发明名称 PYRIDOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
摘要 Compounds of the formula I;;in which R, R1 and R2 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 US2015218186(A1) 申请公布日期 2015.08.06
申请号 US201314420003 申请日期 2013.07.10
申请人 Merck Patent GmbH 发明人 Burgdorf Lars;Kuhn Daniel;Ross Tatjana;Deutsch Carl
分类号 C07D498/04;A61K31/5383;A61K31/538;C07D471/04;A61K31/519 主分类号 C07D498/04
代理机构 代理人
主权项 1. Compounds of the formula I in which R denotes H, OH, A or NR4R4′, R1 denotes Ar1, Het1, CN, A or —C≡C—Ar1, R2 denotes Het2, NR3Cyc, NR3CR3CON(R3)2, NR3[C(R3)2]pCR3(NH2)CH2OA or NR3[C(R3)2]pN(R3)2, Ar1 denotes phenyl, which is mono-, di- or trisubstituted by A, (CH2)nHet3, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, NO2, CN, Hal, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 and/or S(O)mA, Het1 denotes 3,6-dihydro-2H-pyranyl, tetrahydropyridinyl, 1,3-dihydro-benzimidazolyl, pyrazolyl, chromanyl, 1,2,3,4-tetrahydro-pyrazolo[1,5-a]pyridinyl, 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]-oxazinyl, 1,4-dihydro-benzo[d][1,3]oxazinyl, 4H-benzo[1,4]oxazinyl, benzimidazolyl, pyridyl, pyrimidinyl, imidazolyl, pyrazolyl, furyl, thiazolyl, triazolyl, benzotriazolyl, indolyl, indazolyl, 1,3- or 2,3-dihydro-indolyl, each of which is unsubstituted or mono-, di-, tri- or tetrasubstituted by A, CN, OH, OA, Hal, SO2NH2, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2 and/or ═O, Het2 denotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, tetrahydropyranyl, pyrazolyl, indazolyl, azetidinyl or octahydro-benzimidazolyl, each of which is mono-, di- or trisubstituted by Hal, A, (CH2)nNH2, (CH2)nNHA, (CH2)nNA2, (CH2)nOH and/or (CH2)nOA, Het3 denotes piperidinyl, piperazinyl, pyrrolidinyl, morpholinyl, imidazolidinyl, pyridyl, pyrimidinyl, imidazolyl, pyrazolyl, furyl, thiazolyl or triazolyl, each of which is unsubstituted or mono- or disubstituted by A and/or ═O, R3 denotes H or alkyl having 1, 2, 3 or 4 C-atoms, R4, R4′ each, independently of one another, denote H or A, A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by F and/or in which one or two non-adjacent CH2 groups may be replaced by 0 and/or NH, orcyclic alkyl having 3-7 C atoms, Cyc denotes cyclic alkyl having 3-7 C atoms, which may be unsubstituted or monosubstituted by NH2, CN, CONH2 or OH, 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, enantiomers, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstsdt DE