Action Pharma A/s

Anamar Ab

Acure Pharma Ab

Synact Pharma Aps

Arne Boman

Elisabeth Seifert

Anna Skottner

Torbjörn Lundstedt

Victor Andrianov

Per Andersson

Per Lek

Ivars Kalvins

Thomas Engelbrecht Norkild Jonassen

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. 

Amides acting on the adenosine receptors

The present invention relates to phenyl pyrrole aminoguanidine derivatives of the general formula (I): (I) including tautomeric forms thereof, wherein n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof. The present invention further relates to the use of such phenyl pyrrole aminoguanidine derivatives for the treatment of diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones. 

Phenyl pyrrole aminoguanidine derivatives

The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system:  

N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands

The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH)where n is 0, 1 or 2; 

The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH), where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; Rand Rcan be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereof 

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Uppsala, Sweden

Arne Boman