发明名称 Bipyridyl derivatives
摘要 The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
申请公布号 US9051307(B2) 申请公布日期 2015.06.09
申请号 US201414445227 申请日期 2014.07.29
申请人 Merck Patent GmbH 发明人 Hoelzemann Guenter;Dorsch Dieter;Jonczyk Alfred;Amendt Christiane;Zenke Frank
分类号 A61K31/4439;C07D401/14;C07D213/74;C07D471/04;A61K31/444;A61K31/4545;A61K31/496;A61K31/5377;A61K45/06;A61K31/4375;A61K31/497 主分类号 A61K31/4439
代理机构 Millen, White, Zelano & Branigan, P.C. 代理人 Millen, White, Zelano & Branigan, P.C.
主权项 1. A method of inhibiting ATP consuming proteins comprising: administering to a patient a compound of formula (I) wherein:W1, W2, W3 denote CR3,orW1, W2 denote CR3, andW3 denotes N,R1 denotes phenyl optionally substituted by at least one substituent selected from the group consisting of Hal, and CF3,R2 denotes Ar, Het1, Het2, —NH-Het1 or NH-Het2, each of which can be independently from each other substituted by R4,R3 denotes H, NYY or NY—COY,R4 denotes Hal, A, —(CYY)n—OY, —(CYY)n—NYY, (CYY)n-Het3, (CYY)n—O-Het3, SY, NO2, CF3, CN, COOY, —CO—NYY, —NY—COA, —NY—SO2A, —SO2—NYY, S(O)mA, —CO-Het3, —O(CYY)n—NYY, —O(CYY)n-Het3, —NH—COOA, —NH—CO—NYY, —NH—COO—(CYY)n—NYY, —NH—COO—(CYY)n-Het3, —NH—CO—NH—(CYY)n—NYY, —NH—CO—NH(CYY)n-Het3, —OCO—NH—(CYY)n—NYY, —OCO—NH—(CYY)n-Het3, CHO COA, ═S, ═NY, ═O,Y denotes H,A denotes unbranched or branched alkyl having 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 C atoms, in which 1, 2, 3, 4, 5, 6 or 7 H atoms can be replaced independently from one another by Hal and/or in which one or two CH2 groups can each be replaced independently of one another by a O, S, SO, SO2, a —CY═CY— group or a —C≡C— group,Ar denotes a saturated, unsaturated or aromatic, mono- or bicyclic carbocycle having 5, 6, 7, 8, 9, or 10 C atoms,Het1 denotes a saturated or unsaturated, mono, or bicyclic heterocycle having 3, 4, 5, 6, 7, 8, or 9, C atoms and 1, or 2, N atoms,Het2 denotes a mono, or bicyclic heteroaryl having 3, 4, 5, 6, 7, 8, or 9, C atoms and 1, or 2, N atoms,Het3 denotes a saturated or unsaturated, mono, or bicyclic heterocycle having 3, 4, 5, 6, 7, 8, or 9 C atoms and 1 or 2 N and/or O atoms, which can independently from each other be substituted by A,Hal denotes F, Cl, Br or I,m denotes 0, 1 or 2n denotes 0, 1, 2, 3 or 4. and the physiologically acceptable salts, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE