Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors

Details Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors

2004-08-26

2010-10-26

Wilson, James O (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S252160, C514S260100, C544S117000, C544S278000

Reexamination Certificate

active

07820658

ABSTRACT:
Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein R2is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk 2)S-Q wherein Ar1is an optionally substituted aryl or heteroaryl radical, Alk′ and Alk 2 are optionally substituted divalent C1-C3alkylene or C2-C3alkenylene radicals, m, p, r and s 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 RAis hydrogen or C1-C6alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4is a carboxylic ester, carboxamide or sulfonamide group.

REFERENCES:
patent: 0 438 261 (1991-07-01), None
patent: WO 03/037860 (2003-05-01), None
Vippagunta et al. (Advanced Drug Delivery Reviews, 2001, 48, pp. 3-26).
Palmer (Trends in Pharmacological Sciences, 2002, 23, pp. 426-433).
Journal of Heterocyclic Chemistry, vol. 30, No. 4, 1994, pp. 1065-1072, XP002312253, compound12 on p. 1065, 5g on p. 1066.

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