N-(2-phenyl-4-amino-butyl)-1-naphthamides as neurokinin-1...

Details N-(2-phenyl-4-amino-butyl)-1-naphthamides as neurokinin-1... N-(2-phenyl-4-amino-butyl)-1-naphthamides as neurokinin-1...

C - Chemistry, Metallurgy

07

C

C07C 255/57 (2006.01) A61K 31/275 (2006.01) A61P 1/00 (2006.01) A61P 11/00 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) C07D 295/12 (2006.01) C07D 295/125 (2006.01)

Patent

CA 2368240

A compound having the general formula (I): R1R2N-CH2CH2-CHAr1-CH2-NR3-CO-R4 wherein: R1 is hydrogen, C1-6 alkyl, C2-6 alkenyl, aryl, C1-6 alkanoyl C1-6 alkoxycarbonyl or arylcarbonyl; any of such groups being optionally substituted; R2 is hydrogen or C1-6 alkyl; or R1 or R2 are joined to form an optionally substituted morpholino ring; Ar1 is phenyl mono- or di-substituted by halo; R3 is hydrogen or C1-6 alkyl; R4 is optionally substituted naphth-1- yl; or pharmaceutically acceptable salts thereof. These compounds antagonize the pharmacological actions of the endogenous neuropeptide tachykinins, particularly the neurokinin 1 (NK1) receptor.

Cette invention concerne un composé de formule générale (I): R?1¿R?2¿N-CH¿2?CH¿2?-CHAr?1¿-CH¿2?-NR?3¿-CO-R?4¿ dans laquelle: R?1¿ est hydrogène, alkyle en C¿1-6?l, alcényle en C¿2-6?, aryle, alkoxycarbonyle or arylcarbonyle en C¿1-6?; l'un quelconque de tels groupes étant éventuellement substitués; R?2¿ est hydrogène ou alkyle en C¿1-6?; ou R?1¿ ou R?2¿ sont reliés pour former un noyau morpholino éventuellement substitué; Ar?1¿ est phényl mono- ou di-substitué par halo; R?3¿ est hydrogène ou alkyle en C¿1-6?; R?4¿ est naphth-1-yl éventuellement substitué. L'invention concerne également des sels de ces composés acceptables au plan pharmaceutique. Ces composés antagonisent les effets pharmacologiques des tachykinines neuropetidiques endogènes, en particulier le récepteur de la neurokinine-1 (NK1).

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