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PHARMACEUTICALLY ACTIVE HYDROPHILIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF PROTEIN JUNKINASES
专利权人:
发明人:
申请号:
EP01967621.2
公开号:
EP1322641B1
申请日:
2001.09.27
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The present invention is related to substantially hydrophilic sulfonamide derivatives, or sulfonamide derivatives having a substantially hydrophilic moiety, of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formula-tions containing such sulfonamide derivatives. Said sulfonamide derivatives are effi-cient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl Ar2 is an aryl or heteroaryl group carrying at least one hydrophilic substituentX is O or S, preferably O R1 is hydrogen or a C¿1?-C6-alkyl group, or R?1¿ forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1 n is an integer from 0 to 5, preferably between 1-3 and most preferred 1 Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.Cette invention, qui a trait à des dérivés de sulfonamide sensiblement hydrophiles ou à des dérivés de sulfonamide possédant une fraction sensiblement hydrophile, correspondant à la formule (I), utilisables comme composés actifs du point de vue pharmaceutique, concerne également des formulations pharmaceutiques contenant ces dérivés. Ces dérivés de sulfonamide, qui sont des modulateurs efficaces de la voie de la jun-kinase (JNK), se révèlent être des inhibiteurs sélectifs et efficaces de JNK 3. Linvention porte également sur de nouveaux dérivés de sulfonamide ainsi que sur les procédés permettant de les préparer. Les composés selon linvention, cor
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