公开(公告)号：US4792547A

公开(公告)日：1988-12-20

申请号：US941918

申请日：1986-12-15

申请人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani

发明人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  A61K31/55 ,  A61K31/495

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.

摘要翻译： 用于治疗支气管哮喘，过敏性胃炎，花粉荨麻疹，过敏性鼻炎和过敏性结膜炎的新颖吡嗪衍生物及其药物组合物。 化合物具有如下式I：其中R表示氢或者其中R 1和R 2可以相同或不同，并且各自独立地表示氢，直链或支链低级烷基或具有三个至 6个碳原子，可被卤素，低级烷基或低级烷氧基取代的苯基，或其中R 1和R 2一起代表四至六个碳原子的亚烷基，包括任选地被一个或两个氮原子或一个氧 所述环任选被具有1-6个碳原子的直链或支链低级烷基，羟基或苯基取代，及其药学上可接受的盐。

公开(公告)号：US4971990A

公开(公告)日：1990-11-20

申请号：US301354

申请日：1989-01-24

申请人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani ,  Shunichiro Sakurai

发明人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani ,  Shunichiro Sakurai

IPC分类号： C07C311/27 ,  C07D295/26

CPC分类号： C07D295/26 ,  C07C311/27

摘要： Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.

公开(公告)号：US4525356A

公开(公告)日：1985-06-25

申请号：US546481

申请日：1983-10-28

申请人： Yasuo Itho ,  Hideo Kato ,  Nobuo Ogawa ,  Kagari Yamagishi ,  Eiichi Koshinaka ,  Kazuya Mitani

发明人： Yasuo Itho ,  Hideo Kato ,  Nobuo Ogawa ,  Kagari Yamagishi ,  Eiichi Koshinaka ,  Kazuya Mitani

IPC分类号： C07D311/30 ,  C07D405/12 ,  A61K31/35 ,  C07D405/10

CPC分类号： C07D405/12 ,  C07D311/30

摘要： Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith.The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.

摘要翻译： 由通式（I）表示的N-取代的黄酮-8-甲酰胺的衍生物其中R1表示氢原子，甲基或乙基，R2表示氢原子，低级烷基，低级烷氧基 卤素原子或硝基，R3表示氢原子或低级烷基，k表示0,1,2或3，m表示0或1; X和Y必须不同，表示氢原子或甲基。 A表示具有式“IMAGE”的氨基，其中可以相同或不同的R 4和R 5与氮原子一起表示低级烷基或环状氨基，并且具有或不具有氧原子，R6表示 低级烷基和n代表2或3，以及其药物组合物和其处理方法。 N-取代的黄酮-8-甲酰胺衍生物可用作治疗尿素的药剂。

公开(公告)号：US4943581A

公开(公告)日：1990-07-24

申请号：US371392

申请日：1989-06-26

申请人： Hiroyoshi Hidaka ,  Toshio Tanaka ,  Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Kazuya Mitani ,  Shunichiro Sakurai

发明人： Hiroyoshi Hidaka ,  Toshio Tanaka ,  Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Kazuya Mitani ,  Shunichiro Sakurai

IPC分类号： C07D217/02 ,  A61K31/47 ,  A61K31/472 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D217/04

CPC分类号： C07D217/04 ,  Y02P20/55

摘要： An isoquinolinesulfonamide selected from those represented by the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different, and each represent hydrogen or lower-alkyl, and X represents hydrogen or halogen, and pharmacologically-acceptable acid addition salts thereof, pharmaceutical compositions thereof, and use thereof in the treatment of circular disorders, are disclosed.

摘要翻译： 选自由下式表示的异喹啉磺酰胺：其中R 1，R 2和R 3可以相同或不同，并且各自表示氢或低级烷基，X表示氢或卤素，以及其药学上可接受的酸加成盐 ，其药物组合物及其在治疗循环障碍中的用途。