Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): Identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′ H -spiro[chromeno[2,3- b ]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)

Journal of Medicinal Chemistry

Volumn 57, Issue 23, 2014, Pages 9811-9831

  Dineen, Thomas A ^a   Chen, Kui ^a   Cheng, Alan C ^a   Derakhchan, Katayoun ^a   Epstein, Oleg ^a   Esmay, Joel ^a   Hickman, Dean ^a   Kreiman, Chuck E ^a   Marx, Isaac E ^a   Wahl, Robert C ^a   Wen, Paul H ^a   Weiss, Matthew M ^a   Whittington, Douglas A ^a   Wood, Stephen ^a   Fremeau, Robert T ^a   White, Ryan D ^a   Patel, Vinod F ^a,b  

^a AMGEN INC   (United States)

^b Neuroscience Comparative Biology and Safety Sciences Amgen Inc ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (NEOPENTYLOXY) 7 (PYRIMIDIN 3 YL) 5' H SPIRO [CHROMENO [2,3 B] PYRIDINE 5,4' OXAZOL] 2' AMINE; 3 (NEOPENTYLOXY) 7 (PYRIMIDIN 5 YL) 5' H SPIRO [CHROMENO [2,3 B] PYRIDINE 5,4' OXAZOL] 2' AMINE; 7 (2 FLUOROPYRIDIN 3 YL) 3 ((3 METHYLOXETAN 3 YL)ETHYNYL) 5' H SPIRO[CHROMENO [2,3 B] PYRIDINE 5,4' OXAZOL] 2' AMINE; 7 (2 FLUOROPYRIDIN 3 YL) 3 (NEOPENTYLOXY) 5' H SPIRO [CHROMENE [2,3 B] PYRIDINE 5,4' OXAZOL] 2' AMINE; 7 (2,2 DIMETHYLPROPOXY) 3 (5 PYRIMIDINYL) SPIRO [CHROMENE [2,3 B] 5,4' [1,3] OXAZOLE] 2' AMINE; AMYLOID BETA PROTEIN; BETA SECRETASE INHIBITOR; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG; XANTHENE; (S)-7-(2-FLUOROPYRIDIN-3-YL)-3-((3-METHYLOXETAN-3-YL)ETHYNYL)-5'H-SPIRO(CHROMENO(2,3-B)PYRIDINE-5,4'-OXAZOL)-2'-AMINE; ASPARTIC PROTEINASE; BACE1 PROTEIN, HUMAN; BENZOPYRAN DERIVATIVE; KCNH1 PROTEIN, HUMAN; PROTEINASE INHIBITOR; PYRIDINE DERIVATIVE; SECRETASE; SPIRO COMPOUND;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG BRAIN LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MALE; NONHUMAN; PHARMACODYNAMICS; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG EFFECTS; HEK293 CELL LINE; IC50; LIVER MICROSOME; METABOLISM; SPRAGUE DAWLEY RAT; SYNTHESIS;

AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BENZOPYRANS; ETHER-A-GO-GO POTASSIUM CHANNELS; HEK293 CELLS; HUMANS; INHIBITORY CONCENTRATION 50; MICROSOMES, LIVER; PROTEASE INHIBITORS; PYRIDINES; RATS, SPRAGUE-DAWLEY; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84918559343     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5012676     Document Type: Article

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