TETRAHYDROPYRAZOLO[1,5-a]PYRIDOPYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HTRECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF

摘要

The invention relates to the antagonists of serotonin 5-HTreceptors in the form of novel substituted 3-sulphonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulphonyl-5,6,7,8-tetrahydropyrazolo[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-HTreceptors. In formulas 1 and 2Ar is phenyl or phenyl optionally substituted with halogen atoms, C-Calkyl, hydroxy, optionally substituted C-Calkyl, or 6-membered heteroaryl containing a nitrogen atom in a cycle; Ris a hydrogen atom, C-Calkyl, hydroxy C-Calkoxy group, C-Calkylsulphonyl group; Ris a hydrogen atom or C-Calkyl; Ris a hydrogen atom, optionally substituted with phenyl C-Calkyl or tert-butyloxycarbonyl.