发明名称 7-azaindole derivatives
摘要 Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
申请公布号 US9266887(B2) 申请公布日期 2016.02.23
申请号 US201514616113 申请日期 2015.02.06
申请人 Merck Patent GmbH 发明人 Dorsch Dieter;Sirrenberg Christian;Mueller Thomas J. J.;Merkul Eugen;Karapetyan Gnuni Amatunu
分类号 C07D519/00;A61K31/4375;C07D471/04;A61K45/06;A61K31/437 主分类号 C07D519/00
代理机构 Millen White Zelano & Branigan, P.C. 代理人 Millen White Zelano & Branigan, P.C.
主权项 1. Compounds of the formula I wherein R denotes 1,8-naphthyridin-4-yl which is unsubstituted or monosubstituted in the 7-position by R5, or 1,8-naphthyridin-4-yl, which may be substituted in the 2-position by A, Hal, CN, —[C(R6)2]n-Cyc, OR6, N(R6)2, SO2A or SO2Ar, R1 denotes H or A′, R2 denotes H, A′ or —[C(R6)2]n—Ar, R3 denotes H, A, Hal, CN, —[C(R6)2]n—Ar, —[C(R6)2]n-Het, —[C(R6)2]n-Cyc, OR6 or N(R6)2, R5 denotes A, Hal, CN, —[C(R6)2]n—Ar, —[C(R6)2]n-Het, —[C(R6)2]n-Cyc, OCyc, OHet′, OR6, N(R6)2, SO2A, SO2Ar or ═O, R6 denotes H or A′, A denotes unbranched or branched alkyl having 1-6 C atoms, in which one or two CH2 groups may be replaced by O, N and/or S atoms and/or by —CH═CH— groups and/or, in addition, 1-7 H atoms may be replaced by F, A′ denotes unbranched or branched alkyl having 1-4 C atoms or Cyc, Cyc denotes cycloalkyl having 3, 4, 5, 6 or 7 C atoms, Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, —[C(R6)2]nOR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2N(R6)2 and/or S(O)nA, Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms which is unsubstituted or mono- or disubstituted by Hal, A, —[C(R6)2]nOR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2NR6 and/or S(O)nA, Het′ denotes a monocyclic saturated heterocycle having 1 or 2 N, O and/or S atoms which is unsubstituted or mono- or disubstituted by A and/or ═O, Hal denotes F, Cl, Br or I, n denotes 0, 1 or 2, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE