Anamar Ab

Per Lek

Torbjörn Lundstedt

Elisabeth Seifert

Arne Boman

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 Rto Rrepresents halogen; at least one of R, R, R, Rand Ris selected from &#x2014;S&#x2014;R or &#x2014;COOR, or two or more Of R-Rcomprise a linking group such as &#x2014;S&#x2014;(CH2)S&#x2014;, 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 Ris selected from &#x2014;S&#x2014;R, then at least one of R, Rand Ris most preferably selected from halogen; and R, R, R, Rand Rare 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. 

Aminoguanidines as melanocortin receptor ligands

There are described Compounds of formula (I) in which Rto Rare independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; Ris an optionally substituted phenyl, benzyl or cyclohexyl group; Ris selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated Chydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, osteoarthritis, mental disorders, or for inducing central nerve regeneration. 

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Uppsala, Sweden

Per Lek