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    COMPOUND HAVING TAFIA INHIBITORY ACTIVITY
    11.
    发明申请
    COMPOUND HAVING TAFIA INHIBITORY ACTIVITY 审中-公开
    具有TAFIA抑制活性的化合物

    公开(公告)号：US20110213143A1

    公开(公告)日：2011-09-01

    申请号：US13126685

    申请日：2009-10-28

    申请人： Hideaki Amada ,  Daisuke Matsuda ,  Masahiro Bohno ,  Shiuji Saito ,  Ayako Bohno

    发明人： Hideaki Amada ,  Daisuke Matsuda ,  Masahiro Bohno ,  Shiuji Saito ,  Ayako Bohno

    IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D471/14

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula —(CH2)—, the formula —(CH2)2—, an oxygen atom, a nitrogen atom or a single bond; Y is the formula —(CH2)3—NH—R3, the formula —(CH2)4—NH—R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula —CO2R4; R4 is a C1-6 alkyl group, the formula —CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.

    摘要翻译： 提供具有优异TAFIa抑制活性的化合物。 具体地，提供由下式（I）表示的化合物或其药学上可接受的盐：其中A是苯环或吡啶环; X是式 - （CH 2） - ，式 - （CH 2）2 - ，氧原子，氮原子或单键; Y是式 - （CH2）3-NH-R3，式 - （CH2）4-NH-R3或2-氨基吡啶基; R 3是氢原子，C 1-6烷基或式-CO 2 R 4; R4是C1-6烷基，式-CHR5OC（O）R6或具有由下式Ia表示的结构的取代基; R5是C1-6烷基; R6是C1-6烷基，C3-8环烷基或苯基; R7是C1-6烷基或苯基; R1是氢原子，卤素原子，被1-3个卤素原子取代的C1-4烷基，C1-10烷基，C1-8烷氧基，C3-8环烷基，C3-8环烷氧基 基团，C4-14环烷基烷基或苯基; R2是CO2R8或四唑基; R8是氢原子，C1-10烷基或具有由下式Ib或Ic表示的结构的取代基; m和n分别为0或1的整数。

    Thiazole derivative
    12.
    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。

    Thiazole derivative
    13.
    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。