发明名称 Phosphatidylcholine transfer protein inhibitors
摘要 This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.;
申请公布号 US9126938(B2) 申请公布日期 2015.09.08
申请号 US201013390910 申请日期 2010.08.17
申请人 The Brigham and Women's Hospital, Inc. 发明人 Cohen David;Wagle Neil;Cuny Gregory D.;Xian Jun;Glicksman Marcie;Stein Ross L.;Shishova Ekaterina Y.
分类号 C07D239/42;A61K31/505;A61P1/16;A61P3/04;A61P3/10;A61P9/10;A61P11/06;C07D213/60;A61K31/44;C07D239/32 主分类号 C07D239/42
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof; wherein: X is N, Y is N, and Z is CH;X is N, Y is CH, and Z is N;R′, R″, and R′″ are each independently selected from H and C1-3 alkyl;R1, R2, R3, R4, and R5 are each independently selected from H, halogen, cyano, hydroxyl, carboxyl, carbamyl, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkenyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylcarbamyl, di-C1-6 alkylcarbamyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C1-6 alkylthio, C1-6 alkylsulfinyl, and C1-6 alkylsulfonyl;R6 and R7 are each C1-6 alkyl;n is 0;W is O;each R11 is independently selected from halogen, cyano, nitro, hydroxyl, carboxyl, carbamyl, amino, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 haloalkoxy, alkylamino, di-C1-6-alkylamino, C1-6 alkylcarbamyl, di-C1-6 alkylcarbamyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C1-6 alkylcarbonylamino, di-C1-6 alkylcarbonylamino, C1-6 alkylthio, C1-6 alkylsulfinyl, and C1-6 alkylsulfonyl provided that: when the compound has Formula I, W is O, X is N, Y is N, and Z is CR10, then the following provisos apply:(a) when R6 and R7 are each methyl, R10 is H, and R1, R2, R4, and R5 are H, then R3 is not methoxy or chloro; and(b) when R6 and R7 are each methyl and R10 is H, then at least one of R1, R2, R3, R4, and R5 is other than H.
地址 Boston MA US