Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3- dihydroxypropoxy)phenyl]-methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 Map kinase

Journal of Medicinal Chemistry

Volumn 49, Issue 5, 2006, Pages 1562-1575

  Goldstein, David M ^a   Alfredson, Tom ^a   Bertrand, Jay ^b   Browner, Michelle F ^a   Clifford, Ken ^a   Dalrymple, Stacie A ^c   Dunn, James ^a   Freire Moar, Jose ^d   Harris, Seth ^a   Labadie, Sharada S ^a   La Fargue, JoAnn ^a   Lapierre, Jean Marc ^e   Larrabee, Susan ^a   Li, Fujun ^a   Papp, Eva ^a   McWeeney, Daniel ^a   Ramesha, Chakk ^a   Roberts, Rick ^a   Rotstein, David ^a   San Pablo, Bong ^c   Sjogren, Eric B ^a   So, On Yee ^a   Talamas, Francisco X ^a   Tao, Will ^a   Trejo, Alejandra ^a   Villasenor, Armando ^a   Welch, Mary ^a   Welch, Teresa ^a   Weller, Paul ^a   Whiteley, Phyllis E ^f   Young, Kelly ^a   Zipfel, Sheila ^c   more..

^a ROCHE BIOSCIENCE   (United States)

^b PFIZER INC   (United States)

^c CELERA   (United States)

^d FOREST RESEARCH INSTITUTE   (United States)

^e ARQULE INC   (United States)

^f Perlegen Sciences Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; AMINE; BENZENE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE P38; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; PYRAZOLE DERIVATIVE; RO 3201195; S [5 AMINO 1 (4 FLUOROPHENYL) 1H PYRAZOL 4 YL][3 (2,3 DIHYDROXYPROPOXY)PHENYL]METHANONE; THREONINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME ACTIVE SITE; FEMALE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADENOSINE TRIPHOSPHATE; ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; ARTHRITIS, EXPERIMENTAL; BINDING SITES; BIOLOGICAL AVAILABILITY; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DOGS; FEMALE; HAPLORHINI; HUMANS; INTERLEUKIN-1; INTERLEUKIN-6; MODELS, MOLECULAR; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PYRAZOLES; RATS; RATS, INBRED LEW; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR NECROSIS FACTOR-ALPHA;

EID: 33644883681     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm050736c     Document Type: Article

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