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1. 发明授权

US06884810B2 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US06884810B2
公开(公告)日：2005-04-26
申请号：US10380158
申请日：2002-09-18
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Yutaka Shinozaki , Hitoshi Morita
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Yutaka Shinozaki , Hitoshi Morita
IPC分类号： A61K31/4439 , A61P1/04 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4439
摘要： A benzimidazole derivative of formula (1): (wherein R represents a hydrogen atom or a methoxy group, and n is 0 or 1) or a salt thereof; and a medicament containing the same. The compounds of the present invention, due to minimized difference in therapeutic effect between subjects, which difference would otherwise be derived from different CYP2C19 activity from subject to subject, ensure that all patients can enjoy proper therapeutic effects at the same dose of the drug. Also, the compounds of the invention have low risk of drug interaction caused by induction of CYP1A family member enzymes, as well as low risk of development of cancer, and thus is useful as a remedy for peptic ulcer, reliably providing therapeutic effects with safety.
摘要翻译：式（1）的苯并咪唑衍生物：其中R表示氢原子或甲氧基，n为0或1;或其盐; 和含有该药物的药物。本发明的化合物由于受试者之间治疗效果的差异最小化，否则从受试者到受试者的不同CYP2C19活性的差异将确保所有患者在相同剂量的药物中可以获得适当的治疗效果。此外，本发明的化合物由CYP1A家族成员酶的诱导引起的药物相互作用的风险低，并且癌症发展的风险低，因此可用作消化性溃疡的补救剂，可靠地提供安全的治疗效果。

2. 发明授权

US06747022B2 Calcium salts of 1,5-benzodiazepine derivatives, process for producing the salts and drugs containing the same 有权
标题翻译： 1,5-苯并二氮杂衍生物的钙盐，其制备方法和含有该盐的药物
公开(公告)号：US06747022B2
公开(公告)日：2004-06-08
申请号：US10130305
申请日：2002-08-15
申请人： Katsuo Shinozaki , Masakazu Murata , Kiyoto Maeda , Hiroaki Taguchi , Nobuo Kawase , Naoyoshi Miura
发明人： Katsuo Shinozaki , Masakazu Murata , Kiyoto Maeda , Hiroaki Taguchi , Nobuo Kawase , Naoyoshi Miura
IPC分类号： C07D24312
CPC分类号： C07D243/12
摘要： Provided are calcium salts of a 1,5-benzodiazepine derivative represented by the following formula (I): (wherein, R1 represents a lower alkyl group, R2 represents a phenyl or cyclohexyl group, and Y represents a single bond or a lower alkylene group); a process for preparing the salts; and drugs containing the same as the active ingredient. The compounds exhibit a potent inhibitory activity against the secretion of gastric acid and potent antagonism against gastrin and/or CCK-B receptor.
摘要翻译：提供由下式（I）表示的1,5-苯并二氮杂衍生物的钙盐：其中，R 1表示低级烷基，R 2表示苯基或环己基，Y表示单键或低级亚烷基）; 一种制备盐的方法; 和含有与活性成分相同的药物。化合物对胃酸分泌具有有效的抑制活性，并且对胃泌素和/或CCK-B受体有强烈的拮抗作用。

3. 发明授权

US06344452B1 1,5-benzodiazepine derivatives 失效
标题翻译： 1,5-苯并二氮杂衍生物
公开(公告)号：US06344452B1
公开(公告)日：2002-02-05
申请号：US09701562
申请日：2000-12-05
申请人： Katsuo Shinozaki , Tomoyuki Yoneta , Masakazu Murata , Naoyoshi Miura , Kiyoto Maeda
发明人： Katsuo Shinozaki , Tomoyuki Yoneta , Masakazu Murata , Naoyoshi Miura , Kiyoto Maeda
IPC分类号： C07D24312
CPC分类号： C07D243/12
摘要： This invention relates to 1,5-benzodiazepine derivatives, which are each represented by the following formula (1): wherein R1 represents a lower alkyl group, R2 and R3 may be the same or different and represent a hydrogen atom or a lower alkyl group, R4 represents a cyclohexyl group or phenyl group, and n stands for an integer of from 1 to 3, and also to medicines containing the same. These compounds are useful as curatives or preventives for diseases in which a gastrin receptor and/or a CCK-B receptor takes part.
摘要翻译：本发明涉及1,5-苯并二氮杂衍生物，其分别由下式（1）表示：其中R 1表示低级烷基，R 2和R 3可以相同或不同，表示氢原子或低级烷基 R4表示环己基或苯基，n表示1〜3的整数，也表示含有该基团的药物。这些化合物可用作胃泌素受体和/或CCK-B受体参与的疾病的治疗剂或预防剂。

