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5013730 |
Cephem derivatives
Cephalosporins having a 3-position substituent of the formula: ##STR1## are described, wherein R 5 is hydrogen, alkenyl, alkyl or substituted alkyl, Q is a mono- or bicyclic heterocyclic ring,...
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5013833 |
Process for preparing cefuroxime axetil
There is described a product which is a highly pure substantially amorphous form of cefuroxime axetil (cefuroxime 1-acetoxyethyl ester) which is stable, which has increased absorption via the...
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5010188 |
Cephem derivatives
Described herein is a cephem derivative represented by the general formula: ##STR1## wherein n stands for 1 or 2, Y stands for CH or nitrogen atom, R 1 represents a lower hydrocarbon group or a...
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5008258 |
Cephalosporin derivatives
Cephalosporin compounds having as a 3-substituent the group: ##STR1## wherein Y represents a bond, optionally substituted alkylene or --CH 2 CH 2 NHCO--, P is a benzene ring substituted by groups...
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5008259 |
Cephalosporin compounds
Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein R 1 is hydrogen or certain optionally substituted alkyl groups; X is a benzene ring or...
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4994567 |
Process for preparation of cefuroxime ester
There is described a product which is a highly pure substantially amorphous form of cefuroxime axetil (cefuroxime 1-acetoxyethyl ester) which is stable, which has increased absorption via the...
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4992541 |
Process for the preparation of 1,1-dioxo-7-substituted cephems
The present invention relates to an improved process for the preparation of the compounds of formula (I) ##STR1## which involve the direct oxidation without N-protection of the compound of the...
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4988686 |
Cephem compounds and anti-bacterial agent
Disclosed is a novel cephem compound which is either one of a cis- or trans-isomer or a mixture of the cis-and trans-isomers, represented by the following general formula (I) and a...
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4988685 |
Cephalosporins derivatives
Novel cephalosporins of the formula ##STR1## in which R 1 represents hydrogen or an amino-protecting group and R 2 represents alkyl, cycloalkyl or alkenyl.
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4983732 |
Method of deprotection of 3-amino azetidinones
A method for preparing 2-amino-β-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-β-lactam is further acylated with a...
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4980464 |
Method for production of cephalosporin compounds
A method for producing a compound of the formula; ##STR1## wherein R stands for a hydrogen atom, an acyl group or a protective group other than acyl groups, Q stands for a hydrogen atom or an ester...
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4978752 |
Crystals of cephem hydrochloride
Crystals of 7β-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoace
tamido]-3- (1-imidazo[1,2-b]pyridazinium)methyl-3-cephem-4-carboxylate hydrochloride or a solvate thereof, which are stable...
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4973684 |
Cephem compounds
Broad spectrum antibiotics are provided which are compounds of the formula: ##STR1## wherein R 4 is a residue of a nucleophilic compound and R 5 is hydroxyl or protected hydroxyl; or a...
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4971961 |
Cephalosporin compounds and antibacterial agents
This invention provides cephalosporin compounds represented by the following general formula: ##STR1## wherein R 1 and R 2 are same or different hydrogen atom or a lower alkyl group of 1 to 5...
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4966900 |
Cephalosporin β-lactam compound and medicinal composition
There are disclosed a β-lactam compound represented by the formula (I): ##STR1## wherein R 1 and R 2 are independently a hydrogen atom or a lower alkyl group; M is a hydrogen atom, a protective...
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4965358 |
N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine
A new compound called N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine of Formula I ##STR1## A process for the preparation thereof based on the reaction of 4-ethyl-2,3-dioxo-piperazine or a...
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4962100 |
3-Condensed imidazolium-cephem compounds
A compound of the formula: ##STR1## wherein R 1 is an amino group which may be protected, R 3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S➝O, O or CH 2 , R 4 ...
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4958018 |
Method for production of 3-exomethylenecepham derivatives
Disclosed is a method of producing a 3-exomethylenecepham of the formula ##STR1## wherein R 1 is amino or substituted amino and R 2 is a carboxy-protecting group comprising reacting a cephem of...
