141 results about "Cephem" patented technology

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 alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene);Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.

It is intended to provide a reagent composition for detecting beta-lactamase which contains 3-[2,4-dinitrostyryl]-7-(2-thienylacetamido)-3-cephem-4-carboxylic acid or 7-[2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(2,4-dinitrostyryl)-3-cephem-4-carboxylic acid as a substrate for detecting beta-lactamase together with at least one beta-lactamase inhibitor selected from among clavulanic acid, aztreonam, ethylenediaminetetraacetic acid and cloxacillin and by which beta-lactamase can be quickly and easily identified at a high sensitivity. Moreover, a detection kit containing the above detection reagent composition and a method of detecting beta-lactamase comprising contacting a liquid specimen containing the subject to be analyzed with the above composition are provided.

The present disclosure describes Cephem compounds of the formula:wherein,X is N, CH or C—Cl;T is S or the like;A and G are lower alkylene or the like;B is a single bond or the like;D is optionally present, and when present is, —NR7—, —CO—, —CO—NR7—, —NR7—CO—, —NR7—CO—NR7—, or the like;F is optionally present, and when present is or phenylene;R3 and R4 are —OR8;R5 and R6 each is independently hydrogen, halogen, nitrile, or —OR8;or an ester at the carboxyl at the 7-position side chain or at the 4-position, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria.

This invention provides Cephem compounds having the formula:or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, a pharmaceutical composition thereof, and a method for treating a bacterial infectious disease with the compound, the ester, the protected compound, the salt, or the solvate thereof, wherein the symbols in the formula are defined in the specification. The compounds exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and / or Gram positive bacteria, preferably beta-lactamase producing Gram negative bacteria, more preferably, multi-drug resistant microbials, in particular, Class B type metallo-beta-lactamase producing Gram negative bacteria, and still preferably extended-spectrum beta-lactamase (ESBL) producing bacteria. The compounds most preferably do not exhibit cross-resistance against known Cephem drugs or Carbapenem drugs.

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 acid-2-benzothiazolyl thioester of formula (II),with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III)in the presence of a mixture of an water-immiscible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (I) substantially free of impurities by,a) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase,b) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, andc) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a anti-solvent.

A process for the preparation of cefdinir of the formula (I) the said process comprising the steps of: i) condensing 7-amino-3-cephem-4-carboxylic acid of the formula (XII) wherein R1 is as defined above with compound of the formula (XIII) in the presence of a tertiary amine and an organic solvent, followed by treatment with a base to produce a salt of compound formula (XIV), wherein M+ is a counter ion and ii) hydrolyzing the compound of the formula (XIV) using an acid in the presence of a solvent to produce cefdinir of formula (I).

The present invention relates to a process for preparation of 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic acid (I) by the condensation of 7-aminocephalosporanic acid (II) with furyl-2-carbonylthiol (III) in the presence of borontrifluoride or its complex, in an organic solvent or mixture of solvents at 0-50° C.