1067904-88-4Relevant academic research and scientific papers
NEW 7-PHENYL-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3(2H)-ONE DERIVATIVES
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Page/Page column 41, (2011/06/16)
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.
New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
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Page/Page column 24, (2011/06/10)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to pharmaceutical compositions comprising them, and to their use in therapy.
Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Aguilar, Nuria,Mir, Marta,Aiguadé, Josep,Matassa, Victor,Balagué, Cristina,Orellana, Adelina,Domínguez, María
scheme or table, p. 6253 - 6257 (2011/11/29)
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.
3-Amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38α mitogen-activated protein kinase
Pettus, Liping H.,Xu, Shimin,Cao, Guo-Qiang,Chakrabarti, Partha P.,Rzasa, Robert M.,Sham, Kelvin,Wurz, Ryan P.,Zhang, Dawei,Middleton, Scott,Henkle, Bradley,Plant, Matthew H.,Saris, Christiaan J. M.,Sherman, Lisa,Lu, Min Wong,Powers, David A.,Tudor, Yanyan,Yu, Violeta,Lee, Matthew R.,Syed, Rashid,Hsieh, Faye,Tasker, Andrew S.
experimental part, p. 6280 - 6292 (2009/10/09)
The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a variety of cy
Phthalazine, aza- and diaza-phthalazine compounds and methods of use
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Page/Page column 24; 25, (2008/06/13)
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
