AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics

Journal of Alzheimer's Disease

Volumn 50, Issue 4, 2016, Pages 1109-1123

  Eketjäll, Susanna ^a,b   Janson, Juliette ^a,b   Kaspersson, Karin ^c   Bogstedt, Anna ^a,b   Jeppsson, Fredrik ^c   Fälting, Johanna ^c,e   Haeberlein, Samantha Budd ^d,f   Kugler, Alan R ^d   Alexander, Robert C ^d,g   Cebers, Gvido ^d  

^a SCIENCE FOR LIFE LABORATORY   (Sweden)

^b KAROLINSKA INSTITUTE   (Sweden)

^c ASTRAZENECA R AND D   (Sweden)

^d ASTRAZENECA   (United Kingdom)

^e BioArctic Neuroscience   (Sweden)

^f BIOGEN   (United States)

^g PFIZER INC   (United States)

Author keywords

Alzheimer's disease; amyloid ; drug therapy; pharmacology; preclinical drug evaluation

Indexed keywords

(1R,1',4R) 4 METHOXY 5" METHYL 6' [5 (PROP 1 YN 1 YL)PYRIDIN 3 YL] 3'H DISPIRO(CYCLOHEXANE 1,2' INDEN 1',2" IMIDAZOL) 4" AMINE; AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; AMYLOID PRECURSOR PROTEIN; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; UNCLASSIFIED DRUG; 4-METHOXY-5'-METHYL-6'-(5-(PROP-1-YN-1-YL)PYRIDIN-3-YL)-3'H-DISPIRO(CYCLOHEXANE-1,2'-INDEN-1',2'-IMIDAZOL)-4'-AMINE; AMYLOID BETA PROTEIN; AMYLOID BETA-PROTEIN (1-42); ENZYME INHIBITOR; IMIDAZOLE DERIVATIVE; PEPTIDE FRAGMENT; SECRETASE; SPIRO COMPOUND;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; BRAIN NERVE CELL; CEREBROSPINAL FLUID; CONTROLLED STUDY; DOG; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; FEMALE; GUINEA PIG; IN VITRO STUDY; IN VIVO STUDY; KINETICS; MOUSE; NONHUMAN; PHARMACODYNAMICS; PLASMA; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RAT; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD ANALYSIS; BRAIN; C57BL MOUSE; DOSE RESPONSE; DRUG EFFECTS; ENZYMOLOGY; HUMAN; MALE; METABOLISM; ORAL DRUG ADMINISTRATION; PRECLINICAL STUDY;

ADMINISTRATION, ORAL; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; BLOOD CHEMICAL ANALYSIS; BLOOD-BRAIN BARRIER; BRAIN; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; FEMALE; GUINEA PIGS; HUMANS; IMIDAZOLES; KINETICS; MALE; MICE, INBRED C57BL; PEPTIDE FRAGMENTS; SPIRO COMPOUNDS;

EID: 84959432061     PISSN: 13872877     EISSN: 18758908     Source Type: Journal    
DOI: 10.3233/JAD-150834     Document Type: Article

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