A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/505 (2006.01) A61K 31/44 (2006.01)
Patent
CA 2176251
Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'- dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)- 1,2,3,6-tetrahydropyridine or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)- 6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6- (diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4- diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino- 4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock). The latter two types are advantageously administered with nitric oxide synthase inhibitors (concurrent therapy) or to potentiate the effect of .alpha.1-adrenergic agonists in the prophylaxis or treatment of induced hypotension.
Administration d'un inhibiteur de l'utilisation de la tétrahydrobioptérine en tant que cofacteur de la synthase de l'oxyde nitrique, c'est-à-dire des 4-phényl(hydropyridines) substituées telles que la 1-méthyl-4-(3',4'-dihydroxyphényl)-1,2,3,6-tétrahydropyridine ou la 4-(3',4'-dihydroxyphényl-1,2,3,6-tétrahydropyridine) ou un analogue de la tétrahydroptérine qui ne remplace pas la tétrahydrobioptérine comme substrat de la synthase de l'oxyde nitrique, par exemple la (6R,S)-6,7-diméthyl-tétrahydroptérine ou l'acide (6R,S)-tétrahydrofolique ou les 2,4-diamino, 2,6-diamino ou 4,6-diamino-pyrimidines mono- ou bisubstituées ou les 3-oxydes de pyrimidine tels que la 2,4-diamino-6-(diéthylamino)pyrimidine, le 3-oxyde de 2,4-diamino-6-pipéridino-pyrimidine, la 2,4-diamino-6-hydroxypyrimidine, la 4,6-diamino-2-hydroxypyrimidine ou la 2,5-diamino-4,6-dihydroxypyrimidine, en vue d'inhiber la synthèse de l'oxyde nitrique à partir de l'arginine dans les cellules vasculaires chez un subjet nécessitant cette inhibition (p. ex. pour la prévention ou le traitement de l'hypotension induite par des cytokines ou des endotoxines (choc septique p. ex.)). Les deux derniers types sont avantageusement administrés avec des inhibiteurs de la synthase de l'oxyde nitrique (traitement associé) ou pour renforcer les effets des agonistes .alpha.¿1?-adrénergiques dans la prévention ou le traitement de l'hypotension induite.
Gross Steven S.
Cornell Research Foundation Inc.
Macrae & Co.
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