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公开(公告)号：US4833167A
公开(公告)日：1989-05-23
申请号：US743139
申请日：1985-06-10
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, diaklylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，酯，酸酐和酰胺衍生物，其可用作抗生素。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β-甲基 ; R6和R7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，被保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基 取代 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 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。
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公开(公告)号：US4707547A
公开(公告)日：1987-11-17
申请号：US859281
申请日：1986-05-02
IPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/6561 , C07D487/04 , A61K31/40
CPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/65611
摘要： Disclosed are 6- and 6,6-disubstituted-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, aryl, and aralkyl; and R' and R" are independently selected from the group consisting of: H, substituted and unsubstituted alkyl and aralkyl, or together form a substituted or unsubstituted cyclic group.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 compounds and compositions when an antibiotic effect is indicated.
摘要翻译： 公开了6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸（I）：其中R1和R2是 尤其是独立地选自氢，取代和未取代的：烷基，芳基和芳烷基; 并且R'和R“独立地选自：H，取代和未取代的烷基和芳烷基，或一起形成取代或未取代的环状基团。 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，其中包括当指出抗生素效应时施用化合物和组合物。
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公开(公告)号：USRE32465E
公开(公告)日：1987-07-28
申请号：US738702
申请日：1985-05-29
申请人： Adriano Afonso , Frank Hon
发明人： Adriano Afonso , Frank Hon
IPC分类号： C07D205/08 , C07D205/09 , C07D463/00 , C07D477/04 , C07D477/22 , C07D487/04 , C07D499/88 , C07D503/00 , C07F7/18
CPC分类号： C07D487/04 , C07D205/08 , C07D205/09 , C07D463/12 , C07D463/16 , C07D477/04 , C07D477/22 , C07D499/88 , C07D503/00 , C07F7/186
摘要： Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.
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公开(公告)号：US4892869A
公开(公告)日：1990-01-09
申请号：US300738
申请日：1989-01-19
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of 1 from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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： 披露的是2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用的2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，可用作抗生素的酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备1的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 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。
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公开(公告)号：US4782051A
公开(公告)日：1988-11-01
申请号：US87978
申请日：1987-08-17
IPC分类号： C07D477/22 , C07D487/04 , A61K31/495
CPC分类号： C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, trizolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，可用作抗生素的酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 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。
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公开(公告)号：US4431658A
公开(公告)日：1984-02-14
申请号：US387726
申请日：1982-06-11
申请人： Adriano Afonso , Frank Hon
发明人： Adriano Afonso , Frank Hon
IPC分类号： C07D205/08 , C07D205/09 , C07D463/00 , C07D477/04 , C07D477/22 , C07D487/04 , C07D499/88 , C07D503/00 , C07F7/18 , A61K31/415 , C07D233/02
CPC分类号： C07D487/04 , C07D205/08 , C07D205/09 , C07D477/04 , C07D477/22 , C07D499/88 , C07D503/00 , C07F7/186
摘要： Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.This is a division; of application Ser. No. 230,774, filed Feb. 2, 1981 now U.S. Pat. No. 4,347,183.
摘要翻译： 描述了一种用于制备可用作抗菌剂的青霉烯和碳青霉烯类的新方法，其包括在叔胺和碱土金属碳酸盐存在下合适的4-取代的氮杂环丁烷-2-酮与酰卤的反应， 随后将由此形成的1-亚氨基-4-取代的氮杂环丁烷-2-酮与亚磷酸三烷基酯反应。 还描述了通过所述方法制备的用作抗菌剂的新颖的青春期。
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公开(公告)号：US4347183A
公开(公告)日：1982-08-31
申请号：US230774
申请日：1981-02-02
申请人： Adriano Afonso , Frank Hon
发明人： Adriano Afonso , Frank Hon
IPC分类号： C07D499/897 , A61K31/397 , A61K31/40 , A61K31/415 , A61P31/04 , C07D205/08 , C07D205/09 , C07D463/00 , C07D477/00 , C07D477/04 , C07D477/22 , C07D487/04 , C07D499/00 , C07D499/04 , C07D499/06 , C07D499/32 , C07D499/88 , C07D503/00 , C07F7/18
CPC分类号： C07D487/04 , C07D205/08 , C07D205/09 , C07D477/04 , C07D477/22 , C07D499/88 , C07D503/00 , C07F7/186
摘要： Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite.Also described are novel penems useful as antibacterials which are prepared by the described process.
