- 1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one derivative and medical application thereof
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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.
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Paragraph 0063; 0065-0066; 0079-0082
(2019/11/04)
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- SPIROCYCLIC INDOLINES AS IL-17 MODULATORS
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A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
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Page/Page column 118
(2019/01/07)
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- NOVEL SUBSTITUTED PYRIMIDINE COMPOUNDS
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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.
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Page/Page column 110; 111
(2016/02/05)
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- Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors
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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.
- 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.
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p. 7667 - 7685
(2012/10/29)
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- Indolin-2-one p38α inhibitors II: Lead optimisation
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Optimisation of a series of indolin-2-one p38α inhibitors was achieved via both blocking of a potential metabolic 'hot spot' and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat.
- Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Balagué, Cristina,Orellana, Adelina,Domínguez, María
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scheme or table
p. 5270 - 5273
(2011/10/09)
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- New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
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This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
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Page/Page column 46
(2009/10/21)
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- New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
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This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
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Page/Page column 29
(2009/12/04)
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