The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain l-(5-tert-butyl-2-aryl-pyrazol-3-yl)- 3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as "TBAP compounds") that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of mutant BRAF; disorders ameliorated by the inhibition of BRAF and CRAF; disorders associated with RAS mutations and/or MAPK pathway activation; disorders ameliorated by the inhibition of SRC, p38, FGFRA, VEGFR-2 (KDR), and/or LCK; etc.

Preparation of 1-​(5-​tert-​butyl-​2-​aryl-​pyrazol-​3-​yl)​-​3-​[2-​fluoro-​4-​[(3-​oxo-​4H-​pyrido[2,​3-​b]​pyrazin-​8-​yl)​oxy]​phenyl]​urea derivatives as RAF inhibitors for treating cancer / Springer, Caroline Joy; Marais, Richard; Girotti, Romina; Niculescu-Duvaz, Dan; Niculescu-Duvaz, Ion; Zambon, Alfonso. - (2013 Nov 13).

Preparation of 1-​(5-​tert-​butyl-​2-​aryl-​pyrazol-​3-​yl)​-​3-​[2-​fluoro-​4-​[(3-​oxo-​4H-​pyrido[2,​3-​b]​pyrazin-​8-​yl)​oxy]​phenyl]​urea derivatives as RAF inhibitors for treating cancer

Zambon, Alfonso
2013

Abstract

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain l-(5-tert-butyl-2-aryl-pyrazol-3-yl)- 3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as "TBAP compounds") that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of mutant BRAF; disorders ameliorated by the inhibition of BRAF and CRAF; disorders associated with RAS mutations and/or MAPK pathway activation; disorders ameliorated by the inhibition of SRC, p38, FGFRA, VEGFR-2 (KDR), and/or LCK; etc.
13-nov-2013
25-nov-2014
CANCER RESEARCH TECHNOLOGY LIMITED [GB/GB]; INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) [GB/GB] 123 Old Brompton Road, London Greater London SW7 3RP (GB)
WO 2015/075483 Al
Internazionale
Springer, Caroline Joy; Marais, Richard; Girotti, Romina; Niculescu-Duvaz, Dan; Niculescu-Duvaz, Ion; Zambon, Alfonso
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/1172725
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