CANCER RESEARCH TECHNOLOGY LTD;VERNALIS (CAMBRIDGE) LIMITED;THE INSTITUTE OF CANCER RESEARCH
发明人:
DRYSDALE, MARTIN JAMES,DYMOCK, BRIAN WILLIAM,FINCH, HARRY,WEBB, PAUL,MCDONALD, EDWARD,JAMES, KAREN ELIZABETH,CHEUNG, KWAI MING,MATHEWS, THOMAS PETER
申请号：
CA2515726
公开号：
CA2515726C
申请日:
2004.02.09
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and usefulfor treatment of, for example cancers: (A), (B) wherein R1, is a group offormula (IA): -Ar1-(Alk1)p-(Z)r-(Alk2)S-Q, wherein in any compatiblecombination Ar1 is an optionally substituted aryl or heteroaryl radical,Alk1and Alk2 are optionally substituted divalent Cl-C6 alkylene or C2-C6alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -SO2-, -C(=O)O-, -C(=O)NRA-, -C(=S)NRA-, - SO2NRA-, -NRAC(=O)-, -NRASO2- or -NRA- wherein RA is hydrogen or Cl-C6 alkyl, and Q is hydrogenor an optionally substituted carbocyclic or heterocyclic radical； R2 is (i) agroup of formula (IA) above or (ii) a carboxamide radical； or (iii) a nonaromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionallysubstituted, and/or a ring nitrogen is optionally substituted by a group offormula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are asdefined above in relation to group (IA)； and R3 is hydrogen, optionallysubstituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6alkynyl； or a carboxyl, carboxamide, or carboxyl ester group.
