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公开(公告)号:US20110288293A1
公开(公告)日:2011-11-24
申请号:US13142230
申请日:2009-12-25
申请人: Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
发明人: Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
IPC分类号: C07D413/12 , C07D401/12 , C07D405/12 , C07D217/24 , C07D409/12 , C07D471/04 , C07D401/06 , C07D217/16 , C07D417/12
CPC分类号: C07D217/16 , C07D217/18 , C07D217/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用,因此可用作哮喘,特应性皮炎和过敏性鼻炎等过敏性疾病的预防或治疗。
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公开(公告)号:US20070154428A1
公开(公告)日:2007-07-05
申请号:US10591614
申请日:2005-03-04
申请人: Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
发明人: Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
IPC分类号: A61K8/49 , A61K31/5377 , A61K31/496 , A61K31/4709 , A61K31/454 , A61K31/427 , C07D417/02
CPC分类号: A61K8/49 , A61Q7/00 , C07D417/04 , C07D417/06 , C07D417/14
摘要: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
摘要翻译: 由下式表示的噻唑咪唑衍生物或其药学上可接受的盐,以及ALK5抑制剂,秃发治疗剂或具有上述作为活性成分的毛发生长剂,其中:X 1和X 2 2个彼此不同,表示硫原子或碳原子; R 1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R 2表示氢原子,卤素原子,具有1至6个碳原子的烷基,具有1至5个被1至5个卤素原子取代的碳原子的烷基,具有1个 至6个碳原子,具有1至5个碳原子的烷酰基或具有1至6个碳原子的羟烷基,A表示由下式表示的基团。 本发明提供了抗ALK5的抑制物质,其为TGF-β1型受体,并且基于其新的活性提供毛发生长刺激剂或毛发生长剂。
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公开(公告)号:US09181229B2
公开(公告)日:2015-11-10
申请号:US14004997
申请日:2012-03-15
申请人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
发明人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
IPC分类号: C07D413/04 , C07D403/04 , C07D417/04 , C07D413/14
CPC分类号: C07D413/04 , C07D403/04 , C07D413/14 , C07D417/04
摘要: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
摘要翻译: 提供与FKBP12或其药学上可接受的盐结合的新化合物,以及可用于预防或治疗脱发的新治疗剂,其包含那些化合物或其药学上可接受的盐。 具体地,提供由式(1)表示的化合物[其中R 1表示下式(2)或(3)]或其药学上可接受的盐。
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公开(公告)号:US08022225B2
公开(公告)日:2011-09-20
申请号:US11659103
申请日:2005-08-04
申请人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
发明人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
IPC分类号: C07D249/12 , C07D249/08
CPC分类号: C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].
摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。
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公开(公告)号:US20100216787A1
公开(公告)日:2010-08-26
申请号:US12644594
申请日:2009-12-22
申请人: Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
发明人: Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
IPC分类号: A61K31/426 , C07D417/14 , A61K31/427 , A61K31/4439 , C07D417/04 , A61K31/428 , A61K31/5377 , A61K31/454 , C07D277/24 , C07D277/22 , A61P1/16 , A61P17/00 , A61P13/12
CPC分类号: A61K8/49 , A61Q7/00 , C07D417/04 , C07D417/06 , C07D417/14
摘要: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
摘要翻译: 由下式表示的噻唑咪唑衍生物或其药学上可接受的盐,以及ALK5抑制剂,秃发治疗剂或具有上述作为活性成分的毛发生长剂,其中:X1和X2彼此不同,表示 硫原子或碳原子; R1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R2表示氢原子,卤素原子,碳原子数1〜6的烷基,碳原子数1〜5的碳原子数1〜5的烷基,碳原子数1〜6的烷氧基,烷氧基 具有1至5个碳原子,或具有1至6个碳原子的羟烷基,A表示由下式表示的基团。 本发明提供一种抗ALK5抑制物质,其为TGF- I型受体,并且基于其新的活性提供毛发生长兴奋剂或毛发生长剂。
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公开(公告)号:US20090131438A1
公开(公告)日:2009-05-21
申请号:US11659103
申请日:2005-08-04
申请人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
发明人: Naoya Ono , Masakazu Sato , Fumiyasu Shiozawa , Makoto Yagi , Tetsuya Yabuuchi , Tetsuo Takayama , Hironori Katakai
IPC分类号: A61K31/4196 , A61P37/00 , A61P29/00 , A61P17/06 , C07D249/12 , C07D401/12 , C07D403/12 , C07D413/12 , A61K31/5377 , A61K31/454
CPC分类号: C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].
摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。
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公开(公告)号:US08461329B2
公开(公告)日:2013-06-11
申请号:US13142230
申请日:2009-12-25
申请人: Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
发明人: Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
IPC分类号: C07D413/12 , C07D401/12 , C07D405/12 , C07D217/24
CPC分类号: C07D217/16 , C07D217/18 , C07D217/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用,因此可用作哮喘,特应性皮炎和过敏性鼻炎等过敏性疾病的预防或治疗。
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公开(公告)号:US20130096310A1
公开(公告)日:2013-04-18
申请号:US13805944
申请日:2011-06-22
IPC分类号: C07D217/18
CPC分类号: C07D217/18 , C07D217/20
摘要: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a pharmaceutical.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用,因此可用作药物。
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公开(公告)号:US20110269960A1
公开(公告)日:2011-11-03
申请号:US13180011
申请日:2011-07-11
申请人: Naoya ONO , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
发明人: Naoya ONO , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
IPC分类号: C07D249/12 , C07D413/12 , C07D487/04 , C07D491/113 , C07D401/12 , C07D417/14 , C07D249/08 , C07D403/12 , C07D409/12 , C07D405/12 , C07D409/14 , C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14
CPC分类号: C07D249/08
摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).
摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。
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公开(公告)号:US08022091B2
公开(公告)日:2011-09-20
申请号:US12278054
申请日:2007-02-05
申请人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
发明人: Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Makoto Yagi , Masakazu Sato
IPC分类号: A01N43/64 , A61K31/41 , C07D249/12
CPC分类号: C07D249/08
摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).
摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。
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