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    Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same
    5.
    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：US5371097A

    公开(公告)日：1994-12-06

    申请号：US80051

    申请日：1993-06-22

    Applicant: Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

    Inventor： Hisashi Takasugi ,  Yousuke Katsura ,  Tetsuo Tomishi ,  Yoshikazu Inoue

    IPC: C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P1/04 ,  A61P43/00 ,  C07D277/48 ,  C07D417/04 ,  C07D417/14 ,  C07D521/00

    CPC classification number: C07D417/04 ,  C07D277/48 ,  C07D417/14

    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is amino, acylamino, cyclo(lower)alkenylamino having amino and oxo, imido, triazolylamino, benzoisothiazolylamino, wherein each of said heterocyclicamino groups may be substituted by one or more substituent(s) selected from the group consisting of lower alkyl, amino and oxo, 2-cyano-3-lower alkylguanidino, 2-acyl-3-lower alkylguanidino, 2-acylguanidino, (1-lower alkylamino-2-nitrovinyl)amino, hydroxy, halogen, cyano, acyl, benzimidazolylthio, triazolyl substituted with amino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, cyano, or acyl, andR.sup.5 is amino or lower alkoxy,R.sup.2 and R.sup.3 are each hydrogen, acyl or lower alkyl which may have halogen; orR.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen or halogen, andA is lower alkylene, or pharmaceutically acceptable salt thereof.

    Abstract translation: 下式的化合物，其中R 1是氨基，酰氨基，具有氨基和氧代的环（低级）烯基氨基，亚氨基，三唑基氨基，苯并异噻唑基氨基，其中每个所述杂环氨基可以被一个或多个被选择的取代基取代 由2-烷基氨基和氧代低级烷基，2-氰基-3-低级烷基胍基，2-酰基-3-低级烷基胍基，2-酰基胍基，（1-低级烷基氨基-2-硝基乙烯基）氨基，羟基，卤素， 氰基，酰基，苯并咪唑硫基，被氨基取代的三唑基或下式的基团：其中R 4是氢，氰基或酰基，R 5是氨基或低级烷氧基，R 2和R 3各自是氢，酰基或更低级 可以具有卤素的烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢或卤素，A是低级亚烷基或其药学上可接受的盐。

    Therapeutic agent for ischemic diseases
    6.
    发明授权
    Therapeutic agent for ischemic diseases 失效
    缺血性疾病治疗剂

    公开(公告)号：US5290785A

    公开(公告)日：1994-03-01

    申请号：US915877

    申请日：1992-07-20

    Applicant: Masayuki Kato ,  Kiyotaka Ito ,  Hisashi Takasugi

    Inventor： Masayuki Kato ,  Kiyotaka Ito ,  Hisashi Takasugi

    IPC: C07D471/04 ,  C07D221/06 ,  A61K31/44

    CPC classification number: C07D471/04 ,  Y02P20/55

    Abstract: The invention relates to a method of treating cardiac ischemic disease using a compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkenyl or N,N-di(lower)alkylaminomethyl,R.sup.2 is hydrogen, lower alkyl or halogen,R.sup.3 is imidazolyl or pyridyl, each of which may have substituent(s) selected from lower alkyl and imino-protective group, andR.sup.4 is hydrogen, lower alkyl, lower alkenyl or hydroxy(lower)alkyl and R.sup.5 is hydrogen, hydroxy or lower alkanoyloxy, orR.sup.4 and R.sup.5 are linked together to form an additional bond,or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及使用下式化合物治疗心肌缺血疾病的方法：（*化学结构*）其中R1是氢，低级烷基，低级烯基或N，N-二（低级）烷基氨基甲基，R2是氢，低级 烷基或卤素，R 3是咪唑基或吡啶基，其各自可以具有选自低级烷基和亚氨基保护基的取代基，R4是氢，低级烷基，低级烯基或羟基（低级）烷基，R5是氢， 羟基或低级烷酰氧基，或R 4和R 5连接在一起形成另外的键，或其药学上可接受的盐。

    Morpholine containing pyridine compounds, compositions and use
    10.
    发明授权
    Morpholine containing pyridine compounds, compositions and use 失效
    含有吡啶化合物的吗啉，组成和用途

    公开(公告)号：US4857527A

    公开(公告)日：1989-08-15

    申请号：US184195

    申请日：1988-04-21

    Applicant: Takao Takaya ,  Hisashi Takasugi ,  Kimio Esumi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Kazuhiro Maeda ,  Yoshie Sakamoto

    Inventor： Takao Takaya ,  Hisashi Takasugi ,  Kimio Esumi ,  Atsushi Kuno ,  Hiroyoshi Sakai ,  Kazuhiro Maeda ,  Yoshie Sakamoto

    IPC: C07D213/82

    CPC classification number: C07D213/82

    Abstract: An N-containing heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted with hydroxy, halogen or a heterocyclic group, carboxy, esterified carboxy, carbamoyl optionally substituted with heterocyclic(lower)alkyl or lower alkylamino(lower)alkyl, N-containing heterocycliccarbonyl optionally substituted with lower alkyl, or ureido optionally substituted with lower alkylamino(lower)alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andX is .dbd.N--or ##STR2## in which R.sup.4 is lower alkyl or halo(lower)alkyl, or is taken together with R.sup.1 to form an N-containing heterocyclic group optionally substituted with oxo and lower alkylamino(lower)alkyl; orR.sup.2 is lower alkyl, andX is ##STR3## in which R.sup.4 is phenyl substituted with nitro; and a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical (e.g. antihypertension) compositions comprising the same.

    Abstract translation: 含有下式的杂环化合物：其中R 1为任选被羟基，卤素或杂环基取代的低级烷基，羧基，酯化羧基，任选被杂环（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基 ，任选被低级烷基取代的含N杂环羰基或任选被低级烷基氨基（低级）烷基取代的脲基，R 3为氢或卤素; R 2为被硝基取代的苯基，X为= N-或其中R 4为低级烷基或卤代（低级）烷基），或与R 1一起形成任选被氧代取代的含氮杂环基 烷基氨基（低级）烷基; 或R2是低级烷基，X是其中R4是被硝基取代的苯基; 和其药学上可接受的盐，其制备方法和包含其的药物（例如抗高血压）组合物。

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