US Patent:
20050261203, Nov 24, 2005
Inventors:
Frederick Cohen - San Francisco CA, US
Wayne Fairbrother - Burlingame CA, US
John Flygare - Burlingame CA, US
Stephen Keteltas - San Francisco CA, US
Vickie Tsui - San Francisco CA, US
Assignee:
Genentech, Inc. - South San Francisco CA
International Classification:
A61K038/04
A61K031/403
C07D209/02
US Classification:
514019000, 548452000, 514412000
Abstract:
The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: Xand Xare independently O or S; L is a bond or —C(X)—, —C(X)NR, —C(X)O— wherein Xis O or S and Ris H or R; Ris alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; Ris alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; Ris H or alkyl; Rand R are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R, and Rare each independently H or alkyl; Ris H or alkyl; and salts and solvates thereof.