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4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
专利权人:
ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人:
MACK, HELMUT,海姆特 麦克,海姆特 麥克,TEUSCH, NICOLE,尼可 堤斯柯,尼可 堤斯柯,MUELLER, BERNHARD K.,伯恩哈德K 姆乐,伯恩哈德K 姆樂,HORNBERGER, WILFRIED,威尔菲得 霍恩博格,威爾菲得 霍恩博格,JARVIS, MICHAEL F.,麦可F 贾威司,麥可F 賈威司,SAUER, DARYL R.,达瑞尔R 梭儿,達瑞爾R
申请号:
TW097132748
公开号:
TWI437989B
申请日:
2008.08.27
申请国别(地区):
TW
年份:
2014
代理人:
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).R1and R2are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy R3, R4, R5and R6are, 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 R7is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl R8is 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 R9is 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 R15or a 5- or 6-membered saturated, partly unsatu-rated or aromatic heterocyclic ring and Y is linear or branched C1-C4-alkylene which may be partly or fully halo-genated 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.本發明係關於新穎式I之4-(4-吡啶基)-苯甲醯胺。化合物I係具有有價值之治療性質,且特別適合治療對Rho激酶(ROCK)之調節有回應之疾病。R1與R2係互相獨立為、氫、羥基、氰基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷氧基或C1-C8-鹵烷氧基;R3,R4,R5及R6係互相獨立為氫、羥基、鹵素、氰基、C1-C8-烷基、C1-C8-鹵烷基、C1-C8-烷氧基、C1-C8-鹵烷氧基、胺基、C1-C8-烷胺基或二-(C1-C8-烷基)-胺基;R7為氫、C1-C8-烷基、C1-C8-鹵烷基、芳基或芳基-C1-C8-烷基;R8為式-X-W基團,其中X 為單鍵、C1-C4-伸烷基(alkylene)或C1-C
来源网站:
中国工程科技知识中心
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