发明名称 FUROPYRIDINE DERIVATIVES
摘要 Compounds of the formula I;;in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
申请公布号 US2015038527(A1) 申请公布日期 2015.02.05
申请号 US201314379770 申请日期 2013.01.22
申请人 Merck Patent GmbH 发明人 Burgdorf Lars;Ross Tatjana;Deutsch Carl
分类号 A61K31/4355;A61K31/444;C07D491/048 主分类号 A61K31/4355
代理机构 代理人
主权项 1. Compounds of the formula I in which R1 denotes Ar1 or Het1, R2 denotes Ar2, Het2, NH(CH2)nAr2, O(CH2)nAr2, NH(CH2)nHet2, NHCONHA, CONH2 or N3, R4 denotes H or F, Ar1 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]nCN, (CH2)nOH, (CH2)nOA, (CH2)nCOOH, (CH2)nCOOA, S(O)mA, (CH2)nHet3, CON(R3)2, CONH(CH2)nC(R3)2N(R3)2 and/or CONH(CH2)pCH[(CH2)nOR3](CH2)pOR3, Ar2 denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by A, Hal, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, SO2NH2, SO2NHA, SO2NA2, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, [C(R3)2]nN(R3)2, CONH(CH2)pCH[(CH2)nN(R3)2] (CH2)pOR3, CONH(CH2)pCH[(CH2)nOR3]NHSO2A, CONH(CH2)pCH[(CH2)nOR3]OR3, CONH(CH2)p[(CH(OR)]pCH2OR3, CONHR4, CONH(CH2)pCH[(CH2)nN(R3)2]Cyc, CONH(CH2)nC(R3)2N(R3)2 and/or CONHC(R3)2(CH2)pOR3, Het1 denotes benzo-1,3-dioxolyl or indazolyl, each of which is unsubstituted or monosubstituted by A, Het2 denotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, pyridazinyl, pyrazinyl, quinolyl, isoquinolyl, benzimidazolyl, furopyridinyl or indazolyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, NH(CH2)nHet4, A, (CH2)nOH, (CH2)nOA, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2 and/or ═O, Het3 denotes tetrazolyl or oxadiazolyl, each of which is unsubstituted or mono- or disubstituted by A, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2 and/or ═O, Het4 denotes piperidinyl or tetrahydrofuranyl, each of which is unsubstituted or monosubstituted by A or NH2, R3 denotes H or alkyl having 1, 2, 3 or 4 C-atoms, A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH2 groups may be replaced by O and/or NH, or cyclic alkyl having 3-7 C atoms, which may be unsubstituted or monosubstituted by OH, NHCOA or NH2, Cyc denotes cyclic alkyl having 3-7 C atoms, m denotes 0, 1 or 2, n denotes 0, 1, 2, 3 or 4, p denotes 1, 2, 3 or 4, and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstad DE