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150 条记录 (耗时 0.052 秒)

    Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
    84.
    发明授权
    Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
    噻唑衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US4735957A

    公开(公告)日：1988-04-05

    申请号：US932097

    申请日：1986-11-18

    申请人： Takao Takaya ,  Hisashi Takasugi

    发明人： Takao Takaya ,  Hisashi Takasugi

    IPC分类号： C07D213/55 ,  C07D277/24 ,  C07D277/32 ,  C07D277/34 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/44 ,  C07D277/56 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  A61K31/44

    CPC分类号： C07D417/04 ,  C07D213/55 ,  C07D277/24 ,  C07D277/34 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/44 ,  C07D277/56 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

    摘要： New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.3 are lower alkyl then n is an integer of 1 and R.sup.2 is lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy, and when R.sup.1 is lower alkyl and R.sup.3 is halo(lower)alkyl then n is an integer of 1, and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and pharmaceutically acceptable salts thereof are useful as cardiotonic agents and anti-ulcer agents.

    Process for the preparation of 3-phosphoniummethyl-3-cephem compounds
    85.
    发明授权
    Process for the preparation of 3-phosphoniummethyl-3-cephem compounds 失效
    3-鏻甲基-3-头孢烯化合物的制备方法

    公开(公告)号：US4705851A

    公开(公告)日：1987-11-10

    申请号：US655458

    申请日：1984-09-28

    申请人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanada ,  Kohji Kawabata

    发明人： Takao Takaya ,  Hisashi Takasugi ,  Takashi Masugi ,  Hideaki Yamanada ,  Kohji Kawabata

    IPC分类号： C07D501/22 ,  C07D501/00 ,  C07F9/6547 ,  C07F9/6561 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： The invention relates to a process for the preparation of 3-phosphoniummethyl-3-cephem compounds of the formula: ##STR1## wherein R.sub.3 is aryl, or a salt thereof, which is characterized by reacting one equimolar amount of a 3-hydroxymethyl-3-cephem compound of the formula: ##STR2## or a salt thereof, with two or a little over two equimolar amount of triarylphosphine and one or a little over one equimolar amount of iodine, said prepared compounds being useful as intermediates for manufacturing 3-vinyl-3-cephem compounds possessing potent antimicrobial activities.

    摘要翻译： 本发明涉及一种制备下式的3-鏻甲基-3-头孢烯化合物的方法：其中R 3是芳基或其盐，其特征在于使一等摩尔量的3-羟甲基-3 - 下式化合物：其中两个或两个以上等摩尔量的三芳基膦和一个或稍多于一个等摩尔量的碘，所述制备的化合物可用作制备3-乙烯基的中间体 -3-头孢烯化合物具有很强的抗菌活性。

    Imidazo-heterocyclic compounds and pharmaceutical composition comprising the same
    87.
    发明授权
    Imidazo-heterocyclic compounds and pharmaceutical composition comprising the same 失效
    咪唑并杂环化合物及其组合物

    公开(公告)号：US4621084A

    公开(公告)日：1986-11-04

    申请号：US583609

    申请日：1984-02-27

    申请人： Takao Takaya ,  Hisashi Takasugi

    发明人： Takao Takaya ,  Hisashi Takasugi

    IPC分类号： A61K31/435 ,  A61K31/495 ,  A61K31/505 ,  A61P1/04 ,  A61P9/04 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D279/10 ,  C07D471/04 ,  C07D487/04 ,  A61K31/41 ,  C07D471/02 ,  C07D491/02

    CPC分类号： C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D279/10 ,  C07D471/04 ,  C07D487/04

