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公开(公告)号:US4349551A
公开(公告)日:1982-09-14
申请号:US271007
申请日:1981-06-05
IPC分类号: C07D499/12 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/64 , C07D499/68 , C07D499/70 , A61K31/495
CPC分类号: C07D499/00
摘要: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## wherein R is phenyl 4-hydroxy phenyl, or a 5- 6- membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy.Their preparation and use is described.
摘要翻译: 式(I)化合物或其药学上可接受的盐或体内可水解的酯:其中R是苯基4-羟基苯基或含有至多三个选自以下的杂原子的5-6元杂环: 氧,硫或氮,任选被羟基,氨基,卤素或C 1-6烷氧基取代; R1代表氢或C1-6烷基; R2和R3相同或不同,表示氢,C1-6烷基,卤素,氨基,羟基或C1-6烷氧基。 描述了它们的制备和使用。
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公开(公告)号:US4394375A
公开(公告)日:1983-07-19
申请号:US271008
申请日:1981-06-05
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/57 , C07D505/00
CPC分类号: C07D505/00 , A61K31/545
摘要: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxyphenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy;X represents oxygen or sulphur; andA represents hydrogen, pyridyl, acetoxy, carbamoyloxy or a heterocyclicthio group;Their preparation and use is described.
摘要翻译: 式(I)化合物或其药学上可接受的盐或体内可水解的酯:其中R是苯基,4-羟基苯基或含有至多三个杂原子的5-或6-元杂环, 任选被羟基,氨基,卤素或C 1-6烷氧基取代的氧,硫或氮; R1代表氢或C1-6烷基; R2和R3相同或不同,表示氢,C1-6烷基,卤素,氨基,羟基或C1-6烷氧基; X表示氧或硫; A代表氢,吡啶基,乙酰氧基,氨基甲酰氧基或杂环硫基; 描述了它们的制备和使用。
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公开(公告)号:US4609652A
公开(公告)日:1986-09-02
申请号:US694592
申请日:1985-01-24
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D501/14 , C07D241/08 , C07D311/12 , C07D463/00 , C07D499/00 , C07D499/21 , C07D499/44 , C07D501/57 , C07D505/00 , A61K31/43 , A61K31/545
CPC分类号: C07D241/08 , C07D311/12 , C07D463/22 , C07D499/00 , C07D505/00
摘要: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
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公开(公告)号:US4877783A
公开(公告)日:1989-10-31
申请号:US694622
申请日:1985-01-24
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D501/14 , C07D241/08 , C07D311/12 , C07D463/00 , C07D499/00 , C07D499/21 , C07D499/44 , C07D501/57 , C07D505/00
CPC分类号: C07D241/08 , C07D311/12 , C07D463/22 , C07D499/00 , C07D505/00
摘要: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
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公开(公告)号:US4670431A
公开(公告)日:1987-06-02
申请号:US572195
申请日:1984-01-19
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D241/08 , C07D499/00 , C07D499/44 , C07D501/20 , C07D501/57 , A61K31/43 , A61K31/545 , C07D499/46 , C07D501/00 , C07D501/18
CPC分类号: C07D241/08 , C07D499/00
摘要: A compound having the partial structure (A): ##STR1## wherein n is 1 or 2.
摘要翻译: 具有部分结构(A)的化合物:其中n为1或2。
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公开(公告)号:US4661480A
公开(公告)日:1987-04-28
申请号:US572186
申请日:1984-01-19
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D505/00 , A61K31/535 , C07D498/04
CPC分类号: C07D505/00
摘要: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## R is phenyl, substituted phenyl, C.sub.3-6 cycloalkyl cyclohexenyl, cyclohexadienyl, or a 5- or 6-membered heterocyclic ring containing up to three hetero-atoms slected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen, substituted amino or C.sub.1-6 alkoxy; Q represents acetoxy, carbamoyloxy, heterocyclylthio group, or a nitrogen containing heterocyclic group bonded via nitrogen; R.sup.1 is hydrogen or a C.sub.1-6 alkyl group and R.sup.2 is an optionally substituted 5- or 6-membered heterocyclic group containing one or two heteroatoms; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form an optionally substituted five- or six-membered heterocyclic group containing one or two nitrogen heteroatoms; a process for the preparation of such compounds and pharmaceutical compositions comprising them.
摘要翻译: 式(I)化合物或其药学上可接受的盐或体内可水解的酯:(I)R是苯基,取代的苯基,C 3-6环烷基环己烯基,环己二烯基或5-或6-元杂环 含有多至三个选自氧,硫或氮的杂原子,任选被羟基,氨基,卤素,取代的氨基或C 1-6烷氧基取代; Q表示通过氮键合的乙酰氧基,氨基甲酰氧基,杂环硫基或含氮杂环基; R 1是氢或C 1-6烷基,R 2是任选取代的含有一个或两个杂原子的5或6元杂环基; 或R 1和R 2与它们所连接的氮原子一起形成含有一个或两个氮杂原子的任选取代的五元或六元杂环基; 制备这些化合物的方法和包含它们的药物组合物。
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公开(公告)号:US4555363A
公开(公告)日:1985-11-26
申请号:US572196
申请日:1984-01-19
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D463/00 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/44 , C07D501/04 , C07D501/57 , C07D505/00 , C07D501/02
CPC分类号: C07D499/00 , C07D463/06 , C07D505/00
摘要: A process for the preparation of a .beta.-lactam having the partial structure (I): ##STR1## wherein R.sub.1 is an acyl group, which process comprises treating an imine having the partial structure (II): ##STR2## with a nucleophilic derivative of formamide.
摘要翻译: 制备具有部分结构(I)的β-内酰胺的方法:其中R1是酰基,该方法包括处理具有部分结构(II)的亚胺:(II) )与甲酰胺的亲核衍生物。
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公开(公告)号:US4539149A
公开(公告)日:1985-09-03
申请号:US401266
申请日:1982-07-23
申请人: Peter H. Milner
发明人: Peter H. Milner
IPC分类号: C07D501/14 , C07D241/08 , C07D311/12 , C07D463/00 , C07D499/00 , C07D499/21 , C07D499/44 , C07D501/57 , C07D505/00 , C07D499/50 , C07D499/54 , C07D501/24
CPC分类号: C07D241/08 , C07D311/12 , C07D463/22 , C07D499/00 , C07D505/00
摘要: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.
摘要翻译: β-内酰胺抗生素在与β-内酰胺环的羰基相邻的碳原子上具有α-甲酰氨基取代基,特别是具有部分结构的双环化合物:进一步公开了制备化合物的中间体和方法 。
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