Match Document Document Title
6384212 Process for preparing cephalosporin antibiotics using new thiazole compound  
The present invention relates to a new, simple, and easy process for preparing cephalosporin antibiotics of the following formula (I), such as ceftazidime and cefixime. The process comprises...
6384213 Process for preparing a pure, pharmacopoeial grade amorphous form of cefuroxime axetil  
There is described a process for the preparation of a pure amorphous form of cefuroxime axetil which involves dissolving crystalline cefuroxime axetil in acetic acid including at least 5% v/v water...
6350869 Crystalline amine salt of cefdinir  
Cefdinir in the form of a salt with dicyclohexylamine, a process for its production and its use in the purification of impure cefdinir.
6333409 Process for the purification of a 3-cephem-4-carboxylic acid derivative  
The invention relates to a new process for the depletion of 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid in mixtures of 7-amino-3-[(Z)-1-propen-1-yl]-3-cephem-4-carboxylic acid and...
6294668 Vinylpyrrolidinone cephalosporin derivatives  
The present invention relates to cephalosporin derivatives of the general formula ##STR1## where R 1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl,...
6255480 Aminothiazole derivatives useful in the preparation of β-lactam antibiotics  
Aminothiazole derivatives having the carboxyl activated by means of thioesters, said derivatives being condensable with β-lactam nuclei to yield β-lactam antibiotics
6248881 Intermediates and process for the production of 3-vinyl cephalosporins  
A process for the production of a 3-vinylcephalosporin compound of formula I ##STR1## wherein R 1 and R 2 may be the same or different and denote hydrogen or an organic radical, which...
6235896 Process for the preparation of cefuroxime  
There is described a process for the preparation of cefuroxime from predominantly S-cefuroxime axetil, R, S mixture of cefuroxime axetil or R-cefuroxime axetil not meeting the purity criteria. This...
6232306 Derivatives of 3-(2-oxo-[1,3']bipyrrolidinyl-3-ylidenemethyl)-cephams  
The present invention provides compounds of formula I ##STR1## wherein R 1 is hydrogen, C 1 -6 -alkyl, C 1 -6 -alkyl substituted by fluoro, or C 3 -6 -cycloalkyl; R 2 is hydrogen or a...
6232305 Substituted amino bicyclic-β-lactam penam and cepham derivatives as cysteine protease inhibitors  
The present invention provides substituted amino bicyclic-β-lactam penam derivatives and substituted amino bicyclic-β-lactam cepham derivatives and their diastereoisomers of formula I, as well as...
6169180 Process for the production of cephalosporines  
The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of...
6159706 Application of enzyme prodrugs as anti-infective agents  
The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate...
6156889 Reagent useful for cleaving a protected functional group  
The subject matter of the present invention relates to a reagent and a process useful for cleaving a functional group protected by an alkoxycarbonyl group during an organic synthesis. This reagent...
6150350 Antimicrobial compositions  
The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from...
6107481 De-esterification process  
A process to prepare the E isomer of a 3-substituted (6R,7R)-7-phenyl-acetamido-ceph-3-em-4-carboxylic acid from a mixture of the E and Z-isomer of either the corresponding tert-butyl or the...
6100393 Process for purifying 7-substituted aminodeacetoxy-cephalosporins through the use of filtration membranes  
Process for purifying 7-substituted aminodeacetoxycephalosporins through the use of filter membranes. A process for purification by ultrafiltration and/or nanofiltration with a cut-off for...
6093814 Process for preparation of cefdinir  
The present invention relates to a novel crystalline cefdinir intermediate having formula (II) which can be used very usefully for preparing a cephalosporin antibiotics, cefdinir, in which Ph...
6063778 Cephalosporin derivatives and processes for the preparation thereof  
The invention provides novel cephalosporin derivatives of the formula (I) ##STR1## and salts thereof for use in pharmaceutical compositions. Also novel precursors for synthesis of the...
6034237 3-imino-cephalosporins  
3-Imino-cephalosporin derivatives of formula II ##STR1## wherein Y denotes alkyl, aryl or heterocyclyl; and R a and R d denote hydrogen or a silyl group; in free form or in salt form, and methods...
6020329 Cephaloporins and homologues, preparations and pharmaceutical compositions  
β-Lactam antibiotics of formula (I) or a salt thereof, wherein R 1 is hydrogen, methoxy or formamido; R 2 is an acy group; CO 2 R 3 is a carboxy group or a carboxylate anion, or R 3 is a...
6013647 Benzoxazinedione derivatives, method of producing them and uses thereof  
This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R 1 =H or carboxyalkyl, R 2 =H, alkyl or phenyl, and R 3 represents different acid...
6001997 Cephalosporins and homologues, preparations and pharmaceutical compositions  
β-Lactam antibiotics of formula (I) or a salt thereof, wherein R 1 is hydrogen, methoxy or formamido; R 2 is an acyl group; CO 2 R 3 is a carboxy group or a carboxylate anion, or R 3 is a...
5998611 Process for producing cephem compounds in an aqueous medium  
An industrially excellent, novel process for producing cephem compounds which are useful as medicines, particularly, antibiotics and represented by the following formula (III): ##STR1## wherein R 1...
