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公开(公告)号：US4684724A
公开(公告)日：1987-08-04
申请号：US791998
申请日：1985-10-23
IPC分类号： C07D205/08 , C07D205/085 , C07D409/14 , C07D417/12 , C07F7/08 , C07F7/10 , A61K31/395 , C07D401/12 , C07D403/12
CPC分类号： C07D409/14 , C07D205/085 , C07D417/12 , C07F7/0812 , C07F7/10
摘要： 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.
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公开(公告)号：US4782147A
公开(公告)日：1988-11-01
申请号：US499802
申请日：1983-05-31
IPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , A61K31/395 , A61K31/425
CPC分类号： C07D209/48 , C07D205/08 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula ##STR2## wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译： 公开了以下通式的化合物：其中R 1是氨基，酰化氨基或被保护的氨基，X是氢或甲氧基，R'是氢，R或R 4，其中R是与氮杂环丁烷连接的有机残基 R 4为叠氮基，卤素，可任选被酰化的氨基或式为基团的基团，其中R 5为有机残基且n为0,1或2，以及药学上可接受的盐 及其酯。 这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。
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3.发明授权4-carbamoyloxymethyl-1-sulfo-2-oxoazetidine derivatives and their production 失效4-氨基甲酰氧基甲基-1-磺基-2-氧代氮杂环丁烷衍生物及其制备
公开(公告)号：US4673739A
公开(公告)日：1987-06-16
申请号：US778219
申请日：1985-09-18
IPC分类号： C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , C07D205/08 , C07D417/02 , A61K31/425
CPC分类号： C07D209/48 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Compounds of the formula ##STR1## are useful as intermediates in preparing 1-sulfo-2-oxoazetidine compounds having the carbamoyloxymethyl group at the 4-position. The final product compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译： 式“IMAGE”的化合物可用作制备在4-位具有氨基甲酰氧基甲基的1-磺基-2-氧代氮杂环丁烷化合物的中间体。 最终产品化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。
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4.发明授权4-Carbamoyloxymethyl-1-sulfo-2-oxoazetidine derivatives and their production 失效4-氨基甲酰氧基甲基-1-磺基-2-氧代氮杂环丁烷衍生物及其制备
公开(公告)号：US4572801A
公开(公告)日：1986-02-25
申请号：US499801
申请日：1983-05-31
IPC分类号： C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , A61K31/425 , C07D205/08 , C07D277/38
CPC分类号： C07D209/48 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group and R.sup.2 is a hydrogen atom or an ester residue, said derivative having the (3S,4S)-configuration; and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译： 公开了以下通式的化合物：其中R1是氢原子或低级烷基，R2是氢原子或酯残基，所述衍生物具有（3S，4S） - 构型; 及其药学上可接受的盐和酯。 这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。
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公开(公告)号：US4675397A
公开(公告)日：1987-06-23
申请号：US405592
申请日：1982-08-05
IPC分类号： C07D205/085 , C07D205/095 , C07D209/48 , C07D257/04 , C07D277/20 , C07D277/46 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07F7/08 , C07F7/10 , C07F9/6558 , C07D205/08 , A61K31/425 , A61K31/395
CPC分类号： C07D209/48 , C07D205/085 , C07D205/095 , C07D257/04 , C07D277/46 , C07D277/587 , C07D311/22 , C07D401/06 , C07D403/04 , C07D413/14 , C07D417/12 , C07D417/14 , C07F7/0812 , C07F7/10 , C07F9/65583
摘要： Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.
摘要翻译： 公开了以下通式的化合物：其中R 1是氨基，酰化氨基或被保护的氨基，X是氢或甲氧基，R'是氢，R或R 4，其中R是与氮杂环丁烷连接的有机残基 R 4是叠氮基，卤素，可任选被酰化的氨基或式-OR5，或-SS-R5的基团，其中R5是有机残基且n是0， 1或2，及其药学上可接受的盐和酯。 这些化合物具有抗微生物和/或β-内酰胺酶抑制活性，并且对于人类和驯养动物具有价值。
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公开(公告)号：US4560508A
公开(公告)日：1985-12-24
申请号：US451323
申请日：1982-12-20
IPC分类号： C07D205/08 , C07D205/085 , C07D409/14 , C07D417/12 , C07F7/08 , C07F7/10 , A61K31/395 , C07D401/12 , C07D403/12
CPC分类号： C07D409/14 , C07D205/085 , C07D417/12 , C07F7/0812 , C07F7/10
摘要： 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.
摘要翻译： 由下式表示的4-氰基-2-氮杂环丁酮衍生物[Ⅰ]其中R1是可被酰化或保护的氨基，X是氢原子或甲氧基，W是氢原子或磺基 和其制备方法，例如，由如下所示的方法，其中R 2是酰化或保护的氨基，Y是卤素原子或具有式-OCOR 3，-SCOR 3或 - S（O）n -R 3（R 3为烃基，n为整数1或2），R 4为可被酰化或保护的氨基，X如上述定义。 化合物[I]可用作合成光学活性4-取代-2-氮杂环丁酮衍生物的有利中间体，并且当W = SO 3 H时，[I]也可用作抗微生物剂和β-内酰胺酶抑制剂。
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