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1. 发明公开

EP1063230A4 CYCLIC AMINO COMPOUNDS 有权
标题翻译：环氨基债券
公开(公告)号：EP1063230A4
公开(公告)日：2001-12-12
申请号：EP99906508
申请日：1999-02-26
申请人： SANKYO CO , UBE INDUSTRIES
发明人： ASAI FUMITOSHI , SUGIDACHI ATSUHIRO , IKEDA TOSHIHIKO , IWABUCHI HARUO , KUROKI YOSHIAKI , INOUE TERUHIKO , IWAMURA RYO , SHIBAKAWA NOBUHIKO
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/445 , A61P7/02 , C07D205/04 , C07D205/08 , C07D207/04 , C07D207/12 , C07D211/06 , C07D211/20 , C07D211/52 , C07D211/54 , C07D211/72 , C07D471/08
CPC分类号： C07D471/08 , C07D205/04 , C07D207/12 , C07D211/52 , C07D211/54 , C07D211/72
摘要： Cyclic amino compounds represented by general formula (I) or pharmacologically acceptable salts thereof having an excellent antiplatelet aggregation effect, etc. and thus being useful as preventives or remedies for embolism, thrombosis or arterial sclerosis wherein R1 represents optionally substituted phenyl; R2 represents optionally substituted aliphatic acyl, optionally substituted benzoyl or alkoxycarbonyl; and R3 represents substituted and optionally ring-fused saturated cyclic amino.

2. 发明公开

EP0934928A4 CYCLIC AMINE DERIVATIVES 失效
标题翻译：环胺衍生物
公开(公告)号：EP0934928A4
公开(公告)日：2001-05-09
申请号：EP97937814
申请日：1997-08-28
申请人： SANKYO CO , UBE INDUSTRIES
发明人： ASAI FUMITOSHI , SUGIDACHI ATSUHIRO , IKEDA TOSHIHIKO , KOIKE HIROYUKI , INOUE TERUHIKO , TAKATA KATSUNORI , IWAMURA RYO , KITA JUN-ICHIRO , YONEDA KENJI
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： Cyclic amine derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, excellent in the effect of inhibiting platelet aggregation and useful as a preventive or remedy for embolism, thrombosis or arteriosclerosis, wherein R1 represents optionally substituted phenyl; R2 represents optionally substituted C¿1?-C8 acyl, optionally substituted benzoyl or C1-C4 alkoxycarbonyl; and R?3¿ represents optionally fused, substituted three- to seven-membered cyclic saturated amino.

3. 发明公开

EP1350511A4 MEDICINAL COMPOSITIONS CONTAINING ASPIRIN 无效
标题翻译：阿司匹林药物含有组合物
公开(公告)号：EP1350511A4
公开(公告)日：2004-06-23
申请号：EP01271850
申请日：2001-12-20
申请人： SANKYO CO , UBE INDUSTRIES
发明人： ASAI FUMITOSHI , SUGIDACHI ATSUHIRO , OGAWA TAKETOSHI , INOUE TERUHIKO
IPC分类号： A61K31/4365 , A61K31/616 , A61K45/06 , A61P7/02 , A61K31/60
CPC分类号： A61K45/06 , A61K31/4365 , A61K31/60 , A61K31/616 , A61K2300/00
摘要： Medicinal compositions containing as the active ingredients 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or its pharmacologically acceptable salt and aspirin. Because of having excellent inhibitory effects on platelet aggregation and thrombosis, these compositions are useful as preventives or remedies for diseases induced by thrombus or embolization.

4. 发明公开

EP1298132A4 HYDROPYRIDINE DERIVATIVE ACID ADDITION SALTS 有权
标题翻译： SURE-ADDITIONSSALZE VON HYDROPYRIDINDERIVATEN
公开(公告)号：EP1298132A4
公开(公告)日：2004-03-10
申请号：EP01945799
申请日：2001-07-03
申请人： SANKYO CO , UBE INDUSTRIES
发明人： ASAI FUMITOSHI , OGAWA TAKETOSHI , NAGANUMA HIDEO , YAMAMURA NAOTOSHI , INOUE TERUHIKO , NAKAMURA KAZUYOSHI
IPC分类号： A61K31/4365 , A61P7/02 , A61P9/10 , C07D495/04
CPC分类号： C07D495/04
摘要： Acid addition salts of 2-acetoxy-5-(α-cyclopropyl-carbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]-pyridine. These acid addition salts exhibit excellent peroral absorbability, metabolism-activating and platelet aggregation-inhibiting effects, low toxicity, and excellent storage and handling stabilities, and this are useful as drugs, preferably preventive or therapeutic drugs (particularly therapeutic drugs) for diseases caused by thrombus or infarction, still preferably preventive or therapeutic drugs (particularly therapeutic drugs) for thrombosis or infarct.
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。这些酸加成盐表现出优异的经口吸收性，代谢活化和血小板聚集抑制效果，低毒性和优异的储存和操作稳定性，并且这可用作药物，优选预防或治疗药物（特别是治疗药物）血栓或梗塞，更优选用于血栓形成或梗塞的预防或治疗药物（特别是治疗药物）。

