摘要:
This invention relates to novel 7-acylaminocephalosporanic acid derivatives and pharmaceutically acceptable salts thereof, of high antimicrobial activity, said novel derivatives having the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkenyl, protected carboxy(lower)alkenyl, or lower unsaturated aliphatic hydrocarbon,R.sup.3 is hydrogen, halogen, methyl, lower alkoxy, lower alkylthiomethyl, lower alkanoyloxymethyl or a heterocyclicthiomethyl which may have suitable substituents,R.sup.4 is carboxy or protected carboxy,R.sup.5 is hydrogen or lower alkyl, andX is halogen,provided that when R.sup.3 is lower alkanoyloxymethyl, then R.sup.2 is lower unsaturated aliphatic hydrocarbon, and pharmaceutically acceptable salts thereof.
摘要:
The invention relates to novel cephem compounds, of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.
摘要:
There are disclosed compounds of the formula: ##STR1## in which R is lower alkoxycarbonyloxy(lower)alkyl or 1-propionyloxyethyl, or a salt thereof, pharmaceutical compositions containing the same and their use to treat infectious diseases.
摘要:
This invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of high antimicrobial activity, to processes for preparation thereof from novel intermediates, and to said intermediates of the formula: ##STR1## in which R.sub.A is a group of the formula: ##STR2## wherein R.sup.1 is amino-substituted-heterocyclic group which may have halogen, protected amino-substituted-heterocyclic group which may have halogen, or a group of the formula: ##STR3## wherein R.sup.3 is lower alkyl,R.sup.8 is aryl,A is lower alkylene which may have a substituent selected from the group consisting of amino, a protected amino group, hydroxy, oxo and a group of the formula:.dbd.N.about.OR.sup.4,whereinR.sup.4 is hydrogen, cyclo(lower)alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituent(s) selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sub.B is a group of the formula:--CH.sub.2 --X.sup.2, --CH.sub.2 P.sup..sym. (R.sup.7).sub.3 .multidot.X.sup.3.crclbar. or --CH.dbd.P(R.sup.7).sub.3whereinR.sup.7 is aryl, and X.sup.2 and X.sup.3 are each halogen, andR.sup.2 is carboxy or a protected carboxy group, provided that, when R.sub.A is a group of the formula:R.sup.8 --CH.dbd.N--, wherein R.sup.8 is as defined above, then R.sub.B is a group of the formula:--CH.sub.2 P.sup..sym. (R.sup.7).sub.3 .multidot.X.sup.3.crclbar. or --CH.dbd.P(R.sup.7).sub.3,whereinR.sup.7 and X.sup.3 are each as defined above, or a salt thereof.
摘要:
The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR.sup.3 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.
摘要:
This invention relates to novel 7-acylaminocephalosporanic acid derivatives of high antimicrobial activity, to processes for their preparation, and to pharmaceutical compositions comprising said derivatives, said derivatives being of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is dialkanoyloxy(lower)alkyl; alkyl having one or more substituents selected from the group consisting of hydroxy, protected hydroxy, alkoxy, carboxy, protected carboxy, cycloalkylcarbonyloxy and heterocyclic group; lower alkoxycarbonyloxy(lower)alkyl; azido(lower)alkoxycarbonyloxy(lower)alkyl; aroyloxy(lower)alkyl; higher alkanoyloxy(lower)alkyl; phthalidyl; or phthalidylidene(lower)alkyl,R.sup.3 is lower alkyl,Y is thio (--S--) or sulfinyl (--S--), and the dotted line represents 2- or 3-cephem nuclei.
摘要:
The invention relates particularly to syn compounds of the formula: ##STR1## wherein R.sup.2 is hydrogen or an aliphatic hydrocarbon residue which may be substituted with halogen, carboxy or esterified carboxy,R.sup.5 is carboxy or functionally modified carboxy and R.sup.6 is amino or protected amino, and pharmaceutically acceptable salt thereof, their preparation and their pharmaceutical uses.
摘要:
This invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino substituted thiazolyl selected from the group consisting of 2-aminothiazol-4-yl, 2-aminothiazol-5-yl, 4-aminothiazol-2-yl, 2-amino-5-halothiazol-4-yl, 2-amino-4-halothiazol-5-yl, and 4-amino-5-halothiazol-2-yl,protected amino substituted thiazolyl selected from said group,lower alkylamino substituted thiazolyl,amino substituted thiadiazolyl,protected amino substituted thiadiazolyl,amino substituted pyridyl,protected amino substituted pyridyl,furyl,thiazolyl,thiadiazolyl,phenyl, ornaphthyl,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkylthio, andR.sup.4 is carboxy or protected carboxy, and pharmaceutically acceptable salts thereof.
摘要:
This invention relates to novel cephem compounds of high antimicrobial activity, to processes for preparation of said compounds, and to pharmaceutical compositions containing said compounds, the cephem compounds being of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl of from one to six carbon atoms substituted with aryl hydrocarbon of from 6 to 10 carbon atoms or substituted aryl hydrocarbon with at least one halogen, hydroxy, amino (lower) alkyl, amido (lower) alkyl, or lower alkyl substituent,R.sup.3 is carboxy or protected carboxy, andR.sup.4 is hydrogen,and its pharmaceutically acceptable salt.
摘要:
Bacteriostatic cephem compounds and processes for preparing same having the formula: ##STR1## wherein R.sup.1 is amino; R.sup.2 is optionally substituted alkyl, C.sub.3-8 cycloalkyl, lower alkenyl, or lower alkynyl; R.sup.3 is amino and/or alkyl substituted heterocyclic group; and R.sup.4 carboxy.