DERIVATIVES OF PYRIDAZINONE AND TRIAZINONE AND THEIR USING AS PHARMACEUTICAL PREPARATIONS Russian patent published in 2006 - IPC C07D401/04 C07D401/14 C07D405/14 C07D403/04 C07D409/04 C07D417/04 C07D491/52 C07D401/06 C07D237/14 C07D237/04 C07D491/48 C07D253/06 A61K31/01 A61K31/50 A61K31/5025 A61K31/506 A61K31/53 A61P25/08 A61P25/28 A61P43/00 

FIELD: organic chemistry, medicine, neurology, pharmacy.

SUBSTANCE: invention relates to derivatives of pyridazinone or triazinone represented by the following formula, their salts or their hydrates: wherein each among A¹, A² and A³ represents independently of one another phenyl group that can be optionally substituted with one or some groups chosen from the group including (1) hydroxy-group, (2) halogen atom, (3) nitrile group, (4) nitro-group, (5) (C₁-C₆)-alkyl group that can be substituted with at least one hydroxy-group, (6) (C₁-C₆)-alkoxy-group that can be substituted with at least one group chosen from the group including di-(C₁-C₆-alkyl)-alkylamino-group, hydroxy-group and pyridyl group, (7) (C₁-C₆)-alkylthio-group, (8) amino-group, (9) (C₁-C₆)-alkylsulfonyl group, (10) formyl group, (11) phenyl group, (12) trifluoromethylsulfonyloxy-group; pyridyl group that can be substituted with nitrile group or halogen atom or it can be N-oxidized; pyrimidyl group; pyrazinyl group; thienyl group; thiazolyl group; naphthyl group; benzodioxolyl group; Q represents oxygen atom (O); Z represents carbon atom (C) or nitrogen atom (N); each among X¹, X² and X³ represents independently of one another a simple bond or (C₁-C₆)-alkylene group optionally substituted with hydroxyl group; R¹ represents hydrogen atom or (C₁-C₆)-alkyl group; R² represents hydrogen atom; or R¹ and R² can be bound so that the group CR²-ZR¹ forms a double carbon-carbon bond represented as C=C (under condition that when Z represents nitrogen atom (N) then R¹ represents the unshared electron pair); R³ represents hydrogen atom or can be bound with any atom in A¹ or A³ to form 5-6-membered heterocyclic ring comprising oxygen atom that is optionally substituted with hydroxyl group (under condition that (1) when Z represents nitrogen atom (N) then each among X¹, X² and X³ represents a simple bond; and each among A¹, A² and A³ represents phenyl group, (2) when Z represents nitrogen atom (N) then each among X¹, X² and X³ represents a simple bond; A¹ represents o,p-dimethylphenyl group; A² represents o-methylphenyl group, and A³ represents phenyl group, or (3) when Z represents nitrogen atom (N) then each among X¹, X² and X₃ represents a simple bond; A¹ represents o-methylphenyl group; A² represents p-methoxyphenyl group, and A³ represents phenyl group, and at least one among R² and R means the group distinct from hydrogen atom) with exception of some compounds determined in definite cases (1), (3)-(8), (10)-(16) and (19) given in claim 1 of the invention. Compounds of the formula (I) elicit inhibitory activity with respect to AMPA receptors and/or kainate receptors. Also, invention relates to a pharmaceutical composition used in treatment or prophylaxis of disease, such as epilepsy or demyelinization disease, such as cerebrospinal sclerosis wherein AMPA receptors take part, a method for treatment or prophylaxis of abovementioned diseases and using compound of the formula (I) for preparing a medicinal agent used in treatment or prophylaxis of abovementioned diseases.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

32 cl, 10 tbl, 129 ex