Bis-Quinazoline Derivatives as Inhibitors for Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase
AssigneeTetranov International, Inc
InventorsYusheng Wu, Chengshan Niu, Dapeng Zou, Jingya Li, Ruiyun Guo
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Abstract
Novel bis-quinazoline derivatives as tyrosine kinase inhibitors, synthesis of these compounds, and novel methods for treating tyrosine kinase mediated diseases or disorders using these compounds are disclosed. In particular, the present invention provides tethered quinazoline derivative dimers as inhibitors to the epidermal growth factor receptor (EGFR) tyrosine kinase, pharmaceutical compositions thereof, and their therapeutic uses for treating EGFR kinase-mediated diseases or disorders, such as various cancers, as well as synthetic methods for preparing these novel compounds.
Claims20
A compound of formula I
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein:
- R1 and R2 are each independently —O-alkylene-OCH3;
- Z is a linker selected from the group consisting of:
- —O-(alkylene-X1)m-alkylene-(X2-alkylene)n-O—, —O-(alkylene-X1)m-cycloalkylene-(X2-alkylene)n-O—, and —O-(alkylene-X1)m-heterocyclylene-(X2-alkylene)n-O—;
- X1 and X2, at each occurrence, are independently —O—, —NR3—, —S—, —SO—, or —SO2—;
- m and n, at each occurrence, are independently selected from integers from 1 to 10;
- R3 is H, —COR4, or —SO2R4;
- and
- R4 is alkyl or cycloalkyl.
Dependencies are inferred from the claim text.