1226781-80-1Relevant articles and documents
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes
Zhang, Chen,Ye, Fei,Wang, Jianmin,He, Ping,Lei, Ming,Huang, Longbin,Huang, Anbang,Tang, Pingming,Lin, Hongjun,Liao, Yuting,Liang, Yong,Ni, Jia,Yan, Pangke
, p. 7108 - 7126 (2020)
In the present work, a novel series of trifluoromethyl-substituted tetrahydropyran derivatives were rationally designed and synthesized as potent DPP-4 inhibitors with significantly improved duration time of action over current commercially available DPP-4 inhibitors. The incorporation of the trifluoromethyl group on the 6-position of the tetrahydropyran ring of omarigliptin with the configuration of (2R,3S,5R,6S) not only significantly improves the overall pharmacokinetic profiles in mice but also maintains comparable DPP-4 inhibition activities. Further preclinical development of compound 2 exhibited its extraordinary efficacy in vivo and good safety profile. Clinical studies of compound 2 (Haisco HSK7653) are now ongoing in China, which revealed that inhibitor 2 could serve as an efficient candidate with a once-biweekly therapeutic regimen.
Amino six member ring derivatives and their use in medicine (by machine translation)
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, (2017/09/20)
The invention relates to a six-member ring amino derivatives and its application in medicine, specifically relates to the general formula (I) as shown by the six-member ring of the amino derivative or its stereoisomer, pharmaceutically acceptable salt, prodrug, pharmaceutical composition containing the derivative of the dipeptidyl peptidase IV and the preparation (dPP CGI-iV) inhibitors of their medical use, wherein the general formula (I) definition of each substituent in the definition of the description of the same. (by machine translation)
Preparation method for 2-formyl chloride-2,4,5,6-tetrahydropyrrole[3,4-c]pyrazole benzene sulfonate
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Paragraph 0052, (2016/10/07)
The invention discloses a preparation method for 2-formyl chloride-2,4,5,6-tetrahydropyrrole[3,4-c]pyrazole benzene sulfonate. The preparation method comprises the following steps: (1) adding a solvent A and dimethyl formamide-dimethyl adipate (DMF-DMA) i