2. Academic Validation
  3. Discovery of gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors

Discovery of gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors

  • J Med Chem. 2024 Aug 22;67(16):13723-13736. doi: 10.1021/acs.jmedchem.4c00525.
Sandrine Grosse 1,  Ludwig Cooymans 1,  Werner Embrechts 1,  David McGowan 2,  Edgar Jacoby 1,  Bart Stoops 1,  Kusum Gupta 3,  Mark Ackermann 4,  Sarhad Alnajjar 5,  Jerome Guillemont 6,  Zhinan Jin 7,  Bart Kesteleyn 1,  Kiran Matcha 1,  Pun Sriboonyapirat 4,  Anh Truong 3,  Joke Van Den Berg 1,  Xiaodi Yu 8,  Florence Herschke 1,  Dirk Roymans 9,  Pierre Raboisson 10,  Peter Rigaux 1,  Tim H M Jonckers 1
Affiliations

Affiliations

  • 1 Janssen Research & Development, Janssen Pharmaceutica NV, 2340 Beerse, Belgium.
  • 2 Aligos, Gaston Geenslaan 1, 3001 Leuven, Belgium.
  • 3 Neuron23 Inc. 343 Oyster Point Blvd, South San Francisco, California 94080, United States.
  • 4 LambCure LLC, Corvallis, Oregon 97232, United States.
  • 5 Department of Comparative Biomedical Sciences, School of Veterinary Medicine, Faculty of Health and Medical Sciences, University of Surrey, Guildford GU2 7AL, U.K.
  • 6 NovAlix, 27106 Val-de-Reuil, France.
  • 7 Janssen Pharmaceutica NV, Brisbane, California 94005, United States.
  • 8 Janssen Pharmaceutica NV, Spring House, Pennsylvania 19477 United States.
  • 9 DNS Life Sciences Consulting, Brandhoefstraat 63, 2300 Turnhout, Belgium.
  • 10 Galapagos, General De Wittelaan L112, A3, 2800 Mechelen, Belgium.
PMID: 39105710 DOI: 10.1021/acs.jmedchem.4c00525
Abstract

Respiratory syncytial virus (RSV) is an RNA virus infecting the upper and lower respiratory tract and is recognized as a major respiratory health threat, particularly to older adults, immunocompromised individuals, and young children. Around 64 million children and adults are infected every year worldwide. Despite two vaccines and a new generation monoclonal antibody recently approved, no effective Antiviral treatment is available. In this manuscript, we present the medicinal chemistry efforts resulting in the identification of compound 28 (JNJ-8003), a novel RSV non-nucleoside inhibitor displaying subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models.

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