therapeutic compounds . More specifically the present invention pertains to certain 1 - ( 5 - tert - butyl - 2 - aryl - pyrazol - 3 - yl ) - 3 - [ 2 - fluoro - 4 - [ ( 3 - oxo 4H - pyrido [ 2 , 3 - b ] pyrazin - 8 - yl ) oxylphenyl ] urea compounds ( referred herein as “ TBAP compounds ” ) that , inter alia , inhibit RAF ( e . g . , BRAF , CRAF , etc . ) . The present invention also pertains to pharmaceutical com positions 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 .

1 - ( 5 - TERT - BUTYL - 2 - ARYL - PYRAZOL - 3 - YL ) . 3 - 12 - FLUORO - 4 - [ ( 3 - OXO - 4H - PYRIDO [ 2 . 3 - BJPYRAZIN - 8 - YL ) OXY | PHENYLJUREA DERIVATIVES AS RAF INHIBITORS FOR THE TREATMENT OF CANCER / Joy SPRINGER, Caroline; Marais, Richard; Girotti, Romina; - DUVAZ, Dan NICULESCU; - DUVAZ, Ion NICULESCU; Zambon, Alfonso. - (2017 Jun 29).

1 - ( 5 - TERT - BUTYL - 2 - ARYL - PYRAZOL - 3 - YL ) . 3 - 12 - FLUORO - 4 - [ ( 3 - OXO - 4H - PYRIDO [ 2 . 3 - BJPYRAZIN - 8 - YL ) OXY | PHENYLJUREA DERIVATIVES AS RAF INHIBITORS FOR THE TREATMENT OF CANCER

Alfonso ZAMBON
2017-06-29

Abstract

therapeutic compounds . More specifically the present invention pertains to certain 1 - ( 5 - tert - butyl - 2 - aryl - pyrazol - 3 - yl ) - 3 - [ 2 - fluoro - 4 - [ ( 3 - oxo 4H - pyrido [ 2 , 3 - b ] pyrazin - 8 - yl ) oxylphenyl ] urea compounds ( referred herein as “ TBAP compounds ” ) that , inter alia , inhibit RAF ( e . g . , BRAF , CRAF , etc . ) . The present invention also pertains to pharmaceutical com positions 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 .
CANCER RESEARCH TECHNOLOGY LIMITED , London ( GB ) ; INSTITUTE OF CANCER RESEARCH : ROYAL CANCER HOSPITAL ( THE ) , London ( GB
: US 2017 / 0298066 A1
Joy SPRINGER, Caroline; Marais, Richard; Girotti, Romina; - DUVAZ, Dan NICULESCU; - DUVAZ, Ion NICULESCU; Zambon, Alfonso
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/1177262
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