| abstract |
Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-AIk1 -(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; AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene 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), C1C3alkyl optionally substituted with one or more fluorine substituents, C1C3alkoxy optionally substituted with one or more fluorine substituents, -CH=CH2, -C=CH, cyclopropyl and -NH2, or R3 and R4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; Si is hydrogen, or a substituent as defined in the specification. |