Patent RU-2279428-C2 (RU)
Inventor: NAGATO SATOSI
IPC: A61P43/00
Filed: 2001-09-17
Granted: 2006-07-10
Abstract: 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 A 1 , A 2  and A 3  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) (C 1 -C 6 )-alkyl group that can be substituted with at least one hydroxy-group, (6) (C 1 -C 6 )-alkoxy-group that can be substituted with at least one group chosen from the group including di-(C 1 -C 6 -alkyl)-alkylamino-group, hydroxy-group and pyridyl group, (7) (C 1 -C 6 )-alkylthio-group, (8) amino-group, (9) (C 1 -C 6 )-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 X 1 , X 2  and X 3  represents independently of one another a simple bond or (C 1 -C 6 )-alkylene group optionally substituted with hydroxyl group; R 1  represents hydrogen atom or (C 1 -C 6 )-alkyl group; R 2  represents hydrogen atom; or R 1  and R 2  can be bound so that the group CR 2 -ZR 1  forms a double carbon-carbon bond represented as C=C (under condition that when Z represents nitrogen atom (N) then R 1  represents the unshared electron pair); R 3  represents hydrogen atom or can be bound with any atom in A 1  or A 3  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 X 1 , X 2  and X 3  represents a simple bond; and each among A 1 , A 2  and A 3  represents phenyl group, (2) when Z represents nitrogen atom (N) then each among X 1 , X 2  and X 3  represents a simple bond; A 1  represents o,p-dimethylphenyl group; A 2  represents o-methylphenyl group, and A 3  represents phenyl group, or (3) when Z represents nitrogen atom (N) then each among X 1 , X 2  and X 3  represents a simple bond; A 1  represents o-methylphenyl group; A 2  represents p-methoxyphenyl group, and A 3  represents phenyl group, and at least one among R 2  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