The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties

Journal of Medicinal Chemistry

Volumn 60, Issue 23, 2017, Pages 9676-9690

  Siu, Tony ^a   Brubaker, Jason ^a   Fuller, Peter ^a   Torres, Luis ^a   Zeng, Hongbo ^a   Close, Joshua ^a   Mampreian, Dawn M ^a   Shi, Feng ^b   Liu, Duan ^a   Fradera, Xavier ^a   Johnson, Kevin ^a   Bays, Nathan ^a   Kadic, Elma ^a   He, Fang ^b   Goldenblatt, Peter ^a   Shaffer, Lynsey ^a   Patel, Sangita B ^a   Lesburg, Charles A ^a   Alpert, Carla ^a   Dorosh, Lauren ^a   Deshmukh, Sujal V ^a   Yu, Hongshi ^a   Klappenbach, Joel ^a   Elwood, Fiona ^a   Dinsmore, Christopher J ^a   Fernandez, Rafael ^a   Moy, Lily ^a   Young, Jonathan R ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b Pharmaron Beijing Co Ltd   (China)

Author keywords

[No Author keywords available]

Indexed keywords

3 ((4 CHLORO 3 METHOXYPHENYL)AMINO) 1 ((3R,4S) 4 CYANOTETRAHYDRO 2H PYRAN 3 YL) 1H PYRAZOLE 4 CARBOXAMIDE; 3 ((4 CYANOPHENYL)AMINO) 1 ((3R,4S) 4 CYANOTETRAHYDRO 2H PYRAN 3 YL) 1H PYRAZOLE 4 CARBOXAMIDE; AMINO ACID; DEXAMETHASONE; INTERLEUKIN 6; JANUS KINASE 1; JANUS KINASE 2; JANUS KINASE INHIBITOR; LIGAND; POTASSIUM CHANNEL HERG; TOFACITINIB; UNCLASSIFIED DRUG; JAK1 PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR; PYRAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SOLUBILITY; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; INTRINSIC CLEARANCE; LIGAND BINDING; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION; THERAPEUTIC INDEX; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DOG; DRUG DEVELOPMENT; HALOGENATION; METABOLISM; MOLECULAR DOCKING;

ANIMALS; DOGS; DRUG DISCOVERY; HALOGENATION; HUMANS; JANUS KINASE 1; MOLECULAR DOCKING SIMULATION; PROTEIN KINASE INHIBITORS; PYRAZOLES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85038402096     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.7b01135     Document Type: Article

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