SUBSTITUTED ARYLAMINES AND THEIR APPLICATION AS 5-HT-RECEPTOR MODULATORS Russian patent published in 2012 - IPC C07D295/12 A61K31/495 A61K31/496 A61P3/06 A61P9/12 A61P9/00 A61P25/28 A61P25/18 C07D311/68 

FIELD: medicine, pharmaceutics.

SUBSTANCE: given invention refers to arylamines of formula (I) and their pharmaceutically acceptable salts which are active in relation to 5HT receptors, particularly show 5-HT₆ modulating activity, and can be used for treating a number of diseases, such as obesity, or the other diseases, for treating 5-HT-associated condition selected from a group containing Alzheimer's disease, Hundington's disease, obesity, obesity-related disorder, insulin-independent diabetes, Alzheimer's disease related cognitive disorders, schizophrenia related cognitive disorders, reflux gastroesophagitis, non-ulcer dyspepsia, depression, anxiety, migraine, gastritis, gastric emptying disorder, eating disorders, gastrointestinal disorders, constipations, panic attacks, memory impairment, disturbed sleep, alcohol-use disorders, anorexia, bulimia, obsessive-compulsive disorders, psychosis, Parkinson's disease, Hundington's chorea, and/or schizophrenia, drug abuse and attention deficit/hyperactivity disorder (ADHD). In the compound of formula (I) n means 1; A means C₁-C₃alkylene; R₁ means hydrogen or C₁-C₁₀alkyl; R₂ means C₁-C₁₀alkoxy, C(O)CF₃ or SO₂R₆, where R₆ can be C₁-C₄ alkyl R₃ and R₄ independently means hydrogen, substituted or unsubstituted C₁-C₇alkyl, where a substituted is selected from dihydrobenzodioxidine or benzodioxole, probably substituted by halogen; phenyl, probably substituted by C₁-C₄alkyl, C₁-C₄alkoxy, halogen, trifluoromethyl; aryl selected form naphthyl or tetrahydronaphthyl, optionally substituted by C₁-C₄alkyl, C₁-C₄alkoxy; heteroaryl, 5-members heteroaryl condensed with the benzoic ring with sulphur atom as a heteroatom, chromanyl probably substituted by halogen; B means a bound; and X and Y means -CH-.

EFFECT: preparing pharmaceutically acceptable salts which are active in relation to 5HT receptors.

59 cl, 9 dwg, 1 tbl, 57 ex