5981519 Vinyl-pyrrolidinone cephalosporins  
The present invention relates to compounds having the formula ##STR1## wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined herein as well as readily hydrolyzable esters thereof,...
5969131 Cephem compound, its production and its use for producing cephem antibiotics  
A 3-[(E)-1-propenyl]cephem compound represented by formula (I): ##STR1## wherein R represents hydrogen, a protective group for an amino group, or the group shown by formula (II): ##STR2## in which...
5945532 Method for manufacture of cephalosporin and intermediates thereof  
This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, ##STR1## wherein ##STR2## as...
5929233 Cyclization for preparing halo-cephems  
The invention provides a process for preparing an allenyl β-lactam of formula (4), by reacting the hydroxyl group of a β-lactam of formula (1) with a reactive derivative of sulfonic acid of...
5925632 Derivatives of 3-pyrrolidylidene-2-one-cephalsporines  
Compounds of formula (I) ##STR1## wherein R 1 is hydrogen, lower alkyl, aralkyl, cycloalkyl, R 3 CO-- or --C(R 4 R 5 )CO 2 R 6 ; where R 4 and R 5 are each independently hydrogen or lower...
5872249 3-ammoniopropenyl cephalosporin compounds as antibacterial agents and process for preparing the same  
A 3-ammoniopropenyl cephalosporin of the following formula (I): ##STR1## wherein P is hydroxylated alicyclic or aliphatic amines such as meso-3,4-dihydroxy-1-methylpyrrolidine,...
5861508 Purification of a cephalosporin salt  
A p-toluenesulphonic acid salt of 7- 2-(2-aminothiazol-4-yl)-2-(Z)-hydroximino-acetamido!-3-N,N-d imethylcarb amoyloxymethyl-3-cephem-4-carboxylic acid (isopropoxycarbonyloxy)ethylester, e.g. of...
5856320 Cephem compounds, their preparation and their use as antimicrobial agents  
Novel cephalosporin derivatives of formula (II): ##STR1## wherein R 2 is hydrogen, methyl, or fluoromethyl; R 3 is hydrogen, methyl or carboxyl; R 4 is hydrogen or methyl; A is methylene or...
5856474 Cephalosporin synthesis  
Cephalosporin derivatives of formula ##STR1## wherein R 1 signifies hydrogen or a silyl protecting group, processes for their production and their use as intermediate products.
5847118 Methods for the manufacture of amorphous cefuroxime axetil  
A process for preparing pure amorphous cefuroxime axetil comprising the steps of dissolving crystalline cefuroxime axetil in a highly polar organic solvent and adding the resulting solution to...
5847117 Reagent and catalytic process useful for cleaving a protected functional group  
The subject matter of the present invention relates to a reagent and a process useful for cleaving a functional group protected by an alkoxycarbonyl group during an organic synthesis. This reagent...
5843937 DNA-binding indole derivatives, their prodrugs and immunoconjugates as anticancer agents  
The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy...
5840885 Processes for the production of 6-α-aminoacyl-penicillin and 7-.alpha .  
A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a...
5804577 Cephalosporin derivatives  
The present invention relates to compounds of formula I ##STR1## wherein R 1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily...
5801242 Process for making quinolonyl lactam antimicrobials and novel intermediate compounds  
The present invention provides processes for making compounds of the structure (Q--L 1 )--L--(L 2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L 1 ,...
5773435 Prodrugs for β-lactamase and uses thereof  
The instant invention relates to a novel method for the delivery of antitumor drugs to tumor cells by the administration of a tumor-selective antibody-β-lactamase conjugate that binds to tumor...
5756493 Cephalosporin antibiotics  
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide...
5747484 Crystalline cepham acid addition salts and processes for their preparation  
Novel crystalline cephem acid addition salts and processes for their preparation Compounds of the formula I ##STR1## in which n is equal to 1 or 2 and m is 0.4-2.6, and where X is the anion...
5741902 7-acyl-3-(substituted carbamoyloxy) cephem compounds and process for their preparation  
A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH or --N group; R 1 denotes a hydroxyl, lower alkoxyl,...
5741657 Fluorogenic substrates for β-lactamase and methods of use  
Fluorogenic substrates of the general formula I ##STR1## in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R' is selected from the...
RE35754 Cephem derivatives  
Cephem derivatives of the general formula ##STR1## is which the R 2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against...
5719276 Beta lactam production  
A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a...
5710146 Cephem derivatives and processes for their manufacture  
Cephem derivatives of the general formula ##STR1## in which the R 2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against...
5710147 7-benzyloxyimino-cephalosporins  
The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the...
5698703 Syn-isomer of thiazolyl intermediate and process for the preparation thereof  
The present invention provides a stable, crystalline syn-isomer of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetyl chloride hydrochloride substantially free of the anti-isomer and a process for the...
5693791 Antibiotics and process for preparation  
A group of reagents, as diisocyanates, dianhydrides, diacidchlorides, diepoxides, carbodiimides and the like are utilized to link a wide variety of antibiotic moities, reacted two at a time with...
5686588 Amine acid salt compounds and process for the production thereof  
A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and...