Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of Tau aggregation

Journal of Medicinal Chemistry

Volumn 53, Issue 9, 2010, Pages 3739-3747

  Ballatore, Carlo ^a,b   Brunden, Kurt R ^b   Piscitelli, Francesco ^a   James, Michael J ^b   Crowe, Alex ^b   Yao, Yuemang ^b   Hyde, Edward ^b   Trojanowski, John Q ^b   Lee, Virginia M Y ^b   Smith, Amos B ^a  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMINO 3 ( 4 CHLOROPHENYL) N CYCLOPROPYL 4 OXO 3,4 DIHYDROTHIENO[ 3,4 D]PYRIDAZINE 1 CARBOXAMIDE; 5 AMINO 3 ( 4 CHLOROPHENYL) N ISOPROPYL 4 OXO 3,4 DIHYDROTHIENO[ 3,4 D]PYRIDAZINE 1 CARBOXAMIDE; AMINOTHIENOPYRIDAZINE; PROTEIN INHIBITOR; PYRIDAZINE DERIVATIVE; TAU PROTEIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BLOOD BRAIN BARRIER; BRAIN; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SOLUBILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PROTEIN AGGREGATION; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BLOOD-BRAIN BARRIER; DRUG DISCOVERY; MICE; PROTEIN MULTIMERIZATION; PYRIDAZINES; TAU PROTEINS; TAUOPATHIES;

EID: 77952081276     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100138f     Document Type: Article

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