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1. 发明授权

US4224336A 3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyclo[3.2.0]- hept-2-ene-2-carboxylic acid 失效
标题翻译： 3-（2-氨基乙硫基）-6-氨基-7-氧代-1-氮杂双环[3.2.0] - 庚-2-烯-2-羧酸
公开(公告)号：US4224336A
公开(公告)日：1980-09-23
申请号：US30786
申请日：1979-04-17
申请人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07D205/08 , C07D205/085 , C07D477/10 , C07D477/24 , C07D498/04 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07D477/10 , C07C205/42 , C07D205/08 , C07D205/085 , C07D477/24 , C07F7/10
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.
摘要翻译：公开了具有以下结构的3-（2-氨基乙硫基）-6-酰胺基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸二乙酯，其中R1是氢或酰基。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。

2. 发明授权

US4347368A 3 -Substituted-6-substituted-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxyl ic acid 失效
标题翻译： 3-取代的6-取代-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸
公开(公告)号：US4347368A
公开(公告)日：1982-08-31
申请号：US207042
申请日：1980-11-14
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07D205/08 , C07D477/20 , C07D477/26 , C07D498/04 , C07F7/10 , C07D487/04
CPC分类号： C07D477/26 , C07D205/08 , C07D477/20 , C07F7/10
摘要： Disclosed are 3- and 6-substituted 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein 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3-和6-取代的7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸：其中R6，R7和R8特别独立地选自由氢，烷基，烯基，芳基和芳烷基组成的组。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。

3. 发明授权

US4281002A 3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyc lo(3.2.0)-hept-2-ene-2-carboxylic acid 失效
标题翻译： 3-（2-氨基乙硫基）-6-氨基-7-氧代-1-氮杂双环（3.2.0） - 庚-2-烯-2-羧酸
公开(公告)号：US4281002A
公开(公告)日：1981-07-28
申请号：US81518
申请日：1979-10-03
申请人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07D205/08 , C07D205/085 , C07D477/10 , C07D477/24 , C07D498/04 , C07F7/10 , C07D487/04 , A61K31/395
CPC分类号： C07D205/085 , C07C205/42 , C07D205/08 , C07D477/10 , C07D477/24 , C07F7/10
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.
摘要翻译：公开了具有以下结构的3-（2-氨基乙硫基）-6-酰胺基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，其中R 1是氢或酰基。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。

4. 发明授权

US4277482A 3-Substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid s-oxides 失效
标题翻译： 3-取代的硫代-6-氨基-7-氧代-1-氮杂双环[3.2.0] - 庚-2-烯-2-羧酸S-氧化物
公开(公告)号：US4277482A
公开(公告)日：1981-07-07
申请号：US84934
申请日：1979-10-15
申请人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , Ravindra N. Guthikonda , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07D477/24 , C07D487/04 , A61K31/40 , A61K31/44
CPC分类号： C07D477/24
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.
摘要翻译：公开了具有以下结构的3-取代的硫代-6-氨基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸的S-氧化物：其中：n是1或 2; R1是氢或酰基; 并且R8特别地独立地选自烷基，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。

5. 发明授权

US4269873A 2-, 5-, and 6-Substituted-1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-，5-和6-取代的1-碳氮杂环戊烯-2-烯-3-羧酸
公开(公告)号：US4269873A
公开(公告)日：1981-05-26
申请号：US60552
申请日：1979-07-25
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07D205/08 , C07D477/20 , C07D498/04 , C07F7/10 , C07D487/04 , A61K31/40
CPC分类号： C07D205/08 , C07C205/42 , C07D477/20 , C07F7/10
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.
摘要翻译：公开了具有以下结构的2-，5-和6-取代-1-碳代二脱氧-2-烯-3-羧酸：其中R 6，R 7，R 8和R 9特别地独立地选自由氢，（R9不是氢），烷基，烯基，芳基和芳烷基组成。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和治疗方法，包括当指示抗生素效果时施用这些化合物和组合物。