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4956358 |
Tricyclic cepham compounds and use
The compounds having a 4,11-dioxo-3-oxa-8(or 7)-thia-1-azatricyclo[7,2,0,0 2 ,6 ]undecane-2-carboxylic acid skeleton as the base structures, their esters and their salts are useful antibacterial...
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4952578 |
Cephem compound and a process for preparation thereof
The object of the invention is a new cephem compound with antimicrobial activity used for the treatment of infectious diseases of the general formula: ##STR1## wherein R1 is amino or a protected...
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4950753 |
Process for 3-exomethylenecepham sulfoxide esters
3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-acylamino-1-azetidinyl)
-3-butenoic acid esters under anhydrous...
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4950661 |
Cephalosporin derivatives, and their application as antibiotics
The present invention relates to derivatives of the cephalosporin family, of formula: ##STR1## in which: X is an oxygen atom or a sulfur atom n is zero, 1 or 2. R 1 , R 2 and R 3 each...
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4943631 |
Process for cephem compounds
The present invention provides compounds of general formula (III) ##STR1## [wherein R is an amino or protected amino group; R 2a is a straight or branched chain alkyl group containing from 1 to...
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4943568 |
Cephalosporins
Antibacterially active novel cephalosporins of the formula ##STR1## in which R 1 represents alkyl, alkenyl, alkoxy, alkylthio, halogen, trifluoromethyl or trifluoromethoxy, R 2 represents...
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4943567 |
Cephalosporin compound and pharmaceutical composition thereof
Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R 1 and R 5 independently represent a hydrogen atom or a protective group for an amino group; R 2 represents an...
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4942159 |
Cephem compounds, their production and use
Novel cephem compounds of the general formula: ##STR1## wherein R 1 is a lower alkyl group, and salts and esters thereof, showing excellent and balanced antibacterial activity against a broad...
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4939250 |
Process for preparation of β-lactam derivatives
A process for preparing compounds of the formula I: ##STR1## wherein X is sulphur, oxygen, methylene or sulphinyl (R or S configuration), R 3 is hydrogen or methoxy, R 4 is an optionally...
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4937330 |
Conversion of cephalosporin hydrohalide salt to alkali metal salt
The present invention relates to processes for the preparation of alkali metal salts of amino acids. Preferably, the present invention relates to solid phase alkali metal salts of cephalosporins of...
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4935507 |
Crystalline 7-(2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido)-3-vinyl-3-cephem-4-c arboxylic acid (syn isomer)
The invention relates to crystalline 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-vinyl-
3-cephem-4-car boxylic acid (syn isomer) useful as an antimicrobial agent.
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4935508 |
Process for cephem prodrug esters
A process for the selective formation of oximino o-protected derivatives of lower alkyl 2-(2-aminothiazol-4-yl)-2-oximinoacetates, and their use in the acylation of 7-amino-cephalosporin compounds...
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4933443 |
Method for preparing crystalline hydrate of oral celphalosporin and its composition
An antibacterial, 7β-[(Z)-2-(2-aminothiazol-4-yl)-4-carboxybut-2-enoylamino]-
3-cephem-4 -carboxylic acid is stable in a (di or tri)-hydrate crystal form. A pharmacologically effective amount of...
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4931555 |
Disulfide substituted oxazetidine derivatives
A process for producing a 2-cephem or 3-cephem derivative compound of the formula: ##STR1## wherein R 1 represents a substituted or unsubstituted amino radical and R 4 represents hydrogen or a...
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4929612 |
Thiadiazolylacetamide cephem derivatives
Novel thiadiazolylacetamide cephem derivatives of the following formula are described. ##STR1## wherein A represents a quaternary ammonio group; or a pharmaceutically acceptable salt thereof. These...
