[EN] MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] MODULATEURS DU RÉCEPTEUR GPR119 ET TRAITEMENT DE TROUBLES LIÉS À CELUI-CI
申请人:ARENA PHARM INC
公开号:WO2012145604A1
公开(公告)日:2012-10-26
The present invention relates to the GPR119 agonist, 4-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yloxy)-5-fluoro-6-(2-methyl-6-(methylsulfonyl)pyridin-3-yloxy)pyrimidine (Compound 1): and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing the secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
本发明涉及GPR119激动剂4-(1-(5-乙基嘧啶-2-基)哌啶-4-氧基)-5-氟-6-(2-甲基-6-(甲基磺酰基)吡啶-3-氧基)嘧啶(化合物1)及其药学上可接受的盐、溶剂化合物和水合物,这些化合物可用作单一药物或与一个或多个其他药物如DPP-IV抑制剂、双胍类药物、α-葡萄糖苷酶抑制剂、胰岛素类似物、磺脲类药物、SGLT2抑制剂、甲基磺酰基脲、噻唑烷二酮或抗糖尿病肽类似物联合使用,用于治疗例如与GPR119受体相关的疾病;通过增加肠促胰岛素分泌改善的疾病;通过增加血液肠促胰岛素水平改善的疾病;低骨量的疾病;神经系统疾病;代谢相关的疾病;2型糖尿病;肥胖症及其相关并发症。