Reverse-turn mimetics and method relating thereto

Details Reverse-turn mimetics and method relating thereto Reverse-turn mimetics and method relating thereto

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/53 (2006.01) A61P 35/00 (2006.01) C40B 40/00 (2006.01) G01N 33/53 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2521846

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 over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds 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.

L'invention concerne des composés à conformation restreinte qui imitent la structure secondaire de coudes bêta de protéines et de peptides biologiquement actifs. Ces structures mimétiques de coudes bêta présentent une utilité dans de nombreux domaines et peuvent être utilisées notamment comme agents diagnostiques et thérapeutiques. L'invention concerne également des bibliothèques contenant ces structures mimétiques de coudes bêta, ainsi que des procédés de criblage desdites structures pour identifier des éléments biologiquement actifs. L'invention concerne par ailleurs l'utilisation de ces composés pour inhiber ou traiter des troubles modulés par la voie de signalisation de Wnt, tels que le cancer, en particulier le cancer colorectal, la resténose associée à l'angioplastie, la maladie polykystique des reins, l'angiogenèse aberrante, l'arthrite rhumatoïde, la sclérose tubéreuse, la maladie d'Alzheimer, l'hyperpilosité ou la chute excessive des cheveux, ou la colite ulcéreuse.

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