Novel benzylideneamino guanidines and their uses as ligands to the melnocortin receptors
OwnerTorbjorn Lundstedt, Per Andersson +3inventors
InventorsTorbjorn Lundstedt, Per Andersson, Arne Boman, Elisabeth Seifert, Anna Skottner
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Abstract
The present invention relates to novel benzylideneamino guanidines of general formula and to the use of these benzylideneamino guanidines as melanocortin receptor agonists or antagonists. The invention further relates to benzylideneamino guanidines which show selectivity to the MC1 and MC4 melanocortin receptors as agonists and/or antagonists. 1
Claims18
A compound of general formula (I):
- 4
- wherein R2 is selected from a halogen, hydroxy, methyl, methoxy or nitro group;
- wherein R3 is selected from a hydrogen, hydroxy, fluoro, chloro or trifluoromethyl group;
- wherein R4 is selected from a hydrogen, nitro, iodo or bromo group;
- wherein R5 is selected from a hydrogen, fluoro or ethoxy group;
- wherein R6 is selected from a hydrogen, nitro, bromo or methoxy group;
- and provided that
- at least one of R3, R4, R5, R6 is not a hydrogen;
- and when R4, R5, and R6 are hydrogen, then R2 is selected from fluoro, bromo, iodo, hydroxy, methyl, methoxy or nitro group,
- and when R4 is nitro, then R2 is selected from a halogen, methyl or methoxy group,
- and when R3 is a fluoro, then R2 is selected from a halogen, methyl, methoxy or nitro group,
- or a pharmacologically active salt thereof.
A compound according to any of the previous claims wherein R5 is hydrogen.
A compound according to any of the previous claims wherein R2 is bromo or iodo.
A compound according to any of the previous claims wherein R3 is chloro.
A novel compound being any one of the following:
- 6 Name N-(3-Chloro-2-Iodobenzylideneamino)guanidine N-(3-Fluro-2-Methyl-6-Nitrobenzylideneamino)guanidine N-(2-Chloro-3-Hydroxy-4-Nitrobenzylideneamino)guanidine N-(2,3-Dichloro-4-Nitrobenzylideneamino)guanidine N-(5-Ethoxy-2-Nitro-3-Trifluoromethylbenzylideneamino)guanidine N-(2,6-Dibromobenzylideneamino)guanidine N-(2-Bromo-4-Iodobenzylideneamino)guanidine N-(2,5-Difluorobenzylideneamino)guanidine N-(2,6-Dimethoxybenzylideneamino)guanidine N-(2,3-Dihydroxybenzylideneamino)guanidine N-(4-Bromo-2-iodobenzylideneamino)guanidine
- or a pharmacologically active salt thereof.
A compound as claimed in any of the previous claims which additionally comprises a label or a toxic agent.
Dependencies are inferred from the claim text.