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公开(公告)号：US06693115B2
公开(公告)日：2004-02-17
申请号：US10329629
申请日：2002-12-26
申请人： Fumitoshi Asai , Taketoshi Ogawa , Hideo Naganuma , Naotoshi Yamamura , Teruhiko Inoue , Kazuyoshi Nakamura
发明人： Fumitoshi Asai , Taketoshi Ogawa , Hideo Naganuma , Naotoshi Yamamura , Teruhiko Inoue , Kazuyoshi Nakamura
IPC分类号： A61K314365
CPC分类号： C07D495/04
摘要： Acid addition salts of 2-acetoxy-5-(&agr;-cyclopropyl-carbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]-pyridine. The acid addition salts of tetrahydrothienopyridine derivatives of the present invention exhibit excellent oral absorption, metabolization into the active compound, and platelet aggregation-inhibiting effects, low toxicity, and excellent storage and handling stabilities, and are useful as medicaments, preferably preventive or therapeutic agents (particularly therapeutic agents) for diseases caused by a thrombus or an embolus, still more preferably preventive or therapeutic agents (particularly therapeutic agents) for thrombosis or embolism.
摘要翻译： 2-乙酰氧基-5-（α-环丙基 - 羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c] - 吡啶的酸加成盐。 本发明的四氢噻吩并吡啶衍生物的酸加成盐表现出优异的口服吸收，代谢成活性化合物，抑制血小板聚集作用，毒性低，储存和处理稳定性优异，可用作药物，优选预防或治疗剂 （特别是治疗剂），还优选用于血栓形成或栓塞的预防或治疗剂（特别是治疗剂）。
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公开(公告)号：US20070010499A1
公开(公告)日：2007-01-11
申请号：US11520168
申请日：2006-09-13
IPC分类号： A61K31/60 , A61K31/4743
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/60 , A61K31/616 , A61K2300/00
摘要： A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
摘要翻译： 2-乙酰氧基-5-（α-环丙基羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c]吡啶或其药学上可接受的盐和阿司匹林的组合，其具有优异的抑制性 抗血小板聚集和血栓形成的活性，可用于预防或治疗由血栓或栓塞引起的疾病。
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公开(公告)号：US07371760B2
公开(公告)日：2008-05-13
申请号：US10600266
申请日：2003-06-20
IPC分类号： A61K31/60 , A61K31/4743
摘要： A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
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公开(公告)号：US08569325B2
公开(公告)日：2013-10-29
申请号：US12006546
申请日：2008-01-03
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/60 , A61K31/616 , A61K2300/00
摘要： A method for the prevention of diseases caused by thrombus or embolus. The method is to separately administer 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, in their pharmacologically effective amounts, to a warm-blooded animal.
摘要翻译： 一种预防血栓或栓塞引起的疾病的方法。 该方法是分别给予2-乙酰氧基-5-（α-环丙基羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c]吡啶或其药学上可接受的盐和阿司匹林 其药理学有效量，适用于温血动物。
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公开(公告)号：US08404703B2
公开(公告)日：2013-03-26
申请号：US11520168
申请日：2006-09-13
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/60 , A61K31/616 , A61K2300/00
摘要： A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and is useful for preventing or treating diseases caused by thrombus or embolus.
摘要翻译： 2-乙酰氧基-5-（α-环丙基羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c]吡啶或其药学上可接受的盐和阿司匹林的组合，其具有优异的抑制性 抗血小板聚集和血栓形成的活性，可用于预防或治疗由血栓或栓塞引起的疾病。
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公开(公告)号：US20080108589A1
公开(公告)日：2008-05-08
申请号：US12006546
申请日：2008-01-03
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/60 , A61K31/616 , A61K2300/00
摘要： A method for the prevention of diseases caused by thrombus or embolus. The method is to separately administer 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, in their pharmacologically effective amounts, to a warm-blooded animal.
摘要翻译： 一种预防血栓或栓塞引起的疾病的方法。 该方法是分别给予2-乙酰氧基-5-（α-环丙基羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c]吡啶或其药学上可接受的盐和阿司匹林 其药理学有效量，适用于温血动物。
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公开(公告)号：US20050192245A1
公开(公告)日：2005-09-01
申请号：US10522403
申请日：2005-01-18
申请人： Fumitoshi Asai , Toshimori Inaba , Taketoshi Ogawa
发明人： Fumitoshi Asai , Toshimori Inaba , Taketoshi Ogawa
IPC分类号： A61K31/4743 , A61K31/675 , A61K31/7076 , A61K45/06
CPC分类号： A61K45/06 , A61K31/4743 , A61K31/675 , A61K31/7076 , A61K2300/00
摘要： A medicinal composition, wherein an ADP receptor antagonist and an ACAT inhibitor are administered either simultaneously or separately at a defined interval as a preventive or a remedy (in particular, a remedy) for arteriosclerosis or diseases derived from arteriosclerosis such as ischemic heart disease, ischemic brain disease and peripheral circulation failure in warm-blooded animals (in particular, humans).
