NOVEL AMINOGUANIDINES AS MELANOCORTIN RECEPTOR LIGANDS.

摘要

There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0,1,2 or 3, saturated or unsaturated; most preferably at least one of R₁ to R₅ represents halogen; at least one of R₁, R₂, R₃, R₄ and R₅ is selected from -S-R or -COOR, or two or more Of R₁-R₅ comprise a linking group such as -S-(CH2)_mS-, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R₁ is selected from -S-R, then at least one of R₂, R₃ and R₅ is most preferably selected from halogen; and R₁, R₂, R₃, R₄ and R₅ are otherwise the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.