165315-76-4Relevant articles and documents
TRI-CYCLE COMPOUND AND APPLICATIONS THEREOF
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Paragraph 0132-0133; 0135, (2020/01/22)
Disclosed in the present invention are a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt, and applications thereof in the preparation of drugs for treating HBV-related diseases.
HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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Paragraph 000242, (2015/10/05)
ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy
Kempf, Dale J.,Sham, Hing L.,Marsh, Kennan C.,Flentge, Charles A.,Betebenner, David,Green, Brian E.,McDonald, Edith,Vasavanonda, Sudthida,Saldivar, Ayda,Wideburg, Norman E.,Kati, Warren M.,Ruiz, Lisa,Zhao, Chen,Fino, Lynnmarie,Patterson, Jean,Molla, Akhteruzzaman,Plattner, Jacob J.,Norbeck, Daniel W.
, p. 602 - 617 (2007/10/03)
The structure-activity studies leading to the potent and clinically efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable inhibitor A-80987, systematic investigation of peripheral (P3 and P2') heterocyclic groups designed to decrease the rate of hepatic metabolism provided analogues with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chemical stability toward oxidation while maintaining sufficient aqueous solubility for oral absorption. Optimization of hydrophobic interactions with the HIV protease active site produced ritonavir, with excellent in vitro potency (EC50 = 0.02 μM) and high and sustained plasma concentrations after oral administration in four species. Details of the discovery and preclinical development of ritonavir are described.