TETRAHYDRO-PYRAZOLO[1,5-a]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF

摘要

The invention relates to the antagonists of serotonin 5-HT6 receptors in the form of novel substituted 3-sulphonyl-6,7,8,9-tetrahydro-pyrazolo[l,5-a]pyrido [4,3-d]-pyrimidines and to 3-sulphonyl-6,7,8,9-tetrahydro-pyra-zolo[1,5-a]pyrido [4,3-d]-pyrimidines to a medicinal principle and to pharmaceutical compositions containing said medicinal principle in the form of the above-mentioned compounds, as well as to a method for treating and preventing the development of different conditions and diseases of the central nervous system of human beings and endotherms, whose pathogenesis is associated with 5-HT6 receptors. In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; R1 is a hydrogen atom, optionally substituted lower C-Calkyl, a substituted hydroxy group or a substituted sulphonyl group; R2 is a hydrogen atom or optionally substituted C-Calkyl; R3 is a hydrogen atom, optionally substituted C-Calkyl or tert-butyloxycarbonyl.12