Patent ID: 8642594
Filing Date: 2014-02-04
Classification: A61K,A61P,C07D

Abstract:
1. A method of inhibiting Heat Shock Protein 90 (HSP90) activity in mammals, which method comprises administering to the mammal an amount of a compound of formula (I), or a salt, or N-oxide thereof effective to inhibit HSP90 activity: wherein R 2 is a group of formula (IA): wherein R 3 is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy, hydroxy(C 1 -C 6 )alkyl, mercapto, mercapto(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, halo, trifluoromethyl, trifluoromethoxy, nitro, cyano, oxo, phenyl, —COOH, —COOR F , —COR F , —SO 2 R F , —CONH 2 , —SO 2 NH 2 , —CONHR F , —SO 2 NHR F , —CONR F R G , —SO 2 NR F R G NH 2 , —NHR F , —NR F R G , —OCONH 2 , —OCONHR F , —OCONR F R G , —NHCOR F , —NHCOOR F , —NR F COOR F , —NHSO 2 OR F , NR G SO 2 OR F , —NHCONH 2 , —NR F CONH 2 , —NHCONHR G , —NR F CONHR G , —NHCONR F R G , or —NR F CONR F R G wherein R F and R G are independently a (C 1 -C 6 )alkyl group, or an optionally substituted (C 1 -C 6 )alkyl, aryl or heteroaryl radical; and R 4 is a carboxylic ester, carboxamide or sulfonamide group; wherein optionally substituted means optionally substituted with at least one substituent selected from (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy, hydroxy(C 1 -C 6 )alkyl, mercapto, mercapto(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, halo, trifluoromethyl, trifluoromethoxy, nitro, cyano, oxo, phenyl, —COOH, —COOR F , —COR F , —SO 2 R F , —CONH 2 —SO 2 NH 2 , —CONHR F , —SO 2 NHR F , —CONR F R G , SO 2 NR F R G , —NH 2 , —NHR F , —NR F R G , —OCONH 2 , —OCONHR F , —OCONR F R G , —NHCOR F , —NHCOOR F , —NR F COOR F , —NHSO 2 OR F , NR G SO 2 OR F , —NHCONH 2 , —NR F CONH 2 , —NHCONHR G , —NR F CONHR G , —NHCONR F R G , or —NR F CONR F R G wherein R F and R G are independently a (C 1 -C 6 )alkyl group.