127408-03-1Relevant articles and documents
Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes
Zhang, Xuqing,Zhu, Bin,Guo, Lili,Bakaj, Ivona,Rankin, Matthew,Ho, George,Kauffman, Jack,Lee, Seunghun P.,Norquay, Lisa,MacIelag, Mark J.
supporting information, p. 451 - 458 (2021/04/06)
A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK profiling led to multiple compounds with good physical properties, excellent oral bioavailability, and a clean in vitro safety profile. Compound 13 was identified as a lead compound as evidenced by the reversal of sulprostone-induced suppression of glucose-stimulated insulin secretion in INS 1E β-cells in vitro and in a rat ivGTT model in vivo. A glutathione adduction liability was eliminated by replacing the naphthalene of structure 13 with the indazole ring of structure 43.
Compounds and their use in treatment on hepatitis B
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Paragraph 0138-0140, (2020/07/15)
The invention provides compounds, a pharmaceutical composition containing the compounds and an application of the compounds. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The compound provided by the invention can interfere with the shell assembly process of hepatitis B virus, thereby inhibiting hepatitis B virus replication. Moreover, the compound has good absorption, relatively high biological activity and availability and low toxicity, particularly has relatively strong stability in vivo, is not easy to decompose and has long drug effect time, so that an effect of treating hepatitis B is achieved and the compound has a goodapplication prospect.
Method for synthesizing 5-bromo-4-fluoro-1H-indazole
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Paragraph 0020; 0021; 0022; 0028; 0029; 0030; 0035-0037, (2019/11/28)
The invention belongs to the field of organic synthesis, and discloses a method for synthesizing 5-bromo-4-fluoro-1H-indazole. The synthesis method comprises the steps: adopting 3-fluoro-2-methylaniline as a raw material, and performing three steps of rea