179487-85-5Relevant academic research and scientific papers
DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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Page/Page column 39; 60-61, (2020/01/24)
The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
Towards the next generation of dual Bcl-2/Bcl-xL inhibitors
Varnes, Jeffrey G.,Gero, Thomas,Huang, Shan,Diebold, R. Bruce,Ogoe, Claude,Grover, Paul T.,Su, Mei,Mukherjee, Prasenjit,Saeh, Jamal Carlos,Macintyre, Terry,Repik, Galina,Dillman, Keith,Byth, Kate,Russell, Daniel John,Ioannidis, Stephanos
, p. 3026 - 3033 (2014/06/24)
Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-x L in in vitro biochemical assays and had strong activity in an RS4;11 apoptotic cellular assay. For example, sulfoxide diastereomer 13 maintained good binding affinity and comparable cellular potency to 1 while improving aqueous solubility. The corresponding diastereomer (14) was significantly less potent in the cell, and docking studies suggest that this is due to a stereochemical preference for the RS versus SS sulfoxide. Appending a dimethylaminoethoxy side chain (27) adjacent to the benzylic position of the biphenyl moiety of 1 improved cellular activity by approximately three-fold, and this activity was corroborated in cell lines overexpressing Bcl-2 and Bcl-xL.
Fibrinogen receptor antagonists
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, (2008/06/13)
This invention relates to novel compounds which inhibit platelet aggregation, pharmaceutical compositions containing the compounds, and methods of using the compounds.
