3-amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models

Journal of Medicinal Chemistry

Volumn 56, Issue 1, 2013, Pages 345-356

  Soth, Michael ^a   Hermann, Johannes C ^a   Yee, Calvin ^a   Alam, Muzaffar ^a   Barnett, Jim W ^b   Berry, Pamela ^a   Browner, Michelle F ^b   Frank, Karl ^b   Frauchiger, Sandra ^b   Harris, Seth ^b   He, Yang ^a   Hekmat Nejad, Mohammad ^b   Hendricks, Than ^b   Henningsen, Robert ^b   Hilgenkamp, Ramona ^a   Ho, Hoangdung ^b   Hoffman, Ann ^a   Hsu, Pei Yuan ^a   Hu, Dong Qing ^a   Itano, Andrea ^b   Jaime Figueroa, Saul ^a   Jahangir, Alam ^b   Jin, Sue ^a   Kuglstatter, Andreas ^a   Kutach, Alan K ^b   Liao, Cheng ^a   Lynch, Stephen ^a   Menke, John ^a   Niu, Linghao ^a   Patel, Vaishali ^a   Railkar, Aruna ^a   Roy, Douglas ^a   Shao, Ada ^b   Shaw, David ^b   Steiner, Sandra ^a   Sun, Yongliang ^a   Tan, Seng Lai ^a   Wang, Sandra ^b   Vu, Minh Diem ^a   more..

^a HOFFMANN LA ROCHE INC   (United States)

^b ROCHE BIOSCIENCE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 CYCLOPROPYL 5H PYRROLO[2,3 B]PYRAZINE 7 CARBOXYLIC ACID [1 (3 CYANOAZETIDINE 1 CARBONYL) 2,2 DIMETHYLPROPYL]AMIDE; 3 AMIDO 5 CYCLOPROPYLPYRROLOPYRAZINE DERIVATIVE; INTERLEUKIN 2; INTERLEUKIN 6; JANUS KINASE 1; JANUS KINASE 1 INHIBITOR; JANUS KINASE 3; JANUS KINASE 3 INHIBITOR; JANUS KINASE INHIBITOR; PYRAZINE DERIVATIVE; PYRROLE DERIVATIVE; TOFACITINIB; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DETERMINATION; DRUG HALF LIFE; DRUG SYNTHESIS; ENZYME REGULATION; ENZYME SPECIFICITY; FEMALE; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; SIGNAL TRANSDUCTION; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CACO-2 CELLS; CRYSTALLOGRAPHY, X-RAY; CYCLOPROPANES; GENE KNOCKDOWN TECHNIQUES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INTERLEUKIN-2; JANUS KINASE 1; JANUS KINASE 3; MICE; MODELS, MOLECULAR; PYRAZINES; PYRROLES; RATS; RECEPTORS, INTERLEUKIN-6; RNA, SMALL INTERFERING; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; T-LYMPHOCYTES;

EID: 84872312946     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301646k     Document Type: Article

References (31)

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