6 receptors, methods for their production and use. RU patent 2376291.
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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. RU patent 2376291.

Substituted 3,5-diamino-4-sulfonyl-pyrazoles and 2-amino-3-sulfonyl-pyrazolo-[1,5-a]pyrimidines-antagonists of serotonin 5-ht<sub>6</sub> receptors, methods for their production and use. RU patent 2376291.

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; R21,R22, R31, R32 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R31 and R32 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 R21 and R22 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

 


 

IPC classes for russian patent 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. RU patent 2376291. (RU 2376291):

C07D487/04 - Ortho-condensed systems
C07D231/44 - Oxygen and nitrogen or sulfur and nitrogen atoms
A61P25/28 - for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P25/24 - Antidepressants
A61P25/22 - Anxiolytics
A61K31/519 -
A61K31/4155 -
A61K31/415 -
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