4. 发明授权

US5198450A Phenylalkanoylamine derivatives, process for preparing the same, and usage of the same 失效
标题翻译：苯甲酰胺衍生物，其制备方法及其用途
公开(公告)号：US5198450A
公开(公告)日：1993-03-30
申请号：US601795
申请日：1991-01-07
申请人： Kuniyoshi Ogura , Tomoji Aotsuka , Motoki Torizuka , Mitsuo Soeda , Yoshiaki Tanaka , Hisayoshi Kato , Naoyoshi Miura , Noaki Nakata , Hikaru Morita , Akihiro Okubo
发明人： Kuniyoshi Ogura , Tomoji Aotsuka , Motoki Torizuka , Mitsuo Soeda , Yoshiaki Tanaka , Hisayoshi Kato , Naoyoshi Miura , Noaki Nakata , Hikaru Morita , Akihiro Okubo
IPC分类号： C07D295/18 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P25/28 , C07D207/20 , C07D211/70 , C07D277/04 , C07D295/185
CPC分类号： C07D295/185 , C07D207/20 , C07D211/70 , C07D277/04
摘要： An agent for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance is disclosed. The agent comprises as an effective component a phenylalkanoylamine derivative represented by the following formula (I), ##STR1## wherein A represents a 1,3-thiazolidin-3-yl group, a 1,2,3,6-tetrahydropyridin-1-yl group, a morpholino group, a thiomorpholin-4-yl group, or a 3-pyrrolin-1-yl group, R.sup.1 and R.sup.2, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, a guanidino group, or a group ##STR2## (wherein R.sup.3 and R.sup.4 independently represent a lower alkyl group or form in combination 5- or 6-membered heterocyclic group), and n represents an integer of 2-6, or a salt thereof. This agent is effective for treating or preventing cerebral hemorrhage sequela, cerebral infarction sequela, cerebral arterioscleosis, subarachnoid hemorrhage sequela, cranial injury sequela, cerebral operation sequela, cerebrovascular dementia, Parkinson's disease, Alzheimer's disease, Pick's disease, various anoxia toxicosis including, but not limited to anthracemia sequela, cerebral alcoholism related diseases, and the like.

5. 发明授权

US5028604A Condensed benzene derivative 失效
标题翻译：冷凝苯衍生物
公开(公告)号：US5028604A
公开(公告)日：1991-07-02
申请号：US444702
申请日：1989-12-01
申请人： Motoki Torizuka , Tomoji Aotsuka , Mitsuo Soeda , Kuniyoshi Ogura , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata , Naoyoshi Miura , Hikari Morita
发明人： Motoki Torizuka , Tomoji Aotsuka , Mitsuo Soeda , Kuniyoshi Ogura , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata , Naoyoshi Miura , Hikari Morita
IPC分类号： C07D207/16 , C07D211/60 , C07D277/06 , C07D279/12 , C07D417/06 , C07K5/078
CPC分类号： C07D417/06 , C07D207/16 , C07D211/60 , C07D277/06 , C07D279/12 , C07K5/06165
摘要： Novel condensed benzene derivatives having prolyl endopeptidase inhibitory, anti-hypoxic, and anti-amnesic activities are disclosed. The compounds are represented by the following (I), ##STR1## wherein A represents a methylene, ethylene, or propylene group, B represents a methylene or ethylene group, m denotes an integer of 0-5, X and Y, which may be same or different, individually represent a methylene group or sulfur atom, R.sup.1 represents a hydrogen atom, a carboxyl, lower alkyloxycarbonyl, hydroxymethyl, or formyl group, R.sup.2 represents a hydrogen atom, a halogen atom, a lower alkyl, lower alkoxy, nitro, or amino group, R.sup.3 represents a hydrogen atom or a lower alkyl group, and the dotted line may optionally be present. They are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.

