1379312-86-3Relevant academic research and scientific papers
1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one derivative and medical application thereof
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Paragraph 0063; 0065-0066; 0075-0078, (2019/11/04)
The invention discloses a 1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one derivative and medical application thereof. A compound is a compound shown in a formula I, or a pharmaceutically acceptable salt ora stereoisomer or a tautomer thereof, wherein R1-R4 is defined by the specification.
HETEROARYL COMPOUNDS AS INHIBITORS OF NECROSIS, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00194; 00197; 00198, (2019/01/10)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to necrosis. Formula (I) is shown below:
NOVEL SUBSTITUTED PYRIMIDINE COMPOUNDS
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Page/Page column 110; 111, (2016/02/05)
The invention relates to novel substituted pyrimidine compounds of general formula (I), in which the chemical groupings, substituents, variables and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
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.
