SUBSTITUTED QUINOXALINE COMPOUNDS AS INHIBITORS OF FGFR TYROSINE KINASES

• Main Authors: Blake, James F, MORENO, David A, REN, Li, WALLS, Shane M
• Format: Patent
• Language: English
• Published: 10.02.2022
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Provided herein are 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives of the general Formula I; and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which X2 is N and Ring A, Ring B, Ring C, X1, X3, R1, L, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, such as e.g. cancer, e g. bladder cancer, brain cancer, breast cancer, cholangiocarcinoma, head and neck cancer, lung cancer, multiple myeloma, rhabdomyosarcoma, urethral cancer and uterine cancer. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 276 to 308; examples 1 to 30; examples A to E; tables CA to EE). An exemplary compound is e.g. 1-(3-(4-(4-(7-((3,5-dimethoxy phenyl) amino)quinoxalin-2-yl)-1H-pyrazol-1-yl)piperidine-1-carbonyl) azetidin-1-yl)prop-2-en-1-one (e.g. example 1).