专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4146633A .DELTA..sup.3 -Thienamycin 失效
标题翻译： “”3“-THIENAMYCIN
公开(公告)号：US4146633A
公开(公告)日：1979-03-27
申请号：US847292
申请日：1977-10-31
申请人： Burton G. Christensen , Ronald W. Ratcliffe , David H. Shih
发明人： Burton G. Christensen , Ronald W. Ratcliffe , David H. Shih
IPC分类号： C07D477/02 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07D477/02
摘要： The antibiotic .DELTA..sup.3 -thienamycin is disclosed: ##STR1## It is prepared by double bond isomerization of thienamycin. Also disclosed are pharmaceutical compositions comprising .DELTA..sup.3 -thienamycin, and methods of treatment comprising administering .DELTA..sup.3 -thienamycin when an antibiotic effect is indicated.

2. 发明授权

US4226870A O-, N- and carboxyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的O-，N-和羧基衍生物
公开(公告)号：US4226870A
公开(公告)日：1980-10-07
申请号：US861246
申请日：1977-12-16
申请人： Burton G. Christensen , John Hannah , William J. Leanza , Ronald W. Ratcliffe , David H. Shih
发明人： Burton G. Christensen , John Hannah , William J. Leanza , Ronald W. Ratcliffe , David H. Shih
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04 , C07D487/04 , A61K31/40 , A61K31/44
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are O-, N- and substituted carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了抗生素噻吩霉素的O-，N-和取代的羧基衍生物，其具有以下结构：所述衍生物可用作抗生素。还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

3. 发明授权

US4729993A Carbapenems and 1-methylcarbapenems having an externally alkylated mono- or bicyclic 2-quaternary heteroarylalkyl substituent 失效
标题翻译：具有外部烷基化单 - 或双环2-季杂芳基烷基取代基的碳青霉烯和1-甲基碳青霉烯
公开(公告)号：US4729993A
公开(公告)日：1988-03-08
申请号：US681179
申请日：1984-12-13
申请人： Burton G. Christensen , Ronald W. Ratcliffe , James V. Heck , Thomas N. Salzmann , David H. Shih
发明人： Burton G. Christensen , Ronald W. Ratcliffe , James V. Heck , Thomas N. Salzmann , David H. Shih
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/495 , A61K31/53 , A61P31/04 , C07D477/14 , C07F7/18 , C07F9/6558 , C07D499/00 , A61K31/425
CPC分类号： C07D477/14 , C07F7/186 , C07F9/65583
摘要： Carbapenems having the formula: ##STR1## wherein ##STR2## is mono- or bicyclic quaternary heteroaryl, their preparation and antibiotic use are disclosed.
摘要翻译：具有以下分子式的碳青霉烯类似物：其中其中是单环或双环季铵杂芳基，其制备和抗生素使用。

4. 发明授权

US4839352A N-acyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-酰基衍生物
公开(公告)号：US4839352A
公开(公告)日：1989-06-13
申请号：US90400
申请日：1987-08-27
申请人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
发明人： Louis Barash , Burton G. Christensen , John Hannah , William J. Leanza , David H. Shih
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen and acyl. Such derivatives and their pharmaceutically acceptable salts, are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
摘要翻译：公开了具有以下结构式的抗生素硫霉素的N-酰基衍生物：其中R 1和R 2独立地选自氢和酰基。这些衍生物及其药学上可接受的盐可用作抗生素。还公开了制备这种衍生物的方法，包含这种衍生物的药物组合物，以及治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

