申请人:Donde Yariv
公开号:US20070010495A1
公开(公告)日:2007-01-11
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 —(CH
2
)
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
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.
本文披露了一种化合物或其药学上可接受的盐或前药,其中虚线表示有无双键;J为C═O或CHOH;A为—(CH2)6-,或顺式—CH2CH═CH—(CH2)3-,其中1或2个碳原子可以被S或O取代;B为CO2H,或CO2R,CONR2,CONHCH2CH2OH,CON(CH2CH2OH)2,CH2OR,P(O)(OR)2,CONRSO2R,SONR2,或R为H,C1-6烷基;D为—(CH2)n-,—X(CH2)n,或—(CH2)nX-,其中n为0到3,X为S或O;E为具有0到4个取代基的芳香或杂环芳基,所述取代基每个包含1到6个非氢原子。本文还披露了与之相关的方法、组合物和药物,以及实验结果,显示了某些本文披露的化合物的前列腺素EP4选择性激动剂活性。