2. Academic Validation
  3. Spiro-Azetidine Oxindoles as Long-Acting Injectables for Pre-Exposure Prophylaxis against Respiratory Syncytial Virus Infections

Spiro-Azetidine Oxindoles as Long-Acting Injectables for Pre-Exposure Prophylaxis against Respiratory Syncytial Virus Infections

  • J Med Chem. 2024 Jul 11;67(13):10986-11002. doi: 10.1021/acs.jmedchem.4c00514.
Bart Kesteleyn 1,  Florence Herschke 1,  Nicolas Darville 1,  Bart Stoops 1,  Tom Jacobs 1,  Edgar Jacoby 1,  Paul Shaffer 2,  Lieve Lammens 1,  Dries Van Rompaey 1,  Kiran Matcha 1,  Carolina Martinez Lamenca 1,  Erwin Coesemans 1,  Geerwin Hache 1,  Serge Pieters 1,  Morgan Lecomte 1,  Lili Hu 1,  Samuel Demin 1,  Cynthia Milligan 2,  Pravien Abeywickrema 2,  Suzanne De Bruyn 1,  Joke Van Den Berg 1,  Nina Ysebaert 1,  Loeckie De Zwart 1,  Isabel Nájera 1,  Peter Rigaux 1,  Dirk Roymans 1,  Tim H M Jonckers 1
Affiliations

Affiliations

  • 1 Janssen Research & Development, Janssen Pharmaceutica NV, Turnhoutseweg 30, Beerse 2340, Belgium.
  • 2 Janssen Research & Development, 1400 McKean Rd, Spring House, Pennsylvania 19477, United States.
PMID: 38932487 DOI: 10.1021/acs.jmedchem.4c00514
Abstract

Respiratory syncytial virus (RSV) is a major cause of hospitalization in infants, the elderly, and immune-compromised patients. While a half-life extended monoclonal antibody and 2 vaccines have recently been approved for infants and the elderly, respectively, options to prevent disease in immune-compromised patients are still needed. Here, we describe spiro-azetidine oxindoles as small molecule RSV entry inhibitors displaying favorable potency, developability attributes, and long-acting PK when injected as an aqueous suspension, suggesting their potential to prevent complications following RSV Infection over a period of 3 to 6 months with 1 or 2 long-acting intramuscular (IM) or subcutaneous (SC) injections in these immune-compromised patients.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-163773
    Antiviral Compound
    RSV