-
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。
-
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。
-
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。
-
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。
-
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 。
-
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。
-
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。
-
公开(公告)号:US20050153977A1
公开(公告)日:2005-07-14
申请号:US10500964
申请日:2003-01-15
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Kazuyoshi Obitsu , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , A61P7/00 , A61P43/00 , C07D277/44 , C07D277/46 , C07D417/04 , C07D417/12 , C07D417/14 , C07D453/02
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
-
公开(公告)号:US08338429B2
公开(公告)日:2012-12-25
申请号:US12615968
申请日:2009-11-10
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/496 , C07D417/14
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
摘要翻译: 基于促进巨核细胞集落形成的效果,具有对人c-mpl-Ba / F3细胞增殖的优异效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐和增加血小板的活性。 用于治疗血小板减少症的化合物或其药学上可接受的盐。
-
公开(公告)号:US20100222329A1
公开(公告)日:2010-09-02
申请号:US12615979
申请日:2009-11-10
申请人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
发明人: Keizo Sugasawa , Susumu Watanuki , Yuji Koga , Hiroshi Nagata , Ryutaro Wakayama , Fukushi Hirayama , Ken-ichi Suzuki
IPC分类号: A61K31/427 , C07D417/14 , C07D417/12 , C07D453/02 , C07D417/04 , A61K31/55 , A61K31/5377 , A61K31/454 , A61K31/439 , A61K31/496 , A61P7/00
CPC分类号: C07D417/14 , A61K31/426 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/695 , C07D277/46 , C07D417/04 , C07D417/12 , C07D453/02
摘要: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
-
-
-
-
-
-
-
-
-