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
Brevetto
Data di Pubblicazione:
2017
Citazione:
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).
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 .
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 .
Tipologia CRIS:
Brevetto
Elenco autori:
Joy Springer, Caroline; Marais, Richard; Girotti, Romina; - DUVAZ, Dan Niculescu; - DUVAZ, Ion Niculescu; Zambon, Alfonso
Link alla scheda completa: