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

Journal of Medicinal Chemistry

Volumn 54, Issue 7, 2011, Pages 2255-2265

  Goldstein, David M ^a   Soth, Michael ^a   Gabriel, Tobias ^a   Dewdney, Nolan ^a   Kuglstatter, Andreas ^a   Arzeno, Humberto ^a   Chen, Jeffrey ^a   Bingenheimer, William ^a   Dalrymple, Stacie A ^a   Dunn, James ^a   Farrell, Robert ^a   Frauchiger, Sandra ^a   La Fargue, Joann ^a   Ghate, Manjiri ^a   Graves, Bradford ^a   Hill, Ronald J ^a   Li, Fujun ^a   Litman, Renee ^a   Loe, Brad ^a   McIntosh, Joel ^a   McWeeney, Daniel ^a   Papp, Eva ^a   Park, Jaehyeon ^a   Reese, Harlan F ^a   Roberts, Richard T ^a   Rotstein, David ^a   San Pablo, Bong ^a   Sarma, Keshab ^a   Stahl, Martin ^a   Sung, Man Ling ^a   Suttman, Rebecca T ^a   Sjogren, Eric B ^a   Tan, Yunchou ^a   Trejo, Alejandra ^a   Welch, Mary ^a   Weller, Paul ^a   Wong, Brian R ^a   Zecic, Hasim ^a   more..

^a ROCHE BIOSCIENCE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 (2,4 DIFLUOROPHENOXY) 8 METHYL 2 (TETRAHYDRO 2H PYRAN 4 YLAMINO)PYRIDO[2,3 D]PYRIMIDIN 7(8H) ONE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; PAMAPIMOD; SYNAPTOPHYSIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; FEMALE; HUMAN; HYPERALGESIA; NONHUMAN; RAT; RHEUMATOID ARTHRITIS;

ADMINISTRATION, ORAL; ARTHRITIS, RHEUMATOID; BIOLOGICAL AVAILABILITY; CELL LINE; CLINICAL TRIALS AS TOPIC; DRUG DISCOVERY; HUMANS; MITOGEN-ACTIVATED PROTEIN KINASE 14; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PYRIDONES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 79953795938     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm101423y     Document Type: Article

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