abstract |
A compound of formula (II) for use in the treatment of a melanocortin receptor-mediated disorder, and in particular a melanocortin-3 receptor, a melanocortin-4 receptor or a melanocortin-5 receptor, such as a metabolic disorder, CNS disorder or dermatological disorder, for example obesity, mismatched oral tolerance glucose, elevated blood glucose content, type II diabetes, syndrome X, diabetic retinopathy, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathy, erectile dysfunction in men, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis excess of cerumen, disorders of the Meibomius gland, pseudofolliculitis, yeast infections, dandruff, hydradenitis suppurative, redness of the eye or glandular disorder with external secretion, and in particular obesity, mismatched oral glucose tolerance, high blood glucose type II diabetics, diabetes syndrome, , dry skin or seborrhea ni dermatitisgdeR1 is heteroaryl, heteroaryl-alkyl, heterocycloalkyl, heterocycloalkyl-alkyl, cycloalkyl, cycloalkyl-alkyl, substituted aryl or substituted aralkyl, wherein heteroaryl, heteroaryl-alkylcycloalkylalkylalkylalkylalkylalkyl with one or more substituents halogen, hydroxy, alkyl, alkoxy, halogenated alkyl, halogenated alkoxy, amino, alkylamino or di (alkyl) amino, wherein the aryl or aralkyl group is independently substituted with one or more halogen, hydroxy, alkyl, alkoxy substituents, halogenated alkyl, halogenated alkoxy, amino, alkylamino or di (alkyl) amino; or R < 2 > is heteroaryl, heteroaryl-alkyl, heterocycloalkyl, heterocycloalkyl-alkyl, cycloalkyl, cycloalkyl-alkyl, substituted aryl or substituted aralkyl, wherein heteroaryl, heteroaryl-alkyl, heterocycloalkyl, cycloalkylalkyl or cycloalkylalkylalkylalkylalkyl; one or more substituents halogen, hydroxy, alkyl, alkoxy, halogenated alkyl, halogenated alkoxy, amino, alkylamino or di (alkyl) amino; wherein the aryl or aralkyl group is independently substituted by one or more halogen, hydroxy, alkyl, alkoxy, halogenated alkyl , halogenated alkoxy, amino, alkylamino or di (alkyl) amino; and R4 is aryl, aralkyl, heteroaryl, heterocycloalkyl or cycloalkyl-alkyl; wherein aryl, aralkyl, heteroaryl, heterocycloalkyl or cycloalkyl-alkyl groups are optionally independently substituted with one or more substituents halogen, hydroxy, alkyl, alkoxy, halogenated alkyl, alkoxy, halogenated alkyl; amino, alkylamino or di (alkyl) amino; or R2 is aryl, aralkyl, heteroaryl, heteroaryl-alkyl, heterocycloalkyl, heterocycloalkyl-alkyl, cycloalkyl or cycloalkyl |