Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible t-cell kinase inhibitors

Journal of Medicinal Chemistry

Volumn 57, Issue 13, 2014, Pages 5714-5727

  Burch, Jason D ^a   Lau, Kevin ^a   Barker, John J ^b   Brookfield, Fred ^b   Chen, Yong ^d   Chen, Yuan ^a   Eigenbrot, Charles ^a   Ellebrandt, Claire ^c   Ismaili, M Hicham A ^a   Johnson, Adam ^a   Kordt, Daniel ^c   Mackinnon, Colin H ^b   McEwan, Paul A ^b   Ortwine, Daniel F ^a   Stein, Daniel B ^c   Wang, Xiaolu ^c   Winkler, Dirk ^c   Yuen, Po Wai ^d   Zhang, Yamin ^d   Zarrin, Ali A ^a   Pei, Zhonghua ^a   more..

^a GENENTECH INC   (United States)

^b EVOTEC UK LTD   (United Kingdom)

^c EVOTEC AG   (Germany)

^d Pharmaron Beijing Co Ltd   (China)

Author keywords

[No Author keywords available]

Indexed keywords

GNE 9822; INDAZOLE DERIVATIVE; INTERLEUKIN 2 INDUCIBLE T CELL KINASE; INTERLEUKIN 2 INDUCIBLE T CELL KINASE INHIBITOR; N (1 BENZYL 1H PYRAZOL 4 YL) 1',4',5',7' TETRAHYDROSPIRO[CYCLOPROPANE 1,6' INDAZOLE] 3' CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 1',4,4',5,5'7' HEXAHYDRO 2H SPIRO[FURAN 3,6' INDAZOLE] 3' CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 1',4,4A,5,5A,6 HEXAHYDROCYCLOPORPA[F]INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 1,4,5,7 TETRAHYDROSPIRO[INDAZOLE 6,3' OXETANE] 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 5,5 DIMETHYL 4,5,6,7 TETRAHYDRO 1H INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 5A METHYL 1',4,4A,5,5A,6 HEXAHYDROCYCLOPORPA[F]INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 6 (HYDROXYMETHYL) 6 METHYL 4,5,6,7 TETRAHYDRO 1H INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 6 METHOXY 6 METHYL 4,5,6,7 TETRAHYDRO 1H INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 6,6 DIFLUORO 4,5,6,7 TETRAHYDRO 1H INDAZOLE 3 CARBOXAMIDE; N (1 BENZYL 1H PYRAZOL 4 YL) 6,6 DIMETHYL 4,5,6,7 TETRAHYDRO 1H INDAZOLE 3 CARBOXAMIDE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; TETRAHYDROINDAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DOG; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; DRUG SOLUBILITY; DRUG STRUCTURE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; X RAY CRYSTALLOGRAPHY;

ANIMALS; CRYSTALLOGRAPHY, X-RAY; DOGS; DRUG DESIGN; HUMANS; INDAZOLES; JURKAT CELLS; KINETICS; MICE; MODELS, MOLECULAR; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; RATS; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84904345197     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500550e     Document Type: Article

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