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公开(公告)号：US07816522B2
公开(公告)日：2010-10-19
申请号：US11723893
申请日：2007-03-22
申请人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： A61K31/41 , A61K31/415 , C07D233/00 , C07D249/00
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen]
摘要翻译： 由以下通式（1）表示的化合物，其盐或其前体的水合物是可用于治疗和/或预防与血栓形成有关的疾病的新型化合物，其具有合适的理化稳定性更安全。 [其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; 并且Z 1和Z 2各自独立地表示氢]
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公开(公告)号：US20100240654A1
公开(公告)日：2010-09-23
申请号：US12791571
申请日：2010-06-01
申请人： Richard CLARK , Shinsuke HIROTA , Hiroshi AZUMA , Kazunobu KIRA , Nobuhisa WATANABE , Tadashi NAGAKURA , Tatsuo HORIZOE
发明人： Richard CLARK , Shinsuke HIROTA , Hiroshi AZUMA , Kazunobu KIRA , Nobuhisa WATANABE , Tadashi NAGAKURA , Tatsuo HORIZOE
IPC分类号： A61K31/5377 , C07C243/22 , A61K31/15 , C07D211/72 , A61K31/4402 , C07D215/38 , A61K31/47 , C07D239/32 , C07D295/28 , A61K31/5375 , C07D413/04 , A61P7/02 , A61P9/10 , A61P9/00 , A61P7/00
CPC分类号： C07D209/48 , C07C257/18 , C07C311/49 , C07C317/14 , C07C317/44 , C07C337/06 , C07D209/08 , C07D213/30 , C07D213/54 , C07D213/71 , C07D213/77 , C07D213/80 , C07D213/82 , C07D213/86 , C07D213/87 , C07D213/89 , C07D215/38 , C07D233/90 , C07D237/20 , C07D239/28 , C07D239/42 , C07D249/18 , C07D257/04 , C07D295/32 , C07D307/68 , C07D333/24 , C07D471/04
摘要： A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.
摘要翻译： 由下列通式（1）表示的化合物或其盐或其水合物是安全的，同时具有合适的物理化学稳定性，并且可用作与血栓形成相关的疾病的治疗或预防剂。 其中R1a，R1b，R1c和R1d各自独立地表示氢等，R2表示任选取代的苯基等，R 3表示任选取代的C 6-10芳基等，Z 1，Z 2和Z 3各自独立地表示氢等， Z4表示氢等，X表示单键或-CO-等。
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公开(公告)号：US20060276465A1
公开(公告)日：2006-12-07
申请号：US11474225
申请日：2006-06-23
IPC分类号： A61K31/5377 , A61K31/538 , A61K31/496 , A61K31/495 , C07D413/02 , C07D403/02
CPC分类号： C07D295/096 , C07D205/04 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/273 , C07D207/335 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/62 , C07D211/70 , C07D211/74 , C07D211/76 , C07D211/88 , C07D213/38 , C07D213/64 , C07D223/04 , C07D241/08 , C07D243/08 , C07D257/04 , C07D261/08 , C07D263/56 , C07D265/30 , C07D265/36 , C07D271/10 , C07D277/28 , C07D277/64 , C07D279/12 , C07D295/033 , C07D295/067 , C07D295/073 , C07D295/088 , C07D295/108 , C07D295/116 , C07D295/13 , C07D295/135 , C07D295/15 , C07D295/155 , C07D295/16 , C07D295/185 , C07D295/192 , C07D295/205 , C07D295/215 , C07D295/26 , C07D307/14 , C07D307/52 , C07D309/04 , C07D309/14 , C07D317/66 , C07D319/18 , C07D333/20 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/12 , C07D417/12 , C07D487/08 , C07D491/10
摘要： A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc. And A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents 5- to 10-membered cycloalkyl etc. optionally substituted with hydroxyl etc., R30, R31 and R32 may be the same or different and each represents hydrogen etc., R40 represents C1-10 alkyl etc. optionally substituted with hydroxyl etc., n represents an integer of 0, 1 or 2, X1 represents CH or nitrogen, and R20, R21, R22 and R23 may be the same or different and each represents hydrogen etc.
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公开(公告)号：US20110112109A1
公开(公告)日：2011-05-12
申请号：US13006004
申请日：2011-01-13
申请人： Richard CLARK , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard CLARK , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： A61K31/501 , A61K31/4196 , A61K31/506 , A61K31/4439 , A61K31/497 , A61K31/427 , A61K31/4245 , A61P7/02
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
摘要翻译： 由下列通式（1）表示的化合物或其盐或上述的水合物：其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; Z1和Z2各自独立地表示氢。
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公开(公告)号：US20100190783A1
公开(公告)日：2010-07-29
申请号：US12748806
申请日：2010-03-29
申请人： Richard CLARK , Fumiyoshi MATSUURA , Kazunobu KIRA , Shinsuke HIROTA , Hiroshi AZUMA , Tadashi NAGAKURA , Tatsuo HORIZOE , Kimiyo TABATA , Kazutomi KUSANO , Takao OMAE , Atsushi INOUE
发明人： Richard CLARK , Fumiyoshi MATSUURA , Kazunobu KIRA , Shinsuke HIROTA , Hiroshi AZUMA , Tadashi NAGAKURA , Tatsuo HORIZOE , Kimiyo TABATA , Kazutomi KUSANO , Takao OMAE , Atsushi INOUE
IPC分类号： A61K31/5377 , C07D249/12 , A61K31/4192 , C07D401/04 , A61K31/4439 , C07D403/04 , A61K31/506 , C07D401/14 , A61K31/444 , A61K31/501 , A61K31/497 , C07D413/14 , A61P7/02 , A61P9/10
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A Compound represented by the following general formula (1): wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen or salts thereof or hydrates of the foregoing.
