Patent EP0021082A1 successfully refreshed from Google Patents.
EP0021082A1
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N-heterocyclyl thienamycins, process for preparing and antibiotic pharmaceutical composition containing the same
Assignee: Merck and Co Inc
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Filing: 1980-05-28
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Granted: —
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Expires: 2000-05-28
Abstract
Abstract This invention relates to a new class of thienamycins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: wherein the stylized radical (hereafter referred to as R'): attached to the amino nitrogen group of thienamycin represents a mono- or polycyclic N-containing heterocyclic group; R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkenyl, aralkenyl, heterocyclylalkyl, aralkyl, -NR 2 , COOR, CONR 2 , -OR, or CN. It also relates to a process for preparing such compounds and to antibiotic pharmaceutical compositions containing such compounds.
Inventors
- 👤 John Hannah
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-05 23:02
CPC Classifications
C; C07; C07D; C07D477/00; C07D477/10; C07D477/12; C07D477/16; C07D477/20; A; A61; A61P; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
149 words
A compound having the structural formula: and the pharmaceutically acceptable salts and esters thereof wherein: R' is selected from the group consisting of: wherein the dotted line indicates both saturated and unsaturated rings; and wherein: R is hydrogen, alkyl having from 1-6 carbon atoms, substituted alkyl having from 1-6 carbon atoms wherein the substituent is chloro, fluoro, hydroxyl, alkoxyl (C 1-6 ) , carboxyl, amino, sulfo and mono- and dialkylamino wherein each alkyl has 1-6 carbon atoms substituted and unsubstituted phenylalkyl and phenylalkenyl having 7-12 carbon atoms wherein the substituent is selected from chloro, fluoro, carboxyl, amino, cyano, hydroxyl and sulfo; R 3 is chloro, fluoro, hydroxyl, carboxyl, sulfo, cyano, amino, mono- and dialkylamino, alkoxylalkyl having from 1-6 carbon atoms, substituted alkyl having 1-6 carbon atoms wherein the substituent is carboxyl, cyano, alkoxyl having 1-6 carbon atoms, phenyl and phenyloxy; n is an integer selected from 0 to 3.
Claim 2
Dependent Claim
149 words
A compound having the structural formula: and the pharmaceutically acceptable salts and esters thereof wherein: R' is selected from the group consisting of: wherein the dotted line indicates both saturated and unsaturated rings; and wherein: R is hydrogen, alkyl having from 1-6 carbon atoms, substituted alkyl having from 1-6 carbon atoms wherein the substituent is chloro, fluoro, hydroxyl, alkoxyl (C 1-6 ) , carboxyl, amino, sulfo and mono- and dialkylamino wherein each alkyl has 1-6 carbon atoms substituted and unsubstituted phenylalkyl and phenylalkenyl having 7-12 carbon atoms wherein the substituent is selected from chloro, fluoro, carboxyl, amino, cyano, hydroxyl and sulfo; R 3 is chloro, fluoro, hydroxyl, carboxyl, sulfo, cyano, amino, mono- and dialkylamino, alkoxylalkyl having from 1-6 carbon atoms, substituted alkyl having 1-6 carbon atoms wherein the substituent is carboxyl, cyano, alkoxyl having 1-6 carbon atoms, phenyl and phenyloxy; n is an integer selected from 0 to 3.
Claim 3
Dependent Claim
23 words
A compound according to Claim 1 wherein n is 0 or 1; and R is hydrogen or substituted or unsubstituted alkyl or phenylalkyl.
Claim 4
Dependent Claim
24 words
A compound according to Claim 2 wherein R' is selected from the group consisting of: wherein M is hydrogen or a pharmaceutically acceptable cation.
Claim 5
Dependent Claim
59 words
4 A process for preparing a compound according to Claim 1 comprising reacting: with an N-heterocyclic reagent selected from: wherein the dotted line indicates both saturated and unsaturated rings; Y is a counter anion; Di⊕ is H, alkali or alkaline earth metal cation or tertiary amine salt; and wherein X°is a leaving group, and optionally removing a quaternizing group.
Claim 6
Dependent Claim
21 words
An antibiotic pharmaceutical composition comprising a therapeutically effective amount of a compound according to Claim 1 and a pharmaceutical carrier therefor.
References Cited (Backward Citations)
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