Discovery of 5″-chloro-n-[(5,6-dimethoxypyridin-2- yl)methyl]-2,2':5',3″-Terpyridine-3'-carboxamide (mk-1064): A selective orexin 2 receptor antagonist (2-sora) for the treatment of insomnia

ChemMedChem

Volumn 9, Issue 2, 2014, Pages 311-322

  Roecker, Anthony J ^a   Mercer, Swati P ^a   Schreier, John D ^a   Cox, Christopher D ^a   Fraley, Mark E ^a   Steen, Justin T ^a   Lemaire, Wei ^a   Bruno, Joseph G ^a   Harrell, C Meacham ^a   Garson, Susan L ^a   Gotter, Anthony L ^a   Fox, Steven V ^a   Stevens, Joanne ^a   Tannenbaum, Pamela L ^a   Prueksaritanont, Thomayant ^a   Cabalu, Tamara D ^a   Cui, Donghui ^a   Stellabott, Joyce ^a   Hartman, George D ^a   Young, Steven D ^a   Winrow, Christopher J ^a   Renger, John J ^a   Coleman, Paul J ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antagonists; Insomnia; Medicinal Chemistry; Neurotransmitters; Orexin Receptors

Indexed keywords

1 (5,6 DIMETHOXYPYRIDIN 3 YL)METHANAMINE; 2 CHLORO N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL)PYRIDINE 3 CARBOXAMIDE; 2,3 DIMETHOXY 5 AMINOMETHYLPYRAZINE; 2,3 DIMETHOXY 6 AMINOMETHYLPYRIDINE; 5'' CHLORO N [(5,6 DIMETHOXYPYRIDIN 2 YL)METHYL] 2,2':5',3'' TERPYRIDINE 3' CARBOXAMIDE; AMIDE; CYTOCHROME P450 3A4; METHYL 5'' CHLORO 2,2':5',3'' TERPYRIDINE 3' CARBOXYLATE; METHYL 5',6 DICHLORO 3,3' BIPYRIDINE 5 CARBOXYLATE; MK 1064; N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL) 2 (MORPHOLIN 4 YL)PYRIDINE 3 CARBOXAMIDE; N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL) 2 PHENYLPYRIDINE 3 CARBOXAMIDE; N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL) 2,2' BIPYRIDINE 3 CARBOXAMIDE; N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL) 2,3' BIPYRIDINE 3 CARBOXAMIDE; N (3,4 DIMETHOXYBENZYL) 5 (3,5 DIMETHYLPHENYL) 2,4' BIPYRIDINE 3 CARBOXAMIDE; OREXIN 2 RECEPTOR; PYRIDINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; WAKEFULNESS PROMOTING AGENT; NEUROPEPTIDE; NEUROTRANSMITTER; OREXIN RECEPTOR; OREXINS; SIGNAL PEPTIDE;

ADULT; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; ENZYME INHIBITION; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; INSOMNIA; LIVER MICROSOME; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION; ANIMAL; ANTAGONISTS; C57BL MOUSE; CHEMISTRY; DOG; DRUG ANTAGONISM; DRUG DESIGN; MEDICINAL CHEMISTRY; METABOLISM; RHESUS MONKEY; SPRAGUE DAWLEY RAT;

ANTAGONISTS; INSOMNIA; MEDICINAL CHEMISTRY; NEUROTRANSMITTERS; OREXIN RECEPTORS;

ANIMALS; DOGS; DRUG DESIGN; HUMANS; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MACACA MULATTA; MALE; MICE; MICE, INBRED C57BL; NEUROPEPTIDES; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; SLEEP INITIATION AND MAINTENANCE DISORDERS;

EID: 84897024986     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201300447     Document Type: Article

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