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US 2004/0167119 A1Published application
2-(aminomethyl) arylamide analgesics
AssigneePharmacopeia, Inc.
InventorsKoc-Kan Ho, John J. Baldwin, Adolph C. Bohnstedt, Steven G. Kultgen, Edward McDonald, Tao Guo, John Richard Morphy, Zoran Rankovic, Robert Horlick, Kenneth C. Appell
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Abstract
A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the formula I: 1 A representative example is: 2
Claims22
A compound of formula
- 257
- wherein
- U is chosen from CH, N and CR5;
- A is chosen from the group consisting of (C2 to C6)alkane;
- (C2 to C6)fluoroalkane;
- (C2 to C6)alkene;
- (C2 to C6)alkyne;
- (C2 to C6)oxaalkane and (C2 to C6)thiaalkane;
- B is chosen from the group consisting of a direct bond, (C1 to C6)alkane;
- substituted (C1 to C6)alkane;
- and (C2 to C6)azaalkane;
- Ar1 and Ar2 are independently chosen from the group consisting of aryl, heteroaryl, substituted aryl and substituted heteroaryl;
- R2, R3 and R5 are independently chosen from —H, loweralkyl, fluoroloweralkyl, halo, loweralkoxy, fluoroloweralkoxy and NO2;
- and
- R1 is hydrogen or lower alkyl;
- and
- R4 is —B—Ar2, or
- R1 and R4, together with the nitrogen to which they are attached, form a five-, six- or seven-membered nitrogen heterocyle, said nitrogen heterocycle substituted with or fused to Ar2, and said nitrogen heterocycle optionally substituted with from one to three substituents chosen from the group consisting of hydrogen, lower alkyl, —CH2OH, fluoroloweralkyl, —COOH and —COO(lower alkyl), with the proviso that said nitrogen heterocycle is not a 2-oxopyrimidine.
15 more elements
Dependencies are inferred from the claim text.