Patent ID: 6197768
Filing Date: 2001-03-06
Classification: A61P,C07D

Abstract:
A method for preventing or treating ischemic heart disease, said method comprising;administering to a person in need thereof, an effective amount of a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof as active ingredient, and a pharmaceutically acceptable carrier thereof: ##STR229##where R.sup.1 represents a hydrogen atom, a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected carboxymethyl group, an alkoxycarbonyl group having 1-4 carbon atoms, a carbamoyl group, an acetylamino group, a 3-carboxy-1-propenyl group, a 2-hydroxypentyloxy group, a 2,2-diethyoxyethoxy group, an optionally protected hydroxyl group, an optionally protected mercapto group, a straight- or branched-chain alkanoyloxy group having 1-4 carbon atoms, a carbonyloxy group substituted by a phenyl group or a pyridyl group, a straight- or branched-chain alkyl group having 1-4 carbon atoms which may be substituted by one hydroxyl group, an amino group which may be mono- or disubstituted by an alkyl group having 1-4 carbon atoms, an alkylthio group having 1-3 carbon atoms which may be monosubstituted by any group selected from the group consisting of a hydroxyl group, a carboxyl group, a phenyl group and a pyridyl group, or represented by the following formula (XXI):--O--.sub.2).sub.n -Z (XXI)(where Z represents a hydrogen atom, a carboxyl group, an alkoxy group having 1 or 2 carbon atoms which may be substituted by one hydroxyl group, an alkoxycarbonyl group having 1-6 carbon atoms, a carbamoyl group which may be mono- or disubstituted by a hydroxymethyl group or an alkyl group having 1 or 2 carbon atoms, an alkanoyl group having 1-4 carbon atoms which may be substituted by one hydroxyl group or mercapto group, a piperidinylcarbonyl group which may be substituted by one carboxyl group or alkoxycarbonyl group having 1 or 2 carbon atoms, a morpholylcarbonyl group, a hydroxyl group, a mercapto group, an amino group, a phenyl group, a pyridyl group which may be monosubstituted by a hydroxymethyl group or an acetoxymethyl group or an alkyl group having 1-4 carbon atoms or an alkoxycarbonyl group having 1 or 2 carbon atoms, a pyrazinyl group, a pyrimidinyl group, a furyl group, a thienyl group, an oxadiazolyl group or a 4-methoxyphenoxy group; n is 1-6); R.sup.2 represents a hydrogen atom, a halogen atom, an optionally protected hydroxyl group, an optionally protected mercapto group, an optionally protected amino group, a cyano group, a nitro group, a trifluoromethyl group, a trifluoromethoxy group, an optionally substituted carboxylgroup, a 4-morpholylacetyl group, a straight- or branched-chain alkanoyloxy group having 1-4 carbon atoms, a straight- or branched-chain alkanoyl group having 1-4 carbon atoms, a straight- or branched-chain alkyl group having 1-4 carbon atoms, an alkylthio group having 1-3 carbon atoms which may be monosubstituted by any group selected from the group consisting of a hydroxyl group, a carboxyl group, a phenyl group and pyridyl group or a straight- or branched-chain alkoxy group having 1-4 carbon atoms which may be substituted by one alkoxycarbonyl group having 1-4 carbon atoms; R.sup.3 represents a hydrogen atom, a halogen atom, an optionally protected hydroxyl group or a straight- or branched-chain alkoxy group having 1-4 carbon atoms; R.sup.4 represents a hydrogen atom, a halogen atom, an optionally protected carboxyl group, a phenoxy group, an anilino group, a N-methylanilino group, a 4-morpholylcarbonyl group, an alkyl group having 1 or 2 carbon atoms which may be substituted by a cyclic alkyl group having 3-6 carbon atoms, a benzyl group which may be mono- or disubstituted in the phenyl portion by any group selected from the group consisting of a halogen atom, a hydroxyl group, a mercapto group, an alkoxy group having 1 or 2 carbon atoms, an alkylthio group having 1 or 2 carbon atoms, an alkoxycarbonyl group having 1-4 carbon atoms, an acetylamino group, a carboxyl group and an amino group, a pyridylmethyl group which may be substituted by an alkyl group having 1-4 carbon atoms, a morpholylmethyl group, a triazolylmethyl group, a furylmethyl group, a thienylmethyl group, a pyrimidinylmethyl group, a pyrazinylmethyl group, a pyrrolylmethyl group, an imidazolylmethyl group, a quinolylmethyl group, an indolylmethyl group, a naphthylmethyl group, a benzoyl group, an .alpha.-hydroxybenzyl group or an alkoxycarbonyl group having 1 or 2 carbon atoms; R.sup.5 represents a hydrogen atom or a methyl group with the proviso that; when R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are a hydrogen atom at the same time, R.sup.4 is not a hydrogen atom, a benzyl group, a 4-diethylaminobenzyl group or a furylmethyl group.