2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors

…, V Paradkar, C Kingsbury, JG Quintero, H Park…

Index: Cole, Andrew G.; Bohnstedt, Adolph C.; Paradkar, Vidyadhar; Kingsbury, Celia; Quintero, Jorge G.; Park, Haengsoon; Lu, Yingchun; You, Ming; Neagu, Irina; Diller, David J.; Letourneau, Jeffrey J.; Shao, Yuefei; James, Ray A.; Riviello, Christopher M.; Ho, Koc-Kan; Lin, Tsung H.; Wang, Bojing; Appell, Kenneth C.; Sills, Matthew; Quadros, Elizabeth; Kimble, Earl F.; Ohlmeyer, Michael H.J.; Webb, Maria L. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6788 - 6792

Full Text: HTML

Citation Number: 14

Abstract

A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2- benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent of the purinone, compound 24 was identified incorporating a chroman-based functional group. Compound 24 shows excellent kinase activity, good oral bioavailability and demonstrates efficacy in an acute ...