| abstract |
"ISOXAZOLE COMPOUNDS". 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) : -Ar¬ 1¬- (Alk¬ 1¬) ~ p ~ - (Z) ~ r ~ - (ALk¬ 2¬) ~ s ~ -Q, where in any compatible combination Ar¬ 1¬ is a radical of optionally substituted aryl or heteroaryl, Alk¬ 1¬ and Alk¬ 2¬ are optionally substituted divalent C 1 -C 6 alkylene or C 2 -C 6 alkenylene radicals, e.g. 1, Z is -O-, -S-, - (C = O) -, (C = S) -, -SO-2 ~ -, -C (= O) O-, -C (= O) NR ¬ A¬ -C (= S) NR¬ A¬-, -SO ~ 2 ~ NR¬ A¬-, -NR¬ A¬C (= O) -, - NR¬ A¬SO ~ 2 ~ - or - NR¬ A¬- wherein R¬ A¬ is hydrogen or C1 -C6 alkyl and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non-aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and / or a ring nitrogen is optionally substituted by a group of the formula - (Alk¬ 1¬) -p ~ - (Z ) where Q, Alk 1, Alk 2, Z, p, res are as defined above with respect to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6-alkyl, C1-C6-alkenyl or C1-C6-alkynyl; or a carboxyl, carboxamide or carboxyl ester group. |