公开(公告)号：NZ207193A

公开(公告)日：1987-10-30

申请号：NZ20719384

申请日：1984-02-17

Applicant: HOFFMANN LA ROCHE

Inventor： HUBSCHWERLEN C

IPC: C07D307/32 ,  C07D307/33 ,  C07D317/20 ,  C07D317/26 ,  C07D317/28 ,  C07D405/04 ,  C07D405/14 ,  C07D407/04

公开(公告)号：YU216188A

公开(公告)日：1990-04-30

申请号：YU216188

申请日：1988-11-24

Applicant: HOFFMANN LA ROCHE

Inventor： FURLENMEIER A ,  HUBSCHWERLEN C ,  MONTAVON M

IPC: C07D499/897 ,  A61K31/397 ,  A61K31/40 ,  A61K31/435 ,  A61K31/47 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D463/00 ,  C07D477/00 ,  C07D477/08 ,  C07D499/00 ,  C07D499/32 ,  C07D499/893 ,  C07D501/04 ,  C07D501/06 ,  C07D501/16 ,  C07D501/18 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D505/00 ,  C07D513/04 ,  A61K31/43

Abstract: 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 in which R denotes hydrogen or lower alkyl, R denotes hydrogen, lower alkyl, lower haloalkyl, lower alkenyl, lower alkoxycarbonyl, aryl or heteroaryl or, together with R denotes lower alkylene, R denotes hydrogen, lower alkyl or lower alkoxycarbonyl, R denotes the group -COOR , -COR , -SO2-R , -CONR R or -PO(OR )2, R 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 denotes lower alkyl or aryl, R and R 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 denotes lower alkyl. If a basic substituent is present, these esters can also be present in the form of pharmaceutically acceptable acid addition salts.