P
Patrick Robert Verhoest
Researcher at Pfizer
Publications - 121
Citations - 4534
Patrick Robert Verhoest is an academic researcher from Pfizer. The author has contributed to research in topics: Receptor & Phosphodiesterase. The author has an hindex of 26, co-authored 121 publications receiving 3263 citations. Previous affiliations of Patrick Robert Verhoest include Upjohn.
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An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Dafydd R. Owen,Charlotte Moira Norfor Allerton,Annaliesa S. Anderson,Lisa Aschenbrenner,Melissa Avery,Simon Berritt,Britton Boras,Rhonda D. Cardin,Anthony Carlo,Karen J. Coffman,Alyssa Dantonio,Li Di,Heather Eng,RoseAnn Ferre,Ketan S. Gajiwala,Scott A. Gibson,Samantha Elizabeth Greasley,Brett L. Hurst,Eugene P. Kadar,Amit S. Kalgutkar,Jack C. Lee,Jisun Lee,Wei Liu,Stephen W. Mason,Stephen Noell,Jonathan J. Novak,R. Scott Obach,Kevin Ogilvie,Nandini Chaturbhai Patel,Martin Pettersson,Devendra K. Rai,Matthew R. Reese,Matthew F. Sammons,Jean G. Sathish,Ravi Shankar P. Singh,Claire M. Steppan,Al E. Stewart,Jamison B. Tuttle,Lawrence W. Updyke,Patrick Robert Verhoest,Liuqing Wei,Qingyi Yang,Yuao Zhu +42 more
TL;DR: The worldwide outbreak of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome (SARS-CoV-2) has become a global pandemic as discussed by the authors.
Journal ArticleDOI
Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties
TL;DR: Based on six physicochemical properties commonly used by medicinal chemists, the CNS MPO function may be used prospectively at the design stage to accelerate the identification of compounds with increased probability of success.
Journal ArticleDOI
Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes
Travis T. Wager,Ramalakshmi Yegna Chandrasekaran,Xinjun Hou,Matthew D. Troutman,Patrick Robert Verhoest,Anabella Villalobos,Yvonne Will +6 more
TL;DR: A thorough analysis of properties for 119 marketed CNS drugs and a set of 108 Pfizer CNS candidates focused on understanding the relationships between physicochemical properties, in vitro ADME attributes, primary pharmacology binding efficiencies, and in vitro safety data.
Journal ArticleDOI
Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery
TL;DR: The CNS MPO tool has helped to increase the percentage of compounds nominated for clinical development that exhibit alignment of ADME attributes, cross the blood-brain barrier, and reside in lower-risk safety space (low ClogP and high TPSA).
Journal ArticleDOI
Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia
Christopher J. Schmidt,Douglas S. Chapin,Julie Cianfrogna,M. L. Corman,Mihály Hajós,John F. Harms,William E. Hoffman,L. A. Lebel,Sheryl A. McCarthy,Fredrick R. Nelson,C. Proulx-LaFrance,Mark J. Majchrzak,Andres D. Ramirez,K. Schmidt,Patricia A. Seymour,Judith A. Siuciak,Francis David Tingley,R. D. Williams,Patrick Robert Verhoest,Frank S. Menniti +19 more
TL;DR: The discovery of a new class of PDE10A inhibitors exemplified by TP-10 (2-{4-[-pyridin-4-yl-1-(2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline succinic acid), an agent with greatly improved potency, selectivity, and pharmaceutical properties is described.