发明名称 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
摘要 The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula -X-W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m-R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.
申请公布号 US2013310378(A1) 申请公布日期 2013.11.21
申请号 US201313868765 申请日期 2013.04.23
申请人 ABBVIE DEUTSCHLAND GMBH & CO KG;ABBVIE INC.;ABBVIE INC.;ABBVIE DEUTSCHLAND GMBH & CO KG 发明人 MACK HELMUT;TEUSCH NICOLE;MULLER BERNHARD K.;HORNBERGER WILFRIED;JARVIS MICHAEL F.;SAUER DARYL;SWANN, JR. STEVEN L.;BONAFOUX DOMINIQUE;KEDDY RYAN;HOBSON ADRIAN DONALD;VASUDEVAN ANIL
分类号 C07D213/56;C07D401/12;C07D405/12;C07D409/12;C07D413/12;C07D413/14 主分类号 C07D213/56
代理机构 代理人
主权项
地址