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11. 发明授权

US07375119B2 Amide type carboxamide derivative 失效
标题翻译：酰胺型羧酰胺衍生物
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。

12. 发明申请

US20060287329A1 Amide type carboxamide derivative 失效
标题翻译：酰胺型羧酰胺衍生物
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。

13. 发明申请

US20100204218A1 FUSED BICYCLIC COMPOUND 有权
标题翻译：熔融双相化合物
公开(公告)号：US20100204218A1
公开(公告)日：2010-08-12
申请号：US12671479
申请日：2008-07-21
申请人： Yoichi Takahashi , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iijima
发明人： Yoichi Takahashi , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iijima
IPC分类号： A61K31/536 , C07D265/14 , C07D307/94 , A61K31/352 , A61P9/12 , A61P9/06 , A61P9/00
CPC分类号： C07D265/16 , C07D311/20 , C07D311/58 , C07D311/96 , C07D405/14 , C07D413/04
摘要： The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc., R2 and R3 are (a) the same of different and a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, (b) combined each other to form an oxo group or (c) combined each other at its terminal together with the adjacent carbon atom to form a cycloalkyl group, X is a group of ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) a hydrogen atom, (b) a cyano group, (c) a halogen atom, (d) an alkyl group, (e) an alkenyl group, (f) a cycloalkyl group (g) an alkanoyl group, (h) a carbamoyl group or (i) a cycloalkenyl group, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, which is useful as an antihypertensive agent etc.
摘要翻译：本发明提供了对式[I]所示的对矿物质类皮质激素（MR）的受体具有亲和性的新的稠合双环化合物：其中环A是具有取代基R 1的苯环，与相邻的6元杂环，并且还可任选地具有除R1以外的取代基，R 1是烷基磺酰基氨基等，R 2和R 3是（a）不同的，和氢原子，烷基或取代或未取代的芳基，（b）彼此组合以形成氧代基团，或（c）在其末端与相邻的碳原子一起相互结合形成环烷基，X是一个= N - ， - C（R 4） - 或 - CH（R4） - ，R4是（a）氢原子，（b）氰基，（c）卤原子，（d）烷基，（e）烯基，（f）环烷基 g）烷酰基，（h）氨基甲酰基或（i）环烯基，Ar是任选取代的芳环基，虚线表示存在或不存在双键或其药学上可接受的盐，其可用作抗高血压剂等。

14. 发明申请

US20090156803A1 Condensed furan compounds 失效
标题翻译：稠化呋喃化合物
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。

15. 发明授权

US07531537B2 Benzofuran derivative 失效
标题翻译：苯并呋喃衍生物
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。

16. 发明申请

US20060247273A1 Carbamoyl-type benzofuran derivatives 失效
标题翻译：氨基甲酰型苯并呋喃衍生物
公开(公告)号：US20060247273A1
公开(公告)日：2006-11-02
申请号：US10571904
申请日：2004-09-24
申请人： Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Toru Iijima , Jun Murakami
发明人： Takayuki Kawaguchi , Hidenori Akatsuka , Masamichi Morimoto , Toru Iijima , Jun Murakami
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。

17. 发明授权

US08975252B2 Morpholine derivative 有权
标题翻译：吗啉衍生物
公开(公告)号：US08975252B2
公开(公告)日：2015-03-10
申请号：US12664637
申请日：2008-06-16
申请人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： A61K31/535 , C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
摘要翻译：本发明提供式[I]的吗啉衍生物。其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。这些化合物可用作肾素抑制剂。

