[EN] ANTAGONISTS OF GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO<br/>[FR] ANTAGONISTES DU RÉCEPTEUR GPR119 ET TRAITEMENT DE TROUBLES ASSOCIÉS À CEUX-CI
申请人:ARENA PHARM INC
公开号:WO2014074700A1
公开(公告)日:2014-05-15
The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are antagonists of GPR119 useful in the treatment of, for example, a disorder selected from: obesity and diseases/conditions related to obesity such as congestive heart failure, polycystic ovarian syndrome, infertility, gastroesophageal reflux disease, cholelithiasis (gall stones), hernia, erectile dysfunction, urinary incontinence, chronic renal failure, lymphedema, osteoarthritis, hyperuricemia, lower back pain, stroke, headache, asthma, and immobility. In addition, the present antagonists of GPR119 are useful for treating non-alcoholic fatty liver disease, food-dependent Cushing's syndrome, and cancer (e.g., cancers of the esophagus, uterine lining, ovary, kidney, pancreas, and breast; leukemia, multiple myeloma, non-Hodgkin's lymphoma, and colorectal cancer).
本发明涉及公式I的化合物及其药物可接受的盐、溶剂化合物和水合物,它们是GPR119的拮抗剂,可用于治疗例如肥胖和与肥胖相关的疾病/病况,如充血性心力衰竭、多囊卵巢综合症、不孕症、胃食管反流病、胆石症(胆结石)、疝气、勃起功能障碍、尿失禁、慢性肾衰竭、淋巴水肿、骨关节炎、高尿酸血症、腰痛、中风、头痛、哮喘和固定性等疾病。此外,本发明的GPR119拮抗剂还可用于治疗非酒精性脂肪性肝病、食物依赖性库欣综合症和癌症(例如食管癌、子宫内膜癌、卵巢癌、肾癌、胰腺癌和乳腺癌;白血病、多发性骨髓瘤、非何杰金淋巴瘤和结肠直肠癌)。