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1. 发明授权

US06333320B1 Hexahydro-1,4-diazepine derivatives or salts thereof 失效
标题翻译：六氢-1,4-二氮杂衍生物或其盐
公开(公告)号：US06333320B1
公开(公告)日：2001-12-25
申请号：US09463017
申请日：2000-01-19
申请人： Hiroyuki Koshio , Fukushi Hirayama , Tsukasa Ishihara , Masashi Funatsu , Tomihisa Kawasaki , Yuzo Matsumoto
发明人： Hiroyuki Koshio , Fukushi Hirayama , Tsukasa Ishihara , Masashi Funatsu , Tomihisa Kawasaki , Yuzo Matsumoto
IPC分类号： A61K3155
CPC分类号： C07D405/12 , C07D243/08
摘要： Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: —CO—, —CONH—, —CSNH—, —SO2—, —SO2NH—, or the like; Y: a bond or alkylene; R1: hydrogen, alkyl, —Y—(hetero) aryl, or the like; R2: hydrogen, alkoxy, —COOH, or the like; R3: amidino or a group capable of being converted into amidino; and R4, R5: each independently hydrogen or lower alkyl.
摘要翻译：由通式（I）表示的六氢-1,4-二氮杂衍生物; 其药学上可接受的盐; 以及与活性成分相同的药物，例如活化凝血因子X抑制剂，其中A：亚苯基，亚吡啶基等; B：5-或6-元芳基或杂芳基环; X：-CO - ， - CONH - ， - CSH - ， - SO 2 - ， - SO 2 NH-等; Y：一个键或亚烷基; R1：氢，烷基，-Y-（杂）芳基等; R2：氢，烷氧基，-COOH等; R3：脒基或能够转化为脒基的基团; 和R 4，R 5：各自独立地为氢或低级烷基。

2. 发明授权

US5869501A Amidinonaphthyl derivative or salt thereof 失效
标题翻译：脒基萘基衍生物或其盐
公开(公告)号：US5869501A
公开(公告)日：1999-02-09
申请号：US849391
申请日：1997-05-30
申请人： Fukushi Hirayama , Hiroyuki Koshio , Yuzo Matsumoto , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
发明人： Fukushi Hirayama , Hiroyuki Koshio , Yuzo Matsumoto , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
IPC分类号： C07D211/44 , A61K31/445 , A61P7/02 , C07D211/46 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D211/46 , C07D409/12
摘要： An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. ##STR1## (symbols in the formula have the following meanings; R.sup.1 : a hydrogen atom or a group represented by the formula --A--W--R.sup.4,A: a group represented by the formula ##STR2## a group represented by the formula ##STR3## or a group represented by the formula --SO.sub.2 --, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula --NR.sup.5 --, R.sup.4 : a hydroxyl group, a lower alkoxy group, etc., R.sup.5 : a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R.sup.2 : a lower alkyl group, R.sup.3 : a hydrogen atom, a halogen atom, a carboxyl group, B: a lower alkylene group or a carbonyl group, and n: 0 or 1).
摘要翻译： PCT No.PCT / JP95 / 02458 Sec。 371日期1997年5月30日 102（e）日期1997年5月30日PCT提交1995年12月1日PCT公布。公开号WO96 / 16940 日期1996年6月6日由以下通式（I）表示的脒基萘基衍生物，其具有凝血因子X抑制作用，可用作抗血栓剂等，其盐，其中间体和药物组合物，其包含脒基萘基衍生物。由以下通式（I）表示的脒基萘基衍生物或其药学上可接受的盐。（式中的符号具有以下含义：R 1：氢原子或式-AW-R4表示的基团，A：由式SO 2表示的基团，由式 X：氧原子或硫原子，W：单键或由式-NR5-表示的基团，R4表示羟基，低级烷氧基等，R5表示氢原子，氨基甲酰基，低级烷氧基羰基等，R2：低级烷基，R3：氢原子，卤素原子，羧基，B：低级亚烷基或羰基，n：0或1）。

