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1. 发明申请

US20110269960A1 TRIAZOLE DERIVATIVE 审中-公开
标题翻译：三唑衍生物
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）。

2. 发明授权

US08048898B2 Inhibitor of binding of S1P1 失效
标题翻译：抑制S1P1的结合
公开(公告)号：US08048898B2
公开(公告)日：2011-11-01
申请号：US12671401
申请日：2008-08-01
申请人： Naoya Ono , Fumiyasu Shiozawa , Tetsuya Yabuuchi , Hironori Katakai
发明人： Naoya Ono , Fumiyasu Shiozawa , Tetsuya Yabuuchi , Hironori Katakai
IPC分类号： C07D413/14 , C07D413/12 , C07D401/14 , C07D401/12 , C07D213/70 , C07D213/68 , C07D213/643 , A61K31/5377 , A61K31/496 , A61K31/4725 , A61K31/4709 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/44
CPC分类号： C07D213/64 , C07D213/68 , C07D213/70 , C07D213/71 , C07D239/34 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Y1 represents a nitrogen atom or a group represented by CRA, Y2 represents a nitrogen atom or a group represented by CRB, Y3 represents a nitrogen atom or a group represented by CRC, RA, RB and RC, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents an oxygen atom, etc., R1 represents a C1-C6 alkyl group, etc., R2 represents a C1-C6 alkyl group, etc., R3 represents an optionally substituted phenyl group, etc., R4 represents a hydrogen atom, etc., and R5 represents an optionally substituted phenyl group, etc.) has an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1), and is useful as a therapeutic agent for autoimmune diseases, rheumatoid arthritis, asthma, atopic dermatitis, rejection after organ transplantation, cancer, retinopathy, psoriasis, osteoarthritis, or age-related macular degeneration, etc.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐：（其中Y1表示氮原子或由CRA表示的基团，Y2表示氮原子或由CRB表示的基团，Y3表示氮原子或表示通过CRC，RA，RB和RC可以相同或不同，各自表示氢原子等（不包括Y1为CRA，Y2为CRB且Y3为CRC的情况），X为氧原子等 R1表示C1-C6烷基等，R2表示C1-C6烷基等，R3表示可以具有取代基的苯基等，R4表示氢原子等，R5表示任选取代的苯基等）对S1P与其受体Edg-1（S1P1）之间的结合具有抑制作用，并且可用作自身免疫性疾病，类风湿性关节炎，哮喘，特应性皮炎，器官移植后的排斥反应的治疗剂，癌症，视网膜病变，牛皮癣，骨关节炎或年龄相关黄斑变性等

3. 发明申请

US20100234594A1 INHIBITOR OF BINDING OF S1P1 失效
标题翻译： S1P1结合抑制剂
公开(公告)号：US20100234594A1
公开(公告)日：2010-09-16
申请号：US12671401
申请日：2008-08-01
申请人： Naoya Ono , Fumiyasu Shiozawa , Tetsuya Yabuuchi , Hironori Katakai
发明人： Naoya Ono , Fumiyasu Shiozawa , Tetsuya Yabuuchi , Hironori Katakai
IPC分类号： C07D413/12 , C07D239/34 , C07D401/12
CPC分类号： C07D213/64 , C07D213/68 , C07D213/70 , C07D213/71 , C07D239/34 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: (wherein Y1 represents a nitrogen atom or a group represented by CRA, Y2 represents a nitrogen atom or a group represented by CRB, Y3 represents a nitrogen atom or a group represented by CRC, RA, RB and RC, which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents an oxygen atom, etc., R1 represents a C1-C6 alkyl group, etc., R2 represents a C1-C6 alkyl group, etc., R3 represents an optionally substituted phenyl group, etc., R4 represents a hydrogen atom, etc., and R5 represents an optionally substituted phenyl group, etc.) has an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1), and is useful as a therapeutic agent for autoimmune diseases, rheumatoid arthritis, asthma, atopic dermatitis, rejection after organ transplantation, cancer, retinopathy, psoriasis, osteoarthritis, or age-related macular degeneration, etc.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐：（其中Y1表示氮原子或由CRA表示的基团，Y2表示氮原子或由CRB表示的基团，Y3表示氮原子或表示通过CRC，RA，RB和RC可以相同或不同，各自表示氢原子等（不包括Y1为CRA，Y2为CRB且Y3为CRC的情况），X为氧原子等 R1表示C1-C6烷基等，R2表示C1-C6烷基等，R3表示可以具有取代基的苯基等，R4表示氢原子等，R5表示任选取代的苯基等）对S1P与其受体Edg-1（S1P1）之间的结合具有抑制作用，并且可用作自身免疫性疾病，类风湿性关节炎，哮喘，特应性皮炎，器官移植后的排斥反应的治疗剂，癌症，视网膜病变，牛皮癣，骨关节炎或年龄相关黄斑变性等

4. 发明申请

US20070154428A1 Thiazole derivative 失效
标题翻译：噻唑衍生物
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。

5. 发明授权

US08022225B2 Triazole derivative 失效
标题翻译：三唑衍生物
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]。

6. 发明申请

US20100216787A1 THIAZOLE DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
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。

7. 发明申请

US20090131438A1 Triazole derivative 失效
标题翻译：三唑衍生物
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]。

8. 发明授权

US08022091B2 Triazole derivative 失效
标题翻译：三唑衍生物
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）。

9. 发明授权

US07994204B2 Binding inhibitor of sphingosine-1-phosphate 失效
标题翻译：鞘氨醇-1-磷酸的结合抑制剂
公开(公告)号：US07994204B2
公开(公告)日：2011-08-09
申请号：US12278477
申请日：2007-02-06
申请人： Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Takeshi Koami , Rie Nishikawa
发明人： Naoya Ono , Tetsuo Takayama , Fumiyasu Shiozawa , Hironori Katakai , Tetsuya Yabuuchi , Tomomi Ota , Takeshi Koami , Rie Nishikawa
IPC分类号： A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/5377 , C07D233/70 , C07D413/12 , C07D403/12 , C07D413/14 , C07D215/36 , C07D401/12
CPC分类号： C07D233/70 , C07D233/84 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes.A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].
摘要翻译：本发明的目的是提供对S1P与其受体Edg-1（S1P1）之间的结合具有抑制作用并且可用于制药目的的化合物。由式（I）表示的化合物或其药学上可接受的盐：[其中Ar表示含有一个或两个氮原子的单环杂环，A表示氧原子等，Y1，Y2和Y3表示碳原子或氮原子，R1表示氢原子，C1-C6烷基等，R2表示C1-C6烷基，C3-C8环烷基等，R3表示C1-C18烷基等 R4代表氢原子或C1-C6烷基，R5代表C1-C10烷基等]。

10. 发明授权

US07678810B2 Thiazole derivative 失效
标题翻译：噻唑衍生物
公开(公告)号：US07678810B2
公开(公告)日：2010-03-16
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： A61K31/4439 , C07D277/62 , C07D317/48
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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