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公开(公告)号:USRE43481E1
公开(公告)日:2012-06-19
申请号:US12203640
申请日:2008-09-03
申请人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
发明人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
IPC分类号: A61P7/02 , A61K31/55 , C07D223/04 , C07D401/00
CPC分类号: C07D401/04 , A61K31/551 , C07D243/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
摘要翻译: 提供具有基于活化凝血因子X的抑制的抗凝作用的化合物,并且可用作抗凝血剂或用于预防和治疗由血栓或栓塞引起的疾病的药剂。 二氮杂环丁烷衍生物如4 - [(3-氨甲酰氨基)甲基] -3- [4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基氨基]苯甲酸和3-羟基-4'-甲氧基 - 2 - {[4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基]氨基} -N-苯甲酰苯胺或其盐是有效成分。
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公开(公告)号:US07307074B2
公开(公告)日:2007-12-11
申请号:US10656129
申请日:2003-09-08
申请人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
发明人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
IPC分类号: A61P7/02 , A61K31/55 , C07D223/04 , C07D401/00
CPC分类号: C07D401/04 , A61K31/551 , C07D243/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
摘要翻译: 提供具有基于活化凝血因子X的抑制的抗凝作用的化合物,并且可用作抗凝血剂或用于预防和治疗由血栓或栓塞引起的疾病的药剂。 二氮杂环丁烷衍生物如4 - [(3-氨甲酰氨基)甲基] -3- [4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基氨基]苯甲酸和3-羟基-4'-甲氧基 - 2 - {[4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基]氨基} -N-苯甲酰苯胺或其盐是有效成分。
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公开(公告)号:US06642224B1
公开(公告)日:2003-11-04
申请号:US10148544
申请日:2002-10-02
申请人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
发明人: Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
IPC分类号: A61K3155
CPC分类号: C07D401/04 , A61K31/551 , C07D243/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-METHYL-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
摘要翻译: 提供具有基于活化凝血因子X的抑制的抗凝作用的化合物,并且可用作抗凝血剂或用于预防和治疗由血栓或栓塞引起的疾病的药剂。 二氮杂环丁烷衍生物如4 - [(3-甲脒亚氨基苯基氨基)甲基] -3- [4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基氨基]苯甲酸和3-羟基-4'-甲氧基 - 2 - {[4-(4-甲基-1,4-二氮杂环庚烷-1-基)苯甲酰基]氨基} -N-苯甲酰苯胺或其盐是有效成分。
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公开(公告)号:US07504417B2
公开(公告)日:2009-03-17
申请号:US10399625
申请日:2001-11-21
申请人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
发明人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
IPC分类号: A61K31/445 , C07D211/68 , C07D211/80 , C07D213/02
CPC分类号: C07D401/12 , C07D211/26 , C07D401/14 , C07H15/203 , C07H15/26
摘要: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl)carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.
摘要翻译: 提供了基于活化凝血因子X的抑制具有抗凝血作用的化合物,并且可用作血栓形成或栓塞引起的疾病的抗凝剂或预防/治疗剂。 有效成分是诸如4'-溴-2' - [(5-氯-2-吡啶基)氨基甲酰基] -6'-β-D-吡喃半乳糖氧基-1-异丙基哌啶-4-甲酰苯胺,2' - (2 - 乙酰氨基-2-脱氧-β-D-吡喃葡萄糖基氧基)-4'-溴-6' - [(5-氯-2-吡啶基)氨基甲酰基] -1-异丙基哌啶-4-甲酰苯胺等或其盐。
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公开(公告)号:US07786106B2
公开(公告)日:2010-08-31
申请号:US12356376
申请日:2009-01-20
申请人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
发明人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
IPC分类号: A61K31/551 , C07D243/08
CPC分类号: C07D401/12 , C07D211/26 , C07D401/14 , C07H15/203 , C07H15/26
摘要: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl) carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.
