6-substituted heteroquinolinecarboxylic acid derivatives and...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01) A61K 31/4709 (2006.01) A61P 25/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2364754

6-Substituted heteroquinolinecarboxylic acid derivatives represented by general formula (1) and addition salts thereof, exhibiting antagonism against excitatory amino acid receptors, particularly AMPA receptor; and processes for the preparation of both. In formula (1) A is a single bond or methylene (CH2); Y is nitrogen or =CH-; V is a single bond or methylene (CH2); T is hydroxyl, amino, lower alkoxycarbonyl, carboxyl, formyl, or the like; R is nitro, trifluoromethyl, or halogeno; and R1 is hydroxyl or lower alkoxy.

L'invention se rapporte à des dérivés d'acide hétéroquinolinecarboxylique 6-substitués représentés par la formule générale (1) et aux sels d'addition associés, qui s'avèrent posséder une action antagoniste dirigée contre les récepteurs d'acides aminés excitateurs, et notamment le récepteur d'AMPA. L'invention se rapporte également à des procédés de préparation de ces dérivés et de leurs sels. Dans la formule (1), A est une liaison simple ou méthylène (CH¿2?); Y est azote ou =CH-; V est une liaison simple ou méthylène (CH¿2?); T est hydroxyle, amino, alcoxycarbonyle inférieur, carboxyle, formyle ou analogue; R est nitro, trifluorométhyle ou halogéno; et R?1¿ est hydroxyle ou alcoxy inférieur.

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