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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。

3. 发明授权

US06673368B2 Colonic motor dysfunction remedies comprising aminothiazole derivatives as active ingredients 有权
标题翻译：包含氨基噻唑衍生物作为活性成分的结肠运动功能障碍疗法
公开(公告)号：US06673368B2
公开(公告)日：2004-01-06
申请号：US09853746
申请日：2001-05-14
申请人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
发明人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
IPC分类号： A61K3136
CPC分类号： A61K31/426 , A61K31/381
摘要： Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.
摘要翻译：治疗有助于改善结肠运动功能障碍，如肠易激综合征，便秘或肠痛，而不会对中枢神经系统造成副作用。作为活性成分，这些结肠运动障碍疗法包含由下式（I）表示的氨基噻唑衍生物或其盐或水合物：其中R 1，R 2和R 3可以相同或不同，各自独立地表示氢原子或羟基，低级烷基，低级烷氧基，氨基，硝基或氰基，R 4和R 5可以相同或不同，各自独立地表示氢原子或低级烷基，n表示2〜4的整数。

4. 发明授权

US5981557A Aminothiazole derivative, medicament containing the same, and intermediate for preparation of said compound 失效
标题翻译：氨基噻唑衍生物，含有该氨基噻唑衍生物的药物和用于制备所述化合物的中间体
公开(公告)号：US5981557A
公开(公告)日：1999-11-09
申请号：US952106
申请日：1997-11-18
申请人： Masaaki Nagasawa , Masakazu Murata , Hiroyasu Nishioka , Tadashi Kurimoto , Shigeru Ueki , Osamu Kitagawa
发明人： Masaaki Nagasawa , Masakazu Murata , Hiroyasu Nishioka , Tadashi Kurimoto , Shigeru Ueki , Osamu Kitagawa
IPC分类号： C07D277/56 , C07D417/12 , C07D521/00 , A61K31/425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/56 , C07D417/12
摘要： The present invention relates to an aminothiazole derivative represented by the following formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represents a hydrogen atom, a hydroxy group, a lower alkyl group, a lower alkoxy group or the like; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a halogen atom or a lower alkyl group; m stands for an integer of 0 to 4, A represents a substituted amino group, a substituted imino group, a heterocyclic group or the like; and B stands for an imino group or an oxygen atom, a medicament containing it and an intermediate for the preparation of said compound. The compound has strong restoration effects on dysmotility in the gastrointestinal tract and at the same time has high safety so that it is useful as an excellent gastroprokinetic.
摘要翻译： PCT No.PCT / JP96 / 01297 Sec。 371日期：1997年11月18日 102（e）1997年11月18日日期PCT提交1996年5月16日PCT公布。第WO96 / 36619号公报日期：1996年11月21日本发明涉及由下式（I）表示的氨基噻唑衍生物：其中R1，R2和R3各自独立地表示氢原子，羟基，低级烷基，低级烷氧基或喜欢; R4代表氢原子或低级烷基; R5表示氢原子，卤素原子或低级烷基; m表示0〜4的整数，A表示取代氨基，取代亚氨基，杂环基等， B代表亚氨基或氧原子，含有它的药物和制备所述化合物的中间体。该化合物对胃肠道运动障碍具有很强的恢复作用，同时具有较高的安全性，因此作为优良的胃动力学有用。

5. 发明授权

US06562373B2 Colonic motor dysfunction remedies comprising aminothiazole derivatives as active ingredients 有权
标题翻译：包含氨基噻唑衍生物作为活性成分的结肠运动功能障碍疗法
公开(公告)号：US06562373B2
公开(公告)日：2003-05-13
申请号：US09853746
申请日：2001-05-14
申请人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
发明人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
IPC分类号： A61K3136
CPC分类号： A61K31/426 , A61K31/381
摘要： Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.
摘要翻译：治疗有助于改善结肠运动功能障碍，如肠易激综合征，便秘或肠痛，而不会对中枢神经系统造成副作用。这些结肠运动障碍疗法包括作为活性成分的由下式（I）表示的氨基噻唑衍生物或其盐或水合物：其中R1，R2和R3可以相同或不同，并且各自独立地表示氢原子或羟基，低级烷基，低级烷氧基，氨基，硝基或氰基，R 4和R 5可以相同或不同，各自独立地表示氢原子或低级烷基，n表示2〜4的整数。

