Background E7046 is a highly selective, small-molecule antagonist of the E-type prostanoid
receptor 4 (EP4) for prostaglandin E2, an immunosuppressive mediator of the tumor immune …

Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-
ylsulfonyl) aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an …

A series of potent PDGFR inhibitors has been identified. The series was optimized for
duration of action in the lung. A novel kinase occupancy assay was used to directly measure …

Lemborexant is approved for treating insomnia and is under investigation for treating
irregular sleep‐wake rhythm disorder. Based on in vitro drug‐drug interaction (DDI) …

Abstract Nonstructural protein 5A (NS5A) represents a novel target for the treatment of
hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol–Myers–Squibb, is a potent …

In ongoing studies towards novel hepatitis C virus (HCV) therapeutics, inhibitors of
nonstructural protein 5A (NS5A) were evaluated. Specifically, starting from previously …

Several non-benzimidazole containing inhibitors of respiratory syncytial virus are described.
Core template modification, analysis of antiviral activity, physicochemistry and optimisation …

Lemborexant is a dual orexin receptor antagonist approved for treating insomnia. As the
solubility of lemborexant is pH‐sensitive, the impact of the gastric acid‐reducing agent …

The primary aim of this study was to examine the effect of severe renal impairment (SRI) on
the pharmacokinetics of lemborexant, a dual orexin receptor antagonist indicated for the …

Lemborexant, a dual orexin receptor antagonist, is approved in the United States, Japan,
and Canada for the treatment of insomnia in adults. This phase I, multicenter, open‐label …