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 31/4985 (2006.01) A61K 31/53 (2006.01) A61K 31/5513 (2006.01) A61K 45/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2462922

Conformationally constrained compounds which 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,or ulcerative colitis.

L'invention concerne des composés caractérisés par une conformation restreinte qui imitent la structure secondaire des régions de retournement de protéines et de peptides bioactifs. Ces structures mimétiques de retournement sont utilisées dans de nombreux domaines d'application, notamment comme agents diagnostiques et thérapeutiques. Par ailleurs, l'invention concerne des banques contenant ces structures mimétiques de retournement ainsi que des procédés de criblage de ces structures qui visent à identifier des éléments bioactifs. De plus, l'invention concerne l'utilisation de ces composés pour inhiber ou traiter des troubles modulés par la voie de signalisation Wnt, notamment le cancer, en particulier le cancer colorectal, la resténose consécutive à une angioplastie, la maladie polykystique des reins, l'angiogenèse aberrante, l'arthrite rhumatoïde ou la colite ulcéreuse.

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