摘要:
Disclosed are 1-hetero-6-[1-hydroxyethyl)-2-SR 8 -1-carbadethiapen-2-em-3-COOR 4 compounds having the structure: wherein R 4 is, e.g., hydrogen, R 8 is, e.g., alkyl and R 9 is, e.g., halogen; the pharmaceutically acceptable salt and ester derivatives thereof and use as antibiotics. Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds.
摘要:
isclosed are 6-, 1- and 2-substituted-1 dethiapen-2-em-3 -carboxylic acids having the struc- in: R° is H or -SR 1 ; R', R 6 , R' and R 1 are, inter alia, endently selected from the group consisting of hyd- alkyl, alkenyl, aryl and aralkyl. Such compounds as is their pharmaceutically acceptable salt, ester and derivatives are useful as antibiotics. Also disclosed are ses for the preparation of such compounds and phar- tical compositions comprising such compounds.
R' and R 2 are independently H, CH 3 -, CH 3 CH 2 -, (CH 3 ) 2 CH-, HOCH 2 -, CH 3 CH(OH)-, (CH 3 ) 2 C(OH)-, FCH 2 , F 2 CH-, F 3 C-, CH 3 CH(F)-, CH 3 CF 2 - or (CH 3 ) 2 C(F)-; R 3 is CH 3 ; R 4 is a bridging group comprising substituted or unsubstituted C 1 -C 4 straight, C 2 -C 6 branched or C 3 -C 7 cycloalkyl groups wherein the substituents are selected from C 1 -C 6 alkyl, O-C 1 -C 6 alkyl, S-C 1 -C 6 alkyl, CF 3 , N(C 1 -C 6 alkyl) 2 ; X is -S-. -SO 2 -, -O- or -NH: and R 5 is, e. g., C 1 -C 10 straight or branched alkyl; their preparation and antibiotic use are disclosed.
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. wherein R 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 1 , R 2 , R 3 and R 4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl.
摘要:
Disclosed are 1-substituted-6-(1-hydroxyethyl)-2-(2-aminoethylthio)-1-carbadethiapen-2-em-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics; such compounds are prepared by total synthesis. wherein R 1 and R 2 are, inter alia, substituted and unsubstituted alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl and the spiro substituent formed by the joinder of R 1 and R 2 .
R 1 is hydrogen or methyl; R 4 and R 5 are independently H, CH 3 -, CH 3 CH 2 -, (CH 3 ) 2 CH-, HOCH 2 -, CH 3 CH(OH)-, (CH 3 ) 2 C(OH)-, FCH 2 , F 2 CH-, F 3 C-, CH 3 CH(F)-, (CH 3 ) 2 C(F)-, CH 3 CF 2 -; L is a bridging group comprising substituted or unsubstituted C 1 -C 4 straight, C 2 -C 6 branched or C 3 -C 7 cycloalkyl groups wherein the substituents are selected from C 1 -C 6 alkyl, O-C 1 -C 6 alkyl, S-C 1 -C 6 alkyl, CF 3 , N(C 1 -C 6 alkyl) 2 ;
3 2 is mono- or bicyclic quaternary heteroaryl, and Y is i) COOH or a pharmaceutically acceptable ester or salt thereof, ii) COOR wherein R is a removable carboxy protecting group, iii) COOM wherein M is an alkali metal, or iv) COO; provided that when Y is other than iv) a counterion Z is provided;
their preparatrion and antibiotic use are disclosed.
摘要:
Disclosed are antibiotic 6-[1-hydroxy-ethyl]-2-SR 8 -1-methyl-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I): wherein: R 8 is ;and wherein n and m are independently selected from 0, 1, 2, 3, 4; X is -NR; and Y is -R, or -NRR; and wherein R is independently selected from hydrogen, alkyl, alkenyl, alkynyl, (having 1-6 carbon atoms); cycloalkyl and cycloalkenyl (having 3-6 carbon atoms); and heterocyclyl, heteroary. (having 3-6 ring atoms, one or more of which is N, O or S). Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds.
摘要:
Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: wherein: R 1 , R 2 , R 6 , R 7 and R 8 are, inter alia, independently selected from the group consisting of hydrogen (R' and R 2 are 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 pharmaceutical compositions comprising such compounds.