摘要 |
The invention relates to serotonin 5-HT 6 receptor 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-HT 6 receptors 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 represents optionally substituted aryl or optionally substituted heteroaryl; R 1 represents hydrogen, optionally substituted C 1 -C 3 alkyl, C 1 -C 4 alkyloxycarbonyl; R 2 represents hydrogen, halogen or optionally substituted C 1 -C 3 alkyl ; R 1 3 and R 2 3 represent optionally alike: hydrogen, optionally substituted C 1 -C 3 alkyl or R 1 3 and R 2 3 together with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle. |
申请人 |
IVASHCHENKO, ANDREY ALEXANDROVICH;ALLA CHEM, LLC. |
发明人 |
KYSIL, VOLODYMYR MIKHAILOVICH;SAVCHUK, NIKOLAY FILIPPOVICH;IVASHCHENKO, ALEXANDER VASILIEVICH |