摘要翻译： 药物组合物，其中ADP受体拮抗剂和ACAT抑制剂以规定的间隔同时或分开施用作为用于动脉硬化的预防或治疗（特别是补救）或来自动脉硬化的疾病，例如缺血性心脏病，缺血性 温血动物（特别是人类）的脑疾病和周围循环衰竭。
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公开(公告)号：US6087379A
公开(公告)日：2000-07-11
申请号：US257818
申请日：1999-02-25
申请人： Fumitoshi Asai , Atsuhiro Sugidachi , Toshihiko Ikeda , Hiroyuki Koike , Teruhiko Inoue , Katsunori Takata , Ryo Iwamura , Jun-ichiro Kita , Kenji Yoneda
发明人： Fumitoshi Asai , Atsuhiro Sugidachi , Toshihiko Ikeda , Hiroyuki Koike , Teruhiko Inoue , Katsunori Takata , Ryo Iwamura , Jun-ichiro Kita , Kenji Yoneda
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/46 , A61P7/02 , A61P9/10 , C07D205/04 , C07D205/08 , C07D207/08 , C07D207/12 , C07D211/20 , C07D211/54 , C07D211/72 , C07D213/70 , C07D451/02 , C07D451/04
CPC分类号： C07D213/70 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/20 , C07D211/54 , C07D451/02 , C07D451/04 , Y02P20/55
摘要： A cyclic amine derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted of unsubstituted C.sub.1 -C.sub.8 aliphatic acyl group, a substituted or unsubstituted benzoyl group or a C.sub.1 -C.sub.4 alkoxycarbonyl group, and R.sup.3 represents a substituted 3 to 7 membered saturated cyclic amino group which may form a fused ring; or pharmaceutically acceptable salts thereof. The compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the treatment and prevention of such diseases as embolism, thrombosis or arteriosclerosis and for the preparation of pharmaceutical compositions for such uses.
摘要翻译： 由下式表示的环状胺衍生物：其中，R1表示取代或未取代的苯基，R2表示取代未取代的C1-C8脂肪族酰基，取代或未取代的苯甲酰基或C1〜C4烷氧基羰基，R3表示 可以形成稠环的取代的3至7元饱和环氨基; 或其药学上可接受的盐。 化合物和盐具有优异的血小板聚集抑制作用。 它们可用于治疗和预防诸如栓塞，血栓形成或动脉硬化等疾病以及制备用于此类用途的药物组合物。
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9.发明授权Diphenylethane compounds containing a saturated heterocyclic group, their preparation, and their therapeutic use 失效含有饱和杂环基的二苯基乙烷化合物及其制备及其治疗用途
公开(公告)号：US5843983A
公开(公告)日：1998-12-01
申请号：US798489
申请日：1997-02-10
申请人： Koichi Fujimoto , Naoki Tanaka , Fumitoshi Asai , Taketoshi Ogawa , Teiichiro Koga , Tatsuo Tanimoto , Yoshio Tsujita , Hiroyuki Koike
发明人： Koichi Fujimoto , Naoki Tanaka , Fumitoshi Asai , Taketoshi Ogawa , Teiichiro Koga , Tatsuo Tanimoto , Yoshio Tsujita , Hiroyuki Koike
IPC分类号： C07D291/02 , A61K31/4015 , A61K31/445 , A61K31/535 , A61K31/54 , A61P9/00 , C07D207/12 , C07C37/055 , A61K31/135 , A61K31/205 , C07C39/17
CPC分类号： C07D207/12
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are hydrogen or various other groups or atoms; and A represents a single bond or an alkylene group having from 1 to 6 carbon atoms are serotonin 2 receptor antagonists and have the ability to inhibit the activity of squalene synthase. They can not only prevent and inhibit the development and progression of arteriosclerosis but can also inhibit thrombosis in arteriosclerotic lesions and can improve hemodynamics.
摘要翻译： 式（I）的化合物：其中：R1表示通过环碳原子连接到由A表示的键或基团的饱和杂环基; R2a，R2b，R2c，R3a，R3b，R3c和R3d是氢或各种其他基团或原子; 并且A表示单键或具有1至6个碳原子的亚烷基是5-羟色胺2受体拮抗剂，并且具有抑制角鲨烯合酶活性的能力。 它们不仅可以预防和抑制动脉硬化的发展和进展，而且可以抑制动脉硬化病变中的血栓形成，并可以改善血液动力学。
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公开(公告)号：US06610708B1
公开(公告)日：2003-08-26
申请号：US09622849
申请日：2000-08-24
申请人： Fumitoshi Asai , Atsuhiro Sugidachi , Toshihiko Ikeda , Haruo Iwabuchi , Yoshiaki Kuroki , Teruhiko Inoue , Ryo Iwamura , Nobuhiko Shibakawa
发明人： Fumitoshi Asai , Atsuhiro Sugidachi , Toshihiko Ikeda , Haruo Iwabuchi , Yoshiaki Kuroki , Teruhiko Inoue , Ryo Iwamura , Nobuhiko Shibakawa
IPC分类号： A61K31445
CPC分类号： C07D471/08 , C07D205/04 , C07D207/12 , C07D211/52 , C07D211/54 , C07D211/72
摘要： A cyclic amino compound represented by the following formula: or a pharmacologically acceptable salt thereof. R1 is a substitutable phenyl group. R2 is a substitutable aliphatic acyl group, a substitutable benzoyl group or an alkoxycarbonyl group. R3 is a substituted, saturated cyclic amino group which may optionally have a fused ring. These compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the prevention and/or treatment of embolism, thrombosis or arteriosclerosis and other conditions resulting from platelet aggregation.
摘要翻译： 由下式表示的环状氨基化合物或其药理学上可接受的盐。 R1是可取代的苯基。 R2是可取代的脂族酰基，可取代的苯甲酰基或烷氧基羰基。 R3是可以任选地具有稠合环的取代的饱和环状氨基。 这些化合物和盐具有优异的血小板聚集抑制作用。 它们可用于预防和/或治疗由血小板聚集引起的栓塞，血栓形成或动脉硬化以及其它病症。
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