| US 7,414,047 B2 | ||
| Piperazinyl and diazapanyl benzamides and benzthioamides | ||
| Richard L. Apodaca, San Diego, Calif. (US); Jill A. Jablonowski, San Diego, Calif. (US); Kiev S. Ly, San Diego, Calif. (US); Chandravadan R. Shah, San Diego, Calif. (US); Devin M. Swanson, La Jolla, Calif. (US); and Wei Xiao, San Diego, Calif. (US) | ||
| Assigned to Janssen Pharmaceutica N.V., (Belgium) | ||
| Filed on Oct. 21, 2003, as Appl. No. 10/690,115. | ||
| Claims priority of provisional application 60/420495, filed on Oct. 23, 2002. | ||
| Prior Publication US 2004/0110746 A1, Jun. 10, 2004 | ||
| Int. Cl. A61K 31/55 (2006.01); A61K 31/54 (2006.01); A61K 31/535 (2006.01); A61K 31/497 (2006.01); A61K 31/4965 (2006.01); A61P 25/00 (2006.01); C07D 401/00 (2006.01); C07D 417/00 (2006.01); C07D 413/00 (2006.01); C07D 241/02 (2006.01); C07D 403/00 (2006.01) | ||
| U.S. Cl. 514—217.05 [514/227.8; 514/235.8; 514/252.11; 514/253.01; 514/253.05; 514/254.01; 514/255.01; 540/597; 544/60; 544/121; 544/357; 544/360; 544/363; 544/372; 544/391] | 26 Claims |
1. A compound of formula (I):
 R1 is branched C3-5 alkyl, C3-8 alkenyl, C3-8 cycloalkyl, (C3-8 cycloalkyl)C1-6 alkyl, (C3-8 cycloalkyl)C3-8 alkenyl, or (C1-8 alkylcarbonyl)C1-8 alkyl;
n is 1;
X is O;
R2 and R3 independently are hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, methyl, or C1-3alkoxy;
R4is G
G is LQ;
L is —CH2—;
Q is a saturated, un-substituted N-linked heterocyclyl, selected from the group consisting of azepanyl, morpholinyl, piperidinyl
and pyrrolidinyl;
wherein each of the above alkyl, alkenyl, and cycloalkyl, groups may each be independently and optionally substituted with
between 1 and 3 substituents independently selected from trifluoromethyl, methoxy, halo, amino, nitro, hydroxy, and C1-3 alkyl;
or a pharmaceutically acceptable salt, ester, tautomer or amide thereof.
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