公开(公告)号：US4990507A

公开(公告)日：1991-02-05

申请号：US294743

申请日：1989-01-09

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

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

IPC分类号： C07D213/26 ,  C07D213/30 ,  C07D213/36 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D237/08 ,  C07D237/24 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D213/30 ,  C07D213/26 ,  C07D213/36 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D237/08 ,  C07D237/24 ,  C07D413/12 ,  C07D471/04

摘要： The invention relates to a pharmaceutical composition as a therapeutic agent for ischemic disease comprising a compound of the formula ##STR1## wherein R.sup.1 is carbamoyl substituted with morpholino (lower) alkyl, thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl; andR.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substituted with nitro;with proviso that R.sup.1 is carbamoyl substituted with thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl when R.sup.4 is lower alkyl; or its salt, as an active ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.

摘要翻译： 本发明涉及作为缺血性疾病治疗剂的药物组合物，其包含下式化合物其中R 1是被吗啉代（低级）烷基，硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基） 或被低级烷基氨基（低级）烷基取代的脲基; R2是被硝基取代的苯基，R4是低级烷基; 或R 2为低级烷基，R 4为被硝基取代的苯基; 条件是R1是被硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基; 或当R 4为低级烷基时被低级烷基氨基（低级）烷基取代的脲基; 或其盐作为活性成分，与药学上可接受的，基本上无毒的载体或赋形剂结合。

公开(公告)号：US4857527A

公开(公告)日：1989-08-15

申请号：US184195

申请日：1988-04-21

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

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

IPC分类号： C07D213/82

CPC分类号： C07D213/82

摘要： 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.

摘要翻译： 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。