Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3- yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a highly selective thyroid hormone receptor β agonist in clinical trials for the treatment of dyslipidemia

Journal of Medicinal Chemistry

Volumn 57, Issue 10, 2014, Pages 3912-3923

  Kelly, Martha J ^a   Pietranico Cole, Sherrie ^b   Larigan, J Douglas ^b   Haynes, Nancy Ellen ^b   Reynolds, Charles H ^c   Scott, Nathan ^b   Vermeulen, John ^b   Dvorozniak, Mark ^b   Conde Knape, Karin ^b   Huang, Kuo Sen ^b   So, Sung Sau ^b   Thakkar, Kshitij ^b   Qian, Yimin ^b   Banner, Bruce ^b   Mennona, Frank ^b   Danzi, Sara ^d   Klein, Irwin ^e   Taub, Rebecca ^a   Tilley, Jefferson ^b  

^a Madrigal Pharmaceuticals   (United States)

^b HOFFMANN LA ROCHE INC   (United States)

^c Gfree Bio LLC   (United States)

^d QUEENSBOROUGH COMMUNITY COLLEGE   (United States)

^e NEW YORK UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [ 3,5 DICHLORO 4 ( 5 ISOPROPYL 6 OXO 1,6 DIHYDROPYRIDAZIN 3 YLOXY)PHENYL] 3,5 DIOXO 2,3,4,5 TETRAHYDRO[ 1,2,4 ]TRIAZINE 6 CARBONITRILE; ANTILIPEMIC AGENT; ATORVASTATIN; EPROTIROME; LIOTHYRONINE; LOW DENSITY LIPOPROTEIN CHOLESTEROL; MGL 3196; PLACEBO; THYROMIMETIC AGENT; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CHOLESTEROL BLOOD LEVEL; CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DYSLIPIDEMIA; HEART; HUMAN; HUMAN CELL; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; THYROID GLAND; TIME TO MAXIMUM PLASMA CONCENTRATION; TRIACYLGLYCEROL BLOOD LEVEL;

ANIMALS; BONE DENSITY; CLINICAL TRIALS AS TOPIC; DRUG DISCOVERY; DYSLIPIDEMIAS; HUMANS; MALE; MICE; MICE, INBRED C57BL; PYRIDAZINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP; THYROID HORMONE RECEPTORS BETA; URACIL;

EID: 84901273457     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4019299     Document Type: Article

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