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14 条记录 (耗时 0.024 秒)

    Thiazolylacetamido compounds
    6.
    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
    7.
    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。

    Thiazolylacetamido compounds
    9.
    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。

    7.beta.-Phosphoramido-7.alpha.-methoxycephalosporanic acid derivatives
    10.
    发明授权
    7.beta.-Phosphoramido-7.alpha.-methoxycephalosporanic acid derivatives 失效
    7 {62-磷酰胺基-7 {60-甲氧基头孢烷酸衍生物

    公开(公告)号：US4145540A

    公开(公告)日：1979-03-20

    申请号：US708755

    申请日：1976-07-26

    申请人： Michihiko Ochiai ,  Akira Morimoto ,  Osami Aki ,  Taiiti Okada

    发明人： Michihiko Ochiai ,  Akira Morimoto ,  Osami Aki ,  Taiiti Okada

    IPC分类号： C07D499/21 ,  C07D499/00 ,  C07D499/04 ,  C07D499/46 ,  C07D499/60 ,  C07D499/62 ,  C07D499/64 ,  C07D499/72 ,  C07D501/00 ,  C07D501/04 ,  C07D501/18 ,  C07D501/57 ,  C07D501/60 ,  C07F9/6561

    CPC分类号： C07F9/65613 ,  C07D499/00 ,  C07F9/65611

    摘要： Cephem and penam compounds having a partial structure of formula (II): ##STR1## wherein R.sup.1 and R.sup.2, respectively, represent a hydrocarbon group which is attached to P, either directly or through an oxygen atom, and which may optionally be substituted, and R.sup.3 is a hydrocarbon residue, are useful as intermediates for synthetic penicillins and cephalosporins, which in turn are useful as antibiotics or intermediates for some other synthetic penicillins and cephalosporins having antibiotic activity. To the 6- or 7-amino group of these penam or cephem compounds an objective acyl group can be introduced to give 6- or 7-acyl amino compound in a good yield, without isomerization of 6.alpha.-or 7.alpha.-substituent OR.sup.3 of the penam or cephem compounds.

    摘要翻译： 具有式（II）的部分结构的头孢烯和缓释化合物：其中R 1和R 2分别表示直接或通过氧原子与P连接的烃基，并且其可任选地为 并且R3是烃残基，可用作合成青霉素和头孢菌素的中间体，其又可用作一些其它合成青霉素和具有抗生素活性的头孢菌素的抗生素或中间体。 对于这些Penam或头孢烯化合物的6-或7-氨基，可以引入目的酰基以获得6-或7-酰基氨基化合物的良好产率，而不使6α-或7α-取代基OR3异构化 半胱氨酸或头孢烯化合物。