Vernalis (R&D) Limited;Cancer Research Technology Limited;The Institute of Cancer Research
发明人:
DYMOCK, Brian William,DRYSDALE, Martin James,FROMONT, Christofe,JORDAN, Allan,BARRIL-ALONSO, Xavier
申请号：
ES04768197
公开号：
ES2559779T3
申请日:
2004.08.26
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
The use of a compound of formula (I), or a salt, N-oxide, hydrate or solvate thereof in the preparation of a composition for use in inhibiting HSP90 activity in vitro or in vivo: ** Formula ** in where R2 is a group of formula (IA): - (Ar1) m- (Alk1) p- (Z) r- (Alk2) sQ (IA) where Ar1 is an optionally substituted phenyl or heteroaryl radical, Alk1 and Alk2 are optionally substituted C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, rys are independently 0 or 1, Z is -O-, -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 C1-C6 alkyl, and Q is hydrogen or an optionally substituted phenyl or C3-C8 cycloalkyl radical or a heterocyclic radical； R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6) alkyl, phenyl or heteroaryl radical； and R4 is (i) a carboxylic ester group of the formula -COORC wherein RC is a C1-C6 alkyl or C2-C6 alkenyl group, or an optionally substituted aryl or heteroaryl group, or an aryl (C1-C6 alkyl) group - or heteroaryl (C1-C6 alkyl) - optionally substituted or an optionally substituted cycloalkyl group or (ii) carboxamide group of the formula - CONRB (Alk) nRA or a sulfonamide group of the formula -SO2NRB (Alk) nRA wherein Alk is an alkylene radical , optionally substituted alkenylene or divalent alkynylene, n is 0 or 1, RB is hydrogen or a C1-C6 alkyl or C2-C6 alkenyl group, RA is hydrogen, optionally substituted hydrogen, hydroxy or carbocyclic or heterocyclic, or RA and RB taken together with the Nitrogen to which they are attached form a morpholino, piperidinyl or piperazinyl ring which may be optionally substituted at one or more C or N atoms of the ring； and wherein the term "optionally substituted" means substituted with at least one substituent selected from (C1-C6) alkyl, (C1-C6) alkoxy, hydroxy, hydroxyalkyl (C1-C6), mercapto, mercaptoalkyl (C1-C6) alkyl, (C1-C6) alkyl thio, halo (
