Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 207/12 (2006.01) A01N 1/02 (2006.01) C07D 207/10 (2006.01) C07D 207/20 (2006.01) C07D 207/24 (2006.01) C07D 213/82 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2266006

A compound of formula (I) and the salts thereof, wherein A is halo, hydroxy or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, naphthyl, pyridyl and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Composés de la formule (I) et leurs sels. Dans ladite formule, A est halo, hydroxy ou analogue; la ligne en pointillé représente une liaison double facultative, à condition que A soit absent si cette ligne en pointillé est une liaison double; Ar?1¿ est phényle éventuellement substitué ou analogue; Ar?2¿ est aryle ou hétéroaryle choisi parmi phényle, naphtyle, pyridyle et analogue, aryle ou hétéroaryle étant éventuellement substitués, R?1¿ est hydrogène, hydroxy, alkyle C¿1?-C¿4? ou analogue; et R?2¿ et R?3¿ sont choisis indépendamment parmi alkyle C¿1?-C¿7?, cycloalkyle C¿3?-C¿6?, alcényle C¿2?-C¿6?, alkynyle C¿2?-C¿6? et analogue, ou bien R?2¿ et R?3¿, en compagnie de l'atome d'azote auquel ils sont fixés, constituent un anneau pyrrolidine, pipéridine ou morpholine éventuellement substitué. Les composés décrits sont efficaces comme agonistes de récepteur du type kappa.

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