| US 7,504,405 B2 | ||
| Mitotic kinesin inhibitors | ||
| Weibo Wang, Moraga, Calif. (US); Ryan Constantine, Oakland, Calif. (US); and Liana Lagniton, Berkeley, Calif. (US) | ||
| Assigned to Novartis Vaccines and Diagnostics, Inc., Emeryville, Calif. (US) | ||
| Filed on Apr. 06, 2005, as Appl. No. 11/100,923. | ||
| Claims priority of provisional application 60/560235, filed on Apr. 06, 2004. | ||
| Prior Publication US 2005/0228002 A1, Oct. 13, 2005 | ||
| Int. Cl. C07D 487/04 (2006.01); A61K 31/519 (2006.01); A61P 35/00 (2006.01) | ||
| U.S. Cl. 514—259.4 [514/259.41; 514/269; 544/282; 544/319] | 18 Claims |
1. A compound of the formula:
 wherein:
m is 0, 1, 2, or 3;
p is 1,2,3 or 4;
R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, aryl, and heterocyclyl;
R5 is selected from the group consisting of hydrogen, alkyl, aryl, heterocyclyl, alkoxycarbonyl, aryloxycarbonyl, heterocyclyloxycarbonyl,
aminocarbonyl, alkylcarbonyl, arylcarbonyl, heterocyclylcarbonyl, alkylsulfonyl, arylsulfonyl, and heterocyclylsulfonyl
R8 is selected from the group consisting of unsubstituted alkyl, substituted alkyl, aryl, and heterocyclyl;
R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl;
wherein, said compound inhibits kinesin spindle protein with an IC50 value of less than or equal to 25 μM;
or pharmaceutically acceptable salts or stereoisomers thereof.
|