5. 发明授权

US4582643A 6-(1-hydroxyethyl)-2-(2-amin oethylthio)-1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 6-（1-羟基乙基）-2-（2-氨基乙硫基）-1,1-二取代-1-碳代萘-2-烯-3-羧酸
公开(公告)号：US4582643A
公开(公告)日：1986-04-15
申请号：US397734
申请日：1982-07-13
申请人： Burton G. Christensen , David H. Shih
发明人： Burton G. Christensen , David H. Shih
IPC分类号： C07C1/30 , C07C17/16 , C07C17/275 , C07D205/08 , C07D477/20 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07C1/30 , C07C17/16 , C07C17/275 , C07D205/08 , C07F7/10
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. ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, substituted and unsubstituted alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl and the spiro substituent formed by the joinder of R.sup.1 and R.sup.2.
摘要翻译：公开了可用作抗生素的1-取代-6-（1-羟基乙基）-2-（2-氨基乙硫基）-1-碳代萘乙-2-烯-3-羧酸（I）及其药学上可接受的盐和酯; 这些化合物通过全合成制备。其中R1和R2特别是取代和未取代的烷基，芳基，芳烷基，环烷基，环烷基烷基和由R1和R2的连接形成的螺取代基。

6. 发明授权

US4372965A 6-, 1- And 2-substituted-thio-1-carbadethiapen-2-em-3-carboxylic acid S-oxides 失效
标题翻译： 6-，1-和2-取代 - 硫代-1-碳代萘二烯-2-酮-3-羧酸S-氧化物
公开(公告)号：US4372965A
公开(公告)日：1983-02-08
申请号：US223505
申请日：1981-01-08
申请人： Burton G. Christensen , David H. Shih
发明人： Burton G. Christensen , David H. Shih
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： Disclosed are S-oxides of 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 are, inter alia, independently selected from the group consisting of 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, 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：公开了具有以下结构的6-，1-和2-取代-1-碳代二烯-2-烯-3-羧酸的S-氧化物：其中：n为1或2; 并且R 1，R 6，R 7和R 8尤其独立地选自氢，烷基，烯基，芳基和芳烷基。这些化合物及其药学上可接受的盐，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，包括当指出抗生素作用时施用这些化合物和组合物。

7. 发明授权

US4311704A Substituted N-methylene derivatives of thienamycin 失效
标题翻译：噻吩霉素的取代的N-亚甲基衍生物
公开(公告)号：US4311704A
公开(公告)日：1982-01-19
申请号：US159573
申请日：1980-06-16
申请人： Burton G. Christensen , William J. Leanza , David H. Shih , Kenneth J. Wildonger
发明人： Burton G. Christensen , William J. Leanza , David H. Shih , Kenneth J. Wildonger
IPC分类号： C07D477/20 , C07D487/04 , A61K31/40 , A61K31/425 , A61K31/44
CPC分类号： C07D477/20
摘要： Disclosed are substituted N-methylene derivatives of thienamycin having the formula: ##STR1## wherein: (1.) X.dbd.--NR.sup.1 R.sup.2, and Y.dbd.--R'--N.dbd.CRNR.sup.1 R.sup.2, and(2.) X.dbd.R, and Y.dbd.--NR.sup.1 R'N.dbd.CRNR.sup.1 R.sup.2 ; andwherein: R is, inter alia, hydrogen, NH.sub.2, --NHR.sup.1, --NR.sup.1 R.sup.2, R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently selected from: hydrogen, substituted, or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R' is --(CH.sub.2).sub.n.sup.-, n is 1-6, or --(CH.sub.2).sub.m --Q--(CH.sub.2).sub.p.sup.-, m, n.dbd.1-3 and Q is O, S or R' is a carbocyclic or heterocyclic ring. 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：公开了具有下式的噻吩霉素的取代的N-亚甲基衍生物：其中：（1）X = -NR 1 R 2，Y = -R'-N = CRNR 1 R 2，和（2）X = R，Y = -NR1R'N = CRNR1R2; 并且其中：R特别是氢，NH 2，-NHR 1，-NR 1 R 2，R 1和R 2; R 1和R 2独立地选自：氢，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; R'为 - （CH 2）n - ，n为1-6或 - （CH 2）m Q-（CH 2）p - ，m，n = 1-3，Q为O，S或R'为碳环或杂环环。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。

