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7592447 |
Process for production of intermediates for use in cefalosporin synthesis
A process for the production of intermediates having a formula IA
that can be used for the synthesis of cephalosporins, such as cefepime of formula V. The intermediates of formula IA are...
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7544797 |
Processes for the preparation of cephem derivatives
Provided is a process for preparing a compound of formula 1 or its salt, which includes reacting a compound of formula 2 with a compound of formula 3 in the presence of a base.
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7507812 |
Process for producing 3-chloromethyl-3-cephem derivatives
An industrially advantageous process for producing 3-chloromethyl-3-cephem derivative crystals. The process for 3-chloromethyl-3-cephem derivative production comprises: a first step in which a...
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7488724 |
7-alkylidene-3-substituted-3-cephem-4-carboxylates as beta-lactamase inhibitors
The invention provides compounds of formula (I):
wherein: R 1 -R 4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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7459551 |
Method for preparing cyclic compounds
The present invention provides a method for preparing a β-lactam compound of the following Formula (3), which comprises the step of reacting a compound of the following Formula (1) with a trialkyl...
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7396926 |
Beta-lactamase substrates having phenolic ethers
Provided are fluorescent substrates for β-lactamases having the general formula I:
in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R′ is selected from the group consisting of...
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7355041 |
Intermediates in cefprozil production
A salt of PACA with an amidine and its use in the production of cefprozil.
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7339055 |
Process for the preparation of cephalosporin antibiotic
A process for the preparation of cephalosporin antibiotic of the formula (I)
which comprises:
(i) activating the compound of formula (III) as acid halide in an organic solvent
(ii)...
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7157574 |
Process for preparing crystalline 3-chloromethyl-3-cephem derivatives
A chlorinated azetidinone derivative expressed by Formula (1) and an alcoholate are allowed to react in a solvent containing at least one of alcohols and an ether at a pH of 8 or less. Thus a...
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7112672 |
Process for the selective preparation of 3-(z) propenyl-cephem compound
A 3-(Z)-propenyl cephem compound is selectively prepared by reacting a phosphoranylidene cephem compound with acetaldehyde in the presence of a base in a solvent mixture comprising diethyl ether,...
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6949521 |
Therapeutic azide compounds
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and...
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6916801 |
7-Alkylidene-3-substituted-3-cephem-4-carboxylates as β-lactamase inhibitors
The invention provides compounds of formula (I):
wherein: R 1 -R 4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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6903211 |
Process for the preparation of 3-propenyl cephalosporin DMF solvate
The present invention relates to an improved process for the preparation of cefprozil DMF solvate of formula (I),
which is useful for the preparation of cefprozil, comprising:
i)...
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6887992 |
3-cephem derivative crystal
A 3-cephem derivative crystal which is a clathrate compound comprising p-methoxybenzyl ester of 7-phenylacetamide-3-formyl-3-cephem-4-carboxylic acid and dimethylformamide and a process for...
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6683176 |
Intermediates for and synthesis of 3-methylene cephams
The present invention relates to novel processes for the preparation of 3-methylenecephams. More specifically, the present invention relates to the intramolecular cyclization of penicillin...
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6610845 |
Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
The present invention provides new thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R 1 represents H, trityl, CH 3 , CR a R b COOR 2 (R a and R b ...
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6583133 |
Propenyl cephalosporin derivatives and process for the manufacture thereof
Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and...
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6576761 |
Process for the preparation of cephem compounds
1. A process for preparing a 3-alkenylcephem compound or 3-norcephem compound of the formula (3) characterized in that an alkenyl halide of the formula (2), a nickel catalyst, a metal up to −0.3...
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6495539 |
B-lactam-like chaperone inhibitors
Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO 2 or O; each of R 1 , R 2 and R 3 is independently H or substituted or unsubstituted alkyl (1-10C),...
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6458558 |
Process for the preparation of β-lactam derivatives
A process for the preparation of Cefuroxime acid (I), which comprises the following steps: (1) Extraction of deacetyl 7-glutaryl ACA (II) aqueous solution at acid pH with organic solvents (for...
