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公开(公告)号:US20050282808A1
公开(公告)日:2005-12-22
申请号:US10508512
申请日:2003-03-27
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
IPC分类号: A61P7/02 , C07D307/85 , C07D405/04 , C07D405/12 , C07D405/14 , A61K31/551 , A61K31/343 , A61K31/443 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377
CPC分类号: C07D413/14 , C07D307/85 , C07D405/12 , C07D405/14 , C07D417/14
摘要: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式[1]的苯并呋喃衍生物:其中x是下式的基团:-N-或-CH-; Y是任选取代的氨基,任选取代的环烷基或任选取代的饱和杂环基; A是单键,在链的末端或其末端具有双键的碳链或氧原子; R 1是氢原子或卤素原子; 环B是任选取代的苯环; R 3是氢原子或其药学上可接受的盐,其可用作药物,特别是作为活化凝血因子X抑制剂。
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公开(公告)号:US20090209511A1
公开(公告)日:2009-08-20
申请号:US12382787
申请日:2009-03-24
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
IPC分类号: A61K31/397 , A61K31/535 , A61K31/4439 , A61K31/421 , C07D413/14 , C07D405/12 , C07D263/00
CPC分类号: C07D413/14 , C07D307/85 , C07D405/12 , C07D405/14 , C07D417/14
摘要: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式[1]的苯并呋喃衍生物:其中x是下式的基团:-N-或-CH-; Y是任选取代的氨基,任选取代的环烷基或任选取代的饱和杂环基; A是单键,在链的末端或其末端具有双键的碳链或氧原子; R1是氢原子或卤素原子; 环B是任选取代的苯环; 并且R 3是氢原子或其药学上可接受的盐,其可用作药物,特别是作为活化凝血因子X抑制剂。
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公开(公告)号:US07531537B2
公开(公告)日:2009-05-12
申请号:US10508512
申请日:2003-03-27
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Yasunori Tsuboi , Takashi Mitsui , Jun Murakami
IPC分类号: A61K31/5377 , A61K31/443 , C07D413/14 , C07D405/12
CPC分类号: C07D413/14 , C07D307/85 , C07D405/12 , C07D405/14 , C07D417/14
摘要: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式[1]的苯并呋喃衍生物:其中x是下式的基团:-N-或-CH-; Y是任选取代的氨基,任选取代的环烷基或任选取代的饱和杂环基; A是单键,在链的末端或其末端具有双键的碳链或氧原子; R1是氢原子或卤素原子; 环B是任选取代的苯环; 并且R3是氢原子或其药学上可接受的盐,其可用作药物,特别是作为活化凝血因子X抑制剂。
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公开(公告)号:US20060094724A1
公开(公告)日:2006-05-04
申请号:US10540878
申请日:2004-01-08
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
IPC分类号: A61K31/498 , A61K31/4741 , C07D491/02
CPC分类号: C07D491/04 , C07D213/75
摘要: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式(I)的缩合呋喃化合物:其中环X为苯,吡啶等; Y是任选取代的氨基,任选取代的环烷基,任选取代的芳基,任选取代的饱和杂环基,任选取代的不饱和杂环基; A是单键,低级亚烷基,低级亚烯基,低级亚烯基或氧原子; R 3是氢等; 和R 4是氢等,或其药学上可接受的盐,其可用作药物,特别是作为活化凝血因子X抑制剂。
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公开(公告)号:US07737161B2
公开(公告)日:2010-06-15
申请号:US12320583
申请日:2009-01-29
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
IPC分类号: A61K31/444 , C07D491/048
CPC分类号: C07D491/04 , C07D213/75
摘要: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式(I)的缩合呋喃化合物:其中环X为苯,吡啶等; Y是任选取代的氨基,任选取代的环烷基,任选取代的芳基,任选取代的饱和杂环基,任选取代的不饱和杂环基; A是单键,低级亚烷基,低级亚烯基,低级亚烯基或氧原子; R3是氢等; 和R4为氢等,或其药学上可接受的盐,其可用作药物,特别是活性凝血因子X抑制剂。
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公开(公告)号:US07514449B2
公开(公告)日:2009-04-07
申请号:US10540878
申请日:2004-01-08
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
IPC分类号: A61K31/444 , C07D491/048
CPC分类号: C07D491/04 , C07D213/75
摘要: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式(I)的缩合呋喃化合物:其中环X为苯,吡啶等; Y是任选取代的氨基,任选取代的环烷基,任选取代的芳基,任选取代的饱和杂环基,任选取代的不饱和杂环基; A是单键,低级亚烷基,低级亚烯基,低级亚烯基或氧原子; R3是氢等; 和R4为氢等,或其药学上可接受的盐,其可用作药物,特别是活性凝血因子X抑制剂。
