| abstract |
ISOXAZOLE COMPOUNDS, AS WELL AS THEIR USE, PHARMACEUTICAL COMPOSITION AND IN VITRO METHOD FOR INHIBITING HSP90 ACTIVITY. Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for the treatment, for example, of cancers: (A), (B) wherein R1 is a group of formula (IA):-Ar1 -(Alk1)p-(Z)r-(Alk2)s-Q1 wherein in any compatible combination Ari is an optionally substituted aryl or heteroaryl radical, Alky and Alk2 are divalent C1-C6 alkylene or C2-C6 alkenylene radicals optionally substituted,p,r and s are independently 0 or 1, Z is -O-, -S-, -(C=O)-, (C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NRA, -C(=S)NRA-, -SO2NRA-, -NR?C(=0)-, -NRASO2- or -NRA. wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non-aromatic carbocyclic or heterocyclic ring in which an optionally substituted ring carbon 6, and/or a ring nitrogen is optionally substituted with a group of the formula -(Alk1)p-(Z)r-(Alk2) )s-Q where (...). |