Design of pyridopyrazine-1,6-dione γ-secretase modulators that align potency, MDR efflux ratio, and metabolic stability

ACS Medicinal Chemistry Letters

Volumn 6, Issue 5, 2015, Pages 596-601

  Pettersson, Martin ^a   Johnson, Douglas S ^a   Humphrey, John M ^a   Butler, Todd W ^a   Am Ende, Christopher W ^a   Fish, Benjamin A ^a   Green, Michael E ^a   Kauffman, Gregory W ^a   Mullins, Patrick B ^a   O'Donnell, Christopher J ^a   Stepan, Antonia F ^a   Stiff, Cory M ^a   Subramanyam, Chakrapani ^a   Tran, Tuan P ^a   Vetelino, Beth Cooper ^a   Yang, Eddie ^a   Xie, Longfei ^a   Bales, Kelly R ^a   Pustilnik, Leslie R ^a   Steyn, Stefanus J ^a   Wood, Kathleen M ^a   Verhoest, Patrick R ^a   more..

^a PFIZER INC   (United States)

Author keywords

Alzheimer's disease; fluorine; gamma secretase modulators; LipMetE; lipophilic metabolism efficiency

Indexed keywords

AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; FLUORINE; GAMMA SECRETASE INHIBITOR; PF 06442609; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ARTICLE; DEMETHYLATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG ELIMINATION; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HYDROGENATION; IC50; IN VIVO STUDY; LIPOPHILICITY; MDR EFFLUX RATIO; METABOLIC STABILITY; NONHUMAN; PHARMACOKINETICS; PHARMACOLOGICAL PARAMETERS; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RODENT;

CAVIA; RODENTIA;

EID: 84929309797     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00070     Document Type: Article

References (33)

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33. Solubility was measured by Analiza, Inc., Cleveland, OH (http://analiza.com/physchem/logd.html#qf).