| US 7,576,099 B2 | ||
| Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same | ||
| Michael G. Kelly, Thousand Oaks, Calif. (US); John Kincaid, San Mateo, Calif. (US); Matthew Duncton, San Francisco, Calif. (US); Kiran Sahasrabudhe, Fall Church, Va. (US); Satyanarayana Janagani, Santa Clara, Calif. (US); Ravindra B. Upasani, San Jose, Calif. (US); Guoxian Wu, Palo Alto, Calif. (US); YunFeng Fang, San Diego, Calif. (US); Jianhua He, legal representative; Zhi-Liang Wei, Foster City, Calif. (US); and Carl Kaub, San Mateo, Calif. (US) | ||
| Assigned to Renovis, Inc., South San Francisco, Calif. (US) | ||
| Filed on Feb. 24, 2006, as Appl. No. 11/362,451. | ||
| Claims priority of provisional application 60/656984, filed on Feb. 28, 2005. | ||
| Claims priority of provisional application 60/710445, filed on Aug. 23, 2005. | ||
| Prior Publication US 2006/0194801 A1, Aug. 31, 2006 | ||
| This patent is subject to a terminal disclaimer. | ||
| Int. Cl. C07D 215/16 (2006.01); C07D 413/02 (2006.01); A61K 31/47 (2006.01) | ||
| U.S. Cl. 514—311 [546/152; 546/159; 514/313] | 24 Claims |
1. A compound according to formula (I):
 or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, wherein:
each of W, Z and X is CR4 and Y is CR4″;
L is —(CR5═CR6)— or —(C≡C)—;
R1 is quinolinyl substituted with hydrogen, C1-C6 alkyl, hydroxyl C1-C6 alkyl, C1-C6 alkylamino, C1-C6 alkoxy, amino C1-C6 alkoxy, substituted amino C1-C6 alkoxy, di C1-C6 alkylamino C1-C6 alkoxy, cycloalkyl C1-C6 alkoxy, C1-C6 alkoxycarbonyl, C1-C6 alkylarylamino, aryl C1-C6 alkyloxy, amino, aryl, aryl C1-C6 alkyl, substituted sulfonyl, sulfanyl, aminosulfonyl, arylsulfonyl, azido, carboxy, carbamoyl, cyano, cycloheteroalkyl, di
C1-C6 alkylamino, halo, heteroaryloxy, heteroaryl, heteroalkyl, hydroxyl, nitro or thio;
R3 is CR6′R7R8;
each R4 is independently hydrogen, C1-C6 alkyl, hydroxyl C1-C6 alkyl, C1-C6 alkylamino, C1-C6 alkoxy, amino C1-C6 alkoxy, substituted amino C1-C6 alkoxy, di C1-C6 alkylamino C1-C6 alkoxy, cycloalkyl C1-C6 alkoxy, C1-C6 alkoxycarbonyl, C1-C6 alkylarylamino, aryl C1-C6 alkyloxy, amino, aryl, aryl C1-C6 alkyl, substituted sulfonyl, sulfanyl, aminosulfonyl, arylsulfonyl, azido, carboxy, carbamoyl, cyano, cycloheteroalkyl, di
C1-C6 alkylamino, halo, heteroaryloxy, heteroaryl, heteroalkyl, hydroxyl, nitro or thio;
R4″ is substituted alkyl, methyl, halo, substituted sulfonyl, alkoxy, or amino;
each of R5 and R6 is independently H, halo, or C1-C6 alkyl; and
R6′ is hydrogen, halo or C1-C6 alkyl; each of R7 and R8 is independently halo or C1-C6 alkyl; or R7 and R8 together form a C3-C8 cycloalkyl ring.
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