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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...
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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...
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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.
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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...
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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,...
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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
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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 ,...
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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