6. 发明授权

US06197970B1 Process for producing 2-hydroxybenzamide derivatives 有权
标题翻译： 2-羟基苯甲酰胺衍生物的制备方法
公开(公告)号：US06197970B1
公开(公告)日：2001-03-06
申请号：US09446108
申请日：1999-12-23
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Takanori Suzuki , Eiichi Nagano , Katsuyuki Ishii , Ryu Nakao
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Takanori Suzuki , Eiichi Nagano , Katsuyuki Ishii , Ryu Nakao
IPC分类号： C07D27756
CPC分类号： C07D277/56
摘要： The present invention is directed to a process for producing 2-hydroxybenzamide derivatives (2) or (5) according to either one of the following reaction schemes.
摘要翻译：本发明涉及根据以下反应方案之一制备2-羟基苯甲酰胺衍生物（2）或（5）的方法。

7. 发明授权

US5407950A Arylalkanoylamine derivative and drug containing the same 失效
标题翻译：芳基烷酰胺衍生物和含有其的药物
公开(公告)号：US5407950A
公开(公告)日：1995-04-18
申请号：US952499
申请日：1992-12-07
申请人： Akihiro Okubo , Hiroyasu Nishioka , Heihachiro Arai , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata
发明人： Akihiro Okubo , Hiroyasu Nishioka , Heihachiro Arai , Yoshiaki Tanaka , Hisayoshi Kato , Naoki Nakata
IPC分类号： C07D207/16 , C07D277/06 , C07D405/14 , C07D417/06 , C07D417/14 , C07D407/06 , A61K31/40 , A61K31/425 , C07D403/06
CPC分类号： C07D405/14 , C07D207/16 , C07D277/06 , C07D417/06 , C07D417/14
摘要： Arylalkanoylamine derivatives having excellent prolyl endopeptidase inhibitory action and resistances to hypoxia and amnesia which are represented by the following general formula (I): ##STR1## wherein A represents an indanyl, indenyl, 1,2,3,4-tetrahydronaphthalenyl or benzofuranyl group; m represents an integer of 0 to 5; Z represents a hydroxymethyl, formyl, nitrile, hydroxyiminomethyl, semicarbazonomethyl or dialkoxymethyl group; X and Y may be the same or different, and individually represent a methylene group or sulfur atom, wherein compounds defined by the following substituents are excluded: A represents an indanyl, indenyl, or 1,2,3,4-tetrahydronaphthalenyl group; X and Y each represent a methylene group; and Z represents a hydroxymethyl or formyl group. Also disclosed is a pharmaceutical composition and method for improving mneme, cerebral circulation and cerebral metabolism comprising the arylalkanoylamine derivatives as the effective ingredient.
摘要翻译： PCT No.PCT / JP91 / 00771 Sec。 371日期：1992年12月7日 102（e）日期1992年12月7日PCT提交1991年6月7日PCT公布。第WO91 / 18877号公报 1991年12月12日。具有优异的脯氨酰内肽酶抑制作用和由以下通式（I）表示的缺氧和遗忘抗性的芳基烷酰胺衍生物：2,3,4-四氢萘基或苯并呋喃基; m表示0〜5的整数， Z表示羟甲基，甲酰基，腈，羟基亚氨基甲基，氨基丙基甲基或二烷氧基甲基; X和Y可以相同或不同，并且各自表示亚甲基或硫原子，其中排除由以下取代基定义的化合物：A表示茚满基，茚基或1,2,3,4-四氢萘基; X和Y各自表示亚甲基; Z表示羟甲基或甲酰基。还公开了包含芳基烷酰胺衍生物作为有效成分的用于改善大脑，脑循环和脑代谢的药物组合物和方法。

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