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公开(公告)号：US4599426A
公开(公告)日：1986-07-08
申请号：US531669
申请日：1983-09-13
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/12 , C07D501/24 , C07D501/36 , C07D521/00 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561
CPC分类号： C07D209/48 , C07D213/75 , C07D277/46 , C07D277/587 , C07F9/4006 , C07F9/5537 , C07F9/65613 , Y02P20/55
摘要： The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5 or --HNCO--R.sup.5,R.sup.5 is aryl or heterocyclic, either of which may be substituted, andA is lower alkylene, or a salt thereof.
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2.发明授权Amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid 失效氨基或酰氨基 - 噻唑基，取代的氧亚氨基二取代的乙酸
公开(公告)号：US4506076A
公开(公告)日：1985-03-19
申请号：US258661
申请日：1981-04-29
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/12 , C07D501/24 , C07D501/36 , C07D521/00 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561 , C07D277/30
CPC分类号： C07D209/48 , C07D213/75 , C07D277/46 , C07D277/587 , C07F9/4006 , C07F9/5537 , C07F9/65613 , Y02P20/55
摘要： The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5, --NHCO--R.sup.5, or ##STR2## R.sup.5 is aryl or heterocyclic, either of which may be substituted, R.sup.6 is hydrogen or lower alkyl, andA is lower alkylene, or a salt thereof.
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公开(公告)号：US4782158A
公开(公告)日：1988-11-01
申请号：US883165
申请日：1986-07-08
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/12 , C07D501/24 , C07D501/36 , C07D521/00 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561
CPC分类号： C07D209/48 , C07D213/75 , C07D277/46 , C07D277/587 , C07F9/4006 , C07F9/5537 , C07F9/65613 , Y02P20/55
摘要： The present invention involves certain thiazol-4-yl-acetic acid compounds which are valuable intermediates for the preparation of cephem antibiotics. Said intermediates have the following structure: ##STR1## wherein R.sup.1 is an amino or a protected amino group; R.sup.2 is a group of the formula 13 CONH--R.sup.5 or --NHCO--R.sup.5 wherein R.sup.5 is pyridyl, thiazolyl or an isoxazolyl ring having lower alkyl and halogen substituted phenyl substituents, and A is lower alkylene, or a non-toxic salt thereof.
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4.发明授权3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutical antibacterial compositions containing them 失效3,7-二取代-3-头孢烯-4-羧酸化合物和含有它们的药物抗菌组合物
公开(公告)号：US4288435A
公开(公告)日：1981-09-08
申请号：US56504
申请日：1979-07-11
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D213/75 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48 , C07D417/12 , C07D501/24 , C07D501/36 , C07D521/00 , C07F9/40 , C07F9/553 , C07F9/6539 , C07F9/6561 , C07D501/56
CPC分类号： C07D209/48 , C07D213/75 , C07D277/46 , C07D277/587 , C07F9/4006 , C07F9/5537 , C07F9/65613 , Y02P20/55
摘要： The present invention relates to new 3,7 disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in human being and animals.
摘要翻译： 本发明涉及新的3,7二取代的3-头孢烯-4-羧酸化合物及其药学上可接受的盐。 更具体地说，本发明涉及具有抗微生物活性的新的3,7-二取代-3-头孢烯-4-羧酸化合物及其药学上可接受的盐及其制备方法，涉及包含其的药物组合物和 在治疗人和动物中的感染性疾病方面使用相同的治疗方法。
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5.发明授权Amino or acylamino-substituted pyrimidinyl cephalosporanic acid derivatives and pharmaceutical compositions thereof 失效氨基或酰氨基取代的嘧啶基头孢菌酸衍生物及其药物组合物
公开(公告)号：US4267176A
公开(公告)日：1981-05-12
申请号：US32778
申请日：1979-04-24
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10 , C07D501/56
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： The invention relates to novel amino or acylamino-substituted pyrimidinyl cephalosporanic acid derivatives and pharmaceutically acceptable salts thereof, of antibacterial activity, to processes for the preparation thereof, and to pharmaceutical compositions comprising the novel cephalosporanic acid derivatives.
摘要翻译： 本发明涉及具有抗菌活性的新型氨基或酰氨基取代的嘧啶基头孢菌酸衍生物及其药学上可接受的盐，其制备方法以及包含新型头孢烷酸衍生物的药物组合物。
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6.发明授权
公开(公告)号：US4395411A
公开(公告)日：1983-07-26
申请号：US213684
申请日：1980-12-05
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： This invention relates to novel 7-pyrimidinyl and pyridinyl acetamido cephem derivatives of high antibacterial activity.
