发明名称 Disubstituted 5-fluoro-pyrimidines
摘要 The present invention relates to disubstituted 5-fluoro-pyrimidines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
申请公布号 US9108926(B2) 申请公布日期 2015.08.18
申请号 US201214343983 申请日期 2012.09.13
申请人 Bayer Intellectual Property GmbH 发明人 Lücking Ulrich;Kosemund Dirk;Scholz Arne;Lienau Philip;Siemeister Gerhard;Bömer Ulf;Bohlmann Rolf
分类号 C07D239/42;C07D401/12;C07D407/04;A61K31/505;A61K31/506;C07D405/04 主分类号 C07D239/42
代理机构 代理人
主权项 1. A compound of general formula (I)wherein R1 represents a group selected from C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, heteroraryl, phenyl-C1-C3-alkyl- or heteroaryl-C1-C3-alkyl-, wherein said group is optionally substituted with one or two or three substituents, identically or differently, selected from the group of hydroxy, cyano, halogen, halo-C1-C3-alkyl-, C1-C6-alkoxy-, C1-C3-fluoroalkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines; R2 represents a group selected from R3, R4 represent, independently from each other, a group selected from a hydrogen atom, fluoro atom, chloro atom, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R5 represents a group selected from a) a C1-C6-alkyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-, C2-C3-alkenyl-, C2-C3-alkynyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, heteroaryl, wherein said C3-C7-cycloalkyl-, heterocyclyl-, phenyl or heteroaryl group is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, C1-C3-alkyl-, C1-C3-alkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;b) a C3-C7-cycloalkyl- group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-, C2-C3-alkenyl-, C2-C3-alkynyl-;c) a heterocyclyl- group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-, C2-C3-alkenyl-, C2-C3-alkynyl-;d) a phenyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo C1-C3 alkyl C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;e) a heteroaryl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo C1-C3 alkyl C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;f) a phenyl-C1-C3-alkyl- group, which phenyl group is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;g) a heteroaryl-C1-C3-alkyl- group, which heteroaryl group is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;h) a C3-C6-cycloalkyl-C1-C3-alkyl- group, which C3-C6-cycloalkyl group is optionally substituted with one or two or three substituents, identically or differently, selected from halogen, C1-C3-alkyl-, C1-C3, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;i) a heterocyclyl-C1-C3-alkyl- group, which heterocyclyl group is optionally substituted with one or two or three substituents, identically or differently, selected from halogen, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy;j) phenyl-cyclopropyl- group, which phenyl group is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo C1-C3 alkyl C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;k) a heteroaryl-cyclopropyl- group, which heteroaryl group is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-; R6, R7 represent, independently from each other, a group selected from a hydrogen atom, fluoro atom, chloro atom, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; or its salts, solvates or salts of solvates.
地址 Monheim DE