Amidine derivatives with nitric oxide synthetase activities

Details Amidine derivatives with nitric oxide synthetase activities Amidine derivatives with nitric oxide synthetase activities

C - Chemistry, Metallurgy

07

D

C07D 333/38 (2006.01) A61K 31/155 (2006.01) A61K 31/33 (2006.01) C07C 257/14 (2006.01) C07C 257/18 (2006.01) C07D 207/34 (2006.01) C07D 213/81 (2006.01) C07D 277/56 (2006.01) C07D 295/155 (2006.01) C07D 307/68 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2169280

Compounds of formula (I) wherein D represents phenyl, pyridinyl or a 5-membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O S and N, which three groups are optionally substituted by one or more groups selected from alkyl C1 to 6, alkoxy C1 to 6, halogen and perfluoroalkyl C1 to 6; or perfluoroalkyl C1 to 6; R1 represents hydrogen, alkyl C1 to 6 or halogen; R2 represents a group -X(CH2)nZCONR3R4, -X(CH2)nNHCO(CH2)sNR3R4, -X(CH2)pNR3R4, -X(CH2)nNHCOR5 or -(CH2)qNHC(NH)R6; and X, Z, R3, R4, R5, R6, n, s, p and q are defined in the specification are described, together with processes for their preparation and compositions containing them. Compounds of formula (I) have nitric oxide synthetase inhibitory activity.

L'invention concerne des composés de la formule (I) dans laquelle D représente un phényle, un pyridinyle ou un noyau aromatique hétérocyclique pentagonal contenant de 1 à 4 hétéroatomes choisis parmi O, S et N, ces trois groupes étant facultativement substitués par un ou plusieurs groupes choisis dans alkyle C1 à 6, alcoxy C1 à 6, halogène et perfluoroalkyle C1 à 6; ou perfluoroalkyle C1 à 6; R<1> représente hydrogène, alkyle C1 à 6 ou halogène; R<2> représente un groupe -X(CH2)nZCONR<3>R<4>, -X(CH2)nNHCO(CH2)sNR<3>R<4>, -X(CH2)pNR<3>R<4>, -X(CH2)nNHCOR<5>, ou -(CH2)qNHC(NH)R<6>; et X, Z, R<3>, R<4>, R<5>, R<6>; n, s, p et q sont définis dans la description de l'invention, laquelle concerne également les procédés de préparation desdits composés ainsi que les compositions les contenant. Les composés selon la formule (I) ont une activité inhibitrice de la synthétase de l'oxyde nitrique.

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