55770-79-1Relevant academic research and scientific papers
Discovery and structure activity relationship of glyoxamide derivatives as anti-hepatitis B virus agents
Amblard, Franck,Boucle, Sebastien,Bassit, Leda,Chen, Zhe,Sari, Ozkan,Cox, Bryan,Verma, Kiran,Ozturk, Tugba,Ollinger-Russell, Olivia,Schinazi, Raymond F.
, (2021/01/12)
Chronic hepatitis B viral infection is a significant health problem world-wide, and currently available antiviral agents suppress HBV infections, but rarely cure this disease. It is presumed that antiviral agents that target the viral nuclear reservoir of transcriptionally active cccDNA may eliminate HBV infection. Through a series of chemical optimization, we identified a new series of glyoxamide derivatives affecting HBV nucleocapsid formation and cccDNA maintenance at low nanomolar levels. Among all the compounds synthesized, GLP-26 displays a major effect on HBV DNA, HBeAg secretion and cccDNA amplification. In addition, GLP-26 shows a promising pre-clinical profile and long-term effect on viral loads in a humanized mouse model.
PYRROLE COMPOUNDS
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Paragraph 0132; 0136, (2020/10/19)
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
MONOMER AND MULTIMERIC ANTI-HBV AGENTS
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Page/Page column 143; 153-154, (2020/05/15)
The present invention is directed to compounds, compositions and methods for preventing, treating or curing hepatitis B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV infection.
ELIMINATION OF HEPATITIS B VIRUS WITH ANTIVIRAL AGENTS
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Page/Page column 80, (2017/09/27)
The present invention is directed to compounds, compositions and methods for preventing, treating or curing Hepatitis B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV infection.
ORNITHINE DERIVATIVE
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Page/Page column 24; 34, (2010/01/29)
Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.
Synthesis of Functionalized N-Methylpyrroles
Barrero, A. F.,Sanchez, J. F.,Oltra, J. E.,Teva, D.
, p. 939 - 944 (2007/10/02)
The preparation of some new N-methylpyrroles is shown.These heterocyclic compounds were used to synthesize polyenic substances with polysubstituted pyrrole rings.
Some Mercuration Reactions of Substituted Pyrroles
Ganske, Jane A.,Pandey, Ravindra K.,Postich, Michael J.,Snow, Kevin M.,Smith, Kevin M.
, p. 4801 - 4807 (2007/10/02)
Mercuration of N-unsubstituted pyrroles with mercury(II)acetate results in immediate precipitation of the N-mercurated derivative, which is insoluble in virtually all organic solvents.If the pyrrole N atom is protected (e.g.with Me, CH2OCH2Ph, or CO2t-Bu)
Alphacarbamoyl-pyrrolpropionitriles
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, (2008/06/13)
1-Substituted-β-oxo-α-phenylcarbamoyl-pyrrolpropionitriles, e.g. those of the formula STR1 their alkylenol ethers or alkanoylenol esters and salts thereof are antiinflammatory and antiarthritic agents.
