Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 22, 2015, Pages 5384-5388

  Lim, Jongwon ^a   Altman, Michael D ^a   Baker, James ^a   Brubaker, Jason D ^a   Chen, Hongmin ^a   Chen, Yiping ^a   Kleinschek, Melanie A ^a   Li, Chaomin ^a   Liu, Duan ^a   Maclean, John K F ^a   Mulrooney, Erin F ^a   Presland, Jeremy ^a   Rakhilina, Larissa ^a   Smith, Graham F ^a   Yang, Ruojing ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

IRAK4; Kinase inhibitor; N (1H Pyrazol 4 yl)carboxamide; SAR; Serine threonine kinase

Indexed keywords

5 AMINO N (1H PYRAZOL 4 YL)PYRAZOLO[1,5 A]PYRIMIDINE 3 CARBOXAMIDE; AMIDE; INTERLEUKIN 1 RECEPTOR ASSOCIATED KINASE 4; PYRAZOLE DERIVATIVE; PYRAZOLO[1,5 A]PYRIMIDINE DERIVATIVE; PYRROLO[1,2 B]PYRIDAZINE; PYRROLO[2,1 F][1,2,4]TRIZINE; THIENO[2,3 B]PYRIDINE DERIVATIVE; UNCLASSIFIED DRUG; ANTIINFLAMMATORY AGENT; CARBOXYLIC ACID; INTERLEUKIN 1 RECEPTOR ASSOCIATED KINASE; PYRAZOLE;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG PENETRATION; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; INFLAMMATORY DISEASE; LIPOPHILICITY; LIVER MICROSOME; MDCK CELL LINE; MEMBRANE PERMEABILITY; METABOLIC STABILITY; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; RAT; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; CYCLIZATION; DRUG EFFECTS; ENZYME ACTIVATION; IC50; SYNTHESIS;

AMIDES; ANTI-INFLAMMATORY AGENTS; CARBOXYLIC ACIDS; CYCLIZATION; ENZYME ACTIVATION; HUMANS; INHIBITORY CONCENTRATION 50; INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASES; MOLECULAR STRUCTURE; PYRAZOLES;

EID: 84945898903     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.09.028     Document Type: Article

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