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    PROSTAGLANDIN DERIVATIVES
    3.
    发明公开
    PROSTAGLANDIN DERIVATIVES 有权
    前列腺素衍生物

    公开(公告)号：EP1211242A1

    公开(公告)日：2002-06-05

    申请号：EP00957064.9

    申请日：2000-09-08

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： SATO, Fumie ,  TANAMI, Tohru, c/o Taisho Pharmaceutical Co Ltd ,  TANAKA, Hideo, c/o Taisho Pharmaceutical Co Ltd ,  ONO, Naoya, c/o Taisho Pharmaceutical Co Ltd ,  YAGI, Makoto, c/o Taisho Pharmaceutical Co Ltd ,  HIRANO, Hitomi, c/o Taisho Pharmaceutical Co Ltd

    IPC分类号： C07C405/00 ,  A61K31/5575 ,  A61P9/10 ,  A61P27/06 ,  A61P25/20 ,  A61P43/00

    CPC分类号： C07C405/00 ,  C07C405/0016

    摘要： A prostaglandin derivative represented by the formula:
    wherein X is a halogen atom in the α- or β-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: O(CH 2 ) n ,

            S(O) p (CH 2 ) n ,



            O(CH 2 ) q O(CH 2 ) r ,



            O(CH 2 ) q S(O) p (CH 2 ) r ,



            S(O) p (CH 2 ) q S(O) p (CH 2 ) r

    or

            S(O) p (CH 2 ) q O(CH 2 ) r

    (wherein n is an integer of 1 to 5, p is 0, 1 or 2, q is an integer of 1 to 3, and r is 0 or 1),
    R 1 is a C 3-10 cycloalkyl group, a C 1-4 alkyl-C 3-10 cycloalkyl group, a C 3-10 cycloalkyl-C 1-4 alkyl group, a C 5-10 alkyl group, a C 5-10 alkenyl group, a C 5-10 alkynyl group or a bridged cyclic hydrocarbon group,
    R 2 is a hydrogen atom, a C 1-10 alkyl group or a C 3-10 cycloalkyl group, and
    m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    The present invention is to provide novel PG derivatives having an excellent PGD 2 -like agonistic activity and a sleep-inducing action.

    摘要翻译： 由下式表示的前列腺素衍生物：其中X是α-位或β-位的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，A是由下式表示的基团：O （CH2）n，S（O）p（CH2）n，O（CH2）qO（CH2）r，O（CH2）qS（O）p（CH2）r，S（O）p（CH2）qS ）p（CH 2）r或S（O）p（CH 2）q O（CH 2）r（其中n为1〜5的整数，p为0,1或2，q为1〜3的整数，r 是0或1），R 1是C 3-10环烷基，C 1-4烷基-C 3-10环烷基，C 3-10环烷基-C 1-4烷基，C 5-10烷基， C5-10烯基，C5-10炔基或桥连环烃基，R 2为氢原子，C1-10烷基或C3-10环烷基，m为0,1或2Ü ，其药学上可接受的盐或其水合物。 本发明提供具有优异的PGD 2样激动活性和睡眠诱导作用的新型PG衍生物。