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    TRIAZOLE DERIVATIVE
    1.
    发明申请
    TRIAZOLE DERIVATIVE 审中-公开
    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）。

    Inhibitor of binding of S1P1
    2.
    发明授权
    Inhibitor of binding of S1P1 失效
    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

    INHIBITOR OF BINDING OF S1P1
    3.
    发明申请
    INHIBITOR OF BINDING OF S1P1 失效
    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

    Thiazole derivative
    4.
    发明申请
    Thiazole derivative 失效
    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。

    Triazole derivative
    5.
    发明授权
    Triazole derivative 失效
    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]。

    Triazole derivative
    7.
    发明申请
    Triazole derivative 失效
    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]。

    Triazole derivative
    8.
    发明授权
    Triazole derivative 失效
    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）。

    Thiazole derivative
    10.
    发明授权
    Thiazole derivative 失效
    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。