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.
摘要：
呼吸道合胞病毒(RSV)是婴幼儿住院的主要病因,老年人,和免疫力低下的患者。虽然半衰期延长的单克隆抗体和2疫苗最近已被批准用于婴儿和老年人，分别,在免疫受损的患者中仍需要预防疾病的选择.这里,我们描述螺-氮杂环丁烷羟吲哚作为小分子RSV进入抑制剂显示良好的效力，可开发属性，以水性悬浮液形式注射时的长效PK，提示在这些免疫受损的患者中，通过1或2次长效肌内（IM）或皮下（SC）注射，它们有可能在3至6个月内预防RSV感染后的并发症。
