Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)- 3,5-difluorobenzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A phosphonooxymethylene prodrug of a potent and selective hA 2A receptor antagonist

Journal of Medicinal Chemistry

Volumn 54, Issue 3, 2011, Pages 751-764

  Sams, Anette G ^a   Mikkelsen, Gitte K ^a   Larsen, Mogens ^a   Langgård, Morten ^a   Howellŝ, Mark E ^a   Schrøder, Tenna J ^a   Brennum, Lise T ^a   Torup, Lars ^a   Jørgensen, Erling B ^b   Bundgaard, Christoffer ^c   Kreilgård, Mads ^c   Bang Andersen, Benny ^a  

^a H LUNDBECK A S   (Denmark)

^b LEO PHARMA A S   (Denmark)

^c NOVOZYMES A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

4 (3,3 DIMETHYL BUTYRYLAMINO)3,5 DIFLUORO N THIAZOL 2 YL BENZAMIDE; ANTIHISTAMINIC AGENT; HISTAMINE RECEPTOR; LU AA47070; PHOSPHORIC ACID MONO[2 (4 (3,3 DIMETHYL BUTYRYLAMINO) 3,5 DIFLUORO BENZOYLIMINO)THIAZOL 3 YLMETHYL]ESTER; PRODRUG; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG SOLUBILITY; HUMAN; HUMAN CELL; MALE; MOUSE; NONHUMAN; PARKINSON DISEASE; RAT; STRUCTURE ACTIVITY RELATION; SUSPENSION; SYSTEMIC CIRCULATION;

ADENOSINE A2 RECEPTOR ANTAGONISTS; ANIMALS; ANTIPARKINSON AGENTS; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; CHO CELLS; CRICETINAE; CRICETULUS; CRYSTALLOGRAPHY, X-RAY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MALE; MICE; MODELS, MOLECULAR; PHOSPHORIC ACID ESTERS; PRODRUGS; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; WATER;

EID: 79851491088     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm1008659     Document Type: Article

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