发明名称 PYRIDYL PIPERIDINES
摘要 The invention provides novel substituted pyridyl piperidine compounds according to Formula (I) which are Wnt pathway inhibitors, their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.;
申请公布号 US2017107222(A1) 申请公布日期 2017.04.20
申请号 US201515129338 申请日期 2015.03.10
申请人 MERCK PATENT GMBH ;CANCER RESEARCH TECHNOLOGY LIMITED 发明人 SCHIEMANN Kai;STIEBER Frank;CALDERINI Michel;BLAGG Julian;MALLINGER Aurelie;WAALBOER Dennis;RINK Christian;CRUMPLER Simon Ross
分类号 C07D471/20;C07D498/10;C07D401/14;C07D417/14;C07D519/00;A61K31/444;A61K31/499;A61K31/5377;A61K31/4709;A61K31/4725;C07D471/10;A61K45/06 主分类号 C07D471/20
代理机构 代理人
主权项 1. A compound of Formula (I) or its stereoisomers or tautomers, or pharmaceutically acceptable salts of each of the foregoing, including mixtures thereof in all ratios, wherein wherein: X is CH or N, Rl is LA, Hal, CN, R2 is H, Hal, NH2, LA, HO(LA)-, NH(LA), R3 is CN, CONH2, CONH(LA) or R2, R3 together with the C atom they are attached to, form a 5 or 6 membered non-aromatic heterocycle, having 1-3 heteroatoms, selected from O, S and N, which is substituted by 1 or 2 oxo groups, which heterocycle may further be monosubstituted by LA or OH, and which heterocycle may form a condensed ring system with a phenyl or pyridyl group, R4 is Cyc, CONH2, COO(LA) or CONH(LA), R5 is H, or R4, R5 together with the atoms they are attached to, form a 5 or 6 membered heterocycle, having 1-3 heteroatoms, selected from O, S and N, which is, optionally, independently mono- di- or trisubstituted by oxo, OH, LA, NH2, NH(LA), N(LA)2, NHCOO(LA) or HO(LA)-, Cyc is a 5 or 6 membered monocyclic, aliphatic or aromatic homo- or heterocycle having 1-3 heteroatoms, selected from O, S and N, which may be mono- or di-substituted by oxo, LA, NH2, NH(LA), N(LA)2, HO(LA)-, or monosubstituted by CA, LA is unbranched or branched alkyl, having 1, 2, 3, 4 or 5 carbon atoms, which may be saturated or partially unsaturated, wherein 1, 2 or 3 H atoms may be replaced by Hal, and/or 1 CH3 group may be replaced by CN, or1 CH2 group may be replaced by —O—, —NH— or —SO2—, and/or1 CH group may be replaced by N, CA is cycloalkyl having 3, 4, 5 or 6 carbon atoms, or cycloalkyl alkyl having 3, 4, 5 or 6 ring carbon atoms and 1 or 2 non-ring carbon atoms, in which cycloalkyl or cycloalkyl alkyl one ring atom may be replaced by O, and which cycloalkyl or cycloalkyl alkyl may be monosubstituted by OH, Hal is F, Cl, Br or I.
地址 Darmstadt DE