Substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines, serotonin 5-ht6 receptor antagonists and methods for the production and use thereof

Abstract

The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HTreceptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HTreceptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity. In the general formula 1: wherein: X=S, SO or NH; Rrepresents hydrogen, optionally substituted C-Calkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; Rrepresents hydrogen, halogen, optionally substituted C-Calkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; Rrepresents hydrogen, optionally substituted C-Calkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X=S or X=NH, at least one of R, Ror Rrepresent substituted C-Calkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R, Ror Rrepresent hydrogen; Rrepresents C-Calkyl; Rrepresents hydrogen, one or two halogens, C-Calkyl or optionally substituted hydroxyl.