| US 7,414,131 B2 | ||
| Bicycloheteroarylamine compounds as ion channel ligands and uses thereof | ||
| Michael G. Kelly, Thousand Oaks, Calif. (US); Satyanarayana Janagani, Santa Clara, Calif. (US); Guoxian Wu, Foster City, Calif. (US); John Kincaid, Foster City, Calif. (US); David Lonergan, Sunnyvale, Calif. (US); YunFeng Fang, San Diego, Calif. (US); and Zhi-Liang Wei, San Mateo, Calif. (US) | ||
| Assigned to Renovis, Inc., South San Francisco, Calif. (US) | ||
| Filed on Dec. 23, 2004, as Appl. No. 11/22,324. | ||
| Claims priority of provisional application 60/532371, filed on Dec. 24, 2003. | ||
| Prior Publication US 2005/0215572 A1, Sep. 29, 2005 | ||
| Int. Cl. A01N 43/58 (2006.01); C07D 487/00 (2006.01) | ||
| U.S. Cl. 544—236 [514/248] | 7 Claims |
1. A method for ameliorating or delaying the onset of a disease or condition in a mammal, which comprises administering to
the mammal an effective disease- or condition-ameliorating, or onset-delaying amount of a pharmaceutical composition, wherein
said pharmaceutical composition comprises a pharmaceutically acceptable carrier and a pharmaceutically effective amount of
a compound, said compound having a formula:
 A, B and Y are CR2′R2′;
W is N; and Z is CR4;
R1 is selected from phenyl, unsubstituted or substituted with alkyl, substituted alkyl, substituted or unsubstituted alkoxy,
substituted or unsubstituted sulfone, substituted or unsubstituted aminosulfonyl, cyano, and halo; or
R1 is selected from substituted or unsubstituted pyridyl, substituted or unsubstituted indolyl, substituted or unsubstituted
benzimidazolyl, substituted or unsubstituted indazolyl, substituted or unsubstituted tetrahydroquinoline, and substituted
or unsubstituted tetrahydroisoquinoline;
R2 is H; and each R2′ is independently selected from hydrogen, substituted or unsubstituted C1-C6 alkyl;
R3 is selected from substituted or unsubstituted phenyl; or
R3 is 2-pyridyl substituted with alkoxy, sulfonyl, or sulfonamidyl;
R4 is selected from H, alkyl, substituted alkyl, acyl, substituted acyl, substituted or unsubstituted acylamino, substituted
or unsubstituted alkylamino, substituted or unsubstituted alkythio, substituted or unsubstituted alkoxy, alkoxycarbonyl, substituted
alkoxycarbonyl, substituted or unsubstituted benzylamino, benzyloxy, substituted benzyloxy, amino, benzyl, substituted or
unsubstituted sulfoxide, substituted or unsubstituted sulfone, substituted or unsubstituted sulfanyl, substituted or unsubstituted
aminosulfonyl, substituted or unsubstituted dihydroxyphosphoryl, substituted or unsubstituted aminodihydroxyphosphoryl, azido,
carboxy, substituted or unsubstituted carbamoyl, cyano, substituted or unsubstituted cycloalkyl, substituted or unsubstituted
cycloheteroalkyl, substituted or unsubstituted dialkylamino, halo, hydroxy, nitro, and thiol;
or a pharmaceutically acceptable salt, or stereoisomers or tautomers thereof;
wherein the disease or condition is selected from inflammatory pain, neuropathic pain, osteoarthritis, overactive bladder,
migraine and dental pain.
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