发明名称 HYPOLIPEMIC 1,4-BENZOTHIAZEPINE-1,1-DIOXIDE
摘要 PROBLEM TO BE SOLVED: To obtain a new compound capable of reducing the concentration of an (ultra) low density lipoprotein cholesterol in plasma or serum and useful for treating and preventing hyperlipemia such as atherosclerosis. SOLUTION: This compound is represented by formula I R<1> and R<2> are each a straight-chain 1-6C alkyl; R<3> is H or OR<11> [R<11> is H or a (substituted) 1-6C alkyl]; R<4> is pyridyl or a (substituted) phenyl; R<5> , R<6> and R<8> are each H, a halogen, cyano, etc.; R<7> is represented by formula II (R<16> is COOH, CH2 OH, etc.), etc.; X is NH or O; R<9> and R<10> are each H or 1-6C alkyl}. The objective compound is prepared by acylating or alkylating a compound represented by formula III at the group X-H according to the standard method or glycosylating or glucuronidating the compound represented by formula III at the group X-H and then eliminating the protecting group, especially hydroxyl group and amino functional group.
申请公布号 JPH10279568(A) 申请公布日期 1998.10.20
申请号 JP19980062665 申请日期 1998.03.13
申请人 HOECHST AG 发明人 ENHSEN ALFONS DR;FALK EUGEN DR;GLOMBIK HEINER DR;STENGELIN SIEGFRIED DR
分类号 C12N15/09;A61K31/55;A61K31/554;A61K31/675;A61K31/70;A61K48/00;A61P1/16;A61P3/06;A61P3/10;A61P9/10;A61P35/00;C07D281/00;C07D281/10;C07D417/04;C07D417/10;C07D417/12;C07F9/6558;C07H17/00;C12N5/00;C12N5/10;C12N9/12;C12N15/06;C12N15/10;C12N15/11;C12N15/54;C12N15/85;C12P21/02;C12R1/91 主分类号 C12N15/09
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