Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists

ChemMedChem

Volumn 11, Issue 24, 2016, Pages 2640-2648

  Hintermann, Samuel ^a   Guntermann, Christine ^a   Mattes, Henri ^a   Carcache, David A ^a   Wagner, Juergen ^a   Vulpetti, Anna ^a   Billich, Andreas ^a   Dawson, Janet ^a   Kaupmann, Klemens ^a   Kallen, Joerg ^a   Stringer, Rowan ^a   Orain, David ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

imidazopyridines; inverse agonists; oxadiazoles; plasma protein binding; ROR t

Indexed keywords

8 BROMO 7 METHYL 6 NITROIMIDAZOLE[1,2 A]PYRIDINE; 8 BROMO 7 METHYLIMIDAZO[1,2 A]PYRIDIN 6 AMINE; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; CONCANAVALIN A; IMIDAZOPYRIDINE DERIVATIVE; INTERLEUKIN 17; N (8 BROMO 7 METHYLIMIDAZO[1,2 A]PYRIDIN 6 YL) 2 METHYLPYRIMIDINE 5 CARBOXAMIDE; RETINOID RELATED ORPHAN RECEPTOR GAMMA; TERT BUTYL 2 METHYL 4 [(7 METHYL 6 (2 METHYLPYRIMIDINE 5 CARBOXAMIDO)IMIDAZO[1,2 A]PYRIDIN 8 YL)METHYL]PIPERAZINE 1 CARBOXYLATE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; [N [8 [[4 (CYCLOPENTANECARBONYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 7 METHYLIMIDAZOL[1,2 A ]PYRIDIN 6 YL] 2 METHYLPYRIMIDINE 5 CARBOXAMIDE]; [N [8 [[4 [5 (TERT BUTYL) 1,2,4 OXADIAZOL 3 YL] 3 METHYLPIPERAZIN 1 YL]METHYL] 7 METHYLIMIDAZO[1,2 A]PYRIDIN 6 YL] 2 METHYLPYRIMIDINE 5 CARBOXAMIDE]; IMIDAZOLE DERIVATIVE; PROTEIN BINDING; PYRIDINE DERIVATIVE; RETINOIC ACID RECEPTOR;

AEROBIC METABOLISM; ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CD4+ T LYMPHOCYTE; CLEARANCE; CYTOKINE PRODUCTION; DNA BINDING; DRUG CLEARANCE; DRUG HALF LIFE; DRUG SCREENING; DRUG SYNTHESIS; EX VIVO STUDY; FEMALE; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; HUMAN CELL; IN VITRO STUDY; LIGAND BINDING; LIPOPHILICITY; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; METABOLIC STABILITY; NONHUMAN; PHARMACODYNAMIC PARAMETERS; PHARMACOKINETIC PARAMETERS; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION; AGONISTS; ANIMAL; BINDING SITE; BLOOD; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; IC50; INVERSE AGONISM; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

ANIMALS; BINDING SITES; CELLS, CULTURED; CRYSTALLOGRAPHY, X-RAY; DRUG INVERSE AGONISM; HUMANS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; INTERLEUKIN-17; MOLECULAR STRUCTURE; NUCLEAR RECEPTOR SUBFAMILY 1, GROUP F, MEMBER 3; PROTEIN BINDING; PYRIDINES; RATS; RECEPTORS, RETINOIC ACID; TRIAZOLES;

EID: 85006446496     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201600500     Document Type: Article

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