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1. 发明授权

US5583216A Methods for the manufacture of cephems 失效
标题翻译：方法制造流行病
公开(公告)号：US5583216A
公开(公告)日：1996-12-10
申请号：US462492
申请日：1990-01-08
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48 , C07D499/46 , C07D499/58 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/06 , C07D501/56
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/587
摘要： Provided is a process for preparing a cephem compound of the formula: ##STR1## wherein R.sup.3 is hydrogen or methoxy, R.sup.4 is hydrogen or a residue of a nucleophilic compound, R.sup.5 is hydroxyl or a protected hydroxyl, and R.sup.8 is hydrogen or halogen, or a pharmaceutically acceptable salt or ester thereof, which comprises introducing an acyl group of the formula: ##STR2## wherein R.sup.5 and R.sup.8 are as defined above into the amino group of the molecule of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are as defined above or a salt or ester thereof.
摘要翻译：提供了制备下式的头孢烯化合物的方法：其中R 3是氢或甲氧基，R 4是氢或亲核化合物的残基，R 5是羟基或保护的羟基，R 8是氢或卤素，或其药学上可接受的盐或酯，其包括将下式的酰基引入下式的分子的氨基中：其中R 5和R 8如上所定义，其中R 3和R 4如所定义或其盐或酯。

2. 发明授权

US4355160A Thiazolylacetamido cephalosporin type compounds 失效
标题翻译：噻唑基乙酰胺基头孢菌素型化合物
公开(公告)号：US4355160A
公开(公告)日：1982-10-19
申请号：US240466
申请日：1981-03-04
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D501/36 , A61K31/545
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48
摘要： The present invention is directed to a compound having antibacterial activity of the formula ##STR1## wherein R.sup.1 represents amino, protected amino, hydroxy or protected hydroxy;R.sup.4 represents heterocyclic thio wherein heterocyclic is a 5 to 6 membered hetero ring containing 1 to 4 hetero atoms from the group of oxygen, sulfur and nitrogen; andR.sup.5 is hydroxy or protected hydroxy, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有下式的抗菌活性的化合物：其中R 1表示氨基，被保护的氨基，羟基或被保护的羟基; R4表示杂环硫基，其中杂环是含有1至4个来自氧，硫和氮的杂原子的5至6元杂环; R5是羟基或被保护的羟基，或其药学上可接受的盐。

3. 发明授权

US4205180A .alpha.-Alkoxyimino-.beta.-oxo-.gamma.-Bromobutyric acid 失效
标题翻译： α-烷氧基亚氨基-β-氧代-γ-溴丁酸
公开(公告)号：US4205180A
公开(公告)日：1980-05-27
申请号：US870932
申请日：1978-01-18
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48 , C07D499/46 , C07D499/58 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07C119/12
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/587
摘要： Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.

4. 发明授权

US4098888A Thiazolylacetamido cephalosporin type compounds 失效
标题翻译：三唑乙酰胺CEPHALOSPORIN型化合物
公开(公告)号：US4098888A
公开(公告)日：1978-07-04
申请号：US642356
申请日：1975-12-19
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48 , C07D499/46 , C07D499/58 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , A61K31/545
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/587
摘要： Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.
摘要翻译：新型头孢烯化合物的配方; 其中R 1表示可被保护的氨基或羟基，R 2表示氨基或羟基或可转化成这些基团的基团，R 3表示氢或甲氧基或可转化为甲氧基的基团，R 4表示氢或亲核化合物和R8代表氢或卤素或其药学上可接受的盐或酯，对各种微生物（包括革兰氏阳性细菌以及革兰氏阴性细菌）尤其是口服给药具有很强的抗生素特性，并且可以是用作包括人在内的动物的各种细菌感染的治疗剂。

