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    ANTIPRURITIC AGENT
    2.
    发明公开
    ANTIPRURITIC AGENT 有权
    防腐剂

    公开(公告)号：EP1527781A1

    公开(公告)日：2005-05-04

    申请号：EP03784565.8

    申请日：2003-08-07

    申请人： TAISHO PHARMACEUTICAL CO., LTD ,  Sato, Fumie

    发明人： SATO, Fumie ,  ARAI, Iwao, c/o TAISHO PHARMACEUTICAL CO., LTD. ,  TAKANO, Norikazu, c/o TAISHO PHARMACEUTICAL CO.Ltd ,  TANAMI, Tohru, c/o TAISHO PHARMACEUTICAL CO., LTD. ,  YAGI, Makoto, c/o TAISHO PHARMACEUTICAL CO., LTD.

    IPC分类号： A61K31/5575 ,  A61P17/00 ,  A61P17/04 ,  A61P27/02

    CPC分类号： A61K31/5575 ,  Y10S514/861 ,  Y10S514/887

    摘要： A pharmaceutical preparation for preventing or treating pruritic symptoms which contains as an effective ingredient a prostaglandin derivative represented by formula [1]
    wherein X 1 and X 2 which are different from each other represent a hydrogen atom, a halogen atom or a hydroxyl group;

    Y is an ethylene group, a vinylene group or an ethynylene group; Z is the formula
    (CH 2 ) k A(CH 2 ) h B(CH 2 ) q ,
    (CH 2 ) k A(CH 2 ) r A'(CH 2 ) t ,
    (CH 2 ) k B(CH 2 ) h B'(CH 2 ) q
    or

    (CH 2 ) k-1 B'(CH 2 ) q-1 A'
    wherein k is an integer of 1 to 4, h is an integer of 0 to 4, q is an integer 1 to 4, r is an integer of 0 to 4, and t is an integer of 0 to 2;

    A and A' which may be the same or different represent an ethylene group, a vinylene group or an ethynylene group;
    B and B' which may be the same or different represent an oxygen atom or a group represented by the formula S(O) u wherein u is an integer of 0 to 2;
    W 1 is a hydroxyl group, a C 1-10 alkyloxy group, a C 3-10 cycloalkyloxy group, an aryloxy group or an arylalkyloxy group;
    W 2 is a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, a C 3-10 cycloalkyl group, a C 1-5 alkyl group substituted by C 3-10 cycloalkyl group(s), or a group represented by the formula
    wherein W 4 is a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group or a C 1-5 alkyl group substituted by C 3-10 cycloalkyl group(s); v is an integer of 0 to 4;
    W 3 is a hydrogen atom or a methyl group, or W 3 when taken together with W 2 and the adjacent carbon atom forms a C 3-10 cycloalkyl group; m is 0 or 1, a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译： 一种用于预防或治疗瘙痒症状的药物制剂，其含有式[1]所示的前列腺素衍生物作为有效成分，其中彼此不同的X 1和X 2表示氢原子，卤素原子或羟基; Y是亚乙基，亚乙烯基或亚乙炔基; Z是式（CH 2）k A（CH 2）h B（CH 2）q，（CH 2）k A（CH 2） 1B'（CH 2）q-1A'式中，k为1〜4的整数，h为0〜4的整数，q为1〜4的整数，r为0〜4的整数，t为整数 0到2; A和A'可以相同或不同，表示亚乙基，亚乙烯基或亚乙炔基; B和B'可以相同或不同，表示氧原子或由式S（O）u表示的基团，其中u是0-2的整数; W1是羟基，C1-10烷氧基，C3-10环烷氧基，芳氧基或芳基烷氧基; W2为C1-10烷基，C2-10烯基，C2-10炔基，C3-10环烷基，C3-10环烷基取代的C1-5烷基或基团 由下式表示：其中W4是C1-10烷基，C2-10链烯基，C2-10炔基或被C3-10环烷基取代的C1-5烷基; v是0至4的整数; W3是氢原子或甲基，或者W3与W2一起形成并且相邻的碳原子形成C3-10环烷基; m是0或1，其药学上可接受的盐或其水合物。