645418-40-2Relevant academic research and scientific papers
NEXT-GENERATION MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
-
Page/Page column 71-72, (2020/12/30)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIβ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology
Mejdrová, Ivana,Chalupská, Dominika,Pla?ková, Pavla,Müller, Christin,?ála, Michal,Klíma, Martin,Baumlová, Adriana,H?ebabecky, Hubert,Procházková, Eli?ka,Dejmek, Milan,Strunin, Dmytro,Weber, Jan,Lee, Gary,Matou?ová, Marika,Mertlíková-Kaiserová, Helena,Ziebuhr, John,Birkus, Gabriel,Boura, Evzen,Nencka, Radim
supporting information, p. 100 - 118 (2017/04/26)
Phosphatidylinositol 4-kinase IIIβ (PI4KB) is indispensable for the replication of various positive-sense single stranded RNA viruses, which hijack this cellular enzyme to remodel intracellular membranes of infected cells to set up the functional replication machinery. Therefore, the inhibition of this PI4K isoform leads to the arrest of viral replication. Here, we report on the synthesis of novel PI4KB inhibitors, which were rationally designed based on two distinct structural types of inhibitors that bind in the ATP binding side of PI4KB. These “hybrids” not only excel in outstanding inhibitory activity but also show high selectivity to PI4KB compared to other kinases. Thus, these compounds exert selective nanomolar or even subnanomolar activity against PI4KB as well as profound antiviral effect against hepatitis C virus, human rhinovirus, and coxsackievirus B3. Our crystallographic analysis unveiled the exact position of the side chains and explains their extensive contribution to the inhibitory activity.
SUBSTITUTED ANTHRANILIC AMIDE DERIVATIVES AND METHODS OF USE
-
Page 109, (2010/02/06)
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Substituted alkylamine derivatives and methods of use
-
Page 77, (2010/02/05)
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
