2-AMINO-3-SULPHONYLTETRAHYDROPYRAZOLO[1,5-a]PYRIDOPYRIMIDINE 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 2-amino-3-sulphonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-sulphonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, to medicinal principles and to pharmaceutical compositions containing said medicinal principles in the form of the above-mentioned compounds, to drug substances, as well as to the method for treating and preventing the development of different diseases of the central nervous system (CNS) of human beings and animals, whose pathogenesis is associated with 5-HTreceptors. The substituted 2-amino-3-sulphonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of general formula 1 and the substituted 2-amino-3-sulphonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of general formula 2 or pharmaceutically acceptable salts thereof are claimed:wherein Ar is phenyl optionally substituted with halogen atoms, hydroxyl optionally substituted with C-Calkyl, or 6-membered heteroaryl with 1 or 2 nitrogen atoms; Ris a hydrogen atom, C-Calkyl optionally substituted with phenyl, C-Calkoxycarbonyl; Ris a hydrogen atom, halogen or C-Calkyl; Rand Rare the optionally identical substituents selected from a hydrogen atom and C-Calkyl optionally substituted with phenyl, hydroxy group, or Rand Rtogether with a nitrogen atom, with which they are attached, form 6-membered saturated heterocyclyl with 1-2 heteroatoms selected from nitrogen an optionally substituted with C-Calkoxycarbonyl.