发明名称 Novel Heterocyclic Derivatives as Modulators of Kinase Activity
摘要 The invention provides novel imidazol-piperidinyl derivatives of the formula (I);;in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
申请公布号 US2015274750(A1) 申请公布日期 2015.10.01
申请号 US201314432316 申请日期 2013.11.15
申请人 LAN Ruoxi;HUCK Bayard R.;CHEN Xiaoling;XIAO Yufang;MERCK PATENT GMBH 发明人 Lan Ruoxi;Huck Bayard R.;Chen Xiaoling;Xiao Yufang
分类号 C07D498/04;A61K31/496;C07D487/04;A61N5/10;C07D239/70;A61K31/517;A61K31/5383;A61K45/06;C07D471/04;A61K31/519 主分类号 C07D498/04
代理机构 代理人
主权项 1. A compound of formula (I),and pharmaceutically acceptable salts, solvates, solvates of salts, tautomers or stereoisomers, including mixtures thereof in all ratios thereof, wherein: X1 is N or CH, X2 is CH2 or NH, X3 is CH2 or CO, X4 is O, CH2 or NH, W is N or CH, R1 is Ar or Het, R2 is [C(R3)2]pHet1 or [C(R3)2]pN(R3)2, each R3 is independently H or alkyl with 1, 2, 3, or 4 C-atoms, which is optionally substituted; Ar is phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, phenyl, CON(R3)2, COOR3, NHCOA, NHSO2A, CHO, COA, SO2N(R3)2, SO2A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2 and/or [C(R3)2]pCN, Het is furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl or quinolyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, NO2, CN, [C(R3)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA and/or O[C(R3)2]qN(R3)2, Het1 is dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, azepanyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl, pyridyl or piperazinyl, which is unsubstituted or mono- or disubstituted by A, each A is independently unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH- and/or CH2-groups may be replaced by N-, O- and/or S-atoms and wherein 1-7 H-atoms may be replaced by F or Cl, each Hal is independently F, Cl, Br or I, each m is independently 0, 1 or 2, each n is independently 0, 1 or 2, each p is independently 0, 1, 2, 3 or 4, each q is independently 2, 3 or 4.
地址 Waltham MA US