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; R² ₁,R² ₂, R³ ₁, R³ ₂ independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C₁-C₄ alkyl, unnecessarily substituted phenyl, or R³ ₁ and R³ ₂ 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 R² ₁ and R² ₂ 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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