Reverse-turn mimetics and method relating thereto

摘要

Disclosed are compounds having the formula (VI), wherein the substituents are as defined in the specification, and one of the oxygen, sulfur or nitrogen atoms of Ra, Rb, Rc, X1, X2 or X3 is substituted with phosphate, dimethylaminoacetate, dimethylaminoalkylcarbamates or a salt thereof. The compounds are prodrugs of conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins. The compounds are useful for inhibiting or treating disorders modulated by the Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.