3. 发明授权

US6057324A Substituted amidinobenzene derivatives and medicinal compositions thereof 失效
标题翻译：取代的脒基苯衍生物及其药用组合物
公开(公告)号：US6057324A
公开(公告)日：2000-05-02
申请号：US194202
申请日：1998-10-20
申请人： Yuzo Matsumoto , Seijiro Akamatsu , Masato Ichihara , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
发明人： Yuzo Matsumoto , Seijiro Akamatsu , Masato Ichihara , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
IPC分类号： C07D401/04 , A61K31/445 , A61K31/495 , C07D211/46 , C07D211/58 , C07D401/00
CPC分类号： C07D211/58
摘要： A substituted-amidinobenzene derivative of the following general formula (I) or a salt thereof, and a pharmaceutical composition comprising said derivative or a salt thereof and a pharmaceutically acceptable carrier. ##STR1## (the symbols in the above formula have the following meanings: R.sup.1 : a group which can be converted into an amidino group in vivo;R.sup.2 and R.sup.3 : the same or different and each represents a carboxyl group or a group which can be converted into a carboxyl group in vivo;X.sup.1 and X.sup.2 : the same or different and each represents a lower alkylene group;m: 0, 1 or 2;n: 0 or 1, provided that n=1 when m=0.They have GPIIb/IIIa receptor antagonizing activity and are useful as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, And medicines for ameliorating peripheral artery disorders. In addition, they are useful as a prodrug excellent in peroral absorbability and sustainment of the effect.
摘要翻译： PCT No.PCT / JP97 / 01804 Sec。 371日期：1998年11月20日 102（e）1998年11月20日日期PCT提交1997年5月28日PCT公布。公开号WO97 / 45413 日本1997年4月12日由以下通式（I）表示的取代脒基苯衍生物或其盐，以及包含所述衍生物或其盐和药学上可接受的载体的药物组合物。（上式中的符号具有以下含义：R1：可在体内转化成脒基的基团; R2和R3相同或不同，表示可以转化为脒基的羧基或基团羧基; X1和X2：相同或不同，各自表示低级亚烷基; m：0,1或2; n：0或1，条件是当m = 0时n = 1，它们具有GPIIb / IIIa 受体拮抗活性，可用作改善缺血性心脏病，用于心脏手术或血管外科手术的药物，用于改善脑血管障碍的药物和用于改善外周动脉疾病的药物，此外它们可用作口服药物吸收和维持效果。

4. 发明授权

US5773442A Benzamidine derivatives and pharmaceutical composition containing them 失效
标题翻译：苄脒衍生物和含有它们的药物组合物
公开(公告)号：US5773442A
公开(公告)日：1998-06-30
申请号：US875702
申请日：1997-08-04
申请人： Seijiro Akamatsu , Yuzo Matsumoto , Masato Ichihara , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
发明人： Seijiro Akamatsu , Yuzo Matsumoto , Masato Ichihara , Tomihisa Kawasaki , Seiji Kaku , Isao Yanagisawa
IPC分类号： C07D211/58 , C07D401/04 , A61K31/495 , C07D211/60
CPC分类号： C07D401/04 , C07D211/58
摘要： Disclosed are benzamidine derivatives of the following general formula (I), salts thereof, hydrates thereof or solvates thereof, and pharmaceutical compositions comprising the derivatives, salts thereof, hydrates thereof or solvates thereof along with pharmaceutically-acceptable carriers. ##STR1## The derivatives and their compositions have GPIIb/IIIa receptor antagonistic activity and are useful for the treatment and prophylaxis of vascular system disorders as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, and medicines for ameliorating peripheral artery disorders.
摘要翻译： PCT No.PCT / JP96 / 00274 Sec。 371日期：1997年8月4日 102（e）日期1997年8月4日PCT提交1996年2月8日PCT公布。公开号WO96 / 24583 日期1996年8月15日公开了以下通式（I）的苯甲脒衍生物，其盐，其水合物或溶剂化物，以及包含其衍生物，盐，其水合物或溶剂化物以及药学上可接受的载体的药物组合物。（I）衍生物及其组合物具有GPIIb / IIIa受体拮抗活性，可用于治疗和预防血管系统障碍，作为改善缺血性心脏病的药物，心脏手术操作或血管外科手术中的用途，用于改善脑血管障碍，改善外周动脉障碍的药物。

