User profiles for Patrick Verhoest

Patrick Verhoest

pfizer
Verified email at pfizer.com
Cited by 6987

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

…, AE Stewart, JB Tuttle, L Updyke, PR Verhoest… - 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 …

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties

TT Wager, X Hou, PR Verhoest… - ACS chemical …, 2010 - ACS Publications
The interplay among commonly used physicochemical properties in drug design was examined
and utilized to create a prospective design tool focused on the alignment of key druglike …

Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes

…, X Hou, MD Troutman, PR Verhoest… - ACS chemical …, 2010 - ACS Publications
As part of our effort to increase survival of drug candidates and to move our medicinal chemistry
design to higher probability space for success in the Neuroscience therapeutic area, we …

Central nervous system multiparameter optimization desirability: application in drug discovery

TT Wager, X Hou, PR Verhoest… - ACS chemical …, 2016 - ACS Publications
Significant progress has been made in prospectively designing molecules using the central
nervous system multiparameter optimization (CNS MPO) desirability tool, as evidenced by …

Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia

…, FD Tingley, RD Williams, PR Verhoest… - … of Pharmacology and …, 2008 - ASPET
We have recently proposed the hypothesis that inhibition of the cyclic nucleotide
phosphodiesterase (PDE) 10A may represent a new pharmacological approach to the treatment of …

Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl] …

PR Verhoest, DS Chapin, M Corman… - Journal of medicinal …, 2009 - ACS Publications
By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase
(PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a …

Total Synthesis of (+)-Phorboxazole A Exploiting the Petasis− Ferrier Rearrangement

AB Smith, KP Minbiole, PR Verhoest… - Journal of the …, 2001 - ACS Publications
A highly convergent, stereocontrolled total synthesis of the potent antiproliferative agent (+)-phorboxazole
A (1) has been achieved. Highlights of the synthesis include: modified Petasis−…

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 …

…, RG Kurumbail, TT Wager, PR Verhoest… - 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, …

Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the …

…, MB Skaddan, TJ McCarthy, PR Verhoest… - Journal of medicinal …, 2013 - ACS Publications
To accelerate the discovery of novel small molecule central nervous system (CNS) positron
emission tomography (PET) ligands, we aimed to define a property space that would …

(−)-Spiro [1-azabicyclo [2.2. 2] octane-3, 5 '-oxazolidin-2 '-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the α7 …

…, J Loch, E Wu, A Kover, P Verhoest… - Journal of medicinal …, 2000 - ACS Publications
Neuronal nicotinic acetylcholine receptors are members of the ligand-gated ion channel
receptor superfamily and may play important roles in modulating neurotransmission, cognition, …