A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/517 (2006.01) A61P 25/24 (2006.01) C07D 403/10 (2006.01) C07D 405/14 (2006.01)
Patent
CA 2728376
The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2- heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical com-positions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently se-lected from -CH group or a nitrogen atom (-N), W is independently selected from an aryl group, an heteroaryl group, or a benzo-condensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3- dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzoth-iophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). R1 is independently selected from hydrogen (-H), C1-C4alkyl, hydroxymethyl (-CH2OH), aminomethyl (-CH2NH2), alkylaminomethyl [CH2NH(R2)], or di- alkylaminomethyl [CH2N(R2)2], trifluoromethyl (--CF3). Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related dis-orders, Parkinson disease, drug abuse, and morphine tolerance and dependence.
La présente invention porte sur des dérivés de 6-(1H-imidazo-1-yl)-2-aryl et 2-hétéroaryl-quinazoline et de quinoléines, composés de formule (I), leurs sels et solvates pharmaceutiquement acceptables et sur des compositions pharmaceutiques correspondantes, qui servent d'inhibiteurs de la monoamine oxydase (MAO) et des ligands des récepteurs d'imidazolines : où : X est indépendamment choisi parmi un groupe CH ou un atome d'azote (-N), W est indépendamment choisi parmi un groupe aryle, un groupe hétéroaryle ou un groupe hétéroaryle benzocondensé tel que le 1,3-benzodioxole, le benzofurane, le 2,3-dihydrobenzofurane, le benzothiophène, le 2,3-dihydrobenzothiophène, l'indole, le 2,3-dihydroindole, le benzimidazole, le benzoxazole, le benzothiazole, le 2H-3,4-dihydrobenzopyrane, la [1,4]-benzodioxine, la 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxane). R1 est indépendamment choisi parmi hydrogène (-H), alkyle en C1-C4, hydroxyméthyle (-CH2OH), aminométhyle (-CH2NH2), alkylaminométhyle [CH2NH(R2)] ou di-alkylaminométhyle [CH2N(R2)2], trifluorométhyle (-CF3). Les composés de formule (I) ont déclenché un profil pharmacologique approprié pour le traitement clinique de la dépression et de troubles apparentés, la maladie de Parkinson, l'abus de médicaments et la tolérance et la dépendance à la morphine.
Caselli Gianfranco
Giordani Antonio
Lanza Marco
Makovec Francesco
Mandelli Stefano
Macrae & Co.
Rottapharm S.p.a.
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