摘要翻译： 本发明涉及高抗菌活性的新型7-嘧啶基和吡啶基乙酰氨基头孢烯衍生物。
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公开(公告)号：US4596869A
公开(公告)日：1986-06-24
申请号：US777867
申请日：1985-09-19
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： C07D213/55 , A61K31/545 , A61K31/546 , A61P31/04 , C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/46 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/57 , C07D501/59 , C07D519/06 , C07F7/10 , C07D213/53 , C07D213/60 , C07D239/02
CPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D239/42 , C07D239/47 , C07F7/10
摘要： A novel compound, useful as an intermediate in the production of compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sub.a.sup.1 is hydrogen, amino or a protected amino group,R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or arylthio,R.sup.14 is carboxy or a protected carboxy group,X is lower alkylene or a group of the formula: ##STR2## in which R.sup.6 is hydrogen or an organic residue which may have suitable substituent(s), andZ is N or CH,or a salt thereof.
摘要翻译： 一种新型化合物，其用作生产高抗微生物活性化合物的中间体，其具有下式：其中Ra1为氢，氨基或被保护的氨基，Rb1和Rc1各自为氢，卤素，低级烷氧基或芳硫基 R 14为羧基或被保护的羧基，X为低级亚烷基或下式基团：其中R 6为氢或可具有合适取代基的有机残基，Z为N或CH，或 其盐。
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公开(公告)号：US4407798A
公开(公告)日：1983-10-04
申请号：US296301
申请日：1981-08-26
申请人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
发明人： Takashi Kamiya , Tsutomu Teraji , Yoshiharu Nakai , Kazuo Sakane , Jiro Goto
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/74 , C07D213/75 , C07D239/42 , C07D501/46 , C07D501/58
CPC分类号： C07D213/75 , C07D239/42
摘要： This invention relates to novel compounds having antimicrobial activity of the formula ##STR1## in which R.sup.1 is amino or a protected amino group,R.sup.2 is cyclo(lower)alkyl, cyclo(lower)alkenyl, lower alkyl, lower alkynyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or lower alkylthio(lower)alkyl, andY is hydrogen, amino or a protected amino group, and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明涉及具有式（IMAGE）的抗微生物活性的新化合物，其中R1是氨基或被保护的氨基，R2是环（低级）烷基，环（低级）烯基，低级烷基，低级炔基，羧基（低级） 烷基，保护的羧基（低级）烷基或低级烷硫基（低级）烷基，Y为氢，氨基或被保护的氨基，及其药学上可接受的盐。
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公开(公告)号：US4440766A
公开(公告)日：1984-04-03
申请号：US291777
申请日：1981-08-10
申请人： Takashi Kamiya , Kunihiko Tanaka , Yoshiharu Nakai , Kazuo Sakane
发明人： Takashi Kamiya , Kunihiko Tanaka , Yoshiharu Nakai , Kazuo Sakane
IPC分类号： A61K31/545 , C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/52 , C07D501/20 , C07D501/22
CPC分类号： C07D277/20 , A61K31/545 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/587
摘要： 3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutical salts thereof having antibacterial properties in the treatment of animals and processes for preparing the compounds.
摘要翻译： 3,7-二取代-3-头孢烯-4-羧酸化合物及其在治疗动物中具有抗菌性质的药物盐及其制备方法。
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10.发明授权3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and processes for preparation thereof 失效3,7-二取代-3-头孢烯-4-羧酸化合物及其制备方法
公开(公告)号：US4560765A
公开(公告)日：1985-12-24
申请号：US571700
申请日：1984-01-18
申请人： Takashi Kamiya , Kunihiko Tanaka , Yoshiharu Nakai , Kazuo Sakane
发明人： Takashi Kamiya , Kunihiko Tanaka , Yoshiharu Nakai , Kazuo Sakane
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/44 , C07D277/46 , C07D277/48 , C07D277/52 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36
CPC分类号： C07D277/20 , A61K31/545 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/52 , C07D277/587
摘要： Antibiotic cephalosporin compounds, method of making and pharmaceutical composition thereof represented by the general formula ##STR1## wherein R.sup.1 is amino, lower alkylamino, a protected amino, a protected lower alkylamino, hydroxy or lower alkoxy,R.sup.2 is hydrogen, acyloxy, pyridium or a heterocyclicthio group which may have suitable substituent(s),R.sup.3 is carboxy or its derivative,A is carbonyl, hydroxy(lower)alkylene or a protected hydroxy(lower)alkylene andR.sup.4 is hydrogen or halogen, orR.sup.2 and R.sup.3 are linked together to represent a group of the formula --COO--, this divisional application being directed to intermediate compounds of the formula: ##STR2##
摘要翻译： 抗生素头孢菌素化合物，其制备方法及其药物组合物，其通式为其中R 1为氨基，低级烷基氨基，被保护的氨基，保护的低级烷基氨基，羟基或低级烷氧基，R2为氢，酰氧基，吡啶酮或 可以具有合适取代基的杂环硫基，R 3是羧基或其衍生物，A是羰基，羟基（低级）亚烷基或被保护的羟基（低级）亚烷基，R 4是氢或卤素，或者R 2和R 3连接在一起 表示式-COO-的一组，该分案申请涉及下式的中间体化合物：
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