摘要:
A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier. wherein symbols in the above formula represent the following meanings, respectively:
X: N, CH, R: an imidazolyl group or a di-lower alkylamino group, R 1 :
(1) a halogen atom, a nitro group, a cyano group, a carboxyl group, an amino group, a mono- or di-lower alkylamino group, a lower alkanoyl group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group or a carbamoyl group, (2) a lower alkyl group or lower alkoxyl group which may be substituted by a halogen atom, a carboxyl group or an aryl group, (3) a phenyloxy group which may be substituted by a lower alkoxycarbonyl group or a carboxyl group,
R 2 : a hydroxyl group, a lower alkoxyl group, an amino group or a mono- or di-lower alkylamino group, A: a lower alkylene group which may be substituted or a group represented by the formula -O-B-, and B: a lower alkylene group, with the proviso that the case wherein R represents an imidazolyl group, R 1 represents a cyano group, A represents an ethylene group and R 2 represents a hydroxyl group is excluded.
摘要:
Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R 1 , R 2 , R 3 , R 4 and R 5 are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R 2 and R 3 together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.
摘要:
This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives. The novel aminomethyl-substituted thiazolobenzimidazole derivatives which have a metabotropic glutamate receptor action and excellent oral activity are invented and these derivatives are therefore useful as a medicament.
摘要:
Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R , R , R , R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R and R together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.
摘要:
Imidazole-substituted quinoxalinedione derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions useful as glutamate receptor antagonists and the like, which comprise said compounds or salts thereof and pharmaceutically acceptable carriers. (Each symbol in the formula has the following meaning:
A: a group represented by a formula (CH 2 ) m or a group represented by a formula Ph-(CH 2 ) p (Ph: a phenyl group), X: an oxygen atom or a group represented by a formula NR 4 , R 1 : a hydrogen atom, a hydroxyl group or a triazolyl group, with the proviso that X may be a bond when R 1 is a triazolyl group, R 2 : a hydrogen atom, a nitro group, a halogeno-lower alkyl group, a cyano group, an amino group, a mono- or di-lower alkylamino group or a halogen atom, R 3 and R 4 : may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group, n: 0, 1 or 2, m: an integer of 2 to 6, and p: an integer of 1 to 6.)
摘要:
Novel thiazolo[3,2-a]benzimidazol derivatives represented by general formula (1), which act specifically on metabotropic glutamate receptors and are useful as drugs; and novel compounds useful as intermediates for the synthesis of the derivatives wherein, R 1 is optionally substituted carbamoyl, carbonyl, oxy, amino, carbonylamino, or the like; R 2 is hydrogen, lower alkyl, or the like; and R 3 , R 4 and R 5 are each independently hydrogen, lower alkyl, or the like.