[EN] BENZAMIDE DERIVATIVES AND THEIR USE AS APOB-100 AND MTP INHIBITORS<br/>[FR] DERIVES DE BENZAMIDE ET LEUR UTILISATION COMME INHIBITEURS D'APOB-100 ET DE MTP
申请人:GLAXO GROUP LTD
公开号:WO2001092241A1
公开(公告)日:2001-12-06
The present invention relates to a compound of formula (I); wherein R1 represents isopropyl or trifluoromethyl; R2 represents hydrogen, C¿1-4?alkyl, chloro, fluoro or trifluoromethyl; R?3¿ represents(i) phenyl, optionally substituted by cyano, halogen, trifluoromethyl or an optionally substituted 5-membered heteroaromatic group, where optional substitution is effected by C¿1-4?alkyl, (ii) a 5- membered heteroaromatic group, optionally substituted by halogen, cyano or C1-4alkyl, (iii) aminocarbonyl, or(iv) ethyl or eth-1-enyl; R?4¿ represents cyano, methyl, acetyl, a 5- membered heteroaromatic group, optionally substituted by C¿1-4?alkyl or phenyl, or a group X-Y-Z; X represents a carboxy, oxo, C1-6alkylene, carboxamido or thiocarboxamido linking group; Y represents a direct link or C1-6alkylene; Z represents (i) hydrogen, (ii) trifluoromethyl, (iii) cyano, (iv) phenyl, (v) a 5- or 6- membered heteroaromatic group, optionally substituted by C1-4alkyl, with the proviso that when X represents C1-4alkylene, Y and Z do not represent a direct link and hydrogen respectively, or when X represents oxo, Y and Z do not represent C1-6alkylene and hydrogen respectively; or a physiologically acceptable salt, solvate or derivative thereof, to compositions comprising the compound, processes for their preparation and their use in treating conditions ameliorated by an apoB-100 and/or MTP inhibitor.