WNT PROTEIN SIGNALLING INHIBITORS

摘要

The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.

主权项

1. A method of inhibiting Wnt protein signalling in a cell comprising administering to the cell an effective amount of a compound of the formula:wherein:
R1 is alkyl(C≦8) or substituted alkyl(C≦8); and R10 is aryl(C≦8), substituted aryl(C≦8), heterocycloalkyl(C≦8) or substituted heterocycloalkyl(C≦8);wherein R2 is alkoxy(C≦8), substituted alkoxy(C≦8), acyl(C≦8), substituted acyl(C≦8), heterocycloalkyl(C≦8) or substituted heterocycloalkyl(C≦8);wherein:
R3 is acyl(C≦8), substituted acyl(C≦8), heterocycloalkyl(C≦8) or substituted heterocycloalkyl(C≦8); R4 is hydrogen, alkyl(C≦8) or substituted alkyl(C≦8); and R5 alkyl(C≦8) or substituted alkyl(C≦8);wherein:
R6 is hydrogen, alkyl(C≦8), or substituted alkyl(C≦8); R7 is hydrogen, alkyl(C≦8) or substituted alkyl(C≦8); and R8 is alkyl(C≦8), substituted alkyl(C≦8), aryl(C≦8), or substituted aryl(C≦8);wherein:
R9 is acyl(C≦8), substituted acyl(C≦8), alkyl(C≦8), substituted alkyl(C≦8), heterocycloalkyl(C≦8) or substituted heterocycloalkyl(C≦8); oror a pharmaceutically acceptable salt or tautomer thereof.