abstract |
Compounds of formula (I) have HSP90 inhibitory activity: ring A is an aryl or heteroaryl ring or ring system; R 1 is hydrogen, fluoro, chloro, bromo, or formula (1A): -X-Alk 1- (Z) m- (Alk 2 ) n -Q (IA) (In the formula, X is a bond, -O-, -S-, -S (O)-, -SO 2- , or -NH-, and Z is -O-, -S-,-( C = O)-,-(C = S)-, -S (O)-, -SO 2- , -NR A- , or -C (= O) O-, -C (= O) NR A- , -C (= S) NR A- , -SO 2 NR A- , -NR A C (= O)-or -NR A SO 2- (wherein R A is hydrogen or C 1 to C 6 alkyl, and one or more hydrogens may be optionally substituted with fluorine), and Alk 1 and Alk 2 are optionally substituted divalent C 1 to C 3 alkylene or C 2 -C 3 alkenylene group, m and n are independently 0 or 1, Q is a good carbocyclic or heterocyclic group which may be hydrogen or optionally substituted R 2 is cyano (—CN), fluoro, chloro, bromo, methyl, ethyl, —OH, —CH 2 OH, —C (═O) NH 2 , —C (═O) H , -C (= O) CH 3 , or be -NH 2; R 3 and R 4 are independently hydrogen, fluoro, chloro, bromo, shea Roh (-CN), 1 or more fluorine substituents optionally optionally substituted C 1 -C 3 alkyl, one or more fluorine substituents which may be optionally substituted with a group C 1 -C 3 Selected from alkoxy, —CH═CH 2 , —C≡CH, cyclopropyl and —NH 2 , or R 3 and R 4 together are methylenedioxy (—OCH 2 O—) or ethylenedioxy ( -OCH 2 CH 2 O-), any one of which optionally substituted one or more hydrogens with fluorine; S 1 is as defined in the specification. [Selection figure] None |