| 摘要 |
Compounds of formula (I) have HSP90 inhibitory activity: ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, -O-, -S-, -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C-O)-, -(C-S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(-O)O-, -C(-O)NRA-, -C(-S)NRA-, -SO2NRA-, -NRAC(-O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; Alk1 and Alk2 are optionally substituted divalent C1-C3 alkylene or C2-C3alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH2OH, -C(-O)NH2, -C(-O)H, -C(-O)CH3, or -NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C1-C3alkyl optionally substituted with one or more fluorine substituents, C1-C3alkoxy optionally substituted with one or more fluorine substituents, -CH-CH2, -C≡CH, cyclopropyl and -NH2, or R3 and R4 together represent methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; S1 is as defined in the description.
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