摘要翻译： 描述了一种用于制备可用作抗菌剂的青霉烯和碳青霉烯类的新方法，其包括在叔胺和碱土金属碳酸盐存在下合适的4-取代的氮杂环丁烷-2-酮与酰卤的反应， 随后将由此形成的1-亚氨基-4-取代的氮杂环丁烷-2-酮与亚磷酸三烷基酯反应。 还描述了通过所述方法制备的用作抗菌剂的新颖的青春期。
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公开(公告)号：US5140030A
公开(公告)日：1992-08-18
申请号：US569257
申请日：1990-08-16
IPC分类号： C07D477/22 , C07F9/6561
CPC分类号： C07F9/65611 , C07D477/22 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids. I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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： 披露的是2-氮杂取代的1-碳代萘二烯-2-烯-3-羧酸。 I，其中通用2-氮杂基团包括可用作抗生素的叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑啉基，氮丙啶基及其药学上可接受的盐，酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 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。
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公开(公告)号：US4783453A
公开(公告)日：1988-11-08
申请号：US97348
申请日：1987-09-08
IPC分类号： C07D477/22 , C07F9/6561 , C07D487/04 , A61K31/40
CPC分类号： C07D477/22 , C07F9/65611 , Y02P20/55
摘要： Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.2 are, inter alia, hydrogen, alkyl, acyl, and can be joined to form a ring comprising 3 to 7 atoms; R.sup.a is hydrogen, a salt cation, a removable protecting group, or a pharmaceutically acceptable ester moiety.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： 披露的是2-氮杂取代的1-碳代萘二甲酸-2-烯-3-羧酸I，其中通用的2-氮杂基团包括叠氮基，酰氨基，氨基，烷基氨基，二烷基氨基，三唑基，三唑基，氮丙啶基及其药学上可接受的盐 ，可用作抗生素的酯，酸酐和酰胺衍生物。 还公开了通过2-叠氮中心中间体III从已知的适当取代的双环酮酯II制备I的方法：其中R 16是H或CH 3，优选β- 甲基; R 6和R 7独立地是氢，直链，支链或环状的C 1 -C 5烷基，其可以被氟，羟基，保护的羟基，亚磺氧基，氨基，保护的氨基取代，其中R 6和R 7一起也可以是C 2 -C 4亚烷基， 同样取代; 条件是R6和R7都不是未取代的烷基，R1和R2特别是氢，烷基，酰基，并且可以连接形成包含3至7个原子的环; Ra是氢，盐阳离子，可除去的保护基或药学上可接受的酯部分。 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。
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10.发明授权6- And 6,6-disubstituted-3-substituted amino-1-azabicyclo-[3.2.0]hept-2-en-7-one-2-carboxylic acid 失效6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸
公开(公告)号：US4530841A
公开(公告)日：1985-07-23
申请号：US388311
申请日：1982-06-14
IPC分类号： C07D205/08 , C07D477/22 , C07F7/10 , C07F9/6561 , A61K31/40 , C07D487/04
CPC分类号： C07F7/10 , C07D205/08 , C07D477/22 , C07F9/65611
摘要： Disclosed are 6- and 6,6-disubstituted-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R.sup.1 and R.sup.2 are, inter alia, independently selected from the group consisting of hydrogen, substituted and unsubstituted: alkyl, aryl, and aralkyl; and R' and R" are independently selected from the group consisting of: H, substituted and unsubstituted alkyl and aralkyl, or together form a substituted or unsubstituted cyclic group.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 compounds and compositions when an antibiotic effect is indicated.
摘要翻译： 公开了6-和6,6-二取代-3-取代的氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸（I）：其中R1和R2是 尤其是独立地选自氢，取代和未取代的：烷基，芳基和芳烷基; 并且R'和R“独立地选自：H，取代和未取代的烷基和芳烷基，或一起形成取代或未取代的环状基团。 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，其中包括当指出抗生素效应时施用化合物和组合物。
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