5. 发明公开

EP1245564A4 BENZAMIDINE DERIVATIVES 有权
标题翻译： BENZAMIDINDERIVATE
公开(公告)号：EP1245564A4
公开(公告)日：2003-03-05
申请号：EP00970070
申请日：2000-10-25
申请人： SANKYO CO
发明人： FUJIMOTO KOICHI , ASAI FUMITOSHI , MATSUHASHI HAYAO
IPC分类号： C07D207/12 , A61K31/40 , A61K31/4465 , A61P7/02 , A61P9/10 , C07D211/46 , A61K31/44
CPC分类号： C07D211/46
摘要： Benzamidine derivatives of general formula (I) or pharmacologically acceptable salts thereof exhibit excellent inhibitory activity against activated blood coagulation factor X and are useful as therapeutic or preventive drugs for diseases related to blood coagulation. In said formula, R1 is hydrogen, halogeno, alkyl, or hydroxyl; R2 is hydrogen, halogeno, or alkyl; R3 is hydrogen, optionally substituted alkyl, aralkyl, optionally substituted alkanoyl, or optionally substituted alkylsulfonyl; R?4 and R5¿ are each independently hydrogen, halogeno, optionally substituted alkyl, alkoxy, carbonyl, alkoxycarbonyl, or optionally substituted carbamoyl; and R6 is substituted pyrrolidine or substituted piperidine.
摘要翻译：通式（I）的苄脒衍生物或其药理学上可接受的盐对活化血液凝固因子X显示优异的抑制活性，可用作与凝血相关的疾病的治疗或预防药物。在所述式中，R1是氢，卤素，烷基或羟基; R2是氢，卤代或烷基; R3是氢，任选取代的烷基，芳烷基，任选取代的烷酰基或任选取代的烷基磺酰基; R 4和R 5各自独立地为氢，卤素，任选取代的烷基，烷氧基，羰基，烷氧基羰基或任选取代的氨基甲酰基; 和R6是取代的吡咯烷或取代的哌啶。

6. 发明公开

EP1375482A4 ENZAMIDINE DERIVATIVE 审中-公开
标题翻译： BENZAMIDINDERIVATE
公开(公告)号：EP1375482A4
公开(公告)日：2005-01-19
申请号：EP02714444
申请日：2002-04-03
申请人： SANKYO CO
发明人： FUJIMOTO KOICHI , TANAKA NAOKI , SHIMADA IKUKO , ASAI FUMITOSHI
IPC分类号： A61K31/402 , A61K31/422 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/10 , A61P43/00 , C07D207/12 , C07D207/22 , C07D207/48 , C07D211/46 , C07D211/72 , C07D211/96 , C07D223/08 , C07D223/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D413/04 , C07D417/04 , C07D451/06 , C07D471/04 , C07D487/04 , C07D487/08
CPC分类号： C07D451/06 , A61K31/402 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/55 , C07D207/12 , C07D207/22 , C07D207/48 , C07D211/46 , C07D211/72 , C07D211/96 , C07D223/08 , C07D223/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/08
摘要： A benzamidine derivative having the general formula: (1) wherein R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group, R2 represents a hydrogen atom or a halogen atom, R3 represents a hydrogen atom, an alkyl group optionally substituted, an aralkyl group, an alkylcarbonyl group optionally substituted, an alkylsulfonyl group optionally substituted, or the like, R?4 and R5¿ each represent a hydrogen atom, a halogen atom, an alkyl or carbamoyl group optionally substituted, or the like, R6 represents a heteroring or the like, R?7 and R8¿ each represent a hydrogen atom, an alkyl group, or the like, and n represents 0,1 or 2; or a salt thereof being pharmacologically acceptable. The benzamidine derivative and the salt have excellent inhibition action for activated blood coagulation factor X, and are useful as a medicine for therapy or prevention of a disease of blood coagulation.

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