Arginine analogues having nitric oxide synthase inhibitor...

Details Arginine analogues having nitric oxide synthase inhibitor... Arginine analogues having nitric oxide synthase inhibitor...

C - Chemistry, Metallurgy

07

C

C07C 279/36 (2006.01) A61K 31/155 (2006.01) A61K 31/22 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07C 279/04 (2006.01) C07C 279/14 (2006.01) C07D 207/327 (2006.01) C07D 231/04 (2006.01) C07D 231/12 (2006.01) C07D 233/02 (2006.01) C07D 233/61 (2006.01) C07D 275/02 (2006.01) C07D 295/088 (2006.01) C07D 295/15 (2006.01) C07D 295/185 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2215476

L-arginine derivatives of general formula (I), a method for preparing same, and pharmaceutical compositions containing said derivatives, are disclosed. Such compounds are biologically active as nitric oxide synthase inhibitors. In the general formula, A is a hydrogen atom, a lower alkyl grouping or a nitro radical, E is an oxygen atom or a covalent bond, n is 0 or an integer from 1 to 12, and each of R1 and R2 is a straight or branched alkyl chain, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- or 6-membered ring of formula (a), wherein X is a hydrogen, sulphur or nitrogen atom or an imino, alkylimino or methylene radical.

L'invention concerne des dérivés de la L-arginine de formule générale (I), un procédé pour leur préparation et des compositions pharmaceutiques les contenant. Le composé de l'invention présente une activité biologique en tant qu'inhibiteurs de la NO synthase. Dans la formule, A représente un atome d'hydrogène, un groupement alkyl inférieur ou le radical nitro, E représente un atome d'oxygène ou une liaison covalente, n est égal à zéro ou un entier de 1 à 12, et soit R1 et R2 représentent indépendamment une chaîne alkyl linéaire ou ramifiée, soit R1 et R2 forment, ensemble, avec l'atome d'azote sur lequel ils sont rattachés, un cycle à 5 ou 6 chaînons, saturés ou insaturés, de formule (a), dans lequel X représente un atome d'hydrogène, de soufre ou d'azote, le radical imino, alkylimino ou méthylène.

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