%0 Journal Article
%T Spiro-Azetidine Oxindoles as Long-Acting Injectables for Pre-Exposure Prophylaxis against Respiratory Syncytial Virus Infections.
%A Kesteleyn B
%A Herschke F
%A Darville N
%A Stoops B
%A Jacobs T
%A Jacoby E
%A Shaffer P
%A Lammens L
%A Van Rompaey D
%A Matcha K
%A Martinez Lamenca C
%A Coesemans E
%A Hache G
%A Pieters S
%A Lecomte M
%A Hu L
%A Demin S
%A Milligan C
%A Abeywickrema P
%A De Bruyn S
%A Van Den Berg J
%A Ysebaert N
%A De Zwart L
%A Nájera I
%A Rigaux P
%A Roymans D
%A Jonckers THM
%J J Med Chem
%V 67
%N 13
%D 2024 Jul 11
%M 38932487
%F 8.039
%R 10.1021/acs.jmedchem.4c00514
%X 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.