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 31/5513 (2006.01) A61K 45/06 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2562693

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 contraints par conformation qui imitent la structure secondaire de régions à rotation inverse de peptides et de protéines biologiquement actifs. De telles structures mimétiques à rotation inverse ont une utilité dans un grand nombre de domaines, notamment en tant qu'agents diagnostiques et thérapeutiques. L'invention concerne également des bibliothèques contenant les structures mimétiques à rotation inverse de la présente invention, ainsi que des procédés de criblage de celles-ci, en vue d'identifier des éléments biologiquement actifs. L'invention concerne en outre l'utilisation de ces composés pour l'inhibition ou le traitement de troubles modulés par une voie de signalisation, tels que le cancer, en particulier le cancer colorectal, la resténose consécutive à l'angioplastie, la maladie polykistique des reins, l'angiogenèse aberrante, l'arthrite rhumatoïde, le syndrome de la sclérose tubéreuse, la maladie d'Alzheimer, la croissance ou la perte excessive de cheveux, ou la colite ulcéreuse.

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