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    • 8. 发明申请
    • 10-HYDROXY-11-DIHYDROPROSTAGLANDIN ANALOGS AS SELECTIVE EP4 AGONISTS
    • 作为选择性EP4激动剂的10-羟基-11-二氢吡咯烷酮类似物
    • WO2005100339A1
    • 2005-10-27
    • PCT/US2005/010124
    • 2005-03-25
    • ALLERGAN, INC.DONDE, Yariv
    • DONDE, Yariv
    • C07D333/60
    • C07D333/62
    • A compound comprising formula I (I) 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 -CH 2 CH=CH-(CH 2 ) 3 -, wherein 1 or 2 carbons may be substituted with S or O; B is CO 2 H, or CO 2 R, CONR 2 , CONHCH 2 CH 2 OH, CON(CH 2 CH 2 OH) 2 , CH 2 OR, P(O)(OR) 2 , CONRSO 2 R, SONR 2 , or formula II (II), R is H, C 1-6 alkyl; D is -(CH 2 ) n -, -X(CH 2 ) n , or -(CH 2 ) n X-, 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.
    • 包含式I(I)或其药学上可接受的盐或前药的化合物,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)6 - 或顺式-CH 2 CH = CH-(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 OR,P(O)(OR)2,CONRSO 2 R,SONR 2或式II(II) D是 - (CH 2)n - , - X(CH 2)n或 - (CH 2)n 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。