Azomethines agonist compounds of the histamine h3 receptor...

C - Chemistry – Metallurgy – 07 – D

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C07D 233/64 (2006.01) A61K 31/415 (2006.01) C07D 233/54 (2006.01) C07D 403/12 (2006.01)

Patent

CA 2063550

The compounds having the formula: (see formula I) wherein R5, R6, R7 and R8 each denote hydrogen or methyl, R5 and R6 taken together form methylene and R5, R6, R7 and R8 do not simultaneously denote hydrogen, R2 is phenyl or imidazolyl, unsubstituted, monosubstituted or polysubstituted with R4, and R2 is unattached to R3 or is attached to R3, R3 is H, or has the meaning of R2 or R4, and R4 is H, OR3, COOR3, halogen, CF3 or unsubstituted, monosubstituted or polysubstituted alkyl, or a pharmaceutically acceptable salt thereof. The compounds are derived from an R-NH2 amine with a strong affinity for the histamine H3-receptor and to the primary amine function of which is bonded a group forming a bond which can hydrolyze slowly in a neutral medium. The pharmaceutical compositions consist of these compounds and a pharmaceutically acceptable excipient. The compounds are used to produce a drug inhibiting histamine synthesis and release, and having, in particular, sedative, sleep regulating, anti-convulsive, anti-depressive, anti- allergic, anti-inflammatory, anti-secretory or anti-ulcerous effects.

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