10-HYDROXY-11-DIHYDROPROSTAGLANDIN ANALOGS AS SELECTIVE EP4 AGONISTS
    81.
    发明申请
    10-HYDROXY-11-DIHYDROPROSTAGLANDIN ANALOGS AS SELECTIVE EP4 AGONISTS 有权
    作为选择性EP4激动剂的10-羟基-11-二氢吡咯烷酮类似物

    公开(公告)号:US20070010495A1

    公开(公告)日:2007-01-11

    申请号:US11532404

    申请日:2006-09-15

    申请人: Yariv Donde

    发明人: Yariv Donde

    IPC分类号: A61K31/557 A61K31/66

    CPC分类号: C07D333/62

    摘要: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein the dashed line represents the presence or absence of a double bond; J is C═O or CHOH; A is —(CH2)6-, or cis —CH2CH═CH—(CH2)3-, wherein 1 or 2 carbons may be substituted with S or O; B is CO2H, or CO2R, CONR2, CONHCH2CH2OH, CON(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl; D is —(CH2)n-, —X(CH2)n, or —(CH2)nX-, wherein n is from 0 to 3 and X is S or O; and E is an aromatic or heteroaromatic moiety having from 0 to 4 substituents, said substituents each comprising from 1 to 6 non-hydrogen atoms is disclosed herein. Methods, compositions, and medicaments related thereto, as well as experimental results showing prostaglandin EP4 selective agonist activity for certain compounds disclosed herein, are also disclosed.

    摘要翻译: 包含或其药学上可接受的盐或其前药的化合物,其中虚线表示双键的存在或不存在; J为C-O或CHOH; A是 - (CH 2 CH 2)6 - 或顺式-CH 2 CH-CH-(CH 2 CH 2) )3,其中1或2个碳可以被S或O取代; B是CO 2 H,或CO 2 R,CONR 2,CONHCH 2 CH 2, OH,CON(CH 2 CH 2 OH)2,CH 2或OR,P(O )(OR)2,CONRSO 2 R,SONR 2,或R为H,C 1-6烷基, 烷基; D是 - (CH 2)n - , - (CH 2 CH 2)n - 或 - (CH X - ,其中n为0至3,X为S或O; 并且E是具有0至4个取代基的芳族或杂芳族部分,所述取代基各自包含1至6个非氢原子。 还公开了与其相关的方法,组合物和药物,以及显示本文公开的某些化合物的前列腺素EP4选择性激动剂活性的实验结果。