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公开(公告)号:US20090156803A1
公开(公告)日:2009-06-18
申请号:US12320583
申请日:2009-01-29
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Toru Iijima , Tatsuya Watanabe , Jun Murakami , Takashi Mitsui
IPC分类号: C07D491/048
CPC分类号: C07D491/04 , C07D213/75
摘要: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
摘要翻译: 本发明提供式(I)的缩合呋喃化合物:其中环X为苯,吡啶等; Y是任选取代的氨基,任选取代的环烷基,任选取代的芳基,任选取代的饱和杂环基,任选取代的不饱和杂环基; A是单键,低级亚烷基,低级亚烯基,低级亚烯基或氧原子; R3是氢等; 和R4为氢等,或其药学上可接受的盐,其可用作药物,特别是活性凝血因子X抑制剂。
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公开(公告)号:US07375119B2
公开(公告)日:2008-05-20
申请号:US10571900
申请日:2004-09-24
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Tatsuya Watanabe , Toru Iijima , Jun Murakami
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Tatsuya Watanabe , Toru Iijima , Jun Murakami
IPC分类号: A61K31/44 , C07D211/70 , C07D413/00
CPC分类号: C07C237/42 , C07D409/12
摘要: The present invention provides an amide-type carboxamide derivative of the formula [1]: wherein X is a group of the formula: —N═ or the formula: —CH═; R1 is a halogen atom, a lower alkyl group, and the like; R2 is a group of the formula: and the like; Y1 and Y2 are the same or different and each is a group selected from a halogen atom, a lower alkyl group, a lower alkoxy group, and the like; Ring A is phenyl group, and the like, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of FXa.
摘要翻译: 本发明提供式[1]的酰胺型羧酰胺衍生物:其中X是下式的基团:-N-或式:-CH-; R 1是卤素原子,低级烷基等; R 2是下式的基团:等等; Y 1和Y 2相同或不同,各自为选自卤素原子,低级烷基,低级烷氧基等的基团; 环A是可用作FXa抑制剂的苯基等,或其药学上可接受的盐。
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公开(公告)号:US20060287329A1
公开(公告)日:2006-12-21
申请号:US10571900
申请日:2004-09-24
申请人: Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Tatsuya Watanabe , Toru Iijima , Jun Murakami
发明人: Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Tatsuya Watanabe , Toru Iijima , Jun Murakami
IPC分类号: A61K31/50
CPC分类号: C07C237/42 , C07D409/12
摘要: The present invention provides an amide-type carboxamide derivative of the formula [1]: wherein X is a group of the formula: —N═ or the formula: —CH═; R1 is a halogen atom, a lower alkyl group, and the like; R2 is a group of the formula: and the like; Y1 and Y2 are the same or different and each is a group selected from a halogen atom, a lower alkyl group, a lower alkoxy group, and the like; Ring A is phenyl group, and the like, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of FXa.
摘要翻译: 本发明提供式[1]的酰胺型羧酰胺衍生物:其中X是下式的基团:-N-或式:-CH-; R 1是卤素原子,低级烷基等; R 2是下式的基团:等等; Y 1和Y 2相同或不同,各自为选自卤素原子,低级烷基,低级烷氧基等的基团; 环A是可用作FXa抑制剂的苯基等,或其药学上可接受的盐。
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公开(公告)号:US20060247273A1
公开(公告)日:2006-11-02
申请号:US10571904
申请日:2004-09-24
IPC分类号: A61K31/445
CPC分类号: C07D405/12 , C07D405/14
摘要: The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.
摘要翻译: 本发明提供式[1]的氨基甲酰基型苯并呋喃衍生物:其中环Z是下式的基团:等等; A是单键等; Y是环烷二基等; R 4和R 5相同或不同,各自为任选取代的低级烷基等; R 1是卤素原子等; 下式的环B是任选取代的苯环; R 3是氢原子。 等等,或其药学上可接受的盐,其可用作FXa抑制剂。
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