Abstract
We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as γ-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of γ-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting Aβ(42) production.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Alzheimer Disease / drug therapy
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Amyloid Precursor Protein Secretases / metabolism*
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Amyloid beta-Peptides / antagonists & inhibitors*
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Amyloid beta-Peptides / metabolism
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Animals
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Bridged Bicyclo Compounds, Heterocyclic / chemistry*
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Bridged Bicyclo Compounds, Heterocyclic / pharmacokinetics
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Humans
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Rats
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Structure-Activity Relationship
Substances
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Amyloid beta-Peptides
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Bridged Bicyclo Compounds, Heterocyclic
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Amyloid Precursor Protein Secretases