Patent ID: 6710056
Filing Date: 2004-03-23
Classification: A61P,C07C,C07D

Abstract:
Amidinophenylpyruvic acid compounds of the following formula (1) and pharmaceutically acceptable salts thereof: whereinW represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, X represents a hydrogen atom, a carboxyalkyl group having 2 to 5 carbon atoms, or a methyl or ethyl group having a substituent(s) selected from the group consisting of alkoxycarbonyl groups having 2 to 8 carbon atoms, carbamoyl group, tetrazolyl group, sulfo group, sulfamoyl group, phosphono group and hydroxyl group, a benzyl group which may have a substituent(s) selected from the group consisting of hydroxyl group, carboxyl group, tetrazolyl group, sulfo group, sulfamoyl group, phosphono group, halogeno groups and alkyl groups having 1 to 3 carbon atoms, or an alkyl group having 1 to 4 carbon atoms, phenyl group, guanidinopropyl group, mercaptomethyl group, imidazolylmethl group, aminobutyl group, aminopropyl group, (methylthio)ethyl group or indolylmethyl group, X and W may be bonded together to form a ring, and in this cas, â€”Wâ€”Xâ€” represents an ethylene group, trimethylene group or tetramethylene group, V represents any of the following groups (1) to (8): (1) a benzimidazolecarbonyl, quinolinecarbonyl, benzothiazolecarbonyl or benzoxazolecarbonyl group which may have a substituent(s) selected from the group consisting of an amino group(s), an alkyl group(s) having 1 to 6 carbon atoms, a halogeno group(s) and an alkoxyl group(s) having 1 to 6 carbon atoms, (2) a benzoyl group substituted with phenyl, pyridyl or thiophenyl group having a substituent(s) selected from the group consisting of amidino group, guanidino group, amino group, dialkylamino groups having 2 to 5 carbon atoms, carboxyl group and acyl groups having 1 to 6 carbon atoms, (3) a benzoyl group substituted with phenoxymethyl or benzoylamino group which may have a substituent(s) selected from the group consisting of amidino group, methoxyl group, guanidino group, amino group and dialkylamino groups having 2 to 5 carbon atoms, (4) a guanidinocarbonylbenzoyl group or (guanidinomethyl)benzoyl group, (5) a monoalkylguanidinobenzoyl group having 9 to 11 carbon atoms wherein the alkyl group bonded to the guanidino group may be also bonded to a benzoyl group to form a ring, (6) a naphthalenecarboxylic, thiophenecarbonyl or 1-naphthalenesulfonyl group which may have a substituent(s) selected from the group consisting of guanidino group, guanidinocarbonyl group, guanidinomethyl group and amidino group, (7) a benzoyl group which may have a substituent(s) selected from the group consisting of hydroxyl group, N-methylpyrrolidyloxy group, pyrrolidylmethyl group, imidazolylmethyl group and aminoimidazolylmethyl group, and (8) a dihydrobenzofurancarbonyl or dihydrobenzopyrancarbonyl group which may have a substituent(s) selected from the group consisting of amidino group, guanidino group, amino group, alkyl groups having 1 to 6 carbon atoms, halogeno groups and aryl groups having 4 to 6 carbon atoms, groups (1) to (7) described above may further have an alkoxyl group having 1 to 6 carbon atoms on an aromatic carbon at the o-position to the carbonyl group or sulfonyl group bonded to N in formula (1), and when the alkyl group on the alkoxyl group has 2 or 3 carbon atoms, it may be bonded to a carbon atom on the aromatic ring to form a ring, Y represents an oxygen atom or sulfur atom, and Z represents a hydroxyl group or amino group which may have a substituent(s) selected from the group consisting of phenyl group, benzyl group and phenethyl group.