发明名称 SUBSTITUTED 3,5-DIAMINO-4-SULFONYL-PYRAZOLES AND 2-AMINO-3-SULFONYL-PYRAZOLO-[1,5-a]PYRIMIDINES-ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THEIR PRODUCTION AND USE
摘要 FIELD: medicine. ^ SUBSTANCE: invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R2Çè1,R2Çè2, R3Çè1, R3Çè2 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R3Çè1 and R3Çè2 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R2Çè1 and R2Çè2 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl. ^ EFFECT: compounds of invention may find application for treatment and prevention of development of conditions and disorders of central nervous system. ^ 13 cl, 11 dwg, 4 tbl, 11 ex
申请公布号 RU2376291(C1) 申请公布日期 2009.12.20
申请号 RU20080117846 申请日期 2008.05.07
申请人 IVASHCHENKO ANDREJ ALEKSANDROVICH;ALLA KHEM, LLS 发明人 IVASHCHENKO ALEKSANDR VASIL'EVICH;SAVCHUK NIKOLAJ FILIPPOVICH;IVASHCHENKO ANDREJ ALEKSANDROVICH
分类号 A61K31/415;A61K31/4155;A61K31/519;A61P25/22;A61P25/24;A61P25/28;C07D231/44;C07D487/04 主分类号 A61K31/415
代理机构 代理人
主权项
地址