89466-19-3Relevant academic research and scientific papers
POLYCYCLIC PYRIDONE COMPOUNDS AS ANTIVIRALS
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Paragraph 00216, (2018/03/28)
The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
Phenyl substituted 4-hydroxypyridazin-3(2 H)-ones and 5-hydroxypyrimidin-4(3 H)-ones: Inhibitors of influenza a endonuclease
Sagong, Hye Yeon,Bauman, Joseph D.,Patel, Disha,Das, Kalyan,Arnold, Eddy,Lavoie, Edmond J.
, p. 8086 - 8098 (2014/12/10)
Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza endonuclease. These agents identified as bimetal chelating ligands binding to the active site of the enzyme. In the present study, several aza analogues of these phenyl substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity. In contrast to the 4-aza analogue of 6-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one, the 5-aza analogue (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonuclease inhibitor. The 6-aza analogue of 5-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one (6-(4-fluorophenyl)-4-hydroxypyridazin-3(2H)-one) also retained modest activity as an inhibitor. Several varied 6-phenyl-4-hydroxypyridazin-3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease inhibitors. The SAR observed for these aza analogues are consistent with those previously observed with various phenyl substituted 3-hydroxypyridin-2(1H)-ones.
TRIPYRIDYL CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 19, (2010/03/02)
The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 51, (2010/05/14)
The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Th
TETRAHYDROTHIAZOLOPYRIDINE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
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Page/Page column 52-53; 54, (2010/09/17)
The present invention relates to compounds (I) useful as inhibitors of PBK, particularly of PI3K gamma. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders
PYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 73-74, (2009/07/03)
The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved
2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
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, (2008/06/13)
The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) STR1 wherein Ar is a pyridyl, a dimethoxy-pyridyl or dimethoxy-pyrazyl group, R4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group
2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists
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, (2008/06/13)
The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) STR1 wherein Ar is a pyridyl, dimethoxy-pyridyl or a dimethoxy-pyrazinyl group, R4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing gro