5. 发明申请

US20110207655A1 CYCLIC DEPSIPEPTIDE COMPOUND AND USE THEREOF 审中-公开
标题翻译：环糊精化合物及其用途
公开(公告)号：US20110207655A1
公开(公告)日：2011-08-25
申请号：US13126363
申请日：2009-10-23
申请人： Susumu Tsujimoto , Masatoshi Taniguchi , Yoshitaka Hirayama , Jun Takasaki , Tomihisa Kawasaki , Kazutoshi Sakamoto , Shinya Nishiwaki , Yukihiro Kitanaga
发明人： Susumu Tsujimoto , Masatoshi Taniguchi , Yoshitaka Hirayama , Jun Takasaki , Tomihisa Kawasaki , Kazutoshi Sakamoto , Shinya Nishiwaki , Yukihiro Kitanaga
IPC分类号： A61K38/15 , C07K11/02 , A61P11/00 , A61P11/06
CPC分类号： A61K38/12 , A61K38/15 , C07K11/00
摘要： [Problem]A compound useful for the prevention and/or treatment of chronic obstructive pulmonary disease (COPD) or asthma, and a pharmaceutical composition containing the compound as an active ingredient are provided.[Means for Solution]The present inventors have made extensive studies on the pharmacological actions of naturally fermented materials, and as a result, they have found that a cyclic depsipeptide compound derived from a soil bacterium belonging to the genus Chromobacterium which is collected in Okutama-machi, Tokyo has both an inhibitory action on airway contraction and an inhibitory action on airway inflammation, and thus, is useful as an agent for preventing or treating COPD or asthma, thereby completing the present invention. That is, the present invention relates to a pharmaceutical composition for preventing and/or treating chronic obstructive pulmonary disease (COPD) or asthma, which contains a cyclic depsipeptide compound or a salt thereof as an active ingredient and is intended to be administered by intratracheal administration, nasal drop administration, or inhalation administration.
摘要翻译： [问题]提供了用于预防和/或治疗慢性阻塞性肺疾病（COPD）或哮喘的化合物和含有该化合物作为活性成分的药物组合物。 [解决方案]本发明人对天然发酵材料的药理作用进行了广泛的研究，结果发现，源自属于Chromobacterium属的土壤细菌的环状缩肽化合物是在Okutama- 东京都有对气道收缩的抑制作用和对气道炎症的抑制作用，因此可用作预防或治疗COPD或哮喘的药剂，从而完成了本发明。也就是说，本发明涉及用于预防和/或治疗慢性阻塞性肺疾病（COPD）或哮喘的药物组合物，其包含环状缩肽化合物或其盐作为活性成分，并且旨在通过气管内给药，滴鼻给药或吸入给药。

6. 发明申请

US20110034504A1 AGENT FOR PREVENTING AND/OR TREATING VASCULAR DISEASES 审中-公开
标题翻译：用于预防和/或治疗血管疾病的药剂
公开(公告)号：US20110034504A1
公开(公告)日：2011-02-10
申请号：US12935472
申请日：2009-03-31
申请人： Tomihisa Kawasaki , Toshiyuki Funatsu , Chinatsu Sakurai
发明人： Tomihisa Kawasaki , Toshiyuki Funatsu , Chinatsu Sakurai
IPC分类号： A61K31/4365 , C07D471/04 , A61P9/00
CPC分类号： A61K31/496 , A61K31/4196 , A61K45/06 , A61K2300/00
摘要： [Object] To provide an excellent pharmaceutical composition for preventing and/or treating vascular diseases.[Means for Solution] Useful to provide a pharmaceutical composition for preventing and/or treating vascular diseases, which comprises 1) a COX-1 selective inhibitor and 2) clopidogrel or a pharmaceutically acceptable salt thereof. The present invention is useful as an excellent pharmaceutical composition for preventing and/or treating vascular diseases is provided and is particularly useful as a pharmaceutical composition for preventing and/or treating arterial thrombosis, ischemic heart disease, ischemic brain disease, pulmonary embolism, peripheral circulation disorder, restenosis and reocclusion, essential thrombocytosis and so on is provided.
摘要翻译：提供用于预防和/或治疗血管疾病的优异药物组合物。 [用于溶液的方法]可用于提供用于预防和/或治疗血管疾病的药物组合物，其包括1）COX-1选择性抑制剂和2）氯吡格雷或其药学上可接受的盐。本发明可用作预防和/或治疗血管疾病的优异药物组合物，并且特别可用作预防和/或治疗动脉血栓形成，缺血性心脏病，缺血性脑病，肺栓塞，周围循环的药物组合物障碍，再狭窄和再闭塞，原发性血小板增多症等。

7. 发明申请

US20070254861A1 Methods for the prevention and/or treatment of peripheral arterial disease 审中-公开
标题翻译：预防和/或治疗外周动脉疾病的方法
公开(公告)号：US20070254861A1
公开(公告)日：2007-11-01
申请号：US11712397
申请日：2007-03-01
申请人： Tomihisa Kawasaki , Hajime Takamatsu , Toshio Uemura
发明人： Tomihisa Kawasaki , Hajime Takamatsu , Toshio Uemura
IPC分类号： A61K31/395 , A61P9/08
CPC分类号： A61K31/395 , A61K38/15
摘要： A method for the prevention and/or treatment of peripheral arterial disease by compound (I) or its pharmaceutically salts are provided. The compound (I) or its pharmaceutically salts have inhibitory activity against heterotrimeric G protein Gq/11.
摘要翻译：提供了通过化合物（I）或其药学上可接受的预防和/或治疗外周动脉疾病的方法。化合物（I）或其药用盐对异三聚G蛋白Gq / 11具有抑制活性。

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