Sung Hwan Moon;Masakatsu Eguchi;Sung Chan Lee;Jae Uk Chung;Kwang Won Jeong;Cu Nguyen;Michael Kahn
发明人:
Sung Hwan Moon,Jae Uk Chung,Sung Chan Lee,Masakatsu Eguchi,Michael Kahn,Kwang Won Jeong,Cu Nguyen
申请号:
US12553858
公开号:
US08106049B2
申请日:
2009.09.03
申请国别(地区):
US
年份:
2012
代理人:
摘要:
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility as diagnostic and therapeutic agents for inhibiting or treating disorders modulated by 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. In one embodiment, these reverse-term mimetics have a general structure of formula (VI):wherein Ra, Rb, Rc, X1, X2 and X3 are defined as provided herein.