Patent ID: 6214818
Filing Date: 2001-04-10
Classification: A61P,C07D

Abstract:
A cephem compound shown by the formula I: ##STR71##whereinAcyl is selected from the group consisting of formyl, (C.sub.1 -C.sub.6) alkylcarbonyl, (C.sub.3 -C.sub.5) alkenoyl, (C.sub.3 -C.sub.10) cycloalkyl-carbonyl, (C.sub.5 -C.sub.6)cycloalkenyl-carbonyl, arylcarbonyl, aralkyl carbonyl, 5- or 6-membered aromatic heterocyclic carbonyl, 5- or 6-membered aromatic heterocyclic acetyl, alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aminoalkylcarbonyl, monoalkylaminoalkylcarbonyl, and dialkylaminoalkylcarbonyl, optionally substituted with one to three substituents independently selected from the group consisting of amino, nitro, halogen, hydroxy, oxo, carbamoyl, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, (C.sub.1 -C.sub.4) alkoxycarbonyl, (C.sub.1 --C.sub.4) alkoxyimino optionally substituted with carboxyl or halogen, hydroxyimino and 4-ethyl-2,3-dioxopiperadinocarbonylamino, or acyl is represented by formula III: ##STR72##wherein X is CH or N; Y is an optionally protected amino; and Z is hydrogen or an optionally substituted hydrocarbon group;Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R.sup.1 is hydrogen, a straight or branched lower alkyl which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of C.sub.2-6 alkenyl, cycloalkyl, aryl which is optionally substituted with hydroxy, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, an aromatic heterocyclic group comprising 1 to 4 hetero atoms selected from the group consisting of N, O, and S, a bi- or tricyclic aromatic condensed heterocyclic group comprising 1 to 5 hetero atoms selected from the group consisting of N, O, and S, which is formed by condensing one or two 5- or 6-membered-aromatic heterocyclic groups comprising 1 to 4 hetero atoms selected from N, O, and S, a non-aromatic heterocyclic group, amino, mono- or di-alkyl amino, amidino, C.sub.1-6 alkanoyl, carbamoyl, mono- or di-lower alkylcarbamoyl, sulfamoyl, mono- or di-lower alkyl sulfamoyl, carboxyl, lower alkoxycarbonyl, hydroxyl, lower alkoxy, lower alkenyloxy, cycloalkyloxy, aralkyloxy, aryloxy, mercapto, lower alkylthio, aralkylthio, arylthio, sulfo, cyano, azide, nitro, nitroso and halogen, or a straight or branched lower alkenyl which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of C.sub.2-6 alkenyl, cycloalkyl, aryl which is optionally substituted with hydroxy, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, an aromatic heterocyclic group comprising 1 to 4 hetero atoms selected from the group consisting of N, O, and S, a bi- or tricyclic aromatic condensed heterocyclic group comprising 1 to 5 hetero atoms selected from the group consisting of N, O, and S, which is formed by condensing one or two 5- or 6-membered aromatic heterocyclic groups comprising 1 to 4 hetero atoms selected from N, O, and S, a non-aromatic heterocyclic group, amino, mono- or di-alkyl amino, amidino, C.sub.1-6 alkanoyl, carbamoyl, mono- or di-lower alkylcarbamoyl, sulfamoyl, mono- or di-lower alkyl sulfamoyl, carboxyl, lower alkoxycarbonyl, hydroxyl, lower alkoxy, lower alkenyloxy, cycloalkyloxy, aralkyloxy, aryloxy, mercapto, lower alkylthio, aralkylthio, arylthio, sulfo, cyano, azide, nitro, nitroso and halogen; A is a lower alkylene which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of C.sub.2-6 alkenyl, cycloalkyl, aryl which is optionally substituted with hydroxy, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, an aromatic heterocyclic group comprising 1 to 4 hetero atoms selected from the group consisting of N, O, and S, a bi- or tricyclic aromatic condensed heterocyclic group comprising 1 to 5 hetero atoms selected from the group consisting of N, O, and S, which is formed by condensing one or two 5- or 6-membered aromatic heterocyclic groups comprising 1 to 4 hetero atoms selected from N, O, and S, a non-aromatic heterocyclic group, amino, mono- or di-alkyl amino, amidino, C.sub.1-6 alkanoyl, carbamoyl, mono- or di-lower alkylcarbamoyl, sulfamoyl, mono- or di-lower alkyl sulfamoyl, carboxyl, lower alkoxycarbonyl, hydroxyl, lower alkoxy, lower alkenyloxy, cycloalkyloxy, aralkyloxy, aryloxy, mercapto, lower alkylthio, aralkylthio, arylthio, sulfo, cyano, azide, nitro, nitroso and halogen, a lower alkenylene which is optionally substituted with 1 to 3 substituents independently selected from the group consisting of C.sub.2-6 alkenyl, cycloalkyl, aryl which is optionally substituted with hydroxy, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, an aromatic heterocyclic group comprising 1 to 4 hetero atoms selected from the group consisting of N, O, and S, a bi- or tricyclic aromatic condensed heterocyclic group comprising 1 to 5 hetero atoms selected from the group consisting of N, O, and S, which is formed by condensing one or two 5- or 6-membered aromatic heterocyclic groups comprising 1 to 4 hetero atoms selected from N, O, and S, a non-aromatic heterocyclic group, amino, mono- or di-alkyl amino, amidino, C.sub.1-6 alkanoyl, carbamoyl, mono- or di-lower alkylcarbamoyl, sulfamoyl, mono- or di-lower alkyl sulfamoyl, carboxyl, lower alkoxycarbonyl, hydroxyl, lower alkoxy, lower alkenyloxy, cycloalkyloxy, aralkyloxy, aryloxy, mercapto, lower alkylthio, aralkylthio, arylthio, sulfo, cyano, azide, nitro, nitroso and halogen or a single bond; B is --NH-- or a single bond; and D is a single bond or a group of the formula: ##STR73##or an ester, a salt or a hydrate thereof.