发明名称 Pharmaceutically active hydrophilic sulfonamide derivatives as inhibitors of protein junkinases
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 formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. <CHEM> The compounds of formula I according to the present invention being suitable pharmaceutical agents are those wherein Ar<1> is a substituted or unsubstituted aryl or heteroaryl; Ar<2> is an aryl or heteroaryl group carrying at least one hydrophilic substituent; X is O or S, preferably O; R<1> is hydrogen or a C1-C6-alkyl group, or R<1> forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar<1>; 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.
申请公布号 AU8799001(A) 申请公布日期 2002.04.15
申请号 AU20010087990 申请日期 2001.09.27
申请人 APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. 发明人 SERGE HALAZY;DENNIS CHURCH;MONTSERRAT CAMPS;JEAN-PIERRE GOTTELAND;THOMAS RUECKLE;MARCO BIAMONTE;STEPHEN ARKINSTALL
分类号 A61K31/4535;A61P1/04;A61P9/00;A61P9/10;A61P11/06;A61P19/02;A61P25/00;A61P25/08;A61P25/14;A61P25/16;A61P25/28;A61P27/02;A61P31/04;A61P35/00;A61P37/06;A61P43/00;C07D409/12 主分类号 A61K31/4535
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