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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。

    Aminothiazole derivatives
    6.
    发明授权
    Aminothiazole derivatives 失效
    氨基噻唑衍生物

    公开(公告)号：US4008246A

    公开(公告)日：1977-02-15

    申请号：US603237

    申请日：1975-08-08

    申请人： Michihiko Ochiai ,  Akira Morimoto ,  Yoshihiro Matsushita ,  Taiiti Okada

    发明人： Michihiko Ochiai ,  Akira Morimoto ,  Yoshihiro Matsushita ,  Taiiti Okada

    IPC分类号： C07D277/20 ,  C07D20060101 ,  C07D277/46 ,  C07D277/48

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 stands for a halogenoethoxycarbonylamino and R.sup.2 stands for hydrogen or a halogen, is an important intermediate for producing a cephalosporin derivative of the formula: ##STR2## wherein R.sup.3 stands for methyl, acetoxymethyl, carbamoyloxymethyl, an alkoxymethyl, an alkylthiomethyl, 2-carboxy-1-ethenyl, or a heterocyclic thiomethyl, R.sup.5 stands for hydrogen or methoxy and R.sup.2 has the same meaning as defined before, which is active against various pathogenic microorganisms even at a low concentration.

    摘要翻译： 下式的化合物，其中R1代表卤代乙氧基羰基氨基，R2代表氢或卤素，是产生下式的头孢菌素衍生物的重要中间体：其中R3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，R5代表氢或甲氧基，R2表示与上述相同的含义，即使在低浓度下也能对各种病原微生物有活性。

    1-carboxymethoxy acetidinones and their production
    8.
    发明授权
    1-carboxymethoxy acetidinones and their production 失效
    1-羧甲氧基乙酸丁酯及其制备

    公开(公告)号：US4794108A

    公开(公告)日：1988-12-27

    申请号：US651033

    申请日：1984-09-14

    申请人： Shoji Kishimoto ,  Michiyuki Sendai ,  Michihiko Ochiai

    发明人： Shoji Kishimoto ,  Michiyuki Sendai ,  Michihiko Ochiai

    IPC分类号： C07D205/085 ,  C07D209/48 ,  C07D403/12 ,  C07D417/12 ,  A61K31/425 ,  C07D205/08 ,  C07D303/48

    CPC分类号： C07D209/48 ,  C07D205/085 ,  C07D403/12 ,  C07D417/12 ,  Y02P20/55

    摘要： A 2-azetidinone derivative having a group of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a substituent at the 1-position and an amino group, at the 3-position, which may be acylated or protected, its salt or ester, and methods of producing the same, (1) a method comprising subjecting a 2-azetidinone derivative having a group of the formula ##STR2## wherein the symbols are as defined above at the 1-position and an amino group at the 3-position, its salt or ester to an acylation or protective-group introduction reaction, and (2) a method comprising reacting a 2-azetidinone derivative having a hydroxy group at the 1-position and an amino group, at the 3-position, which may be acylated or protected, or its salt with a compound of the formula ##STR3## wherein W is a halogen atom; other symbols are as defined above, its salt or ester. The above objective compounds are utilizable as excellent antimicrobial agents or as valuable intermediates for the synthesis of the same.

    摘要翻译： 具有式“IMAGE”的基团的2-氮杂环丁酮衍生物，其中R 1和R 2相同或不同，并且各自表示可在1位具有取代基的氨基和氢原子的烷基，芳基或芳基烷基， 在可以被酰化或保护的3-位上，其盐或酯及其制备方法，（1）一种方法，包括使具有式“IMAGE”的基团的2-氮杂环丁酮衍生物，其中符号是 如上所述在1-位和3-位上的氨基，其盐或酯进行酰化或保护基导入反应，和（2）包括使具有羟基的2-氮杂环丁酮衍生物在 可以被酰化或保护的3-位上的3-位和氨基，或其与下式的化合物的盐：其中W是卤素原子; 其他符号如上所定义，其盐或酯。 上述目标化合物可用作优异的抗微生物剂或作为其合成的有价值的中间体。