Use of sulfonamide derivatives as ligands for 5-HT6, in treatment of e.g. food ingestion disorder, obesity, bulimia, anorexia, cachexia and type II diabetes

摘要

In the manufacture of medicament for the prophylaxis and/or treatment of food ingestion disorder, at least one sulfonamide derivative (I) is used. In the manufacture of medicament for the prophylaxis and/or treatment of food ingestion disorder, at least one sulfonamide derivative of formula (I), optionally its salts, solvate, stereoisomer (preferably enantiomer or diastereomer), racemate or mixture of at least two of its stereoisomers in any mixing ratio is used. [Image] R 1>linear or branched alkyl, phenyl, benzyl (all optionally substituted) or H; R 2>NR 4>R 5> or optionally saturated, optionally substituted, cycloaliphatic radical (optionally containing at least one heteroatom as ring member and optionally condensed with optionally saturated, optionally substituted mono- or bicyclic cycloaliphatic ring system (optionally containing at least one heteroatom as ring member)); R 3>-R 5>H or optionally substituted linear or branched alkyl; or NR 4>R 5>optionally substituted, optionally saturated heterocyclic ring optionally containing at least one heteroatom as a ring member and/or optionally condensed with optionally saturated, optionally substituted mono- or bicyclic cycloaliphatic ring system optionally containing at least one heteroatom as ring member; A : optionally substituted mono- or polycyclic aromatic ring system optionally bonded via alkylene, alkenylene or alkynylene (all optionally substituted) and/or optionally containing at least one heteroatom as ring member in at least one of its ring; and n : 0-4. ACTIVITY : Anorectic; Eating-Disorders-Gen.; Anabolic; Immunomodulator; Antidiabetic. MECHANISM OF ACTION : 5-Hydroxytryptamine-6 (5-HT 6) receptor binder. N-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-5-chloro-3-methyl-benzo[b]thiophene-2-sulfonamide was tested for its 5-HT 6 receptor binding affinity using method as described in B.L. Roth, S. C. Craigo, M. S. Choudhary, S. Uluer, F. J. Monsma, Y. Shen, H. Y. Meltzer, D. R. Sibley: Binding of Typical and atypical Antipsychotic Agents to 5-hydroxytryptamine-6 and Hydroxytryptamine-7 Receptors. The Journal of Pharmacology and Experimental Therapeutics, 1994, 268, 1403 and showed K i of 0.13 nm and % inhibition of 103/17.9 10 -> 6>M.