Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-Site amyloid precursor protein cleaving enzyme (Bace1) inhibitors

Journal of Medicinal Chemistry

Volumn 55, Issue 21, 2012, Pages 9025-9044

  Dineen, Thomas A ^a   Weiss, Matthew M ^a   Williamson, Toni ^a   Acton, Paul ^a   Babu Khan, Safura ^a   Bartberger, Michael D ^a   Brown, James ^a   Chen, Kui ^a   Cheng, Yuan ^a   Citron, Martin ^a   Croghan, Michael D ^a   Dunn, Robert T ^a   Esmay, Joel ^a   Graceffa, Russell F ^a   Harried, Scott S ^a   Hickman, Dean ^a   Hitchcock, Stephen A ^a   Horne, Daniel B ^a   Huang, Hongbing ^a   Imbeah Ampiah, Ronke ^a   Judd, Ted ^a   Kaller, Matthew R ^a   Kreiman, Charles R ^a   La, Daniel S ^a   Li, Vivian ^a   Lopez, Patricia ^a   Louie, Steven ^a   Monenschein, Holger ^a   Nguyen, Thomas T ^a   Pennington, Lewis D ^a   San Miguel, Tisha ^a   Sickmier, E Allen ^a   Vargas, Hugo M ^a   Wahl, Robert C ^a   Wen, Paul H ^a   Whittington, Douglas A ^a   Wood, Stephen ^a   Xue, Qiufen ^a   Yang, Bryant H ^a   Patel, Vinod F ^a   Zhong, Wenge ^a   more..

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMYLOID BETA PROTEIN; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; CYTOCHROME P450 3A4; ETHANOLAMINE; N [3 HYDROXY 4 [6' NEOPENTYL 3',4' DIHYDROSPIRO[CYCLOBUTANE 1,2' PYRANO[2,3 B]PYRIDINE] 4' YLAMINO] 1 [3 (THIAZOL 2 YL)PHENYL]BUTAN 2 YL] 2 METHOXYACETAMIDE; N [3 HYDROXY 4 [6' NEOPENTYL 3',4' DIHYDROSPIRO[CYCLOBUTANE 1,2' PYRANO[2,3 B]PYRIDINE] 4' YLAMINO] 1 [3 (THIAZOL 2 YL)PHENYL]BUTAN 2 YL] 2 METHOXYPROPANAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CARDIOVASCULAR FUNCTION; CEREBROSPINAL FLUID LEVEL; CHEMICAL MODIFICATION; CONTROLLED STUDY; DOG; DRUG BIOAVAILABILITY; DRUG BRAIN LEVEL; DRUG DESIGN; DRUG EFFICACY; DRUG PENETRATION; DRUG POTENCY; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; MALE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BLOOD PROTEINS; BRAIN; CELL LINE; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; DRUG DESIGN; HUMANS; MALE; MICROSOMES, LIVER; MODELS, MOLECULAR; PEPTIDE FRAGMENTS; PROTEIN BINDING; PROTEIN CONFORMATION; RATS; RATS, SPRAGUE-DAWLEY; SPIRO COMPOUNDS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SWINE; THIAZOLES;

EID: 84867590210     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300118s     Document Type: Article

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