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| Number | Title | Issue Date |
| 7622577 | Processes for the preparation of cephalosporin derivatives Provided is a process for preparing a compound of formula 1 or its salt, which comprises reacting a compound represented by the following formula 4 with acetaldehyde in a mixed solvent comprising water, isopropanol, and methylenechloride in a volume ratio of 1:3-6:1... | 11/24/2009 |
| 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 produced by desilyation of a compoun... | 09/22/2009 |
| 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. ... | 06/09/2009 |
| 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 thiazolineazetidinone derivative (1) is reacted with a sulfonyl halide (2... | 03/24/2009 |
| 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 H, physiologically acceptable ... | 07/08/2008 |
| 7355041 | Intermediates in cefprozil production A salt of PACA with an amidine and its use in the production of cefprozil. ... | 04/08/2008 |
| 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 | 03/04/2008 |
| 7335753 | Bifunctional heterocyclic compounds and methods of making and using same The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using... | 02/26/2008 |
| 7230097 | Process for preparation of 7-[α-Amino (4-hydroxyphenyl) acetamido]-3-substituted-3-cephem-4-carboxylic acid A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cephem-4-carboxylic acid viz. Cefprozil of formula (I) in high purity, substantially free of impurities, which compris... | 06/12/2007 |
| 7196027 | Optical glass suffering little change in refractive index by radiation of light An optical glass wherein an amount of change in refractive index (Δn: difference in refractive index between a state before radiation and a state after radiation) caused by radiation of laser beam at wavelength of 351 nm having average output power of 0.43 W, pulse... | 03/27/2007 |
| 7179794 | Multivalent macrolide antibiotics Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal pro... | 02/20/2007 |
| 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 3-chloromethyl-3-cephem derivative expressed by Formula (2) is prepared. | 01/02/2007 |
| 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, formula (I), wherein R is a carboxyl protecting group; R1 i... | 09/26/2006 |
| 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)... | 08/29/2006 |
| 7091196 | Bifunctional heterocyclic compounds and methods of making and using same The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents,... | 08/15/2006 |
| 7071330 | Process for carbapenem synthesis A process for synthesizing a compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein deprotection is conducted using a prereduced metal catalyst is disclosed. ... | 07/04/2006 |
| 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 hydroxy substituents are converted in vivo to the corresponding drugs... | 09/27/2005 |
| 6947844 | Modulators of ribosomal function and identification thereof The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with p... | 09/20/2005 |
| 6947845 | Method of identifying molecules that bind to the large ribosomal subunit The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with p... | 09/20/2005 |
| 6916801 | 7-Alkylidene-3-substituted-3-cephem-4-carboxylates as β-lactamase inhibitors 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 β... | 07/12/2005 |
| 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) reac... | 06/07/2005 |
| 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 preparing the 3-cephem derivative crystal. ... | 05/03/2005 |
| 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 sulfoxide derived monocyclic azetidinone derivatives with organome... | 01/27/2004 |
| 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), ##STR1## wherein, R1 represents H, trityl, CH3, CRa Rb COOR2 (Ra and R... | 08/26/2003 |
| 6583133 | Propenyl cephalosporin derivatives and process for the manufacture thereof Disclosed are cephalosporin derivatives of the general formula ##STR1## wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfu... | 06/24/2003 |
| 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 (V/SCE) in standard oxidation reduction potential and a comp... | 06/10/2003 |
| 6531465 | Antibacterial cephalosporins A compound of formula ##STR1## wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.... | 03/11/2003 |
| 6495539 | B-lactam-like chaperone inhibitors Compounds of the formula ##STR1## and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubsti... | 12/17/2002 |
| 6458558 | Process for the preparation of ଲ-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 example according to the procedures disclosed in U.S. Pat. No.... | 10/01/2002 |
| 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, ଲ-lactams and vancomycin and the like as the starting materials and chloride linking agents; and the novel compounds prepared by these proc... | 08/20/2002 |
| 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 ଲ-lactam compound represented by the formula (1) with a phosphorus halide compound in the presence of an organic base to give ... | 07/16/2002 |
| 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 3-chloromethylcephem compound of the formula (1) with iodization r... | 07/09/2002 |
| 6414140 | Process for the production of 3-vinyl cephalosporins A process for the production of a 3-vinylcephalosporin compound of formula I ##STR1## wherein R1 and R2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula II ##STR2## with a compound of... | 07/02/2002 |
| 6407091 | ଲ-lactamase inhibiting compounds The invention provides compounds of formula I and IV: ##STR1## wherein R1 -R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ଲ-lactamase enzyme... | 06/18/2002 |
| 6403789 | Method of halogenating hydroxyl group A halogenating agent of the formula (1) and a method of halogenating hydroxyl group ##STR1## wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine ... | 06/11/2002 |
| 6399770 | Preparation of ଲ-hydroxy esters using ammonium borohydrides A process for preparing a ଲ-hydroxyester comprising reducing a ଲ-keto ester in the presence of a salt of ammonium borohydride.... | 06/04/2002 |
| 6369049 | Treatment of mastitis The invention provides new fluorinated cephalosporin antibiotics of Formula I ##STR1## wherein Ra, Rb, Rc, Rd and Re, independently, are H, F or a C1 -C6 alkyl-(Z)n --... | 04/09/2002 |
| 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 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid, by m... | 12/25/2001 |
| 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 vinyl-ACA and a salt of 7-ADCA in a solvent in which the salt of ... | 09/04/2001 |
| 6274730 | Process for producing halogenated ଲ-lactam compound A process for preparing halogenated ଲ-lactam compounds, characterized in that a ଲ-lactam amino compound of the formula (1) is reacted with nitrous acid or nitrite in a slurry dispersion state in water, under acid condition in the presence of h... | 08/14/2001 |
