摘要 |
<p>Novel esters of pharmacologically active carboxylic acids, which can be cleaved under physiological conditions, in particular of antibiotically active carboxylic acids from the beta -lactam antibiotic field, are described, which are characterised in that the alcohol component of the ester is a group of the general formula <IMAGE> in which R<1> denotes hydrogen or lower alkyl, R<2> denotes hydrogen, lower alkyl, lower haloalkyl, lower alkenyl, lower alkoxycarbonyl, aryl or heteroaryl or, together with R<1> denotes lower alkylene, R<3> denotes hydrogen, lower alkyl or lower alkoxycarbonyl, R<4> denotes the group -COOR<5>, -COR<6>, -SO2-R<6>, -CONR<7>R<8> or -PO(OR<9>)2, R<5> denotes a saturated or unsaturated hydrocarbon radical having up to 12 carbon atoms, in which up to two methylene groups can be replaced by oxygen atoms, or denotes aryl or aryl-lower alkyl, R<6> denotes lower alkyl or aryl, R<7> and R<8> each denotes hydrogen or lower alkyl or together denotes lower alkylene in which a methylene group can be replaced by an oxygen or sulphur atom or by an imino or lower alkylimino group, and R<9> denotes lower alkyl. If a basic substituent is present, these esters can also be present in the form of pharmaceutically acceptable acid addition salts.</p> |
申请人 |
F. HOFFMANN-LA ROCHE ET CO. AG.,CH |
发明人 |
FURLENMEIER,ANDRE,CH;HUBSCHWERLEN,CHRISTIAN,FR;MONTAVON,MARC,CH |