Invention Grant
- Patent Title: Small-molecule HSP90 inhibitors
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Application No.: US15620865Application Date: 2017-06-13
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Publication No.: US10167285B2Publication Date: 2019-01-01
- Inventor: Gabriela Chiosis , Huazhong He , Laura Llauger-Bufi , Joungnam Kim , Steven M. Larson , Peter Smith-Jones
- Applicant: Memorial Sloan Kettering Cancer Center
- Applicant Address: US NY New York
- Assignee: Memorial Sloan Kettering Cancer Center
- Current Assignee: Memorial Sloan Kettering Cancer Center
- Current Assignee Address: US NY New York
- Agency: Choate, Hall & Stewart LLP
- Agent Brenda Herschbach Jarrell; John P. Rearick
- Main IPC: C07D473/34
- IPC: C07D473/34 ; A61K51/04 ; C07D491/056 ; G01N33/60

Abstract:
Hsp90 inhibitors havin are provided havin the formula: (I) with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens 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.
Public/Granted literature
- US20170342073A1 SMALL-MOLECULE HSP90 INHIBITORS Public/Granted day:2017-11-30
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