Hydrazide derivatives of 3,4-dihydro-2h-1-benzopyrans

Details Hydrazide derivatives of 3,4-dihydro-2h-1-benzopyrans Hydrazide derivatives of 3,4-dihydro-2h-1-benzopyrans

C - Chemistry, Metallurgy

07

D

C07D 311/58 (2006.01) A61K 31/35 (2006.01) C07D 311/66 (2006.01) C07D 311/72 (2006.01)

Patent

CA 2132831

This invention relates to novel hydrazide acyl hydrazinium derivatives of certain 3,4-dihydro-2H-1-benzopyrans of formula (1), the stereoisomers and mixtures thereof, their inner salts, and the pharmaceutically acceptable salts thereof wherein R is H or C1-6 alkyl, R1 is C1-6 alkyl, R2 is H or -C(O)R, R3 and R4 are independently C1-6 alkyl; R5 is C1-6 alkyl, or (a) with R8 being H or halogeno, n is zero, 1, 2, or 3 and X is a halide, -S(O)3R6, or nothing when the inner salt is formed, R6 is H, C1-6 alkyl, phenyl or 4-methylphenyl, to the intermediates, processes and techniques for their preparation, to their ability to manifest the property of being free radical scavengers, and to their end-use application in the treatment of disease conditions capable of being ameliorated by free radical scavengers.

L'invention porte sur de nouveaux dérivés hydrazide acyle hydrazinium de certains 3,4-dihydro-2H-1-benzopyranes de formule (1), sur leurs stéréoisomères et leurs mélanges, leurs sels internes et leurs sels acceptables en pharmacie, où R est H ou un alkyle C1-6, R1 est un alkyle C1-6, R2 est H ou -C(O)R, R3 et R4 sont indépendamment un alkyle C1-6; R5 est un alkyle C1-6, ou (a) avec R8 étant un H ou un halogène, n est 0, 1, 2 ou 3 et X est un halogénure, -S(O)3R6, ou rien lorsque le sel interne est formé, R6 est H, un alkyle C1-6, un phényle ou le 4-méthylphényle; l'invention porte aussi sur des intermédiaires, des méthodes et des techniques pour leur préparation, sur leur capacité de jouer le rôle de capteurs de radicaux libres, et sur leur utilisation finale pour le traitement de maladies pouvant être soulagées par des capteurs de radicaux libres.

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