Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof

A method of serotonin 5-HT6 receptors antagonizing comprising administering into the cell the compounds of the general formula 1 and 2 or pharmaceutically acceptable salts thereof

• wherein:
• Ar is optionally substituted aryl or optionally substituted heterocyclyl;
• R1 is hydrogen, optionally substituted lower C1-C3 alkyl, substituted hydroxyl group, substituted sulfanyl group;
• R2 is hydrogen or optionally substituted C1-C3 alkyl;
• R3 is hydrogen, optionally substituted C1-C3 alkyl or tert.-butyloxycarbonyl.

A method of treating a disease, pathogenesis of which is associated with 5-HT6 receptors, comprising administering to a subject a pharmaceutically effective amount of a compound of general formula 1 or 2, or a pharmaceutically acceptable salt thereof,

• wherein:
• Ar is an optionally substituted aryl or an optionally substituted heterocyclyl;
• R1 is hydrogen, an optionally substituted lower C1-C3alkyl, a substituted hydroxy group, a substituted sulfanyl group;
• R2 is hydrogen or an optionally substituted C1-C3alkyl;
• R3 is hydrogen, an optionally substituted C1-C3alkyl or tert.-butyloxycarbonyl.

A therapeutic cocktail treating a disease, pathogenesis of which is associated with 5-HT6 receptors, comprising a pharmaceutically effective amount of a medicament including the compounds of the general formulas 1 or 2, or pharmaceutically acceptable salt thereof and pharmaceutically acceptable carriers, including inert excipients and/or solvents placed in a pharmaceutically acceptable packing,

• wherein:
• Ar is an optionally substituted aryl or optionally substituted heterocyclyl;
• R1 is hydrogen, an optionally substituted lower C1-C3alkyl, a substituted hydroxyl group, a substituted sulfanyl group;
• R2 is hydrogen or an optionally substituted C1-C3alkyl;
• R3 is hydrogen, an optionally substituted C1-C3alkyl or tert.-butyloxycarbonyl.