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    Thiazole derivative
    2.
    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
    3.
    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。

    Aminobenzoic acid derivatives
    8.
    发明授权
    Aminobenzoic acid derivatives 失效
    氨基苯甲酸衍生物

    公开(公告)号：US06720424B1

    公开(公告)日：2004-04-13

    申请号：US10019525

    申请日：2002-01-02

    申请人： Hisaya Wada ,  Hajime Asanuma ,  Tetsuo Takayama ,  Masakazu Sato ,  Takehiro Yamagishi ,  Masabumi Shibuya

    发明人： Hisaya Wada ,  Hajime Asanuma ,  Tetsuo Takayama ,  Masakazu Sato ,  Takehiro Yamagishi ,  Masabumi Shibuya

    IPC分类号： C07D21172

    CPC分类号： C07D213/80 ,  C07C235/24 ,  C07C235/38 ,  C07C317/50 ,  C07C323/63 ,  C07C2601/02

    摘要： Aminobenzoic acid derivatives represented by Formula (1) as follows: (wherein, R1 represents a hydrogen atom, a C1-6alkyl group, or the like; R2 represents a hydrogen atom, a C1-6alkyl group, or the like; R3 represents a C8-25alkyl group, or the like; R4 represents a hydrogen atom or a group represented by OR9 or CO2R10 (wherein R9 and R10 represent a hydrogen atom or a C1-6 alkyl group); A represents a group represented by S(O)qR15 (wherein q is 0, 1, or 2, R15 represents a C1-6alkyl group, a phenyl C1-3alkyl group, or a group represented by (CH2)mOR16 (wherein m is 2 or 3, and R16 represents a hydrogen atom or a methoxymethyl group), or the like; X represents O, a single bond, CH═CH, or a group represented by NR27 (wherein R27 represents a hydrogen atom or a t-butoxycarbonyl group); Y represents O, CONH, NHCO, or a group represented by NR28 (wherein R28 represents a hydrogen atom or a t-butoxycarbonyl group); and n is an integer of 0 to 15) or pharmaceutically acceptable salts of the same are employed as VEGF receptor antagonists, and in particular as therapeutic agents for the diseases in which VEGF is involved.

    摘要翻译： 式（1）表示的氨基苯甲酸衍生物如下：（其中，R 1表示氢原子，C 1-6烷基等; R 2表示氢原子，C 1-6烷基或 R 3表示氢原子或由OR 9或CO 2 R 10表示的基团（其中R 9和R 10分别表示碳原子数3〜10的烷基， >表示氢原子或C 1-6烷基）; A表示由S（O）q R 15表示的基团（其中q为0,1或2，R 15为C 1-6烷基， 苯基C 1-3烷基或由（CH 2）mOR 16表示的基团（其中m为2或3，R 16表示氢原子或甲氧基甲基）等; X表示O， 单键，CH = CH或由NR 27表示的基团（其中R 27表示氢原子或叔丁氧基羰基）; Y表示O，CONH，NHCO或由NR a表示的基团， 28>（其中R 28表示氢原子或叔丁氧基羰基），n为0〜15的整数）或药物 其可接受的盐用作VEGF受体拮抗剂，特别是作为涉及VEGF的疾病的治疗剂。

    Method for selective preparation of aryl 5-thio-β-D-aldohexopyranosides
    10.
    发明授权
    Method for selective preparation of aryl 5-thio-β-D-aldohexopyranosides 失效
    芳基5-硫代-β-D-吡喃半乳糖苷的选择性制备方法

    公开(公告)号：US07250522B2

    公开(公告)日：2007-07-31

    申请号：US10521809

    申请日：2003-08-08

    申请人： Masakazu Sato ,  Hiroyuki Kakinuma ,  Hajime Asanuma

    发明人： Masakazu Sato ,  Hiroyuki Kakinuma ,  Hajime Asanuma

    IPC分类号： C07D335/02

    CPC分类号： C07H15/203 ,  C07H15/20

    摘要： The present invention provides a method for preparing an aryl 5-thio-β-D-aldohexopyranoside derivative of Formula (III), which comprises reacting a 5-thio-D-aldohexopyranose derivative of Formula (I) with Ar-OH of Formula (II) in the presence of a phosphine represented by PR11R12R13 and an azo reagent represented by R21—N═N—R22 in accordance with the following scheme

    摘要翻译： 本发明提供了制备式（III）的5-硫代-β-D-吡喃葡萄糖苷衍生物的方法，该方法包括使式（I）的5-硫代-D-去二羟基吡喃糖衍生物与式（I）的Ar-OH反应， II）在由PR 11和12 R 12表示的膦和由R 21表示的偶氮试剂存在下， SUP> -NNR <22>根据以下方案