Melanocortin 1 receptor selective compounds

US7008925B1 · kind B1 · utility

Assignee

• Action Pharma A/S · DK

Inventors

• Michael Szardenings · Leipzig, DE
• Ruta Muceniece · Uppsala, SE
• Ilze Mutule · Uppsala, SE
• Felikss Mutulis · Uppsala, SE
• Jarl Wikberg · Åkersberga, SE

Key dates

• Filing date: May 5, 1999
• Grant date: Mar 7, 2006
• Expiry date: May 5, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound of general formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are H or methyl, R13, R14, R15 and R16 are H or alkyl, wherein L1 and L2 are linkers selected from single bond, methyl, ethyl, wherein R19, R20 and R21 are H or —CH2X, NT is selected from H, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group, CT is selected from hydrogen, hydroxyl, alkyl, aminoacid, aminoacid analogue, polypeptide and functional group shows high selectivity and high affinity for MC1-receptors in combination with effective stimulation or inhibiton of cAMP formation in MC1-receptor expressing cells but low affinity for other subtypes of MC-receptors and may be used to treat a wide range of inflammatory conditions. Also disclosed is a DNA molecule and a corresponding vector encoding the compound, a fusion protein comprising a copy of it, a vector comprising DNA encoding the fusion protein, and a pharmaceutical composition comprising the compound.