发明名称 Substituted piperidinyl-pyridazinyl derivatives useful as SCD 1 inhibitors
摘要 The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
申请公布号 US9102669(B2) 申请公布日期 2015.08.11
申请号 US201214363051 申请日期 2012.12.05
申请人 Janssen Pharmaceutica NV 发明人 Yang Shyh-Ming;Kuo Gee-Hong;Gaul Micheal D.;Rano Thomas A.
分类号 C07D295/00;C07D417/14;C07D401/14;C07D413/14;C07D409/14 主分类号 C07D295/00
代理机构 代理人
主权项 1. A compound of formula (I) wherein R1 is selected from the group consisting of a is an integer from 0 to 3; each R2 is independently selected from the group consisting of halogen, C1-4alkyl, C1-4alkoxy, halogenated C1-2alkyl, and halogenated C1-2alkoxy; R3 is selected from the group consisting of wherein R4 is selected from the group consisting of hydrogen, halogen, C1-4alkyl, halogenated C1-2alkyl, —C1-2alkyl-OH, C1-4alkoxy, halogenated C1-2alkoxy, —C1-2alkyl-O—C1-2alkyl, —CO2H, —C(O)O—C1-4alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C1-2alkyl-OC(O)—C1-2alkyl, —NRARB, —C1-2alkyl-NRARB, —C(O)—NRARB, —C1-2alkyl-C(O)—NRARB and —NRA—C(O)—(C1-2alkyl); wherein R5 is selected from the group consisting of hydrogen, C1-4alkyl, —C2-4alkyl-OH, —C2-3alkyl-O—C1-2alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C2-3alkyl-OC(O)—C1-2alkyl, —C2-4alkyl-NRARB and —C1-2alkyl-C(O)NRARB; and wherein b is an integer from 0 to 2; wherein each R6 is independently selected from the group consisting of halogen, C1-4alkyl, halogenated C1-4alkyl, —C1-2alkyl-OH, C1-4alkoxy, halogenated C1-4alkoxy, —C1-2alkyl-O—C1-2alkyl, —CO2H, —C(O)O—C1-4alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C1-2alkyl-OC(O)—C1-2alkyl,—C(O)—NRARB, —C1-2alkyl-C(O)—NRARB, —NRARB, —C1-2alkyl-NRARB and —NRA—C(O)—C1-2alkyl; and wherein RA and RB are each independently selected from the group consisting of hydrogen and C1-2alkyl; alternatively RA and RB are taken together with the nitrogen atom to which they are bound to form piperidin-1-yl, piperazin-1-yl, morpholin-4-yl and pyrrolidin-1-yl; provided that when R3 is 3-methyl-1,2,4-thiadiazol-5-yl, then R1 is other than unsubstituted indoly-3-yl; or a pharmaceutically acceptable salt thereof.
地址 Beerse BE