Method of treating inflammation
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; R 1 , R 2 , R 3 , R 4 and R 5 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. A method of treating inflammation, comprising administering an effective amount of a compound of general Formula (I)
wherein X is H; R1, R2, R3, R4 and R5 are the same or different and are selected from the group consisting of hydrogen, halogen, methyl, methoxy, hydroxy, nitro and sulpho;
and wherein one or more of R1, R2, R3, R4 and R5 are methoxy or hydroxy;
or a pharmacologically active salt thereof;
to a patient in need thereof.
2. The method of according to claim 1 , wherein one or more of R1, R2, R3, R4 and R5 are methyl.
3. The method according to claim 1 , wherein one or more of R1, R2, R3, R4 and R5 are halogen atoms.
4. The method according to claim 3 , wherein the halogen is fluoro or chloro.
5. The method according to claim 1 , wherein the compound is selected from the group consisting of:
1 N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine acetate,
2 N-(3,4,5-Trimethoxybenzylideneamino)guanidine acetate
3 N-(3,4-Dimethoxy-2-chlorobenzylideneamino)guanidine
4 N-(2,4,6-Trimethoxybenzylideneamino)guanidine acetate
5 N-(2-Hydroxy-4,6-dimethoxybenzylideneamino)guanidine acetate
6 N-(3-Methoxy-2,6-dinitrobenzylideneamino)guanidine hydrochloride
7 N-(2,3-Dimethoxy-5,6-dinitrobenzylideneamino)guanidine acetate
8 N-(5-Bromo-2,4-dimethoxybenzylideneamino)guanidine acetate 0.5 hydrate
9 N-(2,3-Dimethoxy-5-nitrobenzylideneamino)guanidine acetate
10 N-(2,3-Dimethoxy-5-nitrobenzylideneamino)guanidine hydrochloride
11 N-(2-Hydroxy-4-methoxybenzylideneamino)guanidine acetate
12 N-(3-Bromo-4-methoxybenzylideneamino)guanidine hydrochloride
13 N-(4-Methoxy-3-nitrobenzylideneamino)guanidine acetate
14 N-(2-Hydroxy-3-methoxy-5-nitrobenzylideneamino)guanidine hydrochloride
15 N-(2-Hydroxy-4-methoxy-5-nitrobenzylideneamino)guanidine hemiacetate
16 N-(3-Chloro-4-methoxy-5-nitrobenzylideneamino)guanidine
17 N-(3,5-Dichloro-4-methoxybenzylideneamino)guanidine acetate
18 N-(3-Bromo-4-methoxy-5-methylbenzylideneamino)guanidine acetate
19 N-(2,3,4-Trimethoxybenzylideneamino)guanidine hydrochloride
20 N-(4-Chloro-2-methoxy-5-nitrobenzylideneamino)guanidine acetate
21 N-(2-Hydroxy-4-methyl-5-nitrobenzylideneamino)guanidine hydrochloride
22 N-(3-Hydroxy-4-methyl-2-nitrobenzylideneamino)guanidine acetate
23 N-(5-Bromo-2-hydroxy-3-nitrobenzylideneamino)guanidine hydrochloride
24 N-(5-Bromo-2-methoxy-3-nitrobenzylideneamino)guanidine hydrochloride, and
25 N-(2,4-Dimethoxy-5-nitrobenzylideneamino)guanidine acetate,
or a pharmacologically acceptable salt thereof.
6. The method according to claim 1 , wherein the compound of Formula I is present in a pharmaceutical composition together with one or more adjuvants, carriers or excipients.
7. The method according to claim 1 , wherein a label, is additionally present.
8. The method according to claim 7 , wherein the label is a radioactive label.
9. The method according to claim 7 , wherein the label is a toxic agent.