915100-66-2Relevant articles and documents
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes
Li, Shiliang,Qin, Chun,Cui, Shichao,Xu, Hongling,Wu, Fangshu,Wang, Jiawei,Su, Mingbo,Fang, Xiaoyu,Li, Dan,Jiao, Qian,Zhang, Ming,Xia, Chunmei,Zhu, Lili,Wang, Rui,Li, Jia,Jiang, Hualiang,Zhao, Zhenjiang,Li, Jingya,Li, Honglin
, p. 2348 - 2361 (2019)
Poor medication adherence is one of the leading causes of suboptimal glycaemic control in approximately half of the patients with type 2 diabetes mellitus (T2DM). Long-acting antidiabetic drugs are clinically needed for improving patients' compliance. Dipeptidyl peptidase-4 (DPP-4) inhibitors play an increasingly important role in the treatment of T2DM because of their favorable properties of weight neutrality and hypoglycemia avoidance. Herein, we report the successful discovery and scale-up synthesis of compound 5, a structurally novel, potent, and long-acting DPP-4 inhibitor for the once-weekly treatment of T2DM. Inhibitor 5 has fast-associating and slow-dissociating binding kinetics profiles as well as slow clearance rate and long terminal half-life pharmacokinetic properties. A single-dose oral administration of 5 (3 mg/kg) inhibited >80% of DPP-4 activity for more than 7 days in diabetic mice. The long-term antidiabetic efficacies of 5 (10 mg/kg, qw) were better than those of the once-weekly trelagliptin and omarigliptin, especially in decreasing the hemoglobin A1c level.
Preparation method of 2,3-dihydro-1H-benzo[f] chromane-2-amine derivative
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Paragraph 0158; 0163-0164, (2019/10/01)
The invention provides a preparation method of a (2S, 3R)-2-amidogen-3-(2,4,5-trifluorophenyl)-9-methoxyl-2,3-dihydro-1H-benzo[f] chromane-8 bit substitutive derivative shown as a formula I shown in the accompanying drawing, wherein R is selected from H, OCH3, CN, SO2CH3 and NHSO2CH3. The method has the advantages that the yield is high; the purification is convenient; the cost is low, and the like.
Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative
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Paragraph 0130; 0131; 0132; 0133, (2016/10/09)
The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.