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    • 72. 发明申请
    • Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
    • GPR119受体的调节剂和与之相关的疾病的治疗
    • US20140051714A1
    • 2014-02-20
    • US14113081
    • 2012-04-20
    • Robert M. Jones
    • Robert M. Jones
    • C07D401/14A61K45/06A61K31/506
    • C07D401/14A61K31/506A61K45/06
    • 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-基氧基)-5-氟-6-(2-甲基-6-(甲基磺酰基) 吡啶基氧基)嘧啶(化合物1)及其药学上可接受的盐,溶剂合物和水合物,其可用作单一药剂或与一种或多种另外的药剂如DPP-IV抑制剂,双胍类, α-葡萄糖苷酶抑制剂,胰岛素类似物,磺酰脲类,SGLT2抑制剂,氯噻嗪,噻唑烷二酮或抗糖尿病肽类似物,用于治疗例如选自以下的病症:GPR119-受体相关病症; 通过增加肠降血糖素的分泌而改善的状况; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。