发明名称 DISUBSTITUTED 5-FLUORO PYRIMIDINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP
摘要 The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group 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 US2015005329(A1) 申请公布日期 2015.01.01
申请号 US201214345353 申请日期 2012.09.13
申请人 Lücking Ulrich;Kosemund Dirk;Scholz Arne;Lienau Philip;Siemeister Gerhard;Bömer Ulf;Bohlmann Rolf 发明人 Lücking Ulrich;Kosemund Dirk;Scholz Arne;Lienau Philip;Siemeister Gerhard;Bömer Ulf;Bohlmann Rolf
分类号 C07D405/04;C07C381/10;A61K31/506;C07D239/42;A61K31/505 主分类号 C07D405/04
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-, amino, 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, halogen atom, cyano, —SF5, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R5 represents a group selected from a hydrogen atom, cyano, —C(O)R9, —C(O)OR9, —S(O)2R9, —C(O)NR10R11, C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, heteroaryl wherein said C1-C6-alkyl, C3-C7-cycloalkyl-, heterocyclyl-, phenyl or heteroaryl group is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R6, R7 represent, independently from each other, a group selected from a hydrogen atom, halogen atom, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R8 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 the group of halogen, hydroxy, amino, 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, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;b) a C3-C6-alkenyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, amino, 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, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;c) a C3-C6-alkynyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, amino, 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, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;d) 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, amino, 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-;e) a heterocyclyl-group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, amino, 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-; f) a phenyl group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, amino, 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 group, which is optionally substituted with one or two or three substituents, identically or differently, selected from the group of halogen, hydroxy, amino, 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 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, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;i) 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, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, cyano, C1-C3-alkyl-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-, C1-C3-alkoxy-;j) 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 halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-;k) a heterocycly-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-;l) 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-;m) 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-; R9 represents a group selected from C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, benzyl or heteroaryl wherein said group is optionally substituted with one, two or three substituents, identically or differently, selected from halogen, hydroxy, C1-C3-alkyl-, C1-C3-alkoxy-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R10, R11 represent, independently from each other, a group selected from hydrogen, C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl or heteroaryl wherein said C1-C6-alkyl, 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-, amino, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; or its enantiomers, diastereomers, salts, solvates or salts of solvates.
地址 Berlin DE