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    INHIBITOR OF BINDING OF S1P1
    3.
    发明授权
    INHIBITOR OF BINDING OF S1P1 有权
    S1P1约束力的抑制剂

    公开(公告)号：EP2177512B1

    公开(公告)日：2012-04-18

    申请号：EP08792064.1

    申请日：2008-08-01

    申请人： Taisho Pharmaceutical Co., Ltd.

    发明人： ONO, Naoya ,  SHIOZAWA, Fumiyasu ,  YABUUCHI, Tetsuya ,  KATAKAI, Hironori

    IPC分类号： C07D213/68 ,  C07D213/70 ,  C07D213/71 ,  C07D239/34 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D213/64

    CPC分类号： C07D213/64 ,  C07D213/68 ,  C07D213/70 ,  C07D213/71 ,  C07D239/34 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： Disclosed is a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has an inhibitory activity on the binding between S1P and a receptor thereof Edg-1(S1P1) and is therefore useful as a therapeutic agent for an autoimmune disease, rheumatoid arthritis, asthma, atopic dermatitis, rejection after organ transplantation, cancer, retinopathy, psoriasis, osteoarthritis, age-related macular degeneration or the like. (I) wherein Y1 represents a nitrogen atom or a group represented by the formula CRA; Y2 represents a nitrogen atom or a group represented by the formula CRB; Y3 represents a nitrogen atom or a group represented by the formula CRC; RA, RB and RC independently represent a hydrogen atom or the like (provided that a combination of CRA as Y1, CRB as Y2 and CRC as Y3 is excluded); X represents an oxygen atom or the like; R1 represents an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms or the like; R3 represents a phenyl group which may be substituted or the like; R4 represents a hydrogen atom or the like; and R5 represents a phenyl group which may be substituted or the like.

    INHIBITOR OF BINDING OF S1P1
    5.
    发明公开
    INHIBITOR OF BINDING OF S1P1 有权
    HEMMER DER S1P1-BINDUNG

    公开(公告)号：EP2177512A1

    公开(公告)日：2010-04-21

    申请号：EP08792064.1

    申请日：2008-08-01

    申请人： Taisho Pharmaceutical Co. Ltd.

    发明人： ONO, Naoya ,  SHIOZAWA, Fumiyasu ,  YABUUCHI, Tetsuya ,  KATAKAI, Hironori

    IPC分类号： C07D213/64 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/64 ,  A61P1/04 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

    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 Y 1 represents a nitrogen atom or a group represented by CR A , Y 2 represents a nitrogen atom or a group represented by CR B , Y 3 represents a nitrogen atom or a group represented by CR C , R A , R B and R C , which may be the same or different, each represent a hydrogen atom, etc. (excluding the case where Y 1 is CR A , Y 2 is CR B and Y 3 is CR C ), X represents an oxygen atom, etc., R 1 represents a C 1 -C 6 alkyl group, etc., R 2 represents a C 1 -C 6 alkyl group, etc., R 3 represents an optionally substituted phenyl group, etc., R 4 represents a hydrogen atom, etc., and R 5 represents an optionally substituted phenyl group, etc.) has an inhibitory effect on the binding between SIP and its receptor Edg-1(S1P 1 ), 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Y 1表示氮原子或由CR A表示的基团，Y 2表示氮原子或由CR B表示的基团，Y 3表示氮 原子或由CR C，RA，RB和RC表示的基团可以相同或不同，各自表示氢原子等（不包括Y 1为CR A，Y 2为CR B和Y 3的情况 是CR C），X表示氧原子等，R 1表示C 1〜C 6烷基等，R 2表示C 1〜C 6烷基等，R 3表示可以具有取代基的 苯基等，R 4表示氢原子等，R 5表示任意取代的苯基等）对SIP与其受体Edg-1（S1P1）的结合有抑制作用， 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，癌症，视网膜病变，银屑病 sis，骨关节炎或年龄相关性黄斑变性等。

    TRIAZOLE DERIVATIVE
    9.
    发明公开
    TRIAZOLE DERIVATIVE 有权
    TRIAZOLDERIVAT

    公开(公告)号：EP1988083A1

    公开(公告)日：2008-11-05

    申请号：EP07708069.5

    申请日：2007-02-05

    申请人： Taisho Pharmaceutical Co. Ltd.

    发明人： ONO, Naoya ,  TAKAYAMA, Tetsuo ,  SHIOZAWA, Fumiyasu ,  KATAKAI, Hironori ,  YABUUCHI, Tetsuya ,  OTA, Tomomi ,  YAGI, Makoto ,  SATO, Masakazu

    IPC分类号： C07D249/08 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61P1/04 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06

    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 (S1P 1 ), 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 -SO 2 -, or the like, R 1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R 1A represents a hydrogen atom or the like, R 2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R 3 represents an aryl group, R 4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R 5 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（S1P 1）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-SO 2表示的基团）或 R 1表示氢原子，具有1-6个碳原子的烷基等，R 1A表示氢原子等，R 2表示具有1-6个碳原子的烷基，具有 3-6个碳原子等，R 3表示芳基，R 4表示氢原子或具有1-6个碳原子的烷基，任选被羧基取代，R 5表示具有1个 -10个碳原子，具有3-8个碳原子的环烷基，任选取代的芳基等）。