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7511135 |
Method for manufacture of ceftiofur
A process for preparation of ceftiofur of formula (I)
having purity greater than 97% is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic...
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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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7452990 |
Intermediates for synthesis of cephalosporins and process for preparation of such intermediates
A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics
wherein
X is chlorine or...
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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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7384928 |
Broad spectrum cephem compounds
A compound of the formula:
(wherein,
T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower...
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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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7335767 |
Method for preparation of ceftiofur and salts thereof
A process for preparation of ceftiofur sodium of formula (Ib)
possessing high stability and having purity of more than 97% and substantially free of impurities, is disclosed. The process...
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7098329 |
Process for the preparation of a cephalosporin antibiotic
An improved process for the preparation of ceftriaxone sodium comprising the steps of:
i) reacting the 3-cephem derivative of formula (II)
with halo acid derivative of formula (III)
...
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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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6919449 |
Process for the preparation of cephalosporin intermediate and its use for the manufacture of cephalosporin compounds
The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III)
by...
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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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6906187 |
Manufacture of cefalosporins and intermediates
There is described a process for the preparation of 3-disubstituted cepham-4-carboxylic acid derivatives of formula I
wherein R″ is 4-methoxybenzyl, X is the residue of a thioether and Z is...
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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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6787649 |
Cephalosporin intermediates
A process which comprises (i) acylating a compound of formula II with a compound of formula IV to obtain a compound of formula I and (ii) deformylating said compound of formula I to obtain a...
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6777549 |
β-lactam production
A process for the production of a compound of formula comprising i) silylating a compound of formula then reacting a resulting with a compound of formula R′ B S—X′ IVB wherein R′ B is...
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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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6713625 |
Process for the preparation of cefditoren using the thioester of thiazolylacetic acid
The present invention provides a process for the preparation of Cefditoren of the formula (I) which comprises acylating 7-amino-cephem carboxylic acids of the general formula (IV) where R 3 is...
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6642377 |
Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates
A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic...
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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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6555680 |
Method for the preparation of ceftiofur sodium
The present invention relates to a process for the preparation of sodium salt of Ceftiofur as given in Formula I, directly from its amine salt using sodium base.
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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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6552186 |
β-lactam production
The present invention provides processes for the production of a compound of formula I wherein X, R1 and R2 are substituents conventional in cephalosporin chemistry; especially a compound of...
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6504026 |
Process for production of ceftiofur
Process for preparing ceftiofur having formula I: in the form of the sodium salt.
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6468995 |
Cephem compounds
A compound of the formula: wherein R 1 is amino or protected amino; R 2 is hydrogen, lower alkyl or hydroxy protective group; R 3 is carboxy or protected carboxy; R 4 is an unsubstituted 5,...
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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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6441162 |
Crystalline substance of cefditoren pivoxyl and the production of the same
A crystalline substance of Cefditoren pivoxyl is provided which has a high purity and enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process...
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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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6417175 |
Phosphonocephem derivatives, process for the preparation of the same, and use thereof
A novel cephem compound of the formula: wherein R 1 is a phosphono group or a group convertible to a phosphono group; R 2 is a hydrogen atom or a group having a linkage through a carbon atom;...
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6384215 |
Preparation of new intermediates and their use in manufacturing of cephalosporin compounds
The present invention provides new thioester derivatives of 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (I), also, the invention provides a method by which the said...
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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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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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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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6242437 |
Cephem derivatives
A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative...
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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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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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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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5883089 |
Cephem derivatives
Compounds, represented by the following formula (I), having a β-(substituted or unsubstituted imidazo 5,1-b!thiazolyl)vinyl group at the 3-position of the cephem ring and a salt and an ester...
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5869649 |
Process for producing cephalosporin antibiotics
A process for preparing certain cephalosporin antibiotics, namely, cefotaxime, cefetemet, and ceftriaxone sodium comprising acylation of 7-amino-3-cephem-4-carboxylic acid derivatives with...
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5827845 |
Cephalosporin derivative
A cephalosporin derivative which has a substituted or unsubstituted 2-(5-thiazolyl)vinyl group at the 3-position and is represented by the following formula (I) ##STR1## wherein X is CH or N, R 1 ...
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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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5789584 |
Substituted-pyridinyl cephalosporin antibiotics active against methicillin resistant bacteria
The present invention includes (7R)-7-(acylamino)-3-(substituted-pyridinyl)-3-cephem-4-carb
oxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against...
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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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