Abstract: The present invention relates to cephalosporin of formula (I) in crystalline form. The compound of formula (I) in crystalline form is useful as antibiotics having potent and broad antibacterial activity; especially against methicillin resistant Staphylococci (MRSA) and Pseudomonas aeruginosa.

Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

Abstract: The present invention relates to cephalosporin of formula (I) in crystalline form. The compound of formula (I) in crystalline form is useful as antibiotics having potent and broad antibacterial activity; especially against methicillin resistant Staphylococci (MRSA) and Pseudomonas aeruginosa.

Abstract: The present invention discloses a novel powder for oral suspension of cefdinir. Also disclosed are methods of preparing the suspension and methods of treatment using the suspension.

Abstract: A novel process for the preparation of amorphous cefuroxime axetil particles and the amorphous cefuroxime axetil particles therefrom are disclosed in the invention. Specifically, the invention is implemented by means of antisolvent recrystallization to prepare the cefuroxime axetil in an amorphous form; particularly, the amorphous ultrafine or even nanosized cefuroxime axetil with a controllable particle size and a narrow particle size distribution. The cefuroxime axetil according to the invention can used to enhance bioavailability, since it is in an amorphous form and has a controllable particle size and a narrow particle size distribution.

Abstract: The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a ?-lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a ?-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a ?-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a ?-lactmase or instructions for using the components in an assay.

Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and intermediates useful for the synthesis of compounds of formula (I).

Abstract: Disclosed are salts of the general formula (I) wherein R1, R2 and B are as defined in the description and methods for the preparation thereof. These salts are useful intermediates for the preparation of cefdinir.

Abstract: Process for producing Cefepime, Cefpirome and Cefquinome, whereby a cephalosporin containing a quaternary ammonium group is reacted with thiourea to provide the aforesaid cephalosporins.

Abstract: The present invention relates to an improved process for the preparation of cephalosporin antibiotics of formula (I). The present invention also provides new salts of compound of formula (II) and a process for the preparation of these new salts, where n=0.5 to 2. The present invention also provides a process for the preparation of compound of formula (I) using the new salts of formula (II).

Abstract: 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 bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, —CH2COOR5, or —C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII) in an organic solvent at a temperature ranging from ?30° C. to ?15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.

Abstract: A novel crystal (B-type crystal) of 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide-3-vinyl-3-cephem-4-carboxylic acid (a syn isomer) , characterized in that it exhibits peaks at diffraction angles shown in the following Table 1, in its powder X ray diffraction pattern: TABLE 1 Diffraction Angle 2? (°) approximately 11.7 approximately 16.1 approximately 18.6 approximately 21.2 approximately 22.3 approximately 24.4 approximately 26.2 This crystal is obtained by forming a crystal from a solution at a temperature of ?5 to 5° C. in an acidic state. The crystal is not bulky, exhibits good stability and good filterability, and is excellent in the solubility toward water, and thus can be prepared with case.

Abstract: There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and water at 4° C. in the presence of triethylamine. The reaction mass is extracted with ethyl acetate. 7-[2-(2-Amino-4-thiazolyl)-2-(methoxycarbonylmethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid triethylamine salt present in the aqueous layer is hydrolyzed with sodium hydroxide in less than 30 minutes and aqueous hydrochloric acid is added immediately to adjust the pH to 4.8 to 5.2. Then, aqueous hydrochloric acid is added at 35° C. to adjust the pH 2.5 and cooled to crystallize cefixime trihydrate in high purity.

Abstract: Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R1 and R2 are independently selected from H, aliphatic, aromatic, alkyl, and acyl; R4 may be H and lower alkyl; B may be H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR5OCO(CH2)nCH3, —CHR5OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benz, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R5 is selected from the group consisting of H and lower alkyl; n is an integer between 0 and 10, inclusive; and A may be S, O, SO, SO2 or CH2. In embodiments, the beta-lactam ring may be cleaved by a beta-lactamase enzyme effective to free a fluorophore.

Abstract: The present invention relates to novel polymorph of Ceftiofur sodium as a crystalline product. The present invention also provides a process for the preparation of crystalline Ceftiofur sodium of formula (I).

Abstract: Disclosed are salts of the general formula (I) wherein R1, R2 and B are defined in the description. These salts are useful intermediates for the preparation of cefdinir. Also, disclosed are processes for the preparation thereof from the compounds of the general formula (II) and (III). Further, disclosed is a method of producing cefdinir from the salts of the general formula (I) including the steps of removing protecting groups.

Abstract: The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Provided are fluorescent substrates for ?-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 H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, ?-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula I.

Abstract: 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.

Abstract: The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.

