbers WO 02/08221, WO 02/16317, WO 02/16318 and WO 02/16319 each disclose certain vanilloid receptor antagonists and their use in the treatment of diseases associated with the activity of the vanilloid receptor.

Co-pending International Patent Application Number PCT/EP02/04802 discloses a series of urea derivatives and their use in the treatment of diseases associated with the activity of the vanilloid receptor.
According to a first aspect of the present invention, there is provided a


WE CLAIM:
1. The compound N-(2-Bromophenyl)-N'-[((R)-l-(5-trifluoromethyl-2-pyridyl)pyrrolidin-3-yl)]urea, having the formula:

(Formula Removed)


or a pharmaceutically acceptable salt or solvate thereof.
2. A pharmaceutical composition comprising from 0.1 to 99% by weight, preferably from 10 to 60% by weight of the compound as claimed in claim 1 or a pharmaceutically acceptable salt or solvate thereof and from 1 to 99.9% by weight, preferably from 40 to 90% by weight of a pharmaceutically acceptable carrier or excipient therefor.
3. The compound as claimed in claim 1 or a pharmaceutically acceptable salt or solvate thereof for use in the treatment and/or prophylaxis of pain.





Documents:

00473-delnp-2004-abstract.pdf

00473-delnp-2004-claims.pdf

00473-delnp-2004-correspondence-others.pdf

00473-delnp-2004-description (complete)-19-08-2008.pdf

00473-delnp-2004-description (complete).pdf

00473-delnp-2004-form-1.pdf

00473-delnp-2004-form-18.pdf

00473-delnp-2004-form-2.pdf

00473-delnp-2004-form-3.pdf

00473-delnp-2004-form-5.pdf

00473-delnp-2004-gpa.pdf

00473-delnp-2004-pct-101.pdf

00473-delnp-2004-pct-210.pdf

00473-delnp-2004-pct-220.pdf

00473-delnp-2004-pct-301.pdf

00473-delnp-2004-pct-304.pdf

00473-delnp-2004-pct-332.pdf

00473-delnp-2004-pct-401.pdf

00473-delnp-2004-pct-409.pdf

00473-delnp-2004-pct-416.pdf

473-DELNP-2004-Abstract-(19-08-2008).pdf

473-DELNP-2004-Claims-(19-08-2008).pdf

473-DELNP-2004-Correspondence-Others-(19-08-2008).pdf

473-DELNP-2004-Form-1-(19-08-2008).pdf

473-DELNP-2004-Form-2-(19-08-2008).pdf

473-DELNP-2004-Form-3-(19-08-2008).pdf

473-DELNP-2004-GPA-(19-08-2008).pdf

473-DELNP-2004-Petition-137-(19-08-2008).pdf

473-DELNP-2004-Petition-138-(19-08-2008).pdf

abstract.jpg


Patent Number 225277
Indian Patent Application Number 00473/DELNP/2004
PG Journal Number 48/2008
Publication Date 28-Nov-2008
Grant Date 05-Nov-2008
Date of Filing 27-Feb-2004
Name of Patentee SMITHKLINE BEECHAM P.L.C.
Applicant Address 980 GREAT WEST ROAD, BRENTFORD, MIDDLESEX TW8 9GS ENGLAND.
Inventors:
# Inventor's Name Inventor's Address
1 HARSHAD KANTILAL RAMI GLAXOSMITHKLINE, NEW FRONTIERS SCIENCE PARK SOUTH, THIRD AVENUE, HARLOW, ESSEX CM19 5AW, ENGLAND.
2 MERVYN THOMPSON GLAXOSMITHKLINE, NEW FRONTIERS SCIENCE PARK SOUTH, THIRD AVENUE, HARLOW, ESSEX CM19 5AW, ENGLAND.
3 PAUL ADRIAN WYMAN GLAXOSMITHKLINE, NEW FRONTIERS SCIENCE PARK SOUTH, THIRD AVENUE, HARLOW, ESSEX CM19 5AW, ENGLAND.
PCT International Classification Number C07D 401/04
PCT International Application Number PCT/GB02/04206
PCT International Filing date 2002-09-13
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 0130505.1 2001-12-20 U.K.
2 0122156.3 2001-09-13 U.K.
3 0130503.6 2001-12-20 U.K.
4 0130547.3 2001-12-20 U.K.