IP Library Granted Patent US 7,538,121
Granted Patent B2
US 7,538,121 · App. 10/503,648 · Granted May 26, 2009

Vanilloid receptor modulators

Assignee: Glaxo Group Limited
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Quick Facts
Patent No.
US 7,538,121
App. No.
10/503,648
Granted
May 26, 2009
Kind
B2
Abstract

Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , P, X, Y, q, r ans s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.

Claims (36)

1. A compound of formula (IB),

or a pharmaceutically acceptable salt thereof,

wherein, P is selected from the group consisting of phenyl, pyridyl, piperidinyl, piperazinyl, and morpholinyl;

R 1 is CH 3 ;

R 2 is Cl;

each R 3 is independently selected from the group consisting of alkyl; alkoxy; —CF 3 ; halo—O(CH 2 ) OR 6 ; —O(CH 2 ) NR 4 R 5 ; phenyl optionally substituted with one or more C 1 -C 6 -alkyl, trifluoromethyl, methoxy, acetyl, halo, or CH 3 ) 2 NS(O) 2 -groups cyclohexyl;

benzo[1,3]dioxolyl; morpholinyl pyridyl optionally substituted with one or more chloro or methyl groups; piperazinyl optionally substituted with a methoxycarbonyl group; piperidinyl; thienyl; furyl; pyrazolyl; indanyl; oxazolyl; methylthiazolyl; oxadiazolyl; isothiazolyl; isoxazolyl; and thiadiazolyl;

R 4 and R 5 are each methyl;

R 6 is methyl;

X is N and Y is CR 9 ; or X is CR 9 and Y is N;

R 9 is H or R 1 ;

n is an integer value from 1 to 6;

q is 0 or 1;

r is 0 or 1, and

s is 0, 1, 2 or 3.

2. A pharmaceutical composition, which comprises the compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or excipient therefor.

3. The compound of claim 1 which is represented by the following formula:

or a pharmaceutically acceptable salt thereof; wherein

P is phenyl or pyridyl;

Y is CH and X is N; or Y is N and X is CH;

each R 3 is independently; —CF 3 ; methyl; fluoro; chloro; bromo; morpholinyl; piperidinyl;

thienyl; pyrazolyl; methylthiazolyl; phenyl optionally substituted with one or more substituents selected from the group consisting of methyl, trifluoromethyl, methoxy, and chloro; or pyridyl optionally substituted with methyl or chloro;

q is 0;

r is 0; and

s is 1, 2, or 3.

4. The compound of claim 3 which is represented by the following structure:

or a pharmaceutically acceptable salt thereof; wherein

P is phenyl;

Y is CH; and

X is N.

5. The compound of claim 3 or a pharmaceutically acceptable salt thereof wherein:

P is pyridyl;

Y is CH; and

X is N.

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof which is represented by the following formula:

7. The compound of claim 1 or a pharmaceutically acceptable salt thereof which is represented by the following formula:

Priority Claims (7)
GB 0203673 · Feb 15, 2002 · national
GB 0203677 · Feb 15, 2002 · national
GB 0203680 · Feb 15, 2002 · national
GB 0209003 · Apr 19, 2002 · national
GB 0209032 · Apr 19, 2002 · national
GB 0209035 · Apr 19, 2002 · national
GB 0221318 · Sep 13, 2002 · national
Continuity (1)
Related Publication 20060142333A1 · Jun 29, 2006