8. 发明授权

US4206219A 6- and 1-Substituted-1-carbadethiapen-2-em-3-carboxylic acid 失效
标题翻译： 6-和1-取代的1-碳代萘二烯-2-烯-3-羧酸
公开(公告)号：US4206219A
公开(公告)日：1980-06-03
申请号：US954274
申请日：1978-10-24
申请人： Burton G. Christensen , David H. Shih
发明人： Burton G. Christensen , David H. Shih
IPC分类号： C07C205/42 , C07D205/08 , C07D477/20 , C07D477/26 , C07D498/04 , C07F7/18 , C07F9/568 , C07D487/04 , A61K31/40
CPC分类号： C07D477/20 , C07C205/42 , C07D205/08 , C07D477/26 , C07F7/1804 , C07F9/5683
摘要： Disclosed are 6- and 1-substituted-1-carbadethiapen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, 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 antibiotics effect is indicated.
摘要翻译：公开了以下结构的6-和1-取代-1-碳氮杂萘-2-烯-3-羧酸：其中R 1，R 2和R 3特别地独立地选自氢，烷基，芳基和芳烷基。这些化合物及其药学上可接受的盐，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。

9. 发明授权

US4696923A 6-[1-hydroxyethyl]-2-SR.sup.8 -1-methyl-1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 6- [1-羟乙基] -2-SR8-1-甲基-1-碳代萘二烯-2-烯-3-羧酸
公开(公告)号：US4696923A
公开(公告)日：1987-09-29
申请号：US603036
申请日：1984-04-23
申请人： Burton G. Christensen , David H. Shih
发明人： Burton G. Christensen , David H. Shih
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , A61P31/04 , C07D207/12 , C07D211/46 , C07D211/54 , C07D279/12 , C07D295/205 , C07D477/20 , C07D487/04
CPC分类号： C07D295/205 , C07D207/12 , C07D211/46 , C07D211/54 , C07D279/12 , C07D477/20
摘要： Disclosed are antibiotic 6-[1-hydroxyethyl]-2-SR.sup.8 -1-methyl-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I): ##STR1## wherein: R.sup.8 is ##STR2## and ##STR3## wherein: R.sup.8 is ##STR4## and wherein n and m are independently selected from 0, 1, 2, 3, 4 and 5; 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, heteroaryl (having 3-6 ring atoms, one or more of which is N, O or S).
摘要翻译：公开了抗生素6- [1-羟乙基] -2-SR8-1-甲基-1-碳代萘二酚-2-烯-3-羧酸及其药学上可接受的盐和酯（I）：其中：R8是＆lt; IMAGE＆gt; I其中：R8是，其中n和m独立地选自0,1,2,3,4和5; X是-NR; 并且Y是-R或-NRR; 并且其中R独立地选自氢，烷基，烯基，炔基，（具有1-6个碳原子）; 环烷基和环烯基（具有3-6个碳原子）; 和杂环基（具有3-6个环原子，其中一个或多个是N，O或S）。

10. 发明授权

US4350631A 6- and 4-Substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylates 失效
标题翻译： 6-和4-取代的-1-氮杂双环[3.2.0]庚-3,7-二酮-2-羧酸酯
公开(公告)号：US4350631A
公开(公告)日：1982-09-21
申请号：US245005
申请日：1981-03-18
申请人： Burton G. Christensen , David H. Shih
发明人： Burton G. Christensen , David H. Shih
IPC分类号： C07D477/00 , A61K31/00 , A61K31/397 , A61K31/40 , A61K31/407 , A61P31/00 , A61P31/04 , C07C17/275 , C07C29/147 , C07D205/08 , C07D477/18 , C07F7/10
CPC分类号： C07F7/10 , C07C17/275 , C07C29/147 , C07D205/08 , C07D477/18 , Y02P20/55
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.
摘要翻译：公开了6-和4-取代-1-氮杂双环[3.2.0]庚烷-3,7-二酮-2-羧酸酯和盐（I），其可用于制备6-，1-和2- 替代的碳青霉烯类抗生素。其中R 5是药学上可接受的酯部分或可除去的保护基团或碱金属或碱土金属阳离子如钠或钾，并且其中R 1，R 2，R 3和R 4特别地独立地选自的氢，烷基，芳基和芳烷基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式