abstract |
"PIRAZOL COMPOUNDS". The present invention relates to compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof which are HSP90 inhibitors, and are of value in treating diseases responsive to HSP90 inhibition such as cancers. In the formulas, Ar is an aryl, aryl (C 1 -C 6 alkyl) aryl, aryl (C 1 -C 6 alkyl), heteroaryl, heteroaryl (C 1 -C 6) alkyl), or (C 1 -C 6 alkyl) heteroarylaryl, any of which being optionally substituted on the aryl or heteroaryl portion thereof; R1 is hydrogen or C1-6 alkyl optionally substituted alkyl; R 2 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, or C 1 -C 6 alkynyl; or a carboxyl, carboxamide or carboxyl ester group; and ring A is a non-aromatic heterocyclic or carbocyclic ring where (I) a ring carbon is optionally substituted, and / or (ii) a ring nitrogen is optionally substituted by a group of formula - (Alk¬ 1¬) ~ p ~ (Cic) ~ n ~ - (Alq¬ 3¬) ~ m ~ (Z) ~ r ~ (Alq¬ 2¬) ~ s ~ Q where Alq¬ 1¬, Alq¬ 2¬ and Alq¬ 3¬ are Optionally substituted C1 -C3 alkyl, C1 -C is an optionally substituted heterocyclic or carbocyclic radical; m, n, p, res are independently 0 or 1, Z is -O-, -S-, - (C = O) -, -SO ~ 2 ~ -, C (= O) O-, -OC (= O) -, -NW-, -C (= O) NRA-, -NR¬ A¬C (= O) -, -SO ~ 2 ~ NR¬ A¬-, or NR¬ A¬SO ~ 2 ~ - where R¬ A¬ is hydrogen or C 1 -C 6 alkyl, and Q is hydrogen or an optionally substituted heterocyclic or carbocyclic radical. |