1202765-53-4Relevant articles and documents
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors
Gonzalez-Lopez De Turiso, Felix,Shin, Youngsook,Brown, Matthew,Cardozo, Mario,Chen, Yi,Fong, David,Hao, Xiaolin,He, Xiao,Henne, Kirk,Hu, Yi-Ling,Johnson, Michael G.,Kohn, Todd,Lohman, Julia,McBride, Helen J.,McGee, Lawrence R.,Medina, Julio C.,Metz, Daniela,Miner, Kent,Mohn, Deanna,Pattaropong, Vatee,Seganish, Jennifer,Simard, Jillian L.,Wannberg, Sharon,Whittington, Douglas A.,Yu, Gang,Cushing, Timothy D.
, p. 7667 - 7685 (2012/10/29)
Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pharmacokinetic profile for animal studies. Analogue 63 was found to be efficacious in animal models of inflammation including a keyhole limpet hemocyanin (KLH) study and a collagen-induced arthritis (CIA) disease model of rheumatoid arthritis. These studies highlight the potential therapeutic value of inhibiting both the PI3Kβ and δ isoforms in the treatment of a number of inflammatory diseases.
ALKYNYL ALCOHOLS AS KINASE INHIBITORS
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Page/Page column 60, (2010/01/30)
Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. 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, inflammation and the like.