| 摘要 |
There is disclosed amidino derivatives of formula (I), pharmaceutical compositions containing these derivatives, and their use in therapy, in particular their use as nitric oxide synthase inhibitors wherein: X is alkyl, alkenyl, alkynyl, -(CH2)kQ(CH2)l- where k is 2 or 3, l is 1 or 2 and Q is 0, Se SiY2 where Y is alkyl, S(O)z where z is 0, 1 or 2, NR where R is hydrogen or alkyl, or -(CH2)mA(CH2)n- where m is 0, 1 or 2, n is 0, 1 or 2, A is 3 to 6 membered aromatic hydrocarbon radical or 3 to 6 membered heterocyclic radical wherein 1 to 3 hetero atoms are oxygen, sulfur or nitrogen and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; R1 may be a bond to X or hydrogen (when Q is Se), hydroxyalkyl, alkyl, alkenyl, alkynyl or haloalkyl and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; R2 is alkyl, alkenyl, alkynyl, aromatic hydrocarbon radical, haloalkyl, hydroxylamine or heterocyclic radical wherein 1 to 3 hetero atoms are oxygen, sulfur or nitrogen and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; and R3 is amino, alkylamine, amino acid, hydroxy, alkoxy, tetrazole or tetrazoloamine. |