    摘要： New imidazo-heterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or halogen,R.sup.2 is hydrogen, lower alkyl, halogen, aminomethyl optionally substituted with lower alkyl, or piperazin-1-yl-methyl optionally substituted with lower alkyl,R.sup.3 is a partially suturated heterocyclic group selected from benzothiazolinyl, benzoxazolinyl, benzimidazolinyl, 3,4-dihydro-2H-1,4-benzothiazinyl, 3,4-dihydro-2H-1,4-benzoxazinyl and 1,2,3,4-tetrahydroquinoxalinyl, which is substituted with oxo, thioxo, imino or lower alkylimino, and which may be substituted with lower alkyl optionally substituted with lower alkanoyloxy, lower alkoxycarbonyl, pyridyl or lower alkylamino; or an unsaturated heterocyclic group selected from benzoxazolyl and benzimidazolyl, which may be substituted with lower alkyl or pyridyl(lower)alkylthio, andY is .dbd.N-- or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, hydroxy, lower alkyl, lower alkoxy or ar(lower)alkoxy,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and pharmaceutically acceptable salts thereof are useful as cardiotonic agents and untiulcer agents.

    摘要翻译： 下式的新的咪唑并杂环化合物：其中R 1是氢，低级烷基或卤素，R 2是氢，低级烷基，卤素，任选被低级烷基取代的氨基甲基或任选被低级烷基取代的哌嗪-1-基 - 甲基 烷基，R3是选自苯并噻唑啉基，苯并恶唑啉基，苯并咪唑啉基，3,4-二氢-2H-1,4-苯并噻嗪基，3,4-二氢-2H-1,4-苯并恶嗪基和1,2,3 可被氧代，硫代，亚氨基或低级烷基亚氨基取代的4-四氢喹喔啉基，其可以被任选被低级烷酰氧基，低级烷氧基羰基，吡啶基或低级烷基氨基取代的低级烷基取代; 或选自苯并恶唑基和苯并咪唑基的不饱和杂环基，其可以被低级烷基或吡啶基（低级）烷硫基取代，Y为= N-或其中R 4为氢，羟基，低级 烷基，低级烷氧基或芳（低级）烷氧基及其药学上可接受的盐，及其制备方法和包含其的药物组合物。 这些衍生物及其药学上可接受的盐可用作强心剂和脱臼剂。

    Syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and processes for the preparation thereof
    89.
    发明授权
    Syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and processes for the preparation thereof 失效
    3,7-二取代-3-头孢烯-4-羧酸化合物的同分异构体及其制备方法

    公开(公告)号：US4544653A

    公开(公告)日：1985-10-01

    申请号：US883395

    申请日：1978-03-06

    申请人： Takao Takaya ,  Takashi Masugi ,  Hisashi Takasugi ,  Hiromu Kochi

    发明人： Takao Takaya ,  Takashi Masugi ,  Hisashi Takasugi ,  Hiromu Kochi

    IPC分类号： C07D277/20 ,  C07D277/38 ,  C07D277/46 ,  C07D277/48 ,  C07D333/16 ,  C07D501/32 ,  C07D501/34 ,  C07D501/36 ,  A61K31/545 ,  C07D501/24

    CPC分类号： C07D277/20 ,  C07D277/38 ,  C07D277/46 ,  C07D277/48 ,  C07D277/587 ,  C07D333/16 ,  C07D501/18

    摘要： The present invention relates to a new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antibacterial activities and to processes for the 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 beings and animals. New cephems disclosed herein are ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is lower alkyl, R.sup.3 is carboxy, R.sup.4 is carbamoyloxy methyl which may be substituted with a trihalo- (lower) alkanoyl; and R.sup.7 is amino, lower alkanoylamino or halo (lower)alkanoylamino.

    摘要翻译： 本发明涉及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的新的顺式异构体。 更具体地，本发明涉及具有抗菌活性的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的新的顺式异构体及其制备方法，涉及包含其的药物组合物， 以及在治疗人和动物中的感染性疾病方面使用相同治疗方法。 本文公开的新头皮是其中R 1为低级烷基，R 3为羧基，R 4为可被三卤代（低级）烷酰基取代的氨基甲酰氧基甲基的化合物。 并且R 7是氨基，低级烷酰基氨基或卤代（低级）烷酰基氨基。