99898-84-7Relevant academic research and scientific papers
Pyrazolopyrimidine compound as an ATR kinase inhibitor
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Page/Page column 30, (2022/01/24)
Disclosed is a compound of a general formula (I), which may be used for the treatment of ATR kinase-mediated diseases, for example, proliferative diseases such as cancer. Further disclosed are a preparation method for the compound of the general formula (I), a pharmaceutical composition, and use of the pharmaceutical composition for the treatment of ATR kinase-mediated diseases.
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors
Deng, Xinxian,Shen, Jian,Zhu, Hui,Xiao, Jia,Sun, Ran,Xie, Fangzhou,Lam, Celine,Wang, Juntao,Qiao, Yixue,Tavallaie, Mojdeh S.,Hu, Yang,Du, Yi,Li, Jianqi,Fu, Lei,Jiang, Faqin
, p. 903 - 912 (2018/01/27)
The initial focus on characterizing novel pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as DPP-4 inhibitors, led to a potent and selective inhibitor compound b2. This ligand exhibits potent in vitro DPP-4 inhibitory activity (IC50: 80 nM), while maintaining other key cellular parameters such as high selectivity, low cytotoxicity and good cell viability. Subsequent optimization of b2 based on docking analysis and structure-based drug design knowledge resulted in d1. Compound d1 has nearly 2-fold increase of inhibitory activity (IC50: 49 nM) and over 1000-fold selectivity against DPP-8 and DPP-9. Further in vivo IPGTT assays showed that compound b2 effectively reduce glucose excursion by 34% at the dose of 10 mg/kg in diabetic mice. Herein we report the optimization and design of a potent and highly selective series of pyrazolo[1,5-a]pyrimidin-7(4H)-one DPP-4 inhibitors.
Novel DPP-4 enzyme inhibitor as well as preparation and application thereof
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Paragraph 0110; 0180-0181, (2017/09/01)
The invention provides a novel dipeptidyl peptidase-4 (DPP-4) inhibitor as well as preparation and application thereof and particularly discloses two pyrazolo[1,5-A]pyridine(4H)-one and pyrazolo[1,5-a]pyridine derivatives represented by a formula A and a formula B (shown in the description), preparation methods of the derivatives and use of the derivatives as the DPP-4 inhibitor, wherein each group is defined as shown in the description. A compound provided by the invention presents an excellent inhibition effect to DPP-4 and is used for preparing a pharmaceutical composition for treating diseases such as diabetes mellitus.
