摘要:
The invention relates to a new and improved process for the preparation of 6-methyl-2-(4-methyl-phenyl)-imidazo[1,2-a]pyrimidine-3-(N,N-dimethyl-acetamide) of Formula (I) and pharmaceutically acceptable acid addition salts thereof which comprises reacting an ester of general Formula (II) (wherein R is lower alkyl or phenyl-lower alkyl) in a polar protic or aprotic solvent with dimethyl amine and, if desired, converting the compound of the Formula (I) thus obtained into a pharmaceutically acceptable acid addition salt. The compound of Formula I is a known valuable sedative used in therapy. The invention also relates to new intermediates of general Formula (II) (wherein R is lower alkyl or phenyl-lower alkyl) useful in the process.
摘要:
The invention relates to new acid amide derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said acid amide derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The new compounds according to the invention can be characterized by formula (I), wherein R1 represents hydrogen or nitro, R?2 and R3¿ stand, independently from each other, for hydrogen, lower alkyl or lower alkenyl optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated heteroring containing 1 or 2 nitrogen and/or oxygen atom(s); or R?2 and R3¿ form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group containing optionally 1 or 2 additional nitrogen atoms and/or oxygen atom(s), said ring optionally carrying a hydroxy or a hydroxy-lower alkyl group, and possess valuable AMPA and kainate antagonizing properties, so they can be used to advantage in the therapy.
摘要:
The invention refers to novel benzofuran derivatives of formula (I), a process for preparing these compounds and to pharmaceutical compositions containing these active substances.