公开(公告)号：US5556851A

公开(公告)日：1996-09-17

申请号：US286220

申请日：1994-08-05

申请人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

发明人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

IPC分类号： A61K31/50 ,  A61P1/00 ,  A61P1/08 ,  A61P25/04 ,  A61P25/20 ,  C07D403/12 ,  C07D451/04 ,  C07D451/06 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  A61K31/55

CPC分类号： C07D451/04 ,  C07D451/06 ,  C07D453/02

摘要： A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT.sub.3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the prevention and/or treatment of various disorders such as nausea and/or emesis caused by anticancer drugs or X-ray treatment, central nervous disorders such as anxiety and/or neuropathy, gastroenteric diseases such as indigestion, chronic gastritis, digestive ulcer, irritable bowel syndromes and the like, hemicrania, cluster headache, trigeminal neuralgia, arrhythmia and the like.

公开(公告)号：US5391549A

公开(公告)日：1995-02-21

申请号：US29431

申请日：1993-03-10

申请人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

发明人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

IPC分类号： A61K31/50 ,  A61P1/00 ,  A61P1/08 ,  A61P25/04 ,  A61P25/20 ,  C07D403/12 ,  C07D451/04 ,  C07D451/06 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  A61K31/55 ,  C07D237/28 ,  C07D401/12

CPC分类号： C07D451/04 ,  C07D451/06 ,  C07D453/02

摘要： A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT.sub.3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the prevention and/or treatment of various disorders such as nausea and/or emesis caused by anticancer drugs or X-ray treatment, central nervous disorders such as anxiety and/or neuropathy, gastroenteric diseases such as indigestion, chronic gastritis, digestive ulcer, irritable bowel syndromes and the like, hemicrania, cluster headache, trigeminal neuralgia, arrhythmia and the like.

摘要翻译： 对5-羟色胺5-HT 3受体具有拮抗活性的新颖的噌啉衍生物，其药学上可接受的盐，其N-氧化物衍生物或溶剂合物，以及含有其的预防和/或治疗各种疾病如恶心和/ 或由抗癌药物或X线治疗引起的呕吐，焦虑和/或神经病变等中枢神经障碍，消化不良，慢性胃炎，消化性溃疡，肠易激综合征等胃肠疾病，血红素，丛集性头痛，三叉神经痛， 心律失常等。

公开(公告)号：US5352685A

公开(公告)日：1994-10-04

申请号：US29551

申请日：1993-03-11

申请人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

发明人： Akira Maruyama ,  Shigeru Ogawa ,  Satoshi Yamazaki ,  Akihiro Tobe

IPC分类号： A61K31/435 ,  A61P1/00 ,  A61P1/08 ,  A61P9/00 ,  A61P25/04 ,  A61P25/20 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D519/00

摘要： The thieno[3.2-b]pyridine derivative of the present invention promote the gastric emptying in male ddy mice and the gastric contraction in dogs sutured with a strain-gauge transducer. It is believed that the derivatives have the action to enhance gastric motor action and gastric emptying. Therefore, the compound of the present invention are effective for the prevention and therapeutical treatment of the symptoms caused by gastric hypanakinesis, such as heartburn, abdominal distension feeling, anorexia, unpleasant feeling on upper abdomen, abdominalgia, nausea, vomiting, etc. caused by the underlying diseases such as acute and chronic gastritis, stomach and duodenum ulcer, gastroneurosis, gastroptosis, etc. The present invention also encompasses a pharmaceutical composition containing as the effective ingredient a compound of the present invention, and a method for producing the same.

摘要翻译： 本发明的噻吩并[3,2-b]吡啶衍生物促进雄性ddy小鼠胃排空，并用应变计换能器缝合狗的胃收缩。 据信这些衍生物具有增强胃运动作用和胃排空的作用。 因此，本发明的化合物可有效预防和治疗由胃灼热引起的症状，例如胃灼热，腹胀，厌食，上腹部不适感，腹痛，恶心，呕吐等引起的症状。 基础疾病如急性和慢性胃炎，胃和十二指肠溃疡，胃肠炎，胃食管狭窄等。本发明还包括含有本发明化合物作为有效成分的药物组合物及其制备方法。

公开(公告)号：US4977151A

公开(公告)日：1990-12-11

申请号：US501591

申请日：1990-03-29

申请人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

发明人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： C07D295/12 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K31/54 ,  A61K31/5415 ,  A61P1/04 ,  C07D233/61 ,  C07D279/18 ,  C07D279/30 ,  C07D295/125 ,  C07D307/91 ,  C07D333/76 ,  C07D339/08 ,  C07D521/00

CPC分类号： C07D307/91 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D279/30 ,  C07D295/125 ,  C07D333/76 ,  C07D339/08

摘要： Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.4 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable acid addition salts thereof are disclosed. They are a potent antiulcer agent.