Abstract: There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclizing a compound of Formula (III): wherein R1, R2, R3, R4, X and m have meanings which are given in the description.

Abstract: 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) treating the reaction mass obtained from step (i) with water (iii) separating the organic layer containing the reactive derivative of formula (III) and condensing it with 7-amino cephalosporin derivative by maintaining the pH in the range 5.0-10.0 using an inorganic base of the formula (XV), and iv) cyclizing the compound of formula (XVI) with thiourea in the presence of solvent and salt of organic or inorganic acid at a temperature in the range of ?50 to +50° C. to produce compound of formula (I).

Abstract: An amino acid in solution is precipitated with concentrated hydrochloric acid and isolated as the dihydrochloride monohydrate. Said dihydrochloride is redissolved and reprecipitated by adding a solvent.

Abstract: Crystalline hydrates of (6R-(6?,7?(Z))-7-((2-amino-4-thiazolyl)(hydroxyimino)acetyl)amino)-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cefdinir), calcium salt, ways to make them, compositions comprising them and made with them, and methods of treatment using them are disclosed.

Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.

Abstract: 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).

Abstract: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R is -A-R6 wherein A is bond, —NHCO—(CH2CO)n—, lower alkylene, —NH—CO—CO— or the like, and R6 is wherein R7, R8, R9 and R10 are independently amino, guanidino, amidino or the like; R4 is carboxy or protected carboxy; and R5 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

Abstract: The present invention relates to a compound of the formula [I]: wherein A is lower alkylene or lower alkenylene; R1 is lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl or protected amino(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R3 and R5 are independently amino or protected amino; and R4 is carboxy or protected carboxy, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

Abstract: Cefdinir crystalline salts of formula (I), in which n ranges from 1 to 3, the preparation and use thereof for the preparation and purification of cefdinir are herein disclosed. The salts of formula (I) can be obtained from cefdinir intermediates or crude cefdinir by treatment with phosphoric acid.

Abstract: Substrates for ?-lactamase of the general formula I 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 group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R? is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z? and Z? are linkers for the fluorescent donor and quencher moieties.

Abstract: High purity cefdinir is prepared in a high yield by a process comprising the steps of: treating a crystalline salt of a cefdinir intermediate with a formic acid-sulfuric acid mixture or a formic acid-methanesulfonic acid mixture to obtain a crystalline salt of cefdinir and reacting the crystalline salt with a base in a solvent.

Abstract: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl, hydroxy(lower)alkyl or halo(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene or lower alkenylene; R3 is hydrogen or lower alkyl; R4 is R5 is carboxy or protected carboxy; and R6 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

Abstract: 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, formula (I), wherein R is a carboxyl protecting group; R1 is hydrogen or R2CH2CO—; and R2 is ethyl, 2-thiophenyl, phenyl, p-hydroxyphenyl or phenoxy

Abstract: The present invention relates to a novel process for the preparation of a cefdinir by reacting O-acetyl thioester of Formula I with in the presence of a base in suitable solvent wherein R? represents H or any carboxyl protecting group, and then converting to the cefdinir by the removal of protecting groups. This invention also relates to making the cefdinir using a novel process to prepare the O-acetyl thioester intermediate (Formula I) by condensing (Z)-2-(2-amino-4-thiazolyl)-2-acetyloxyiminoacetic acid with bis(benzothiazol-2-yl)disulphide in the presence of triphenylphosphine and a base in a suitable solvent.

Abstract: Cephalosporins may be conveniently prepared by a process in which a benzathinium salt of formula (V) wherein: Z is benzathine; and X and R2 are as defined in the specification, is reacted with thiourea. The resulting product may be crystallized as a sodium salt, as an internal salt, or as a pharmaceutically acceptable salt.

Abstract: The invention is concerned with a process for the manufacture of vinylpyrrolidinone-cephalosporin derivatives from 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; Z signifies hydrogen or an amino protecting group; and * represents a center of chirality.

Abstract: A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous ?2-isomer of formula (II) and other impurities. The process comprises reacting cefuroxime acid of formula (III) with (R,S)-1-acetoxyethyl bromide of formula (IV), and a Group I or II metal carbonate in the presence of a compound of formula (V), MmHnPqOr??(V) wherein M is Group I or II metal; m is 1, 2, 3; n is 0, 1, 2, or 4; q is 1 or 2; r is 4, 7 or 8; in the presence of a C1-4 alcohol and a polar tertiary amide solvent selected from N,N-dimethylacetamide, N,N-dimethylformamide, N,N-dimetheylpropionamide, N,N-diethylacetamide, N,N-diethylformamide and N,N-diethylpropionamide at a temperature ranging from about ?30 to +30° C. and subjecting the product thus obtained to a desired step of purification.

