DERIVATIVES OF PYRAZOLE AS MEDICINAL AGENTS FOR TREATMENT OF DISEASES THAT OCCUR AS RESULT OF DISFUNCTION OF NICOTINE RECEPTORS ALFA7 Russian patent published in 2009 - IPC C07D231/12 C07D231/20 C07D231/14 C07D401/04 C07D401/06 C07D403/04 C07D403/06 C07D409/04 C07D453/02 C07D453/06 A61K31/4155 A61K31/416 A61K31/4523 A61K31/454 A61K31/55 A61P25/28 A61P25/18 A61P25/30 

Abstract RU 2376290 C2

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of common formula (I) , in which: A, if available, means (C1-C6)-alkyl; R1 means group NR6R7, (C4-C7)-azacycloalkyl, (C5-C9)-azabicycloalkyl, besides, these groups, unnecessarily, are substituted with one or more substituents, selected from (C1-C5)-alkyl or halogen; A-R1 is such that nitrogen of radical R1 and nitrogen in position 1 of pyrazole are necessarily separated at least by two atoms of carbon; R3 means radical H, OH, NH2, ORc, NHC(O)Ra or NHSO2Ra; R4 means phenyl or heteroaryl, unnecessarily, substituted with one or more substituents, selected from halogen, CN, NH2, OH, ORc, C(O)NH2, phenyl, polyfluoroalkyl, linear or ramified (C1-C6)-alkyl, besides these substituents, unnecessarily, are substituted with halogen, and moreover, heteroaryl radicals are 3-10-member, containing one or more heteroatoms, selected from sulphur or nitrogen; R5 means radical H, linear or ramified (C1-C6)-alkyl; Ra means linear or ramified (C1-C6)-alkyl; Rc means linear or ramified (C1-C6)-alkyl, (poly)fluoroalkyl or phenyl; R6 and R7, independently from each other, means hydrogen, (C1-C6)-alkyl; R6 and R7 may create 5-, 6- or 7-member saturated or non-saturated cycle, which includes one heteroatom, such as N, and which, unnecessarily, substituted with one or more atoms of halogen; to its racemates, enantiomers, diastereoisomers and their mixtures, to their tautomers and their pharmaceutically acceptable salts, excluding 3-(3-pyridinyl)-1H-pyrazole-1- butanamine, 4-(3-pyridinyl)-1H-pyrazole-1-butanamine and N-(diethyl)-4-phenyl-1H-pyrazole-1-ethylamine. Invention is also related to methods for production of compounds of formula (I) and to pharmaceutical composition intended for treatment of diseases that appear as a result of disfunction of nicotine receptors α7 or favorably responding to their modulation, on the basis of these compounds.

EFFECT: production of new compounds and pharmaceutically acceptable composition on their basis, which may find application in medicine for treatment, prophylaxis, diagnostics and observance over development of psychiatric or neurological disorders or diseases of central nervous system, when cognitive functions deteriorate or quality of sensor information processing drops.

16 cl, 106 ex

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RU 2 376 290 C2

Authors

Zhenevua-Borella Ariel'

Malleron Zhan-Ljuk

Bukerel' Zhan

Derflinzhe Zhill'

Bome Andrees

Tuje Gaehtan

Sabjuko Zhan-Fransua

Terr'E Korin

Min'Jani Serzh

Ehver Mishel'

Ehl'-Amad Jussef

Dates

2009-12-20Published

2004-11-22Filed