| abstract |
Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity and useful for the treatment of, for example, cancers: (A), (B) wherein R1 is a group of formula (IA): -Ar1- (Alk1) p- (Z) r- (Alk2) sQ, wherein in any compatible combination Ar1 is optionally substituted aryl or heteroaryl radicals, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenyl radicals, and s are independently 0 or 1, Z is -0-, -S-, - (C = O) -, - (C = S) -, -SO2-, -C (= O) NRA-, -C (= S) NRA-, -SO2NRA-, -NRAC (= O) -, -NRASO2- or -NRA-, wherein RA is hydrogen or C1-C6 alkyl and Q is hydrogen or optionally substituted carbocyclic or heterocyclic radical, R2 is (i) a group of formula (IA) above or (ii) carboxamide radical or (iii) non-aromatic carbocyclic or heterocyclic ring, wherein the carbon of the ring is optionally substituted or substituted is optionally substituted with a group of formula - (Alk1) p- (Z) r- (Alk2) sQ wherein Q, Alk1, Alk2, Z, p, r and s are as defined above with respect to group (IA) and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl or carboxyl, carbon boxamido or carboxyl ester group. |