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 

Abstract RU 2440996 C2

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

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RU 2 440 996 C2

Authors

Beker Oren

Lobera Mersedes

Melendes Rosa Eh.

Sharadendu Anurag

Vu Lorens

Juj Sjan J.

Danoa Dehjl S.

Cheruku Srinivasa Rao

Marantts Jaehl

Nojman Sil'Via

Fichman Merav

Senderovitts Khanoch

Shacham Sharon

Sakha Ashis

Orbakh Pini

Dates

2012-01-27Published

2006-01-25Filed