[EN] SMALL MOLECULE DEGRADERS OF HELIOS AND METHODS OF USE<br/>[FR] AGENTS DE DÉGRADATION À PETITES MOLÉCULES D'HÉLIOS ET PROCÉDÉS D'UTILISATION
申请人:DANA FARBER CANCER INST INC
公开号:WO2021087093A1
公开(公告)日:2021-05-06
Disclosed are compounds and pharmaceutically acceptable salts, hydrates, solvates, prodrugs, stereoisomers, or tautomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with Helios and which may benefit from Helios degradation.
[EN] AMIDE PHOSPHINE OXIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF<br/>[FR] DÉRIVÉ D'OXYDE DE PHOSPHINE AMIDE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 酰胺膦氧类衍生物及其制备方法和用途
This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
Compounds of Formula 1, as shown below and defined herein:
and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.