US 2004/0024060 A1 · Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands

Abstract

The present invention relates to the 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 is H or OH; R1, R2, R3, R4 and R5 are 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 the pharmacologically active salts thereof. 1

Claims28

Dependent claims

The use of a compound of general formula (I)

4
wherein R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, and methyl;
from electron donor groups such as methoxy or hydroxy;
and from electron acceptor groups selected from nitro or sulpho;
or a pharmacologically active salt thereof;
as a melanocortin receptor ligand and/or in the preparation of a medicament for treatment of disorders related to the melanocortin system.

3 more elements

Use of a compound selected from:

N-(2-Hydroxy-4,6-dimethoxybenzylideneamino)guanidine acetate
N-(3-Bromo-4-fluorobenzylideneamino)guanidine acetate
N-(2,3-Difluorobenzylideneamino)guanidine acetate
N-(4-Chloro-3-fluorobenzylideneamino)guanidine acetate
N-(3-Methoxy-2,6-dinitrobenzylideneamino)guanidine hydrochloride
N-(3-Bromo-2,6-dinitrobenzylideneamino)guanidine hydrochloride
N-(2,3-Dimethoxy-5,6-dinitrobenzylideneamino)guanidine acetate
N-(5-Bromo-2,4-dimethoxybenzylideneamino)guanidine acetate 0.5 hydrate
N-(2,3-Dimethoxy-5-nitrobenzylideneamino)guanidine acetate
N-(3,4-Difluorobenzylideneamino)guanidine acetate
N-(2-Fluoro-5-nitrobenzylideneamino)guanidine acetate
N-(4-Bromo-2-fluorobenzylideneamino)guanidine acetate
N-(3,5-Dinitrobenzylideneamino)guanidine acetate dihydrate
N-(3-Chloro-4-fluorobenzylideneamino)guanidine acetate
N-(2-Bromo-4-nitroobenzylideneamino)guanidine acetate
N-(2-Bromo-5-nitroobenzylideneamino)guanidine acetate
N-(2-Iodobenzylideneamino)guanidine acetate
N-(2,3-Dimethoxy-5-nitrobenzylideneamino)guanidine hydrochloride
N-(2-Hydroxy-4-methoxybenzylideneamino)guanidine acetate
N-(4-Bromo-3-nitrobenzylideneamino)guanidine acetate
N-(6-Chloro-2,3-dinitrobenzylideneamino)guanidine hydrochloride
N-(3-Iodobenzylideneamino)guanidine hydrochloride
N-(2-Sulphobenzylideneamino)guanidine hydrochloride
N-(4-Fluoro-3-nitrobenzylideneamino)guanidine acetate
N-(4-Methoxy-3-nitrobenzylideneamino)guanidine acetate
N-(3,5-Dichloro-2-nitrobenzylideneamino)guanidine acetate
N-(2-Hydroxy-3-methoxy-5-nitrobenzylideneamino)guanidine hydrochloride
N-(2-Hydroxy-4-methoxy-5-nitrobenzylideneamino)guanidine hemiacetate
N-(3-Chloro-4-methoxy-5-nitrobenzylideneamino)guanidine
N-(3,5-Dichloro-4-methoxybenzylideneamino)guanidine acetate
N-(3-Bromo-4-methoxy-5-methylbenzylideneamino)guanidine acetate
N-(2,3,4-Trimethoxybenzylideneamino)guanidine hydrochloride
N-(4-Chloro-2-methoxy-5-nitrobenzylideneamino)guanidine acetate
N-(3,6Dichloro-2-nitrobenzylideneamino)guanidine acetate
N-(2-Hydroxy-4-methyl-5-nitrobenzylideneamino)guanidine hydrochloride
N-(3-Hydroxy-4-methyl-2-nitrobenzylideneamino)guanidine acetate
N-(5-Bromo-2-hydroxy-3-nitrobenzylideneamino)guanidine hydrochloride
N-(5-Bromo-2-methoxy-3-nitrobenzylideneamino)guanide hydrochloride
N-(2,4-Dimethoxy-5-nitrobenzylideneamino)guanidine acetate
N-(4-Bromo-2-fluoro-5-nitrobenzylideneamino)guanidine acetate
or a pharmacologically acceptable salt thereof, as a melanocortin receptor ligand and/or in the preparation of a medicament for treatment of disorders related to the melanocortin system.

38 more elements

Dependencies are inferred from the claim text.

Facts

Application

10/343,325Filed 23 Jun 2003

Priority

GB 0019357.37 Aug 2002

Published

5 Feb 2004

Term ends

Not estimatedThe source records don’t support an estimate.

Classification82 codes

C07C 281/16
Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these…:…
A61K 31/155
Amines: amidines , e.g. guanidine , isourea , isothiourea
A61P 1/04
Drugs for disorders of the alimentary tract or the digestive system: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of…
A61P 1/14
Drugs for disorders of the alimentary tract or the digestive system: prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics,…

Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands

Life of this patent

Use of benzylideneaminoguanidines and hydroxyguanidines as melanocortin receptor ligands

Life of this patent

Abstract

Claims28