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Madina Georgievna Kadieva

Oleg Dmitrievich Mitkin

Alexandre Vasilievich Ivachtchenko

Andrey Alexandrovich Ivashchenko

Nikolay Filippovich Savchuk

Alexander Vasilievich Ivashchenko

Yan Lavrovsky

The present invention relates to novel substituted methyl-amines, serotonin 5-HTreceptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and 'molecular tools', in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.

Substituted methyl amines, serotonin 5-HT6 receptor antagonists, methods for production and use thereof

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.

Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof

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Podosinki, Russia

Madina Georgievna Kadieva