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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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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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7459550 |
Process for the preparation of Cefditoren
The present invention relates to an improved process for the preparation of Cefditoren of formula (I), the said process comprising the steps of: i) converting the compound of formula (II) to a...
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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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7071329 |
Process for preparing cephalosporins with salified intermediate
Cephalosporins may be conveniently prepared by a process in which a benzathinium salt of formula (V)
wherein:
Z is benzathine; and X and R 2 are as defined in the specification, is...
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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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6803461 |
Synthesis of ceftiofur intermediate
The present invention relates to a process for preparation of 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxyli
c acid (I) by the condensation of 7-aminocephalosporanic acid (II) with...
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6800756 |
Method for the preparation of ceftiofur sodium and its intermediates
The present invention relates to preparation of Ceftiofur acid of formula (I), and its pharmaceutically acceptable salts. The process includes the steps of (i) condensing an activated derivative...
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6723716 |
7-acylamino-3-heteroarylthio-3-cephem carboxylic acid antibiotics and prodrugs thereof
The present invention relates to a cephem prodrug having formula III or formula IV: or a pharmaceutically acceptable salt thereof, wherein R′ 1 is selected from the group consisting of...
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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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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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6555679 |
Method for preparation of ceftiofur sodium from its hydrohalide salts
The present invention relates to a process for preparing sodium salt of cephalosporins from their corresponding hydrohalide salt, which is neutralized with trimethylsilylating agent for the first...
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6476220 |
Process for the preparation of furaca
A process is disclosed for the preparation of 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxyli
c acid (also known as Furaca). The process comprises of the steps of reacting...
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6458949 |
Ceftiofur, its intermediate and a process for the preparation of the same
A novel process for the preparation of ceftiofur, a cephalosporin antibiotic useful in the treatment of bovine respiratory disease using a novel bromo or chloro intermediate. the process comprises...
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6448393 |
Process for producing 3-cephem compounds
3-Halogenomethylcephem compound of the formula (2) or its salt is obatined by deprotecting with phenol derivative a carboxylic acid protecting group at the 4-position of...
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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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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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6329363 |
Cephalosporin antibiotics
The invention provides new fluorinated cephalosporin antibiotics and methods of preventing or treating infection, particularly mastitis in ruminants, using these antibiotics, and veterinary 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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6294527 |
Cephem compounds
An antibacterial compound ##STR1## wherein ##STR2## represents benzene ring, pyridine ring, pyrazine ring or 5-membered aromatic neterocycle (having one oxygen or sulfur atom as...
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6288223 |
Process for the selective preparation of Z-isomers of 3-2(substituted vinyl)cephalosporins
There can be produced, at a high selectivity and in a high yield, the Z-isomer of a 7-N-unsubstituted or substituted-amino-3-[2-(4-substituted or unsubstituted-thiazol-5-yl)...
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6235897 |
Separation of cephalosporin isomers
Process of depleting 7-amino-3-[(E)-2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-car
boxylic acid in Z/E mixtures of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxy
lic acid a) by...
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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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6150351 |
Cephem compounds and pharmaceutical use thereof
This invention relates to new cephem compound represented by the following general formula (I): ##STR1## wherein each symbol is as defined in the specification or a salt thereof, which has...
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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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6087355 |
Cephalosporin antibiotics
The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R 99 is selected from the group...
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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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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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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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5945414 |
Process for the preparation of new intermediates useful in the synthesis of cephalosporins
Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II): R--SH ...
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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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5705496 |
Crystalline benzathine salt of cefonicid and its preparation
The present invention relates to benzathine salts of cefonicid, a member of the cephalosporin family of antibiotics, which are crystalline. ##STR1##
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5698547 |
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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5663162 |
Cephem derivatives
Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted imidazo[5,1-b]thiazolium-6-yl as a substituent at the 3-position of the cephem...
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5639877 |
Intermediates in the synthesis of cephalosporins
Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of...
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5635501 |
Alphalosporins and 1-carba-1-dethia cephalosporins
Compound of formula (I) or salts 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 readily removable...
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5625058 |
Process for the preparation of cephalosporins
The present invention relates to a process for the preparation of 7-(α-hydroxyacylamino)-3-(1-sulphoalkyl-tetrazol-5-yl-thiom
ethyl)-3- cephem-4-carboxylic acids and relevant salts, via acylation...
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5596095 |
Formation and utility of sulfonic acid protecting groups
The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion...
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5594132 |
7-acylamino-3-substituted cephalosporanic acid derivatives
A compound of the formula: ##STR1## in which R 2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl, R 3 is carboxy or a protected carboxy group, A 5 is lower alkylene...
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5580865 |
2,2-disubstituted cephem sulphones
The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R 1 is hydrogen,...
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5574153 |
Oxime derivatives of cephalosporanic structure
The invention relates to oxime derivatives of cephalosporanic structure, possessing antibacterial activity.
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5527906 |
Process for the preparation of ceftriaxon disodium salt hemiheptahydrate
A new and improved process for the preparation of ceftriaxon disodium salt hemiheptahydrate of formula I ##STR1## is described, wherein...
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5521308 |
Process for the preparation of crystalline TACA
Process for the preparation of crystalline TACA ##STR1## in the presence of a base and subsequent precipitation by addition of a TACA solution to a partial amount of an acid, which can also contain...
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5498787 |
Method for preparing cephalosporin derivatives
A method for preparing cephalosporm derivatives by reacting cephalosporin alkaline metal salts with organic halide in the presence of quaternary ammonium salts catalyst is disclosed. Δ 3 ➝Δ 2 ...
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5446037 |
2-[(substituted) methylene]cephalosporin sulfones as antiinflammatory, antidegenerative and antithrombin agents
This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as...
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5439904 |
2-spiro(2'-spirocycloalkyl)cyclopropyl cephalosporin sulfones as antiinflammatory and antigenerative agents
2-spiro (2'-spirocycloalkyl) cyclopropyl cephalosporin sulfone compounds, methods of treating patients for elastase inhibition, and processes for preparing such compounds.
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5412093 |
3-heterocyclic thiomethyl cephalosporins
Cephalosporin compounds having a 3-position substituent of the formula (I) are described: --CH 2 --S--Q--(Y) n --P wherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring...
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5407930 |
Cephalosporin derivatives
The present invention relates to a compound represented by the structural formula I: ##STR1## its pharmaceutically acceptable salt or ester, or its crystalline, which is a novel optically active...
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