发明名称 LIVER X RECEPTOR MODULATORS
摘要 Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
申请公布号 US2015336963(A1) 申请公布日期 2015.11.26
申请号 US201514721262 申请日期 2015.05.26
申请人 Vitae Pharmaceuticals, Inc. 发明人 Dong Chengguo;Fan Yi;Leftheris Katerina;Lotesta Stephen D.;Singh Suresh B.;Tice Colin M.;Zhao Wei;Zheng Yajun;Zhuang Linghang
分类号 C07D487/04;C07F7/18 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound represented by the following structural formula:or a pharmaceutically acceptable salt thereof, wherein: X is N or CRc; R1 is alkyl or —NRaRb; R2 is H; halogen; —CN; —NRC(O)R; —C(O)OR; —C(O)NRaRb; monocyclic heteroaromatic optionally substituted with one or more groups selected from alkyl, —CN, —NRC(O)R, —C(O)OR, —C(O)NRaRb and halogen; monocyclic non-aromatic heterocycle optionally substituted with one or more groups selected from alkyl, halogen, —CN and ═O; or alkyl optionally substituted by one or more groups selected from halogen, hydroxy, alkoxy, —NRaRb, —NRC(O)R, —NRC(O)O(alkyl), —NRC(O)N(R)2, —C(O)OR, thiol, alkylthiol, nitro, —CN, ═O, —OC(O)H, —OC(O)(alkyl), —OC(O)O(alkyl), —OC(O)N(R)2 and —C(O)NRaRb; R3 is alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, monocyclic non-aromatic heterocycle, monocyclic heteroaromatic or phenyl, wherein the phenyl, monocyclic non-aromatic heterocycle and monocyclic heteroaromatic group represented by R3 are optionally substituted with one or more groups selected from alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, nitro and —CN; R4 and R5 independently are halogen, —CN, —OR, —SR, —N(R)2, —C(O)R, —C(O)OR, —OC(O)O(alkyl), —C(O)O(haloalkyl), —OC(O)R, —C(O)N(R)2, —OC(O)N(R)2, —NRC(O)R, —NRC(O)O(alkyl), —S(O)R, —SO2R, —SO2N(R)2, —NRS(O)R, —NRSO2R, —NRC(O)N(R)2, —NRSO2N(R)2, haloalkyl, haloalkoxy, cycloalkoxy, cycloalkyl, monocyclic non-aromatic heterocycle, monocyclic heteroaromatic or alkyl, wherein the alkyl, monocyclic non-aromatic heterocycle and monocyclic heteroaromatic group represented by R4 or R5 are optionally substituted with one or more groups selected from —CN, —OR, —SR, —N(R)2, ═O, —C(O)R, —C(O)OR, —C(O)O(haloalkyl), —OC(O)R, —OC(O)O(alkyl), —C(O)N(R)2, —OC(O)N(R)2, —NRC(O)R, —NRC(O)O(alkyl), —S(O)R, —SO2R, —SO2N(R)2, —NRS(O)R, —NRSO2R, —NRC(O)N(R)2 and —NRSO2N(R)2; R6 is H, halogen, —CN, —OR, —SR, —N(R)2, —C(O)R, —C(O)OR, —OC(O)O(alkyl), —C(O)O(haloalkyl), —OC(O)R, —C(O)N(R)2, —OC(O)N(R)2, —NRC(O)R, —NRC(O)O(alkyl), —S(O)R, —SO2R, —SO2N(R)2, —NRS(O)R, —NRSO2R, —NRC(O)N(R)2, —NRSO2N(R)2, haloalkyl, haloalkoxy, cycloalkoxy, cycloalkyl or alkyl, wherein the alkyl group represented by R6 is optionally substituted with one or more groups selected from —CN, —OR, —SR, —N(R)2, ═O, —C(O)R, —C(O)OR, —C(O)O(haloalkyl), —OC(O)R, —OC(O)O(alkyl), —C(O)N(R)2, —OC(O)N(R)2, —NRC(O)R, —NRC(O)O(alkyl), —S(O)R, —SO2R, —SO2N(R)2, —NRS(O)R, —NRSO2R, —NRC(O)N(R)2 and —NRSO2N(R)2; or R5 and R6, taken together with the carbon atoms to which they are bonded, form a moncyclic non-aromatic heterocycle opotionally substituted with one or more groups selected from alkyl, halogen, hydroxyalkyl, alkoxyalkyl, haloalkyl and ═O; and each R independently is H or alkyl; Ra and Rb are independently H, alkyl or Ra and Rb can be taken together with the nitrogen to which they are attached to form a monocyclic non-aromatic heterocycle; and Rc is H, alkyl, or halogen.
地址 Fort Washington PA US