摘要翻译: 提供了基于活化凝血因子X的抑制具有抗凝血作用的化合物,并且可用作血栓形成或栓塞引起的疾病的抗凝剂或预防/治疗剂。 有效成分是诸如4'-溴-2' - [(5-氯-2-吡啶基)氨基甲酰基] -6' - (b-)-D-吡喃半乳糖氧基-1-异丙基哌啶-4-甲酰苯胺,2' - ( -2'-乙酰氨基-2-脱氧-α-D-吡喃葡萄糖基氧基)-4'-溴-6' - [(5-氯-2-吡啶基)氨基甲酰基] -1-异丙基哌啶-4-甲酰苯胺等或其盐 。
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公开(公告)号:US20090137498A1
公开(公告)日:2009-05-28
申请号:US12356376
申请日:2009-01-20
申请人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
发明人: Tsukasa Ishihara , Fukushi Hirayama , Keizo Sugasawa , Yuji Koga , Takeshi Kadokura , Takeshi Shigenaga
IPC分类号: A61K31/704 , C07D211/26
CPC分类号: C07D401/12 , C07D211/26 , C07D401/14 , C07H15/203 , C07H15/26
摘要: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl)carbamoyl]-6′-β-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-β-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.
摘要翻译: 提供了基于活化凝血因子X的抑制具有抗凝血作用的化合物,并且可用作血栓形成或栓塞引起的疾病的抗凝剂或预防/治疗剂。 有效成分是诸如4'-溴-2' - [(5-氯-2-吡啶基)氨基甲酰基] -6'-β-D-吡喃半乳糖氧基-1-异丙基哌啶-4-甲酰苯胺,2' - (2 - 乙酰氨基-2-脱氧-β-D-吡喃葡萄糖基氧基)-4'-溴-6' - [(5-氯-2-吡啶基)氨基甲酰基] -1-异丙基哌啶-4-甲酰苯胺等或其盐。
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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。
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公开(公告)号:US08486970B2
公开(公告)日:2013-07-16
申请号:US12600894
申请日:2008-05-26
申请人: Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
发明人: Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
IPC分类号: A01N43/40 , A61K31/445
CPC分类号: A61K31/4725 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/472 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/695 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04
摘要: [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
摘要翻译: [问题]提供药物,特别是可用作肠易激综合征(IBS)治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2(BB2)受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。 从上述可以看出,本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体,特别是IBS相关疾病的治疗剂。
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公开(公告)号:US20100227866A1
公开(公告)日:2010-09-09
申请号:US12600894
申请日:2008-05-26
申请人: Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
发明人: Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
IPC分类号: A61K31/4725 , C07D401/12 , C07D401/14 , A61K31/53 , A61K31/506 , A61P1/00 , A61P35/00
CPC分类号: A61K31/4725 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/472 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/695 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04
摘要: [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
摘要翻译: [问题]提供药物,特别是可用作肠易激综合征(IBS)治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2(BB2)受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。 从上述可以看出,本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体,特别是IBS相关疾病的治疗剂。
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公开(公告)号:US08518490B2
公开(公告)日:2013-08-27
申请号:US12749921
申请日:2010-03-30
申请人: Koju Ito , Tsukasa Ishihara , Hidekazu Yamazaki
发明人: Koju Ito , Tsukasa Ishihara , Hidekazu Yamazaki
IPC分类号: B05D5/00
摘要: In a coating zone, a cylindrical tube is soaked in and taken out from a solution, such that a coating film is formed on a curved surface of the tube. In a wet gas zone, while a first gas feeding nozzle having a gas outlet moves in a state where the gas outlet faces an outer peripheral surface of the tube, wet gas is blown toward the coating film through the gas outlet. Water drops are generated on the coating film and grown up. In a dry gas zone, as in the case of the first gas feeding nozzle, while a second gas feeding nozzle having a gas outlet moves, dry gas is blown toward the coating film through the gas outlet. Solvent and water drops are evaporated from the coating film. Pores form from the water drops as a template for the porous material on the coating film.
摘要翻译: 在涂布区域中,将圆筒形管浸泡并从溶液中取出,使得在管的弯曲表面上形成涂膜。 在湿气区域中,具有气体出口的第一气体供给喷嘴在气体出口朝向管的外周面的状态下移动,湿气通过气体出口吹向涂膜。 在涂膜上产生水滴并长大。 在干燥气体区域中,与第一气体供给喷嘴的情况相同,当具有气体出口的第二气体供给喷嘴移动时,干燥气体通过气体出口吹向涂膜。 溶剂和水滴从涂膜中蒸发掉。 从水滴形成孔,作为涂膜上的多孔材料的模板。
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