449811-92-1Relevant articles and documents
Development of radioiodinated pyrimidinopyridone derivatives as targeted imaging probes of activated p38α for single photon emission computed tomography
Hashimoto, Tomoyuki,Kondo, Naoya,Hirata, Masahiko,Temma, Takashi
, p. 1293 - 1304 (2021/08/23)
Objective: p38α, a member of the mitogen-activated protein kinase superfamily, is ubiquitously expressed in a variety of mammalian cells. Activated p38α induces inflammatory responses to external stimuli, suggesting that non-invasive detection of activate
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl) propylamino]-8-methyl-8 H -pyrido[2,3- d ]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2 H -pyran-4-ylamino)pyrido[2,3- d ]pyrimidin-7(8 H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase
Goldstein, David M.,Soth, Michael,Gabriel, Tobias,Dewdney, Nolan,Kuglstatter, Andreas,Arzeno, Humberto,Chen, Jeffrey,Bingenheimer, William,Dalrymple, Stacie A.,Dunn, James,Farrell, Robert,Frauchiger, Sandra,La Fargue, Joann,Ghate, Manjiri,Graves, Bradford,Hill, Ronald J.,Li, Fujun,Litman, Renee,Loe, Brad,McIntosh, Joel,McWeeney, Daniel,Papp, Eva,Park, Jaehyeon,Reese, Harlan F.,Roberts, Richard T.,Rotstein, David,San Pablo, Bong,Sarma, Keshab,Stahl, Martin,Sung, Man-Ling,Suttman, Rebecca T.,Sjogren, Eric B.,Tan, Yunchou,Trejo, Alejandra,Welch, Mary,Weller, Paul,Wong, Brian R.,Zecic, Hasim
, p. 2255 - 2265 (2011/06/21)
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently inhibited p38α, was a screening hit from our kinase inhibitor library. This manuscript describes the optimization of the lead to p38-selective examples with good pharmacokinetic properties.
6-Substituted pyrido-pyrimidines
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, (2008/06/13)
The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.