DRYSDALE MARTIN JAMES,DRYSDALE Martin James Vernalis (Cambridge) Ltd,DYMOCK BRIAN WILLIAM,DYMOCK Brian William Vernalis (Cambridge) Ltd,FINCH HARRY VERNALIS,FINCH Harry Vernalis (Cambridge) Ltd,WEBB P
申请号：
SI200431954
公开号：
SI1611112T1
申请日:
2004.02.09
申请国别(地区):
SI
年份:
2012
代理人:
摘要：
Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): &mdashAr1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is &mdashO&mdash, &mdashS&mdash, &mdash(C&boxHO)&mdash, &mdash(C&boxHS)&mdash, &mdashSO2&mdash, &mdashC(&boxHO)O&mdash, &mdashC(&boxHO)NRA&mdash, &mdashC(&boxHS)NRA&mdash, &mdashSO2NRA&mdash, &mdashNRAC(&boxHO)&mdash, &mdashNRASO2&mdash or &mdashNRA&mdash 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 wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation 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.
