J
John W. Clader
Researcher at Merck & Co.
Publications - 114
Citations - 5530
John W. Clader is an academic researcher from Merck & Co.. The author has contributed to research in topics: Alkyl & SCH-48461. The author has an hindex of 37, co-authored 113 publications receiving 5383 citations. Previous affiliations of John W. Clader include Schering-Plough.
Papers
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Journal ArticleDOI
Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption.
Stuart B. Rosenblum,Tram Huynh,Adriano Afonso,Harry R. Davis,Yumibe Nathan P,John W. Clader,Duane A. Burnett +6 more
TL;DR: Through the SAR analysis of a series of putative metabolites of 2, compound 1 was targeted and found to exhibit remarkable efficacy with an ED50 of 0.04 mg/kg/day for the reduction of liver cholesteryl esters in a 7-day cholesterol-fed hamster model.
Journal ArticleDOI
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo.
Julie M. Strizki,Serena Xu,Nicole Wagner,Lisa Wojcik,Jia Liu,Yan Hou,Matthias Endres,Anandan Palani,Sherry Shapiro,John W. Clader,William J. Greenlee,Jayaram R. Tagat,Stuart W. McCombie,Kathleen Cox,Ahmad Fawzi,Chuan-Chu Chou,Catherine Pugliese-Sivo,Liza Davies,Mary E. Moreno,David D. Ho,Alexandra Trkola,Cheryl A. Stoddart,John P. Moore,Gregory R. Reyes,Bahige M. Baroudy +24 more
TL;DR: SCH-C has broad and potent antiviral activity in vitro against primary HIV-1 isolates that use CCR5 as their entry coreceptor, with mean 50% inhibitory concentrations ranging between 0.4 and 9 nM.
Journal ArticleDOI
HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use
Alexandra Trkola,Shawn E. Kuhmann,Julie M. Strizki,Elizabeth S. Maxwell,Tom Ketas,Thomas Hunt Morgan,Pavel Pugach,Serena Xu,Lisa Wojcik,Jayaram R. Tagat,Anandan Palani,Sherry Shapiro,John W. Clader,Stuart W. McCombie,Gregory R. Reyes,Bahige M. Baroudy,John P. Moore +16 more
TL;DR: HIV-1 acquires the ability to use CCR5 despite the inhibitor, first by requiring lower levels of C CR5 for entry and then probably by using the drug-bound form of the receptor.
Journal ArticleDOI
The discovery of ezetimibe: a view from outside the receptor.
TL;DR: The discovery of the novel cholesterol-lowering agent ezetimibe represents a distinct outlier from these trends, and this perspective will focus on the unusual process that led to its discovery and what lesson can be gleaned from this process.
Patent
Piperidine derivatives useful as CCR5 antagonists
Bahige M. Baroudy,John W. Clader,Hubert B. Josien,Stuart W. McCombie,Mckittrick Brian A,Michael W. Miller,Bernard R. Neustadt,Anandan Palani,Steensma Ruo,Jayaram R. Tagat,Vice Susan F,Laughlin Mark A +11 more
TL;DR: The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is -C(R13)2-, -C (R13)(R13), R19)-, -c(O)-, O-, -NH-, -N(alkyl)-, (a), (b), (c), (d), (e), (f), (g, (h), (h, (i), (j), (k, (k), (l), (m), (n) or (n