6. 发明授权

US4997936A 2-carbamimidoyl-6-substituted-1-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-甲脒基-6-取代-1-碳代二烯-2-烯-3-羧酸
公开(公告)号：US4997936A
公开(公告)日：1991-03-05
申请号：US898887
申请日：1986-08-21
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07C205/43 , C07D205/08 , C07D477/04 , C07D477/20 , C07D477/26 , C07D498/04 , C07D519/00 , C07F7/10
CPC分类号： C07F7/10 , C07C205/42 , C07C205/43 , C07D205/08 , C07D477/04 , C07D477/20 , C07D477/26
摘要： Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R.sup.6, and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, 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, cyclalkyl, aryl, heteroaryl, heteroalkyl; R.sup.1 and R.sup.2 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 carbammidoyl. 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; pharamaceutical 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2-和6-取代-1-碳代二脱氧-2-烯-3-羧酸：其中R 6和R 7尤其独立地选自氢，烷基，烯基，芳基和芳烷基; A是连接所指示的S和C原子的直接的单键，或A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。 R1和R2特别地独立地选自氢，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”是通过所述碳酰胺基的氮原子之一的季化来公开的。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用组合物; 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。

7. 发明授权

US4347367A 3-Substituted-6-(1'-hydroxyethyl)-7-oxo-1-azabicyc lo[3.2.0]-hept-2-ene-2-carboxylic acid 失效
标题翻译： 3-取代的6-（1'-羟乙基）-7-氧代-1-氮杂双环[3.2.0] - 庚-2-烯-2-羧酸
公开(公告)号：US4347367A
公开(公告)日：1982-08-31
申请号：US206935
申请日：1980-11-14
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07D205/08 , C07D477/20 , C07D477/26 , C07D498/04 , C07F7/10 , C07D487/04
CPC分类号： C07D477/20 , C07C205/42 , C07D205/08 , C07D477/26 , C07F7/10
摘要： Disclosed are 3-substituted-6-(1'-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R.sup.8 is, inter alia, selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl. Such compounds as well as their pharmaceutically acceptable 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的3-取代-6-（1'-羟乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，其中R8尤其是，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。

8. 发明授权

US4264621A 5-Substituted-3 -(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-en e-2-carboxylic acid 失效
标题翻译： 5-取代的3-（2-氨基乙硫基）-6-（1-羟基乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸
公开(公告)号：US4264621A
公开(公告)日：1981-04-28
申请号：US60551
申请日：1979-07-25
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07D205/08 , C07D477/20 , C07D498/04 , C07F7/10 , C07D487/04
CPC分类号： C07D477/20 , C07D205/08 , C07F7/10
摘要： Antibiotic 5-substituted-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids (I) are disclosed: ##STR1## wherein R is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or heteroaryl.
摘要翻译：公开了抗生素5-取代-3-（2-氨基乙硫基）-6-（1-羟乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸（I）其中R是烷基，环烷基，环烷基烷基，芳基，芳烷基或杂芳基。

9. 发明授权

US4234596A 3-(2-Aminoethyl thio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid 失效
标题翻译： 3-（2-氨基乙硫基）-6-（1-羟乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸
公开(公告)号：US4234596A
公开(公告)日：1980-11-18
申请号：US017680
申请日：1979-03-05
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07C205/42 , C07D205/08 , C07D477/20 , C07D477/26 , C07D487/04 , C07D498/04 , A61K31/40
CPC分类号： C07D477/20 , C07C205/42 , C07D205/08 , C07D477/26 , C07D487/04
摘要： Isomeric forms of 3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (I) ##STR1## are disclosed; also disclosed is a process for their total synthesis; such isomers individually, and as mixtures, are useful as antibiotics.
摘要翻译：公开了3-（2-氨基乙硫基）-6-（1-羟乙基）-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸（I）的异构体形式 ; 还公开了它们的全合成方法; 这些异构体单独和作为混合物可用作抗生素。

10. 发明授权

US4992542A 2-substituted-6-carbadethiapen-2-em-3-carboxylic acids 失效
标题翻译： 2-取代-6-碳氮杂萘-2-烯-3-羧酸
公开(公告)号：US4992542A
公开(公告)日：1991-02-12
申请号：US20189
申请日：1987-02-26
申请人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
发明人： Burton G. Christensen , David B. R. Johnston , Susan M. Schmitt
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： Disclosed are 2- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein 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2-和6-取代-1-碳代二脱氧-2-烯-3-羧酸：其中R6，R7和R8特别地独立地选自氢，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。

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