Reverse-turn mimetics and methods relating thereto

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

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/4985 (2006.01) A61K 31/551 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07D 235/00 (2006.01) C07D 241/00 (2006.01) C07D 243/00 (2006.01) C07D 245/00 (2006.01) C07K 5/078 (2006.01) G01N 33/50 (2006.01) A61K 38/00 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2384126

Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having structure (I) are disclosed, wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti- inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Cette invention concerne des composés de conformation contrainte, qui imitent la structure secondaire des régions à rotation inverse de peptides et de protéines biologiquement actifs possédant la structure (I) suivante. Dans cette structure, A, R¿1?, R¿2?, R¿2a?, R¿3?, R¿3a? et R¿4? sont comme définis dans le descriptif. Ces composés trouvent de multiples applications, notamment comme agents diagnostiques et thérapeutiques. Ils sont tout particulièrement utiles comme agents anti-inflammatoires dans des compositions pharmaceutiques. L'invention porte également sur des banques renfermant ces composés ainsi que sur des méthodes de criblage de ces composés en vue de l'identification d'éléments biologiquement actifs.

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