C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 311/08 (2006.01) A61K 31/353 (2006.01) A61K 31/37 (2006.01) A61P 25/00 (2006.01) C07D 311/58 (2006.01) C07D 311/74 (2006.01) C07D 405/12 (2006.01)
Patent
CA 2601126
This invention is related to novel aminoalkyl- and amidoalkyl- b enzopyran derivatives of the following general formula (I) wherein: the group (a) is a substituent in position 6 or 7 wherein: R is amono- or bi-cyclic (C6-C10) aryl or a mono- or bi-cyclic (5-10) membered heteroaryl radical, said radicals rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halo and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.
L'invention porte sur des dérivés substitués d'aminoalkyl- et amidoalkyl-benzopyran de formule générale (I) dans laquelle: le groupe (II) est un substituant en position 6 ou 7 dans lequel: R est amono- ou aryle (C6-C10) bicyclique ou un radical hétéroaryle mono ou bicyclique à (5-10) éléments, lesdits cycles des radicaux étant facultativement substitués par un ou deux substituants choisis parmi alkyle (C1-C5) droit ou ramifié, alkoxy, hydroxy, halo et trifluorométhyle (C1-C5), droits ou ramifiés et m est zéro ou un entier de 1 à 3; dans la formule (I): n, p, R1 et R2 sont tels que définis dans la description; et R3 et R4 sont tous deux H, ou représentent pris ensemble un atome d'O, ou leurs sels pharmacocompatibles. Lesdits composés agissent en tant qu'inhibiteurs sélectifs et réversibles du MAO-B in vivo et in vitro utiles comme médicaments pour la prévention et le traitement de troubles dégénératifs du SNC.
Caccia Carla
Carotti Angelo
Maestroni Sara
Melloni Piero
Salvati Patricia
Newron Pharmaceuticals S.p.a.
Robic
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