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4921954 |
Process for the preparation of cephem compounds
Process for the preparation of 7β-amino-3-substituted methyl-3-cephem-4-carboxylic acid derivatives, new intermediates comprising 7β-(cyclo)alkylideneammonio-3-halomethyl-3-cephem-4-carbox ylic...
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4918068 |
Cephem compounds
There are provided new cephem compounds (synisomers) represented by the following general formula (I): ##STR1## wherein R 1 means a lower group, R 2 denotes an ester-forming group of the carboxyl...
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4912211 |
Method for producing pure crystalline antibiotic products
A process is described for producing pure crystalline products, in particular penicillin and cephalosporin, wherein the desired product, prepared according to a known method, is treated with...
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4910301 |
Cefepime cephalosporin salts
Crystalline sulfuric, di-nitric, mono-hydrochloric, di-hydrochloric, and di- and sesqui-orthosphosphoric acid addition salts of 7-[α-(2-aminothiazol-4-yl)-α-(Z)-methoxyiminoacetamido]-3-
[(1-...
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4906623 |
3-Imidazolium cephalosporin derivatives
A cephalosporin compound substituted by imidazolium ring in 3-position of cephem having the following formula (I), and pharmaceutically acceptable salt thereof, ##STR1## wherein R 1 is an organic...
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4906748 |
Cephem derivative crystals
Disclosed herein are 7β-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoace
tamido]-3- (4-carbamoyl-1-quinuclidinio)methyl-3-cephem-4-carboxylate crystals comprising X-ray diffraction pattern...
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4902793 |
Process for preparing 3-alkoxymethylcephalosporins
A process for preparing 3-alkoxymethylcephalosporins which are useful as an intermediate for various cephalosporin derivatives having a high antimicrobial activity is disclosed. According to the...
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4894371 |
3-substituted-aminomethyl cephalosporin derivatives
An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X is S,O,CH 2 or S0; R2 is hydrogen, methoxy or formylamino; R3 is carboxy or a biodegradable ester thereof; R1...
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4883868 |
7-amino-3-(substituted isoindolinium)methyl-3-cephem derivatives
A compound having the formula: ##STR1## wherein R 1 is an amino group or a protected amino group, R 2 is a hydrogen atom or a protecting group for a hydroxyl group, R 3 represents negative...
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4880798 |
Cephalosporin derivatives
The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel...
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4880795 |
Cephalosporins
Novel cephalosporins of the formula ##STR1## in which R 1 is an aliphatic or cycloaliphatic hydrocarbyl radical of up to 6 carbon atoms which is optionally substituted by a carboxyl group,...
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4879381 |
7-(substituted or unsubstituted amino) 3-substituted methyl-.sup.3 cephem-4-carboxylic acid
Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl...
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4877782 |
Zinc ceftiofur complexes
Zinc ceftiofur complexes, e.g., zinc ceftiofur hydrochloride and zinc ceftiofur sodium complexes, have been found to provide the good antibiotic activity of ceftiofur while providing low...
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4876351 |
Process for the separation of a mixture of "syn" and "anti" oxime isomers
A process for the separation of a mixture of syn and anti oxime isomers one from the other which comprises adsorbing said mixed oxime isomers onto a non-functional macroreticular adsorption resin,...
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4874856 |
3-(substituted)propenyl-7-(aminothiazolylacetamido) ceph-3-em-4-carboxylic acids and esters thereof
This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R 2 is hydrogen, or lower acyl, R 3 is hydrogen, or lower alkanoyloxy, and R...
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4870168 |
3-Unsaturated alkyl cephems from 3-triflyl cephems
There is disclosed a process for the production of certain 3-hydrocarbyl-3-cephem derivatives wherein the hydrocarbyl group is selected from 1-alkenyl and conjugated and unconjugated 1-polyalkenyl,...
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4868294 |
Process for preparing cephalosporin intermediates
Processes for the preparation of stable, crystalline cephalosporin intermediates of the formula ##STR1## wherein X is HI or HCl, and Nu and Nu ♁ are certain N-containing heterocyclic rings...
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