Reverse-turn mimetics and composition and methods relating...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2502644

Reverse-turn mimetics and methods relating to the same having Structure (I) are disclosed, including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.

La présente invention concerne des mimétiques à rotation inverse et des techniques associées, qui possèdent une structure (I), des sels et des stéréo-isomères de ceux-ci répondant aux normes pharmaceutiques. Dans cette structure (I) R¿1?, R¿2?, R¿3? et R¿4? sont tels que définis dans les spécifications. Ces composés conviennent pour une grande gamme d'applications, notamment l'utilisation de ceux-ci comme agents diagnostiques et thérapeutiques. Les composés et les compositions pharmaceutiques de cette invention contenant ces composés sont, en particulier, des antagonistes de neurokinine (tachykinine). Cette invention concerne aussi des bibliothèques contenant ces mimétiques à rotation inverse.

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