Title of Invention

N-SUBSTITUTED NONARYL-HETEROCYCLIC NMDA/NR2B ANTAGONISTS

Abstract TITLE OF THE INVENTION N-SUBSTITUTED NONARYL-HETEROCYCLIC NMDA/NR2B ANTAGONISTS Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
Full Text We claim:
1 A compound having the formula (I):

(I)
or a pharmaceutically acceptable salt thereof, wherein
NonAr is piperidine ring;
HetAr is a 6 membered Iheteroaromatic ring containing 2 nitrogen ring
atoms;
HetAr is optionally substituted with I or 2 substituents, each substituent independently is CMalkyl^ CMalkoxy, C2-4aIkynyl, trifluoromethyl,
hydroxy, hydroxyCi^alkyl, fluoro, chloro, bromo, iodo, cyano, methylsulfanyl,
cyclopropylethynyl-, phenylethynyH heteroaryleth3myI-,-N(Co-4alkyl)(Co-4alkyl),
nitro, (Ci-2aIkyl)(Ci.2alkyl)NCH2- CCl-2alkyl)HNCH2- Si(CH3)3~C- or NH2C(0)-
A is methylene;
B is aryl(CH2)o.3-0-CCOH and
X is H, OH, F, Cl-4alkyl, Ci-4alkoxy, NH2, or X taken with an adjacent bond is =0.
2. The compound as claimed in claim 1, wherein said compound is:








6. A pharmaceutical composition comprising an inert carrier and an
amount of a compound according to claim 1 effective to treat pain.


Documents:

1316-chenp-2003 abstract duplicate.pdf

1316-chenp-2003 claims duplicate.pdf

1316-chenp-2003 description (complete) duplicate-1.pdf

1316-chenp-2003 description (complete) duplicate-2.pdf

1316-chenp-2003 description (complete) duplicate.pdf

1316-chenp-2003-abstract.pdf

1316-chenp-2003-claims.pdf

1316-chenp-2003-correspondnece-others.pdf

1316-chenp-2003-correspondnece-po.pdf

1316-chenp-2003-description(complete).pdf

1316-chenp-2003-form 1.pdf

1316-chenp-2003-form 13.pdf

1316-chenp-2003-form 26.pdf

1316-chenp-2003-form 3.pdf

1316-chenp-2003-form 5.pdf

1316-chenp-2003-pct.pdf

abs-1316-chenp-2003.jpg


Patent Number 223179
Indian Patent Application Number 1316/CHENP/2003
PG Journal Number 47/2008
Publication Date 21-Nov-2008
Grant Date 05-Sep-2008
Date of Filing 22-Aug-2003
Name of Patentee MERCK & CO., INC.
Applicant Address 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907
Inventors:
# Inventor's Name Inventor's Address
1 CLAIBORNE CHRISTOPHER, F 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907
2 PHILLIPS, BRIAN 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
3 BUTCHER, JOHN, W 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
4 LIVERTON, NIGEL, J 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
5 CLAREMON, DAVID, A 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
6 LIBBY, BRIAN, E 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
7 MUNSON, PETER, M 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
8 NGUYEN, KEVIN, T 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
9 THOMPSON, WAYNE 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
10 MCCAULEY, JOHN, A 126 EAST LINCOLN AVENUE, RAHWY, NJ 07065-0907,
PCT International Classification Number C07D401/12
PCT International Application Number PCT/US02/05226
PCT International Filing date 2002-02-20
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 60/271,100 2001-02-23 U.S.A.