Abstract: 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 photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).

Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), wherein R1 and R2 are each independently hydrogen, (C1-C10)alkyl, (C2-C10)alkenyl, (C2-C10)alkenyl, (C3-C8)cycloalkyl, (C1-C10)alkoxy, (C1-C10)alkanoyl, (C1-C10)alkanoyloxy, (C1-C10)alkoxycarbonyl, aryl, heterocycle, halo, cyano, nitro, —COORe, —C(?O)NRfRg, —OC(?O)NRfRg, NRfRg, or —S(O)nRh; R3 is hydrogen, halo, aryl, heteroaryl, —S(O)nRh, or —CH?CHC(?O)NRmRp; R4 is hydrogen; A is thio, sulfinyl, or sulfonyl; and intermediates useful for the synthesis of compounds of formula (I).

Abstract: 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 a residue of a nucleophilic compound, such as 2-furoylthio, acetoxy or 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-ylthio, by reaction of a functional derivative of ?-(2-chloroacetamido)thiazol-4-yl-?-methoxyiminoacetic acid with 7?-amino-3-methylenecepham-4-carboxylic acid 4-methoxybenzyl ester, subsequent treatment of the obtained 4-methoxybenzyl 7?-[?-(2-chloroacetamido)thiazol-4-yl-?-methoxyimino]acetamido-3-methylenecepham-4-carboxylate with a S-chloromercaptan of formula X—S—Cl, such as methanesulfenyl chloride, and final treatment of the corresponding 4-methoxybenzyl 7?-[?-(2-chloroacetamido)thiazol-4-yl-?-methoxyimino]acetamido-3-thio-3-chloromethylcepham-4-carboxylate thus obtained of formula V wherein R? and X are as defined above, with a compound of formula M-Z, in which M is an alkaline metal

Abstract: A cephem compound or pharmaceutically acceptable salt thereof represented by the formula I: wherein R1 and R2 may be the same or different and each represent hydrogen atom, nitro or cyano; R3 represents C1-C6 alkyl which may be substituted with carboxyl; R4 represents hydrogen atom or amino; X represents —S— or —SO—, there being no case where both of R1 and R2 are simultaneously hydrogen atom.

Abstract: Cefuroxime in the form of a salt with n-butylamine; and its use for the production of cefuroxime axetil or for the production of the sodium salt of cefuroxime.

Abstract: This invention relates a process for preparing a compound of formula (I) 1

Abstract: Processes for the depletion of 7-ADCA in mixtures of vinyl-ACA with 7-ADCA via novel salts of vinyl-ACA or via chromatography.

Abstract: The compounds of the general formula (I) wherein R1 denotes a pharmaceutically acceptable side chain radical as used conventionally in the field of cephalosporins and wherein R2 denotes a pharmaceutically acceptable group which is bonded to the remaining part of the molecule by an oxygen-carbon single bond or a nitrogen-carbon single bond, and their pharmaceutically acceptable salts, esters and amide derivatives are effective antibiotics.

Abstract: A process for the preparation of highly pure crystalline form of cefuroxime-1-acetoxyethyl ester (cefuroxime axetil) from cefuroxime by reacting an amine salt of cefuroxime with an esterifying reagent.

Abstract: The present invention relates to a compound of the formula [I]: wherein A is lower alkylene or lower alkenylene; R1 is lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl or protected amino(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R3 and R5 are independently amino or protected amino; and R4 is carboxy or protected carboxy, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

Abstract: The present invention relates to a novel process for the preparation of intermediate, 2-mercapto-benzothiazolyl (Z)-2-(2-amino-4-thiazolyl)-2-acetyloxyiminoacetate of Formula I and its use in the preparation of Cefdinir.

Abstract: A fullerene-antibiotic conjugate including at least one antibiotic molecule per fullerene moiety. The fullerene may comprise C60 and the antibiotic may comprise vancomycin or may be selected from the group consisting of penicillins, cephalosporins, quinolones, fluoroquinolones, macrolides, lincosamines, carbepenems, conobactams, aminoglycosides, glycopeptides, tetracyclines, sulfonamides, rifampin, oxazolidonones, and streptogramins. The conjugate preferably includes at least two and more preferably at least three antibiotic molecules per C60 center. A method for making a fullerene(C60)-antibiotic conjugate, comprises: synthesizing a linker precursor (I); reacting the linker precursor (I) with C60 via a Bingel-reaction, to produce a fullerene-linker conjugate (II); hydrolyzing the fullerene-linker conjugate (II), resulting in a desired derivative of C60 (III); and reacting the derivative (III) with a desired antibiotic to produce a fullerene-antibiotic conjugate (IV).