671-93-2Relevant academic research and scientific papers
Design, synthesis and anti-HBV activity of NVR3-778 derivatives
Lv, Kai,Wu, Shuo,Li, Wenyan,Geng, Yunhe,Wu, Meng,Zhou, Jinming,Li, Yuhuan,Gao, Qiang,Liu, Mingliang
, (2019/11/13)
NVR3-778, one of the most advanced capsid assembly modulators (CAMs), is currently in phase II clinical trial for the treatment of HBV infection. In this study, we reported the first structure optimization of NVR3-778. Compound 2d was found to exhibit more potent anti-HBV activity (IC50: 0.25 μM), lower cytotoxicity (CC50: 10.68 μM) and higher selectivity index (SI: 40.72) than NVR3-778 (IC50: 0.33 μM; CC50: 5.14 μM; SI: 18.36) in vitro, and also display similar inhibitory effect on the assembly of HBV capsids as NVR3-778. Molecular docking further suggested that compound 2d might form a stronger interaction with core protein. Moreover, compound 2d also showed acceptable pharmacokinetic profiles. Currently compound 2d was selected as a new lead for further modifications, and studies to determine the in vivo anti-HBV studies of 2d will begin soon.
CYCLIC INHIBITORS OF HEPATITIS B VIRUS
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Page/Page column 76; 77, (2020/02/14)
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
INHIBITORS OF HEPATITIS B VIRUS
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Page/Page column 40, (2020/02/14)
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditio
HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Paragraph 00215, (2016/10/31)
Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
2-Halobenzenesulfonyl chlorides in the synthesis of pyrido[2,1-c][1,2,4]benzothiadiazine 5,5-dioxide derivatives
Shlenev,Filimonov,Tarasov,Danilova,Agat’ev,Ivanovskii
, p. 1839 - 1845 (2017/03/22)
A number of new functional derivatives of pyrido[2,1-c][1,2,4]benzothiadiazine 5,5-dioxide was obtained based on the reactions of 2-halobenzenesulfonyl chlorides with 2-aminopyridine derivatives. A quantitative criterion for the evaluation of a possibility for the reaction to proceed under noncatalytic conditions depending on the type of halogen and substituents in the starting compounds was suggested.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Paragraph 0797; 0798; 0799, (2015/07/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Paragraph 0794, (2015/09/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
PRODRUGS OF PEPTIDE EPOXY KETONE PROTEASE INHIBITORS
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Page/Page column 182, (2014/02/15)
This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.
HEPATITIS B ANTIVIRAL AGENTS
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Page/Page column 248, (2013/07/05)
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
ARYLSULFONAMIDE-BASED MATRIX METALLOPROTEASE INHIBITORS
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Page/Page column 43, (2009/10/22)
The present invention provides a compound of formula (I):said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP- 13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP- 13. Finally, the present invention also provides a pharmaceutical composition.
