Evaluation of a Series of β-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads

Author:

Oehlrich DanielORCID,Peschiulli Aldo,Tresadern GaryORCID,Van Gool Michiel1,Vega Juan Antonio1,De Lucas Ana Isabel1,Alonso de Diego Sergio A.1,Prokopcova Hana,Austin Nigel,Van Brandt Sven,Surkyn Michel,De Cleyn Michel,Vos Ann,Rombouts Frederik J. R.ORCID,Macdonald Gregor,Moechars Dieder,Gijsen Harrie J. M.ORCID,Trabanco Andrés A.1ORCID

Affiliation:

1. Discovery Sciences Medicinal Chemistry, Janssen Research & Development, Janssen−Cilag S.A., C/Jarama 75A, 45007 Toledo, Spain

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Reference22 articles.

1. Alzheimer's Disease: The Amyloid Cascade Hypothesis

2. Purification and cloning of amyloid precursor protein β-secretase from human brain

3. The evolution of amidine-based brain penetrant BACE1 inhibitors

4. New evolutions in the BACE1 inhibitor field from 2014 to 2018

5. Efficacy and Safety Trial of Verubecestat (MK-8931) in Participants With Prodromal Alzheimer's Disease (MK-8931-019) (APECS). ClinicalTrials.gov; U.S. National Library of Medicine, 2013. https://clinicaltrials.gov/ct2/show/NCT01953601.

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