Triazolopyridines as selective JAK1 inhibitors: From hit identification to GLPG0634

Journal of Medicinal Chemistry

Volumn 57, Issue 22, 2014, Pages 9323-9342

  Menet, Christel J ^a   Fletcher, Stephen R ^b   Van Lommen, Guy ^a   Geney, Raphael ^c   Blanc, Javier ^a   Smits, Koen ^a   Jouannigot, Nolwenn ^a   Deprez, Pierre ^c   Van Der Aar, Ellen M ^a   Clement Lacroix, Philippe ^c   Lepescheux, Liên ^c   Galien, René ^c   Vayssiere, Béatrice ^c   Nelles, Luc ^a   Christophe, Thierry ^a   Brys, Reginald ^a   Uhring, Muriel ^d   Ciesielski, Fabrice ^d   Van Rompaey, Luc ^a  

^a GALAPAGOS NV   (Belgium)

^b BioFocus DPI   (United Kingdom)

^c Galapagos SASU   (France)

^d Building A: Chemistry   (France)

Author keywords

[No Author keywords available]

Indexed keywords

(5 PHENYL [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL)AMIDE; 1 (6 BROMO PYRIDIN 2 YL) 3 CARBOETHOXY THIOUREA; 1 [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL] 3 METHYLUREA; 2 IODO 5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDINE; 4 BROMO [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YLAMINE; 5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YLAMINE; 5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]DIMETHYLAMINE; 5 (4METHOXYPHENYL) 2 PYRIDIN 3 YL [1,2,4]TRIAZOLO[1,5 A]PYRIDINE; ANTIRHEUMATIC AGENT; CYCLOPROPLYMETHYL [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMINE; ETANERCEPT; FILGOTINIB; JANUS KINASE 1; JANUS KINASE INHIBITOR; N [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]ACETAMIDE; N [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]BENZAMIDE; N [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]PROPIONAMIDE; PYRIDINE DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; [5 (1H PYRAZOL 4 YL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (2 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (2 METHOXYPYRIMIDIN 5 YL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (3 BENZYLOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (3 CHLOROPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (4 CHLOROPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]METHYLAMIDE; [5 (4 METHOXYPHENYL) [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]PHENYLAMINE; [5 BROMO [1,2,4]TRIAZOLO[1,5 A]PYRIDIN 2 YL]AMIDE; ADENOSINE TRIPHOSPHATE; COLLAGEN; CYTOKINE; PROTEIN KINASE INHIBITOR; RECOMBINANT PROTEIN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTHRITIS; ARTICLE; CANINE MODEL; CONCENTRATION RESPONSE; CONTROLLED STUDY; CROHN DISEASE; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC50; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PHASE 2 CLINICAL TRIAL (TOPIC); PROCESS OPTIMIZATION; RAT; RHEUMATOID ARTHRITIS; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DIMERIZATION; DISEASE MODEL; DRUG DESIGN; DRUG SCREENING; KINETICS; MEDICINAL CHEMISTRY; METABOLISM; PHOSPHORYLATION; PROCEDURES; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADENOSINE TRIPHOSPHATE; ANIMALS; ARTHRITIS; CHEMISTRY, PHARMACEUTICAL; COLLAGEN; CROHN DISEASE; CRYSTALLOGRAPHY, X-RAY; CYTOKINES; DIMERIZATION; DISEASE MODELS, ANIMAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; INHIBITORY CONCENTRATION 50; JANUS KINASE 1; KINETICS; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PYRIDINES; RATS; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 84913558440     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501262q     Document Type: Article

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