摘要:
3-Phosphonate carbapenems of the Formula: wherein R.sup.1 is hydrogen, alkyl, amino, --NHCO-alkyl, hydroxy, alkoxy, halo, hydroxyalkyl, carboxyl or trifluoromethyl; R.sup.2 is alkyl, substituted alkyl, heterocyclic or substituted heterocyclic; R.sup.3 is hydrogen, alkyl or substituted alkyl; and M is a metal cation of H.sup.+ are disclosed. The compounds are useful as antibiotics.
摘要:
In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## there is disclosed a process for preparing III via ##STR2## wherein R is a protecting group.
摘要:
Disclosed are 3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R is, inter alia, acyl, alkyl, and aralkyl. Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要:
Disclosed are 6- and 4-substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2-substituted carbapenem antibiotics. ##STR1## wherein R.sup.5 is a pharmaceutically acceptable ester moiety or a removable protecting group or an alkali or alkaline earth metal cation such as sodium or potassium and wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl.
摘要:
Disclosed are substituted N-methylene derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要翻译:公开了噻吩霉素的取代的N-亚甲基衍生物,其可以由以下结构式表示:其中X和Y选自氢,R,OR,SR和NR 1 R 2,其中除了其中R是 取代或未取代的:烷基,烯基,炔基,环烷基,环烷基烷基,芳基,芳烷基,杂芳基,杂芳烷基,杂环基和杂环基烷基; R1和R2是氢或R.这些化合物及其药学上可接受的盐,醚,酯和酰胺衍生物可用作抗生素。 还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法,包括当指出抗生素效应时施用这些化合物和组合物。
摘要:
A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-aminodecephalosporanic acid or 6-APA and reacts with a carbonyl containing compound to form a Schiff's base (imino) adduct. This latter compound is then treated with a defined reactant yielding a novel Schiff's base adduct having a side chain on the carbon adjacent to the imino-nitrogen. The amino moiety can be regenerated and further reacted to form end compounds which are active against both gram-positive and gram-negative bacteria.
摘要:
Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R.sup.1 is hydrogen or acyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要:
Disclosed are S-oxides of 3-substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; R.sup.1 is hydrogen or acyl; and R.sup.8 is, inter alia, independently selected from the group consisting of alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
摘要:
Disclosed is a process for the total synthesis of thienamycin from 4-allylazetidinone (IIIa) via ##STR1## L-aspartic acid (III): ##STR2## R.dbd.H, blocking group or salt cation.
摘要:
Disclosed are 2-, 5- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are, inter alia, independently selected from the group consisting of hydrogen, (R.sup.9 is not hydrogen), alkyl, alkenyl, aryl and aralkyl. Such compounds, as well as their pharmaceutically acceptable salt, ester and amide derivatives, are useful as antibiotics. Also disclosed are processes for the preparation of such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.