An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

…, S Berritt, B Boras, RD Cardin, A Carlo, KJ Coffman… - Science, 2021 - science.org
The worldwide outbreak of COVID-19 caused by severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) has become a global pandemic. Alongside vaccines, antiviral …

Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant …

…, BL Kormos, MM Hayward, KJ Coffman… - Journal of medicinal …, 2015 - ACS Publications
Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson’s disease (PD)
by genome-wide association studies (GWAS). The most common LRRK2 mutation, …

Memory distortions in coerced false confessions: A source monitoring framework analysis

LA Henkel, KJ Coffman - … Psychology: The Official Journal of the …, 2004 - Wiley Online Library
Confessions are routinely offered as evidence and are potentially damning to defendants.
However, not all confessions are truthful. Suspects can be coerced into falsely confessing to …

Design and Discovery of 6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one …

…, MM Claffey, JB Tuttle, KJ Coffman… - Journal of medicinal …, 2012 - ACS Publications
6-[(3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
(PF-04447943) is a novel PDE9A inhibitor …

Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): A Highly Potent …

…, MM Claffey, L Chen, KJ Coffman… - Journal of medicinal …, 2014 - ACS Publications
A novel series of pyrazolopyrazines is herein disclosed as mGluR5 negative allosteric
modulators (NAMs). Starting from a high-throughput screen (HTS) hit (1), a systematic structure–…

Pharmacodynamics and pharmacokinetics of the γ-secretase inhibitor PF-3084014

…, SA Sokolowski, CD Hicks, KJ Coffman… - … of Pharmacology and …, 2010 - ASPET
PF-3084014 [(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide]
is a novel γ-secretase …

Identification of Multiple 5-HT4 Partial Agonist Clinical Candidates for the Treatment of Alzheimer's Disease

…, A Sawant-Basak, KJ Coffman… - Journal of medicinal …, 2012 - ACS Publications
The cognitive impairments observed in Alzheimer’s disease (AD) are in part a consequence
of reduced acetylcholine (ACh) levels resulting from a loss of cholinergic neurons. …

Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: Discovery of PF-3084014

…, SL Becker, BS Bronk, TM Brown, KJ Coffman… - Bioorganic & medicinal …, 2011 - Elsevier
A novel series of tetralin containing amino imidazoles, derived from modification of the
corresponding phenyl acetic acid derivatives is described. Replacement of the amide led to …

Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

TJ Rosen, KJ Coffman, S McLean, RT Crawford… - Bioorganic & medicinal …, 1998 - Elsevier
The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist
CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in …

Scalable, Telescoped Hydrogenolysis–Enzymatic Decarboxylation Process for the Asymmetric Synthesis of (R)-α-Heteroaryl Propionic Acids

…, E Yang, RM Howard, KJ Coffman… - … Process Research & …, 2020 - ACS Publications
Enantiopure α-aryl propionic acids are useful building blocks for pharmaceutical research
and can be accessed enzymatically using arylmalonate decarboxylases (AMDases) from the …