Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy-Reference-Cited by-同舟云学术

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Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy

Published:2017 Issue:4 Volume:8 Page:730-743
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Pettersson Martin¹²³,Johnson Douglas S.¹²³,Rankic Danica A.¹⁴³,Kauffman Gregory W.¹²³,am Ende Christopher W.¹⁴³,Butler Todd W.¹⁴³,Boscoe Brian¹⁴³,Evrard Edelweiss¹²³,Helal Christopher J.¹⁴³,Humphrey John M.¹⁴³,Stepan Antonia F.¹²³,Stiff Cory M.¹⁴³,Yang Eddie¹⁴³,Xie Longfei¹⁴³,Bales Kelly R.⁵²³,Hajos-Korcsok Eva⁵²³,Jenkinson Stephen⁶⁷⁸³,Pettersen Betty⁹⁷⁴³,Pustilnik Leslie R.¹⁰⁴³,Ramirez David S.⁶⁷⁸³,Steyn Stefanus J.¹¹⁷²³,Wood Kathleen M.⁵²³,Verhoest Patrick R.¹²³

Affiliation:

1. Neuroscience and Pain Medicinal Chemistry

2. Cambridge

3. USA

4. Groton

5. Neuroscience and Pain Research Unit

6. Global Safety Pharmacology

7. Pfizer Worldwide Research and Development

8. La Jolla

9. Drug Safety R&D

10. Primary Pharmacology Group

11. Pharmacokinetics, Dynamics and Metabolism

Abstract

γ-Secretase modulators for the treatment of Alzheimer's disease.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2017/MD/C6MD00406G

Reference34 articles.

1. 2013 Alzheimer's disease facts and figures

2. The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

3. A subset of NSAIDs lower amyloidogenic Aβ42 independently of cyclooxygenase activity

4. Modulation of γ-Secretase Reduces β-Amyloid Deposition in a Transgenic Mouse Model of Alzheimer's Disease

5. Amyloid β Protein: Aβ40 Inhibits Aβ42 Oligomerization

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1. LipMetE (Lipophilic Metabolism Efficiency) as a Simple Guide for Half-Life and Dosing Regimen Prediction of Oral Drugs;ACS Medicinal Chemistry Letters;2022-08-23

2. Evaluation of chromane derivatives: Promising privileged scaffolds for lead discovery within Alzheimer’s disease;Bioorganic & Medicinal Chemistry;2022-08

3. Small molecules targeting γ-secretase and their potential biological applications;European Journal of Medicinal Chemistry;2022-03

4. Characterizing the Chemical Space of γ-Secretase Inhibitors and Modulators;ACS Chemical Neuroscience;2021-07-22

5. Condensed Pyridopyrimidines and Pyridopyrazines Containing a Bridgehead Nitrogen Atom: Synthesis, Chemical Properties and Biological Activity;Current Organic Chemistry;2021-07-14

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