2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidine antagonists of serotonin 5-ht6 receptors, methods for the production and use thereof

Abstract

The invention relates to serotonin 5-HTreceptor antagonists—novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HTreceptors including cognitive and neurodegenerative diseases. Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; Ris hydrogen, optionally substituted C-Calkyl, C-Calkyloxycarbonyl; Ris hydrogen, halogen or optionally substituted C-Calkyl; Rand Rrepresent optionally alike: hydrogen, optionally substituted C-Calkyl or Rand Rtogether with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.