5. 发明授权

US4514565A Thiazolylacetamido cephalosphorin compounds 失效
标题翻译：噻唑基乙酰氨基头孢菌素化合物
公开(公告)号：US4514565A
公开(公告)日：1985-04-30
申请号：US525663
申请日：1983-06-24
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48 , C07D499/46 , C07D499/58 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/38 , A61K31/545
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/587
摘要： 3-Tertiary ammoniomethyl-7-beta-[alpha-(hydroxy or protected hydroxy)imino-alpha-(2-aminothiazol-4-yl)acetamido]-3-cephem-4-carboxylic acid, pharmaceutically acceptable salt or 4-carboxy ester is provided which is a broad spectrum antibiotic.
摘要翻译： 3-叔氨基甲基-7-β-（α-羟基或被保护的羟基）亚氨基-α-（2-氨基噻唑-4-基）乙酰氨基] -3-头孢烯-4-羧酸，其药学上可接受的盐或4-羧基酯是广谱抗生素。

6. 发明授权

US4203899A Thiazolylacetamido compounds 失效
标题翻译：噻唑基乙酰氨基化合物
公开(公告)号：US4203899A
公开(公告)日：1980-05-20
申请号：US897239
申请日：1978-04-17
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/34 , C07D277/38 , C07D277/48 , A61K31/545 , C07D277/44
CPC分类号： C07D277/587 , C07D277/48
摘要： Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.Also disclosed are novel thiazolylacetic acid compounds of the formula: ##STR2## wherein R.sup.1 represents amino, protected amino, hydroxyl or protected hydroxyl, R.sup.2 represents amino, protected amino, hydroxyl, protected hydroxyl or the group ##STR3## represents a group of the formula ##STR4## wherein R.sup.5 represents hydroxyl or lower alkoxy and R.sup.8 represents hydrogen or a halogen, or a salt, an ester or a reactive derivative thereof, and to processed for preparing these compounds. These latter compounds are useful as intermediates in the preparation of the novel cephem compounds.
摘要翻译：新型头孢烯化合物的配方; 其中R 1表示可被保护的氨基或羟基，R 2表示氨基或羟基或可转化成这些基团的基团，R 3表示氢或甲氧基或可转化为甲氧基的基团，R 4表示氢或亲核化合物和R8代表氢或卤素或其药学上可接受的盐或酯，对各种微生物（包括革兰氏阳性细菌以及革兰氏阴性细菌）尤其是口服给药具有很强的抗生素特性，并且可以是用作包括人在内的动物的各种细菌感染的治疗剂。还公开了下式的新的噻唑基乙酸化合物：其中R 1表示氨基，被保护的氨基，羟基或被保护的羟基，R 2表示氨基，被保护的氨基，羟基，被保护的羟基或基团表示基团其中R5表示羟基或低级烷氧基，R8表示氢或卤素，或其盐，酯或其活性衍生物，并用于制备这些化合物。这些后一种化合物可用作制备新型头孢烯化合物的中间体。

7. 发明授权

US4668783A Thiazolylacetamido cephalosporin compounds 失效
标题翻译：噻唑基乙酰氨基头孢菌素化合物
公开(公告)号：US4668783A
公开(公告)日：1987-05-26
申请号：US824578
申请日：1986-01-23
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/48 , C07D501/20 , A61K31/545
CPC分类号： C07D277/20 , C07D277/48
摘要： Novel cephem compounds of the formula: ##STR1## wherein R.sup.4 is a residue of a nucleophilic compound selected from hydroxyl, mercapto, cyano, azido, amino, carbamoyloxy, carbamoylthio and thiocarbamoyloxy, said group being unsubstituted or substituted by alkyl of up to three carbons, and R.sup.5 is hydroxyl or lower alkoxy, or a pharmaceutically acceptable ester thereof, have strong antibiotic properties against a wide variety of microorganisms.
摘要翻译：新的头孢烯化合物，其分子式为：其中R 4是选自羟基，巯基，氰基，叠氮基，氨基，氨基甲酰氧基，氨基甲酰硫基和硫代氨基甲酰氧基的亲核化合物的残基，所述基团是未取代的或被至多三个碳的烷基取代 R5为羟基或低级烷氧基，或其药学上可接受的酯对各种微生物具有较强的抗生素性能。

