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11. 发明授权

US4748162A 6-substituted-2-carbaminidoyl-pen-2-em-3-carboxylic acids 失效
标题翻译： 6-取代-2-氨基甲酰基 - 二氧戊环-3-羧酸
公开(公告)号：US4748162A
公开(公告)日：1988-05-31
申请号：US605338
申请日：1984-04-30
申请人： William J. Leanza , Burton G. Christensen , Frank P. DiNinno , Ronald W. Ratcliffe
发明人： William J. Leanza , Burton G. Christensen , Frank P. DiNinno , Ronald W. Ratcliffe
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： Disclosed are 6-substituted-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein R.sup.6, and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkoxyl, halo, OH, COOH, alkenyl, aryl and aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acyclic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of one of the nitrogen atoms of said carbamimidoyl. 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：公开了具有以下代表性结构的6-取代-2-氨基甲脒基 - 二-2-碳-3-羧酸（I）：其中R 6和R 7尤其独立地选自氢烷基，烷氧基，卤素，OH，COOH，烯基，芳基和芳烷基; A是连接指示的S和C原子的直接的单键，或A是特别是选自烷基，环烷基，芳基，杂芳基，杂烷基的环状或无环连接基团; 定义氨基甲酰基官能团的R 1和R 2尤其独立地选自氢，烷基，芳基; 另外，所述的氨基甲脒基的特征在于通过两个氮原子通过它们的取代基并通过它们与连接基团A的连接而实现的环状结构; 此外，“氨基甲酰胺”是通过季铵化所述氨甲脒基的氮原子而公开的。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。

12. 发明授权

US4335043A 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：US4335043A
公开(公告)日：1982-06-15
申请号：US84013
申请日：1979-10-11
申请人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
发明人： Burton G. Christensen , William J. Leanza , Kenneth J. Wildonger
IPC分类号： C07D205/08 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07F7/10 , C07D205/08
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。

13. 发明授权

US4150145A N-alkylated derivatives of thienamycin sulfoxide and sulfone 失效
标题翻译：噻吩霉素亚砜和砜的N-烷基化衍生物
公开(公告)号：US4150145A
公开(公告)日：1979-04-17
申请号：US833618
申请日：1977-09-15
申请人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
发明人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
IPC分类号： C07D477/20 , C07D487/04
CPC分类号： C07D477/20
摘要： Disclosed are N-alkylated derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2): ##STR1## wherein n=1 or 2; and R.sup.5, R.sup.6, and R.sup.7 are, inter alia, hydrogen or alkyl. Such compounds the their pharmaceutically acceptable O- and carboxyl- 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：公开了噻吩那霉素亚砜（I，n = 1）和砜（I，n = 2）的N-烷基化衍生物：其中n = 1或2; 和R 5，R 6和R 7尤其是氢或烷基。这些化合物其药学上可接受的O-和羧基衍生物可用作抗生素。还公开了制备这种衍生物的方法，包含这些衍生物的药物组合物和治疗方法，包括当指示抗生素效果时施用这样的衍生物和组合物。

14. 发明授权

US4235920A N-Alkylated derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-烷基化衍生物
公开(公告)号：US4235920A
公开(公告)日：1980-11-25
申请号：US861235
申请日：1977-12-16
申请人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
发明人： Burton G. Christensen , Raymond A. Firestone , William J. Leanza
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04 , C07D407/04 , A61K31/40
CPC分类号： C07D477/20 , C07D205/08
摘要： Disclosed are N-alkylated derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such compounds and their pharmaceutically acceptable salt, ester and amide 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：公开了抗生素硫霉素的N-烷基化衍生物，其具有以下结构：此类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。

15. 发明授权

US4235917A N-Alkyl-N-acyl derivatives of thienamycin 失效
标题翻译：噻吩霉素的N-烷基-N-酰基衍生物
公开(公告)号：US4235917A
公开(公告)日：1980-11-25
申请号：US793974
申请日：1977-05-05
申请人： Burton G. Christensen , William J. Leanza
发明人： Burton G. Christensen , William J. Leanza
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/20 , C07F9/6561 , C07D487/04
CPC分类号： C07D477/20 , C07F9/65611
摘要： Disclosed are N-alkyl- N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 is, inter alia, alkyl, alkenyl, aryl or aralkyl; and R.sup.2 is acyl. Such compounds, including their O- and carboxyl 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式的抗生素硫霉素的N-烷基-N-酰基衍生物：其中R 1特别是烷基，烯基，芳基或芳烷基; R2是酰基。这些化合物，包括其O-和羧基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，以及治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

16. 发明授权

US3931150A Probenecidoxymethyl and 1-ethyl esters of ampicillin 失效
标题翻译：氨苄西林的丙磺舒啶氧基甲基和1-乙基酯
公开(公告)号：US3931150A
公开(公告)日：1976-01-06
申请号：US492654
申请日：1974-07-30
申请人： Burton G. Christensen , William J. Leanza
发明人： Burton G. Christensen , William J. Leanza
IPC分类号： C07D499/00 , C07D499/68
CPC分类号： C07D499/00
摘要： New ampicillin derivatives, probenecidoxymethyl and 1-ethyl esters of ampicillin and their pharmaceutically acceptable salts, useful as antibiotics. A method for preparing these antibiotics by condensing probenecidoxymethyl or 1-ethyl halide with an acid salt of 6[D(-)-.alpha.-azidophenylacetamido] penicillanic acid, hydrogenating the azido group and isolating the product as a pharmaceutically acceptable salt of an acid. Pharmaceutical preparations containing the new antibiotics.
摘要翻译：新氨苄青霉素衍生物，氨磺青霉素的丙磺舒氧甲基和1-乙基酯及其药学上可接受的盐，可用作抗生素。通过将丙磺舒氧甲基或1-乙基卤与6 [D（ - ） - α-叠氮基苯乙酰氨基]青霉烷酸的酸盐缩合来制备这些抗生素的方法，氢化叠氮基并分离作为药学上可接受的酸的产物。含有新抗生素的药物制剂。

17. 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。

18. 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。

19. 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。

20. 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.

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