发明名称 NOVEL MACROCYCLIC COMPOUNDS
摘要 The present invention relates to novel macrocyclic compounds 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 US2017029439(A1) 申请公布日期 2017.02.02
申请号 US201515303212 申请日期 2015.04.08
申请人 Bayer Pharma Aktiengesellschaft 发明人 LÜCKING Ulrich;WASNAIRE Pierre;SCHOLZ Arne;LIENAU Philip;SIEMEISTER Gerhard;STEGMANN Christian;BÖMER Ulf;ZHENG Kunzeng;GAO Ping;CHEN Gang;XI Jiajun
分类号 C07D498/14;C07C53/18;A61K31/4375;C07D498/04;A61K31/519 主分类号 C07D498/14
代理机构 代理人
主权项 1. A compound of general formula (I) wherein A represents a bivalent group selected from the group consisting of —S—, —S(═O)—, —S(═O)2—, —S(═O)(═NR5)—; L represents a C2-C6-alkylene group, wherein said group is optionally substituted with(i) one substituent selected from hydroxy, C2-C3-alkenyl, C2-C3-alkynyl, C3-C4-cycloalkyl, hydroxy-C1-C3-alkyl, —(CH2)NR6R7, and/or(ii) one or two or three substituents, identically or differently, selected from halogen and C1-C3-alkyl, with the proviso that a C2-alkylene group is not substituted with a hydroxy group,or whereinone carbon atom of said C2-C6-alkylene group forms a three- or four-membered ring together with a bivalent group to which it is attached, wherein said bivalent group is selected from —CH2CH2—, —CH2CH2CH2—, —CH2OCH2—; X, Y represent CH or N with the proviso that one of X and Y represents CH and one of X and Y represents N; R1 represents a group selected from C1-C6-alkyl-, C3-C6-alkenyl, C3-C6-alkynyl, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, heteroaryl, phenyl-C1-C3-alkyl- and heteroaryl-C1-C3-alkyl-, wherein said group is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of hydroxy, cyano, halogen, C1-C6-alkyl-, halo-C1-C3-alkyl-, C1-C6-alkoxy-, C1-C3-fluoroalkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, —OP(═O)(OH)2, —C(═O)OH, —C(═O)NH2; R2 represents a group selected from a hydrogen atom, a fluoro atom, a chloro atom, a bromo atom, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, C1-C3-fluoroalkoxy-; R3, R4 represent, independently from each other, a group selected from a hydrogen atom, a fluoro atom, a chloro atom, a bromo atom, cyano, 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)R8, —C(═O)OR8, —S(═O)2R8, —C(═O)NR6R7, 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 the group consisting of halogen, hydroxy, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, —NH2, 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, C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, benzyl and heteroaryl, wherein said C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, benzyl or heteroaryl group is optionally substituted with one, two or three substituents, identically or differently, selected from the group consisting of 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-, or R6 and R7, together with the nitrogen atom they are attached to, form a cyclic amine; R8 represents a group selected from C1-C6-alkyl-, halo-C1-C3-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl, benzyl and heteroaryl, wherein said group is optionally substituted with one, two or three substituents, identically or differently, selected from the group consisting of 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-, or an enantiomer, diastereomer, salt, solvate or salt of solvate thereof.
地址 Berlin DE