2257-69-4Relevant articles and documents
Discovery of Phthalazinone Derivatives as Novel Hepatitis B Virus Capsid Inhibitors
Chen, Wuhong,Liu, Feifei,Zhao, Qiliang,Ma, Xinna,Lu, Dong,Li, Heng,Zeng, Yanping,Tong, Xiankun,Zeng, Limin,Liu, Jia,Yang, Li,Zuo, Jianping,Hu, Youhong
, p. 8134 - 8145 (2020)
HBV capsid assembly has been viewed as an attractive target for new antiviral therapies against HBV. On the basis of a lead compound 4r, we further investigated this target to identify novel active compounds with appropriate anti-HBV potencies and improved pharmacokinetic (PK) properties. Structure-activity relationship studies based on metabolic pathways of 4r led to the identification of a phthalazinone derivative 19f with appropriate anti-HBV potencies (IC50 = 0.014 ± 0.004 μM in vitro), which demonstrated high oral bioavailability and liver exposure. In the AAV-HBV/mouse model, administration of 19f resulted in a 2.67 log reduction of the HBV DNA viral load during a 4-week treatment with 150 mg/kg dosing twice daily.
Phthalazinone compound and preparation method, pharmaceutical composition and use thereof
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Paragraph 0106; 0108; 0109; 0110, (2019/01/23)
The invention relates to a phthalazinone compound and a preparation, pharmaceutical composition and use thereof, wherein the structure of the phthalazinone compound is shown as formula one, and the compound of the formula one is targeted to a virus nuclea
TOLL-LIKE RECEPTOR 8 (TLR8)-SPECIFIC ANTAGONISTS AND METHODS OF MAKING AND USES THEREOF
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Page/Page column 52, (2019/05/22)
Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.