发明名称 MATRIX METALLOPROTEASE INHIBITORS________________________________
摘要 This invention is directed to compounds of formula (I): wherein R<1> is mercapto, acetylthio, carboxy, hydroxycarbamoyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, benzyloxycarbamoyl or (i) (where R<6> is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl); R<2> is alkyl, aralkyl or cycloalkylalkyl; R<3> is cycloalkyl, alkyl (optionally substituted by cycloalkyl, hydroxy, mercapto, alkylthio, aralkoxy, carboxy, amino, alkylamino, guanidino, carbamoyl, pyridyl or indolyl), or aralkyl (optionally substituted by hydroxy, carboxy, alkyl or alkoxy); R<4> is nitro, amino, cyano, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylsulfonyl, haloalkyl, alkoxycarbonylalkyl, tetrazolyl, carbamoyl (optionally substituted by alkyl or dialkylaminoalkyl), or aminosulfonyl (optionally substituted by alkyl); and R<5> is hydrogen, halo or hydroxy; as single stereoisomers or as mixtures thereof; or the pharmaceutically acceptable salts thereof. These compounds are useful in inhibiting matrix metalloprotease activity in mammals.
申请公布号 WO9512603(A1) 申请公布日期 1995.05.11
申请号 WO1994US12214 申请日期 1994.11.03
申请人 SYNTEX (U.S.A.) INC. 发明人 CASTELHANO, ARLINDO, L.;YUAN, ZHENGYU;HORNE, STEPHEN;LIAK, TENG, J.
分类号 C07D213/82;A61K31/195;A61K31/215;A61K31/235;A61K31/403;A61K31/404;A61K31/405;A61K31/44;A61K31/4406;A61K31/4418;A61K31/662;A61P27/02;A61P29/00;A61P35/00;A61P43/00;C07C51/60;C07C53/42;C07C57/72;C07C67/313;C07C67/317;C07C69/353;C07C69/533;C07C233/47;C07C237/22;C07C237/42;C07C255/57;C07C255/60;C07C259/06;C07C271/22;C07C279/14;C07C311/46;C07C317/38;C07C317/40;C07C323/52;C07C323/59;C07C323/60;C07C323/63;C07C327/12;C07C327/22;C07C327/32;C07D209/20;C07D213/75;C07D263/26;C07D295/13;C07F9/30;C07F9/32;C07F9/34;C07F9/36;C07F9/48;C07F9/58;C07F9/60;C07F9/62;C07F9/6558;(IPC1-7):C07F9/30;A61K31/66 主分类号 C07D213/82
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