8. 发明授权

US4298606A Thiazolylacetamido compounds 失效
标题翻译：噻唑基乙酰氨基化合物
公开(公告)号：US4298606A
公开(公告)日：1981-11-03
申请号：US71032
申请日：1979-08-28
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/48 , C07D501/20
CPC分类号： C07D277/20 , C07D277/48 , C07D277/587
摘要： Novel cephem compounds of the formula; ##STR1## wherein R.sup.1 represents amino or hydroxyl group which may be protected, R.sup.2 represents amino or hydroxyl group or a group convertible into these groups, R.sup.3 represents hydrogen or methoxy group or a group convertible into methoxy group, R.sup.4 represents hydrogen or a residue of a nucleophilic compound and R.sup.8 represents hydrogen or a halogen, or a pharmaceutically acceptable salt or ester thereof, have strong antibiotic properties against a wide variety of microorganisms including gram-positive bacteria as well as gram-negative ones, especially by oral administration and can be used as therapeutic agent for various bacterial infections of animals including human beings.
摘要翻译：新型头孢烯化合物的配方; 其中R 1表示可被保护的氨基或羟基，R 2表示氨基或羟基或可转化成这些基团的基团，R 3表示氢或甲氧基或可转化为甲氧基的基团，R 4表示氢或亲核化合物和R8代表氢或卤素或其药学上可接受的盐或酯，对各种微生物（包括革兰氏阳性细菌以及革兰氏阴性细菌）尤其是口服给药具有很强的抗生素特性，并且可以是用作包括人在内的动物的各种细菌感染的治疗剂。

9. 发明授权

US4182868A 7-Methoxycephalosporin derivatives 失效
标题翻译： 7-甲氧基头孢菌素衍生物
公开(公告)号：US4182868A
公开(公告)日：1980-01-08
申请号：US794818
申请日：1977-05-06
申请人： Michihiko Ochiai , Akira Morimoto , Yoshihiro Matsushita , Osami Aki , Taiiti Okada , Kenji Kawakita
发明人： Michihiko Ochiai , Akira Morimoto , Yoshihiro Matsushita , Osami Aki , Taiiti Okada , Kenji Kawakita
IPC分类号： C07D501/36 , C07D501/57
CPC分类号： C07D501/57
摘要： A compound of the formula: ##STR1## wherein R.sup.2 is hydrogen or a halogen and R.sup.3 stands for methyl, acetoxymethyl, carbamoyloxymethyl, an alkoxymethyl, an alkylthiomethyl, 2-carboxy-1-ethenyl, or a heterocyclic thiomethyl, or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against Gram-negative bacteria including Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescense as well as Gram-positive ones including antibiotic resistant strains. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.
摘要翻译：下式的化合物：其中R 2是氢或卤素，R 3代表甲基，乙酰氧基甲基，氨基甲酰氧基甲基，烷氧基甲基，烷硫基甲基，2-羧基-1-乙烯基或杂环硫甲基或其药学上可接受的盐被发现具有广泛的抗菌谱，特别是对革兰氏阴性菌有效，包括大肠杆菌，普通变形杆菌，铜绿假单胞菌，粘质沙雷氏菌以及包括抗生素抗性菌株在内的革兰氏阳性细菌。因此，这些化合物可用于治疗目的的抗微生物剂。

10. 发明授权

US4973684A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4973684A
公开(公告)日：1990-11-27
申请号：US203410
申请日：1988-06-07
申请人： Michihiko Ochiai , Taiiti Okada , Osamu Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osamu Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48 , C07D499/46 , C07D499/58 , C07D501/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/587
摘要： Broad spectrum antibiotics are provided which are compounds of the formula: ##STR1## wherein R.sup.4 is a residue of a nucleophilic compound and R.sup.5 is hydroxyl or protected hydroxyl; or a pharmaceutically acceptable salt or ester thereof.

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