发明名称 7-azaindole derivatives suitable for treatment of cancers
摘要 Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.
申请公布号 US8993564(B2) 申请公布日期 2015.03.31
申请号 US201214126857 申请日期 2012.05.29
申请人 Merck Patent GmbH 发明人 Heinrich Timo;Wucherer-Plietker Margarita;Buchstaller Hans-Peter
分类号 A61K31/535;C07D471/04;A61K31/437;A61K31/5377;A61K45/06 主分类号 A61K31/535
代理机构 Millen, White, Zelano & Branigan, P.C. 代理人 Millen, White, Zelano & Branigan, P.C.
主权项 1. a compound of the formula Iin which R1 denotes H, A, CH2CN, CH2CONH2, CH2CONHA′, CH2CONA′2, CH2COOH, CH2COOA′ or CH2COHet1, R2 denotes (CH2)nAr, COAr, (CH2)nHet, Cyc, Alk or A, R3 denotes CH3 or (CH2)nNHCOOA′, R4 denotes phenyl, Alk denotes unbranched or branched alkenyl having 2-6 C atoms, A denotes unbranched or branched alkyl having 1-8 C atoms, in which one or two non-adjacent CH2 and/or CH groups may be replaced by O, N and/or S atoms and/or 1-7 H atoms may be replaced by F and/or Cl, A′ denotes unbranched or branched alkyl having 1-4 C atoms, Cyc denotes cycloalkyl having 3-7 C atoms, Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, (CH2)2CN, (CH2)2COOH, (CH2)2COOA, (CH2)2OH, (CH2)2OA, COHet1, O(CH2)2R4, NO2, CONHHet1, NHCOCyc, CONH(CH2)2CONH2, CONH(CH2)2CONHA′, CONH(CH2)2CONA′2, CONH2, CONHA′, CONA′2, NHCOAlk, CONHCH(R4)CONH2, CONH(CH2)nCONHHet1, CONH(CH2)nCOHet1 and/or CONH(CH2)nCyc, Het denotes a mono- or bicyclic aromatic heterocycle having 1 to 4 N, and/or O and/or S atoms which is unsubstituted or mono- or disubstituted by Hal and/or A, Het1 denotes a monocyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, and/or O and/or S atoms which is unsubstituted or mono- or disubstituted by A, Hal denotes F, Cl, Br or I, n denotes 0, 1 or 2, or pharmaceutically acceptable salts, tautomers and stereoisomers thereof.
地址 Darmstadt DE