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6437119 |
Compounds formed from two or three antibiotics and their processes of preparation
Processes for preparing compounds having two or three antibiotic functionalities using quinolone derivatives, β-lactams and vancomycin and the like as the starting materials and chloride linking...
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6420554 |
Process for preparation of 3-cephem compound
A process for preparing a 3-cephem compound represented by the formula (3), the process comprising the steps of reacting a β-lactam compound represented by the formula (1) with a phosphorus halide...
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6417351 |
Process for producing 3-alkenylcephem compounds
A process for preparing 3-alkenylcephem compounds characterized in that 3-alkenylcephem compound of the formula (3) is prepared in a single step by simultaneously conducting reactions of a...
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6414140 |
Process for the production of 3-vinyl cephalosporins
A process for the production of a 3-vinylcephalosporin compound of formula I wherein R 1 and R 2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula...
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6407091 |
β-lactamase inhibiting compounds
The invention provides compounds of formula I and IV: wherein R 1 -R 11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for...
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6403789 |
Method of halogenating hydroxyl group
A halogenating agent of the formula (1) and a method of halogenating hydroxyl group wherein R 1 and R 2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or...
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6399770 |
Preparation of β-hydroxy esters using ammonium borohydrides
A process for preparing a β-hydroxyester comprising reducing a β-keto ester in the presence of a salt of ammonium borohydride.
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6369049 |
Treatment of mastitis
The invention provides new fluorinated cephalosporin antibiotics of Formula I wherein R a , R b , R c , R d and R e , independently, are H, F or a C 1 -C 6 alkyl-(Z) n — group having at...
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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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6284888 |
Vinyl-ACA purification process
A process for purification of vinyl-ACA of formula ##STR1## from a mixture of vinyl-ACA and 7-ADCA of formula ##STR2## is provided. The process comprises a) producing a mixture of a salt of...
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6274730 |
Process for producing halogenated β-lactam compound
A process for preparing halogenated β-lactam compounds, characterized in that a β-lactam amino compound of the formula (1) is reacted with nitrous acid or nitrite in a slurry dispersion state in...
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6255479 |
Process for the preparation of α-oxolactams
A method for preparing an α-oxolactam comprising, reacting a corresponding α-diazolactam with an oxygen donor, in the presence of a transition metal catalyst, to yield the corresponding...
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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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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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6121255 |
Phloroglucide derivatives and their pharmceutical use
A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH 2 or CO; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or...
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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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6093813 |
Cephalosporin compounds
Cephalosporin derivatives of formula II ##STR1## wherein R a denotes hydrogen or a silyl group; R b denotes a group of formula --OR e , wherein R e denotes hydrogen or alkyl; and R c and R d ...
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6077952 |
Cephaloporins and homologues
A compound of formula (II) or a salt: ##STR1##
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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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6005101 |
Glutaryl 7-ACA derivatives and processes for obtaining them
A compound having the following general formula (I): ##STR1## where R is a hydrogen atom; a linear or branched C 1 -C 4 alkyl group, unsubstituted or substituted by at least a phenyl group or at...
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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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5998610 |
Silylation process
A process for the silylation of 6-aminopenicillanic acid or 7-amino-desacetoxy-cephalosporanic acid by silylation in certain carboxylic acid esters and its use in the production of...
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5986091 |
Process for preparation of β-lactam compounds
The present invention provides a process for preparing an allenyl β-lactam compound represented by the formula (II) or a process for preparing a 3-halocephem compound of the formula (III) by...
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5977352 |
Process for preparing 3-norcephem compounds
The present invention provides a process for preparing 3-norcephem compound represented by the formula (2), characterized in that a hydride reagent is acted on a halogenated β-lactam compound...
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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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5935831 |
Mutated β-lactam acylase genes
New mutant β-lactam acylases are provided exhibiting altered substrate specificities. These β-lactam acylases are obtained by expression of a gene encoding said β-lactam acylase and having an...
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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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5919924 |
Process for preparing 3-halogenated cephem derivative
A process for preparing a 3-halogenated cephem derivative represented by the formula (2), characterized by causing a halogenating reagent to act on an allenyl β-lactam compound represented by the...
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5880111 |
Therapeutic derivations of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by...
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