发明名称 PENICILLANIC ACID DERIVATIVES
摘要 The compounds of the general formula I in which R is hydrogen, a readily hydrolyzable ester group or a protecting group, R1 is hydrogen and R2 is hydrogen or an acyl group, or R1 and R2 taken together are the group in which n is 5, 6 or 7, X is fluoro, thiocyanato, azido or the group R3aCO2 , , -SR3 , -OR3 , , , or ; R3a is C2- to C16-alkyl, aryl, a heterocycle, -(CH2)m-aryl, -(CH2)m-heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R3 is C1- to C16-alkyl, aryl, a heterocycle, -(CH2)m-aryl, a -(CH2)m-heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R4 and R4' independently are hydrogen, lower alkyl, lower alkenyl or lower alkynyl, Ra is hydrogen, halogen, amino, amino-lower alkyl, carboxy, carbamoyl, carboxy-lower alkyl, carbamoyl-lower alkyl or lower carbalkoxy-lower alkyl, m is from 1 to 4 and p is 3, 4 or 5, provided that X is other than fluoro when R is a protecting group, a hydrate, a readily hydrolyzable ester or salt thereof, or a hydrate of the ester or the salt, when R is hydrogen are useful as anti-bacterial agents for the prevention and treatment of bacterial infections in mammals, including humans.
申请公布号 CA2001642(A1) 申请公布日期 1990.04.30
申请号 CA19892001642 申请日期 1989.10.27
申请人 HOFFMANN LA ROCHE 发明人 BARTKOVITZ DAVID J;KEITH DENNIS D;MOOK ROBERT;WEI CHUNG-CHEN
分类号 C07D499/21;A61K31/43;A61P31/04;C07D499/00;C07D499/46;C07D499/87;(IPC1-7):C07D499/02;C07F9/654 主分类号 C07D499/21
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