作者
Bart Kesteleyn,Florence Herschke,Nicolas Darville,Bart Stoops,Tom Jacobs,Edgar Jacoby,P.L. Shaffer,Lieve Lammens,Dries Van Rompaey,Kiran Matcha,Carolina Martínez Lamenca,Erwin Coesemans,Geerwin Haché,Serge Pieters,Morgan Lecomte,Lili Hu,Samuël Demin,Cynthia Milligan,Pravien Abeywickrema,Suzanne de Bruyn,Joke Van Den Berg,Nina Ysebaert,Loeckie De Zwart,Isabel Nájera,Peter Rigaux,Dirk Roymans,Tim H. M. Jonckers
摘要
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.