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    Thiazolylacetamido compounds
    5.
    发明授权
    Thiazolylacetamido compounds 失效
    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。

    Thiazolylacetamido compounds
    7.
    发明授权
    Thiazolylacetamido compounds 失效
    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。

    7-Methoxycephalosporin derivatives
    8.
    发明授权
    7-Methoxycephalosporin derivatives 失效
    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。