摘要翻译： 由以下通式（1）表示的化合物：其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; 并且Z 1和Z 2各自独立地表示氢或其盐或前述的水合物。
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公开(公告)号：US20080015199A1
公开(公告)日：2008-01-17
申请号：US11723893
申请日：2007-03-22
申请人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： A61K31/4196 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61P7/02 , A61P9/00 , C07D249/08 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen]
摘要翻译： 由以下通式（1）表示的化合物，其盐或其前体的水合物是可用于治疗和/或预防与血栓形成有关的疾病的新型化合物，其具有合适的理化稳定性更安全。 [其中R 1a，R 1b，R 1c和R 1d各自独立地表示氢等。 R 2表示任选取代的苯基等; R 3表示任选取代的C 6-10芳基等; Z 1和Z 2各自独立地表示氢]
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公开(公告)号：US08436009B2
公开(公告)日：2013-05-07
申请号：US13695665
申请日：2011-05-18
申请人： Richard Clark , Fumiyoshi Matsuura , Masanobu Shinoda , Shinsuke Hirota , Kazunobu Kira , Hiroshi Azuma , Atsushi Takemura , So Yasui , Kazutomi Kusano , Masaki Mikamoto , Takao Omae
发明人： Richard Clark , Fumiyoshi Matsuura , Masanobu Shinoda , Shinsuke Hirota , Kazunobu Kira , Hiroshi Azuma , Atsushi Takemura , So Yasui , Kazutomi Kusano , Masaki Mikamoto , Takao Omae
IPC分类号： A61K31/506 , C07D239/42
CPC分类号： C07D401/14 , C07D403/04
摘要： By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation.
摘要翻译： 通过口服给药由下式（I）表示的化合物：对血液凝固因子VIIa具有优异抑制作用的化合物（IV）的血液水平和抗凝血作用达到足以表达其药理作用的水平 。 因此，本发明的化合物可用作由血栓形成引起的疾病的治疗和/或预防剂。
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公开(公告)号：US20130053563A1
公开(公告)日：2013-02-28
申请号：US13695665
申请日：2011-05-18
申请人： Richard Clark , Fumiyoshi Matsuura , Masanobu Shinoda , Shinsuke Hirota , Kazunobu Kira , Hiroshi Azuma , Atsushi Takemura , So Yasui , Kazutomi Kusano , Masaki Mikamoto , Takao Omae
发明人： Richard Clark , Fumiyoshi Matsuura , Masanobu Shinoda , Shinsuke Hirota , Kazunobu Kira , Hiroshi Azuma , Atsushi Takemura , So Yasui , Kazutomi Kusano , Masaki Mikamoto , Takao Omae
IPC分类号： C07D403/04 , C07D401/14
CPC分类号： C07D401/14 , C07D403/04
摘要： By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation.
摘要翻译： 通过口服给药由下式（I）表示的化合物：对血液凝固因子VIIa具有优异抑制作用的化合物（IV）的血液水平和抗凝血作用达到足以表达其药理作用的水平 。 因此，本发明的化合物可用作由血栓形成引起的疾病的治疗和/或预防剂。
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公开(公告)号：US08163787B2
公开(公告)日：2012-04-24
申请号：US13006004
申请日：2011-01-13
申请人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： A61K31/41 , A61K31/415 , C07D233/00 , C07D249/00
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
摘要翻译： 由下列通式（1）表示的化合物或其盐或前述的水合物：其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R3代表任选取代的C6-10芳基等; Z1和Z2各自独立地表示氢。
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公开(公告)号：US07928228B2
公开(公告)日：2011-04-19
申请号：US12748806
申请日：2010-03-29
申请人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
发明人： Richard Clark , Fumiyoshi Matsuura , Kazunobu Kira , Shinsuke Hirota , Hiroshi Azuma , Tadashi Nagakura , Tatsuo Horizoe , Kimiyo Tabata , Kazutomi Kusano , Takao Omae , Atsushi Inoue
IPC分类号： C07D207/00 , C07D233/00 , C07D249/00 , C07D257/04
CPC分类号： C07D249/12 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/04
摘要： A Compound represented by the following general formula (1): wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen or salts thereof or hydrates of the foregoing.
摘要翻译： 由以下通式（1）表示的化合物：其中R1a，R1b，R1c和R1d各自独立地表示氢等; R2代表任选取代的苯基等; R 3表示任选取代的C 6-10芳基等; 并且Z 1和Z 2各自独立地表示氢或其盐或前述的水合物。
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