Satoki Doi

TL;DR: The antiviral activity and resistance profile in vitro of a novel IN inhibitor, elvitegravir (EVG) (also known as JTK-303/GS-9137), currently being developed for the treatment of HIV-1 infection are described, suggesting that IN inhibitors bind to a conformationally conserved region of various retroviral IN enzymes and are an ideal drug for a range of Retroviral infections.

TL;DR: A new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold and displaying a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.

TL;DR: A novel series of RORγ inhibitors was identified starting with the HTS hit 1.0 and significant improvement of metabolic stability as well as reduction of CYP inhibition was observed, which finally led to discovery of a selective and orally efficacious Rorγ inhibitor 3z.

TL;DR: A series of JAK inhibitors are developed, which incorporate novel three-dimensional spiro motifs and unexpectedly possess both excellent physicochemical properties and anti-dermatitis efficacy in the animal models.

TL;DR: Introduction of metabolically beneficial motifs in conjunction with scaffold hopping was examined, resulting in discovery of the second generation RORγ inhibitor composed of a 4-(isoxazol-3-yl)butanoic acid scaffold.