Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase

Journal of Medicinal Chemistry

Volumn 55, Issue 10, 2012, Pages 4580-4593

  Gingrich, Diane E ^a   Lisko, Joseph G ^a   Curry, Matthew A ^a   Cheng, Mangeng ^a   Quail, Matthew ^a   Lu, Lihui ^a   Wan, Weihua ^a   Albom, Mark S ^a   Angeles, Thelma S ^a   Aimone, Lisa D ^a   Haltiwanger, R Curtis ^a   Wells Knecht, Kevin ^a   Ott, Gregory R ^a   Ghose, Arup K ^a   Ator, Mark A ^a   Ruggeri, Bruce ^a   Dorsey, Bruce D ^a  

^a CEPHALON INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [5 CHLORO 2 [1 METHOXY 7 (2 METHOXY ETHYL AMINO) 6,7,8,9 TETRAHYDRO 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; 3 [5 CHLORO 2 [1 METHOXY 7 (4 METHYLPIPERAZIN 1 YL) 6,7,8,9 TETRAHYDRO 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; 3 [5 CHLORO 2 [1 METHOXY 7 MORPHOLIN 4 YL 6,7,8,9 TETRAHYDRI 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; 3 [5 CHLORO 2 [3 METHOXY 7 (2 METHOXYETHYLAMINO) 6,7,8,9 TETRAHYDRO 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; 3 [5 CHLORO 2 [3 METHOXY 7 (4 METHYLPIPERAZIN 1 YL) 6,7,8,9 TETRAHYDRO 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; 3 [5 CHLORO 2 [3 METHOXY 7 MORPHOLIN 4 YL 6,7,8,9 TETRAHYDRO 5H BENZOCYCLOHEPTEN 2 YLAMINO] PYRIMIDIN 4 YLAMINO]BICYCLO[2.2.1]HEPT 5 ENE 2 CARBOXYLIC ACID AMIDE; ANAPLASTIC LYMPHOMA KINASE; ANAPLASTIC LYMPHOMA KINASE INHIBITOR; ANTINEOPLASTIC AGENT; CRIZOTINIB; INSULIN RECEPTOR; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; FEMALE; FOOD AND DRUG ADMINISTRATION; HAPLORHINI; HYDROGENATION; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; TUMOR XENOGRAFT;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CYCLOHEPTANES; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHER-A-GO-GO POTASSIUM CHANNELS; FEMALE; HUMANS; LYMPHOMA, LARGE-CELL, ANAPLASTIC; MICE; MICE, SCID; MODELS, MOLECULAR; MORPHOLINES; PHOSPHORYLATION; PIPERAZINES; PROTEIN BINDING; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR PROTEIN-TYROSINE KINASES; RECEPTOR, INSULIN; STRUCTURE-ACTIVITY RELATIONSHIP; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84861501385     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201550q     Document Type: Article

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