Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation-Reference-Cited by-同舟云学术

Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation

Published:2018-04-03 Issue:10 Volume:61 Page:4476-4504
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

O’Neill Brian T.¹^ORCID,Beck Elizabeth M.²,Butler Christopher R.²^ORCID,Nolan Charles E.³,Gonzales Cathleen³,Zhang Lei²^ORCID,Doran Shawn D.⁴,Lapham Kimberly⁴,Buzon Leanne M.¹,Dutra Jason K.¹,Barreiro Gabriela²,Hou Xinjun²,Martinez-Alsina Luis A.¹,Rogers Bruce N.²,Villalobos Anabella²,Murray John C.¹,Ogilvie Kevin¹,LaChapelle Erik A.¹,Chang Cheng⁴,Lanyon Lorraine F.⁵,Steppan Claire M.⁵,Robshaw Ashley³,Hales Katherine³,Boucher Germaine G.⁶,Pandher Karamjeet⁶,Houle Christopher⁶,Ambroise Claude W.³,Karanian David⁶,Riddell David³,Bales Kelly R.³,Brodney Michael A.²^ORCID

Affiliation:

1. Medicine Design, Medicinal Chemistry, Pfizer Inc., Groton, Connecticut 06340, United States

2. Medicine Design, Medicinal Chemistry, Pfizer Inc., Cambridge, Massachusetts 02139, United States

3. Internal Medicine, Pfizer Inc., Cambridge, Massachusetts 02139, United States

4. Medicine Design, Pharmacokinetics, Dynamics and Metabolism, Pfizer Inc., Groton, Connecticut 06340, United States

5. Discovery Sciences, Primary Pharmacology, Pfizer Inc., Groton, Connecticut 06340, United States

6. Drug Safety Research and Development, Pfizer Inc., Groton, Connecticut 06340, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b00246

Reference44 articles.

1. The -Secretase Enzyme BACE in Health and Alzheimer's Disease: Regulation, Cell Biology, Function, and Therapeutic Potential

2. BACE and γ-Secretase Characterization and Their Sorting as Therapeutic Targets to Reduce Amyloidogenesis

3. Additive Effects of PS1 and APP Mutations on Secretion of the 42-Residue Amyloid β-Protein

4. A mutation in APP protects against Alzheimer’s disease and age-related cognitive decline

5. Amyloid deposition as the central event in the aetiology of Alzheimer's disease

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