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Compounds and procedures for HDAC inhibition
专利权人:
Inc.;Tempero Pharmaceuticals
发明人:
BALOGLU, Erkan,GHOSH, Shomir,LOBERA, Mercedes,SCHMIDT, Darby
申请号:
ES11733353
公开号:
ES2560627T3
申请日:
2011.01.13
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound according to Formula (I-a) or (I-b): ** Formula ** in which: R1 is a haloalkyl (C1-C2) group containing at least 2 fluorine atoms; A is (C3-C6) cycloalkyl, phenyl, naphthyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl or optionally substituted 9-10 member heteroaryl, wherein any cycloalkyl, phenyl, naphthyl, heterocycloalkyl or optionally heteroaryl substituted is optionally substituted with 1-3 groups independently selected from (C1-C4) alkyl, halogen, cyano, haloalkyl (C1-C4), alkoxy (C1-C4), haloalkoxy (C1-C4), -NRARA and - (alkyl (C1-C4)) NRARA; Z is -C (>; = O) NRX-, -NRXC (>; = O) NRX, -NRXC (>; = O) -, -SO2-, -SO2NRx-, -NRXSO2-, -NHCH (CF3) -, - CH (CF3) NH-, -CH (CF3) -, (C1-C4) alkyl -, -NRx- or (C1-C3) -NRX- alkyl; n is 0-4; when n is 0, R2 and R3 are independently selected from H and optionally substituted (C1-C4) alkyl, arylalkyl (C1-C4) - and cycloalkyl (C3-C7) alkyl (C-C4) -; when n is 1-4, R2 and R3 are independently selected from H, fluorine, and (C1-C4) alkyl, arylalkyl (C1-C4) - and cycloalkyl (C3-C7) alkyl (C1-C4) - optionally substituted, where, when n is 1, R2 is F and R3 is H, then Z is -C (>; = O) NRX-, -NRXC (>; = O) NRX, -SO2NRx-, -NHCH (CF3) -, -CH (CF3) NH-, -CH (CF3) -, -alkyl (C1-C4) -, -NRx-, or -alkyl (C1-C3) -NRX-, and; when n is 1-4, R2 is selected from -NRARB, -alkyl (C1-C4) -NRARB, -CONRARB, -alkyl (C1-C4) -CONRARB, -CO2H, -alkyl (C1-C4) -CO2H, hydroxyl, hydroxyalkyl (C1-C4) -, alkoxy (C1-C3) and alkoxy (C1-C3) alkyl (C1-C4) -, and R3 is selected from H and (C1-C4) alkyl, arylalkyl (C1-C4) ) - and (C3-C7) cycloalkyl (C1-C4) alkyl - optionally substituted, wherein the aryl, cycloalkyl and each of the (C1-C4) alkyl moieties of said (C1-C4) alkyl, aryl (C1-alkyl) -C4) - and cycloalkyl (C3-C7) alkyl (C1-C4) - optionally substituted with any of R2 and R3 are optionally substituted with 1, 2 or 3 groups independently selected from halogen, cyano, (C1-C4) alkyl, halo (C1-C4) alkyl, (C1-C4) alkoxy, (C1-C4) h
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