Small-molecule Hsp90 inhibitors

Details Small-molecule Hsp90 inhibitors Small-molecule Hsp90 inhibitors

2006-02-01

2010-11-16

Berch, Mark L (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C544S276000

Reexamination Certificate

active

07834181

ABSTRACT:
Hsp90 inhibitors are provided having the formula:with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2−alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2NSO2X5, C═OR2, where X5is F, NH2, alkyl or H, and R2is alkyl, NH2, NH-alkyl or O-alkyl, C1to C6alkyl or alkoxy; or wherein X1has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

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