6. 发明授权

US4916146A Amino acid imide derivatives, usage thereof, and medicinal composition containing the same 失效
标题翻译：氨基酰亚胺衍生物，其用途和含有它们的药物组合物
公开(公告)号：US4916146A
公开(公告)日：1990-04-10
申请号：US288556
申请日：1988-12-22
申请人： Yoshiaki Tanaka , Tomoji Aotsuka , Naomi Kobayashi , Naoki Nakata , Kuniyoshi Ogura , Motoki Torizuka , Naoyoshi Miura , Heihachiro Arai
发明人： Yoshiaki Tanaka , Tomoji Aotsuka , Naomi Kobayashi , Naoki Nakata , Kuniyoshi Ogura , Motoki Torizuka , Naoyoshi Miura , Heihachiro Arai
IPC分类号： C12N9/99 , A61K31/425 , A61K31/426 , A61P25/28 , A61P43/00 , C07D207/00 , C07D277/06 , C07D413/06 , C07D417/06
CPC分类号： C07D417/06 , C07D277/06
摘要： Novel N-substituted amino acid imide derivatives are disclosed. The compounds are represented by formula (I): ##STR1## wherein n represents an integer of 0 to 5, and X and Y, which may be the same or different, represent a methylene group or a sulfur atom, provided that not both X and Y are methylene groups at the same time. The compounds are useful as a medicine for treating or preventing cerebral circulation disorder, cerebral metabolism disorder, or memory disturbance.

7. 发明申请

US20050148634A1 1-N-Aminobenzimidazole derivatives 审中-公开
标题翻译： 1-N-氨基苯并咪唑衍生物
公开(公告)号：US20050148634A1
公开(公告)日：2005-07-07
申请号：US10507361
申请日：2003-03-28
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Hideki Nakamura , Hitoshi Morita
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Hideki Nakamura , Hitoshi Morita
IPC分类号： A61P1/04 , A61P43/00 , C07D401/12 , A61K31/4439 , C07D43/02
CPC分类号： C07D401/12 , C07D471/04 , C07D495/04
摘要： Provided are 1-N-aminobenzimidazole derivatives represented by the following formula (I): wherein R1 and R2 each represents a substituted or unsubstituted alkyl group or the like, R3, R5 and R6 each represents an alkyl group, alkoxy group, hydrogen atom or the like, R4 represents a substituted or unsubstituted alkyl group or the like, A represents a benzene ring or the like, B represents a hydrogen atom or the like, an n stands for an integer of from 0 to 2, or salts thereof; and medicines containing them. The compounds (I) according to the present invention do not bring about much individual differences in therapeutic effects despite the existence of individual differences in the CYP2C19 activity. At the same dose, they can hence bring about appropriate therapeutic effects for all patients. In addition, they are low in the risk of induction of an interaction or a cancer caused by induction of the CYP1A family. Accordingly, they are useful as peptic ulcer therapeutic agents which are safe and surely bring about therapeutic effects.
摘要翻译：提供由下式（I）表示的1-N-氨基苯并咪唑衍生物：其中R 1和R 2各自表示取代或未取代的烷基等，R R 5，R 5和R 6各自表示烷基，烷氧基，氢原子等，R 4， SUP>表示取代或未取代的烷基等，A表示苯环等，B表示氢原子等，n表示0〜2的整数，或其盐; 和含有它们的药物。尽管CYP2C19活性存在个体差异，但是本发明的化合物（I）不会在治疗效果上产生太多的个体差异。在相同剂量下，它们可以为所有患者带来适当的治疗效果。此外，它们诱导由CYP1A家族诱导引起的相互作用或癌症的风险较低。因此，它们可用作消化性溃疡治疗剂，其是安全的并且确实具有治疗效果。

8. 发明授权

US06239131B1 1,5 Benzodiazepine derivatives 有权
标题翻译： 1,5苯二氮卓衍生物
公开(公告)号：US06239131B1
公开(公告)日：2001-05-29
申请号：US09319249
申请日：1999-06-08
申请人： Katsuo Shinozaki , Tomoyuki Yoneta , Masakazu Murata , Naoyoshi Miura , Kiyoto Maeda
发明人： Katsuo Shinozaki , Tomoyuki Yoneta , Masakazu Murata , Naoyoshi Miura , Kiyoto Maeda
IPC分类号： A61K3155
CPC分类号： C07D401/06 , C07D243/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12
摘要： 1,5-Benzodiazepine derivatives represented by formula (I), salts thereof, and medicines containing the same as the active ingredient: The compounds exhibit excellent gastrin and/or CCK-B receptor antagonism and are useful as remedies for gastric ulcer and gastrointestinal movement disorder.
摘要翻译：由式（I）表示的1,5-苯并二氮杂衍生物及其盐，以及含有与活性成分相同的药物：该化合物表现出优异的胃泌素和/或CCK-B受体拮抗作用，可用作胃溃疡和胃肠道运动的补救措施紊乱。

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