2-Benzimidazolyl-9-(chroman-4-yl)-purinone derivatives as JAK3 inhibitors
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 mechanistic mouse model through inhibition of interleukin-2 (IL-2) induced interferon-γ (INF-γ) production.
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.
scheme or table
p. 6788 - 6792
(2010/06/12)
7-SUBSTITUTED PURINE DERIVATIVES FOR IMMUNOSUPPRESSION
The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula (III).
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(2008/12/05)
7-Substituted Purine Derivatives for Immunosuppression
The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula III:
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(2008/12/05)
8-SUBSTITUTED 2-(BENZIMIDAZOLYL)PURINE DERIVATIVES FOR IMMUNOSUPPRESSION
The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula I:
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Page/Page column 9
(2008/06/13)
PURINE AND IMIDAZOPYRIDINE DERIVATIVES FOR IMMUNOSUPPRESSION
The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas ( I ) and ( II ).
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Page/Page column 97-98
(2010/11/24)
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