公开(公告)号：US4883822A

公开(公告)日：1989-11-28

申请号：US248087

申请日：1988-09-23

申请人： Kohtaro Matsuo ,  Youichirou Ezaki ,  Akihiro Tobe ,  Satoshi Yamazaki ,  Kozue Enda ,  Mariko Kitsukawa

发明人： Kohtaro Matsuo ,  Youichirou Ezaki ,  Akihiro Tobe ,  Satoshi Yamazaki ,  Kozue Enda ,  Mariko Kitsukawa

IPC分类号： A61K31/12 ,  A61P1/00 ,  A61P1/14 ,  C07C49/675 ,  C07C49/755

CPC分类号： A61K31/12

摘要： An agent for regulating the motional function of the gastrointestinal tract, which contains as an active ingredient a 41-metyl-4,4a,9,10-tetrahydro-2(3H)-phenanthrenone derivative represented by the following formula I; ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group or an alkoxy group and R.sup.2 represents a hydrogen atom or an alkyl group.

公开(公告)号：US4933344A

公开(公告)日：1990-06-12

申请号：US239169

申请日：1988-08-31

申请人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

发明人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： C07D295/12 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K31/54 ,  A61K31/5415 ,  A61P1/04 ,  C07D233/61 ,  C07D279/18 ,  C07D279/30 ,  C07D295/125 ,  C07D307/91 ,  C07D333/76 ,  C07D339/08 ,  C07D521/00

CPC分类号： C07D307/91 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D279/30 ,  C07D295/125 ,  C07D333/76 ,  C07D339/08

摘要： Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.4 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable acid addition salts thereof are disclosed. They are a potent antiulcer agent.

公开(公告)号：US4883802A

公开(公告)日：1989-11-28

申请号：US243322

申请日：1988-09-09

申请人： Kunihiro Ninomiya ,  Ken-Ichi Saito ,  Shuji Morita ,  Akihiro Tobe ,  Issei Nitta

发明人： Kunihiro Ninomiya ,  Ken-Ichi Saito ,  Shuji Morita ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： A61K31/445 ,  A61K31/4427 ,  A61K38/00 ,  A61P25/28 ,  C07D401/12 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/097

CPC分类号： C07K5/0825 ,  C07K5/06139 ,  C07K5/0821

摘要： A novel 4-piperidinecarboxamide derivatives represented by the general formula (I): ##STR1## wherein each R.sup.1 and R.sup.2 represents a hydrogen atom, or R.sup.1 together with R.sup.2 represents a cyclopentanespiro or cyclohexanespiro group; R.sup.3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group or an indolylalkyl group; and n is an integer of 1 or 2;is disclosed herein. The novel compound is useful as the agent for improving the impaired brain fuction.

公开(公告)号：US4880819A

公开(公告)日：1989-11-14

申请号：US242333

申请日：1988-09-09

申请人： Kunihiro Ninomiya ,  Ken-Ichi Saito ,  Shuji Morita ,  Akihiro Tobe ,  Issei Nitta

发明人： Kunihiro Ninomiya ,  Ken-Ichi Saito ,  Shuji Morita ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K38/00 ,  A61P25/28 ,  C07D401/12 ,  C07D401/14 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097

CPC分类号： C07K5/0821 ,  C07K5/06139 ,  A61K38/00

摘要： Novel 4-aminopyridine derivatives represented by the general formula (I): ##STR1## wherein A and B independently represent ##STR2## and n is an integer of 1 or 2; as well as their pharmaceutically acceptable acid addition salts are disclosed herein. The novel compounds are useful as the agent for improving impaired brain function.

公开(公告)号：US5397785A

公开(公告)日：1995-03-14

申请号：US115257

申请日：1993-09-02

申请人： Kunihiro Ninomiya, deceased ,  Ken-ichi Sato ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

发明人： Kunihiro Ninomiya, deceased ,  Ken-ichi Sato ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

IPC分类号： C07D219/10 ,  C07D221/16 ,  C07D221/20 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/44

CPC分类号： C07D221/20 ,  C07D219/10 ,  C07D221/16 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

摘要： A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

摘要翻译： 公开了由下式（I）表示的新型4-酰氨基吡啶衍生物。 （I）本发明的4-酰基氨基吡啶衍生物作为治疗老年性痴呆和阿尔茨海默氏病等记忆障碍的药物是有用的，因为它具有直接激活故障胆碱能神经元的作用。

公开(公告)号：US5168099A

公开(公告)日：1992-12-01

申请号：US668480

申请日：1991-03-14

申请人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

发明人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P25/20 ,  C07D319/20 ,  C07D407/12

CPC分类号： C07D407/12 ,  C07D319/20

摘要： Optically active alkylenedioxybenzene derivatives of the formula: ##STR1## wherein m is an integer of 2-5, and n is an integer of 1-3, and acid addition salts thereof. A pharmaceutical composition containing a compound (I) or racemate, and a method of treating anxiety in a warm-blooded animal by administering the above compound (I) to said animal are also provided.