
基本信息:
- 专利标题: 4-(4-吡啶基)-苯甲酰胺及其作为ROCK活性调节剂的应用
- 专利标题(英):4-(4-pyridinyl)-benzamides and their use as ROCK activity modulators
- 申请号:CN200880114671.3 申请日:2008-08-26
- 公开(公告)号:CN101903349A 公开(公告)日:2010-12-01
- 发明人: H·麦克 , N·托希 , B·K·米勒 , W·霍恩伯格 , M·F·贾维斯 , D·索尔 , S·小斯万 , D·博纳富克斯 , R·克迪 , A·D·霍布森 , A·瓦素德万
- 申请人: 雅培股份有限两合公司 , 雅培制药有限公司
- 申请人地址: 德国威斯巴登
- 专利权人: 雅培股份有限两合公司,雅培制药有限公司
- 当前专利权人: ABBVIE德国有限责任两合公司,艾伯维公司
- 当前专利权人地址: 德国威斯巴登
- 代理机构: 中国专利代理(香港)有限公司
- 代理人: 刘健
- 优先权: 60/966278 2007.08.27 US
- 国际申请: PCT/EP2008/061135 2008.08.26
- 国际公布: WO2009/027392 EN 2009.03.05
- 进入国家日期: 2010-04-26
- 主分类号: C07D213/56
- IPC分类号: C07D213/56 ; C07D401/12 ; C07D405/12 ; C07D413/12 ; C07D417/12 ; A61K31/44 ; A61K31/4427 ; A61P9/00 ; A61P25/00 ; A61P35/00 ; A61P29/00
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.
公开/授权文献:
- CN101903349B 4-(4-吡啶基)-苯甲酰胺及其作为ROCK活性调节剂的应用 公开/授权日:2014-01-08
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D213/00 | 杂环化合物,含六元环、不与其他环稠合、有1个氮原子作为仅有的杂环原子、环原子间或环原子与非环原子间有3个或更多个双键 |
--------C07D213/02 | .环原子间或环原子与非环原子间有3个双键 |
----------C07D213/04 | ..在环氮原子与非环原子间没有键或只有氢或碳原子直接连在环氮原子上 |
------------C07D213/06 | ...除了环氮原子外,只含氢和碳原子 |
--------------C07D213/28 | ....被以单键键合的氧原子或硫原子取代的基 |
----------------C07D213/56 | .....酰胺 |