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US 9,006,244 B2Granted
Liver X receptor modulators
AssigneeVitae Pharmaceuticals, Inc.
InventorsChengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
Life of this patent
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Abstract
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.
Claims49
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 is 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 monocyclic non-aromatic heterocycle, monocyclic heteroaromatic and alkyl group represented by R4 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;
- 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.
17 more elements
Dependencies are inferred from the claim text.