18. 发明授权

US08258131B2 Fused bicyclic compound 有权
标题翻译：稠合双环化合物
公开(公告)号：US08258131B2
公开(公告)日：2012-09-04
申请号：US12671479
申请日：2008-07-21
申请人： Yoichi Takahashi , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iijima
发明人： Yoichi Takahashi , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iijima
IPC分类号： C07D265/16 , A61K31/352 , A61K31/353
CPC分类号： C07D265/16 , C07D311/20 , C07D311/58 , C07D311/96 , C07D405/14 , C07D413/04
摘要： The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc., R2 and R3 are (a) the same of different and a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, (b) combined each other to form an oxo group or (c) combined each other at its terminal together with the adjacent carbon atom to form a cycloalkyl group, X is a group of ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) a hydrogen atom, (b) a cyano group, (c) a halogen atom, (d) an alkyl group, (e) an alkenyl group, (f) a cycloalkyl group (g) an alkanoyl group, (h) a carbamoyl group or (i) a cycloalkenyl group, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, which is useful as an antihypertensive agent etc.
摘要翻译：本发明提供了对式[I]所示的对矿物质类皮质激素（MR）的受体具有亲和性的新的稠合双环化合物：其中环A是具有取代基R 1的苯环，与相邻的6元杂环，并且还可任选地具有除R1以外的取代基，R 1是烷基磺酰基氨基等，R 2和R 3是（a）不同的，和氢原子，烷基或取代或未取代的芳基，（b）彼此组合以形成氧代基团，或（c）在其末端与相邻的碳原子一起相互结合形成环烷基，X是一个= N - ， - C（R 4） - 或 - CH（R4） - ，R4是（a）氢原子，（b）氰基，（c）卤原子，（d）烷基，（e）烯基，（f）环烷基 g）烷酰基，（h）氨基甲酰基或（i）环烯基，Ar是任选取代的芳环基，虚线表示存在或不存在双键或其药学上可接受的盐，其可用作抗高血压剂等。

19. 发明授权

US07605158B2 Carbamoyl-type benzofuran derivatives 失效
标题翻译：氨基甲酰型苯并呋喃衍生物
公开(公告)号：US07605158B2
公开(公告)日：2009-10-20
申请号：US10571904
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： A61K31/5355 , A61K31/443 , C07D413/04 , C07D401/12 , C07D307/85
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; R4和R5相同或不同，各自为任选取代的低级烷基等; R1是卤素原子等; 下式的环B是任选取代的苯环; R3为氢原子。等等，或其药学上可接受的盐，其可用作FXa抑制剂。

20. 发明申请

US20130029979A1 FUSED BICYCLIC COMPOUND 有权
标题翻译：熔融双相化合物
公开(公告)号：US20130029979A1
公开(公告)日：2013-01-31
申请号：US13561662
申请日：2012-07-30
申请人： Yoichi TAKAHASHI , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iljima
发明人： Yoichi TAKAHASHI , Nobumasa Awai , Hidenori Akatsuka , Takayuki Kawaguchi , Toru Iljima
IPC分类号： C07D265/16 , C07D311/04 , A61K31/352 , C07D413/04 , A61P9/06 , C07D405/04 , A61K31/4433 , A61P9/12 , A61P9/04 , A61K31/536 , C07D307/94
CPC分类号： C07D265/16 , C07D311/20 , C07D311/58 , C07D311/96 , C07D405/14 , C07D413/04
摘要： Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: wherein ring A is benzene having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is alkylsulfonylamino, etc., R2 and R3 are (a) the same of different and are hydrogen, alkyl, or optionally substituted aryl, or (b) combined with each other to form an oxo group or (c) combined with each other at its terminal together with the adjacent carbon atom to form cycloalkyl, X is ═N—, ═C(R4)— or —CH(R4)—, R4 is (a) hydrogen, (b) cyano, (c) halogen, (d) alkyl, (e) alkenyl, (f) cycloalkyl, (g) alkanoyl, (h) carbamoyl, or (i) cycloalkenyl, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, useful e.g. as an antihypertensive agent.
摘要翻译：具有式[I]的矿物质类皮质激素受体（MR）的亲和性的稠合双环化合物：其中环A是具有取代基R 1的苯，与相邻的6元杂环稠合，并且进一步任选具有除 R 1，R 1是烷基磺酰基氨基等，R 2和R 3是（a）不同的并且是氢，烷基或任选取代的芳基，或（b）彼此结合形成氧代基或（c）与 X是= N - ， - C（R4） - 或-CH（R4） - ，R4是（a）氢，（b）氰基，（c）卤素，（d）烷基，（e）烯基，（f）环烷基，（g）烷酰基，（h）氨基甲酰基或（i）环烯基，Ar是任选取代的芳族环状基团，虚线表示存在或不存在双键或其药学上可接受的盐，例如，作为抗高血压药。

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