5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01)

Patent

CA 2669561

The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.

L'invention porte sur des dérivés de 5,6,7,8-tétrahydro-imidazo[1,5-a]pyrazine de formule (1), dans laquelle X représente CH2 ou O ; R1 représente un groupe phényle, lequel groupe est indépendamment mono-, di- ou tri- substitué, les substituants étant indépendamment choisis dans le groupe constitué par alkyle en C1-C4, alcoxy en C1-C4, halogène, cyano, trifluorométhoxy et trifluorométhyle ; R2 représente alkyle en C1-C4, alcoxy en C1-C4, alcényle en C2-C4, halogène, cyano, hydroxyméthyle, trifluorométhyle, C(O)NR5R6ou cyclopropyle ; R3 représente alkyle en C1-C4, alcoxy en C1-C4-méthyle, ou halogène ; R4représente alkyle en C1-C4 ; R5 représente hydrogène ou alkyle en C1-C4 ; et R6 représente hydrogène ou alkyle en C1-C4. L'invention porte également sur des sels pharmaceutiquement acceptables de tels composés ; et sur l'utilisation de tels composés en tant que médicaments, notamment en tant qu'antagonistes du récepteur de l'orexine.

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