C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/4745 (2006.01) A61P 13/12 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2755045
Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H- pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4- difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3- (5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5- difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3- fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, glioma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, and biliary tract cancer.
L'invention concerne le propane-1-acide sulfonique {2,4-difluoro-3-[5-(2-méthoxy-pyrimidine-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phényl}-amide, le propane-1-acide sulfonique [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phényl]-amide, le propane-1-acide sulfonique [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phényl]-amide, le N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phényl]-2,5-difluoro-benzènesulfonamide, le N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phényl]-3-fluoro-benzènesulfonamide, le pyrrolidine-1-acide sulfonique [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phényl]-amide, le N,N-diméthylamino-acide sulfonique [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phényl]-amide, et leurs sels, leurs formulations, leurs conjugués, leurs dérivés, leurs formes et leurs utilisations. Dans certains aspects et modes de réalisation, les composés selon l'invention ou leurs sels, leurs formulations, leurs conjugués, leurs dérivés, et leurs formes sont actifs sur au moins une protéine kinase Raf. L'invention concerne également leurs procédés d'utilisation pour traiter des maladies et des états, y compris des maladies et états associés à l'activité des protéines kinases Raf, notamment le mélanome, le gliome, le cancer colorectal, le cancer de la thyroïde, le cancer du poumon, le cancer de l'ovaire, le cancer de la prostate, et le cancer du tractus biliaire.
Cho Hanna
Ibrahim Prabha N.
Spevak Wayne
Zhu Hongyao
Mbm Intellectual Property Law Llp
Plexxikon Inc.
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