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| Number | Title | Issue Date |
| 7355040 | Process for the preparation of cephalosporin compounds and synthetic intermediates 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, R... | 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 |
| 7273935 | Process for the preparation of 3-methylcepham derivatives A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I). wherein R2 and R3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido, sub... | 09/25/2007 |
| 7091355 | Chiral scaffolds and their preparation A crystalline salt according to formula (1): or the opposite enantiomer thereof, wherein X+ is a cation. Such salts are useful in preparing chiral scaffolds, in particular of formulae (a)–(d) ... | 08/15/2006 |
| 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 R2 are as defined in the spec... | 07/04/2006 |
| 7045618 | Cefpodixime proxetil The present invention relates to an improved and cost effective process for the industrial manufacture of cefpodoxime proxetil. More specifically, the present invention relates to the preparation of cefpodoxime proxetil of high purity and yield. The process comprise... | 05/16/2006 |
| 6949641 | Crystalline β-lactam intermediate The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspend... | 09/27/2005 |
| 6825344 | Process for the preparation of cephalosporin compounds and synthetic intermediates There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclising a compound of Formula (III): wherein R1... | 11/30/2004 |
| 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 |
| 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: ##STR1## wherein the ring A means the basic antibiotic; R10 means a protected func... | 11/04/2003 |
| 6639068 | Method of preparing highly pure cefpodoxime proxetil Highly pure cefpodoxime proxetil can be prepared by a simple process comprising the step of reacting a cefpodoxime salt with 1-iodoethylisopropylcarbonate in an organic solvent in the presence of a crown ether.... | 10/28/2003 |
| 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 |
| 6602999 | Amorphous form of cefpodoxime proxetil A novel process for the production of an improved amorphous form of cefpodoxime proxetil [(6R-[6,7ଲ(Z))]-7-{E(2-Amino-4-thiazolyl)(methoxyimino)acetyl] amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2. 0]oct-2-ene-2-carboxylic acid-... | 08/05/2003 |
| 6552186 | ଲ-lactam production ##STR1## 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 formula I is ceftrixone, cefotaxime; e.g., in the form ... | 04/22/2003 |
| 6504025 | Process for the preparation of vinyl-pyrrolidinone cephalosporin derivatives Disclosed is a process for the preparation of vinyl-pyrrolidinone cephalosporine derivatives of formula ##STR1## Also disclosed are intermediate compounds of formulas ##STR2## wherein R1 and R2 are as defined herein.... | 01/07/2003 |
| 6489470 | Process for the preparation of cefpodoxime proxetil diastereoisomers A process for increasing the diastereoisomeric ratio (B/A+B), wherein B is the more apolar and A is the more polar of two diastereoisomers, of a mixture of diastereoisomers of a compound of formula ##STR1## the diastereoisomers being with respect to the c... | 12/03/2002 |
| 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 |
| 6388070 | Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), ##STR1## wherein, R1 represents H, trityl, CH3, or CRa Rb COOR3, in which Ra ... | 05/14/2002 |
| 6384212 | Process for preparing cephalosporin antibiotics using new thiazole compound The present invention relates to a new, simple, and easy process for preparing cephalosporin antibiotics of the following formula (I), such as ceftazidime and cefixime. The process comprises acylating a 7-amino cephalosporanic acid derivative of the follo... | 05/07/2002 |
| 6303592 | 7-alkylidene cephalosporanic acid derivatives and methods of using the same Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of ଲ-lactamase enzymes.... | 10/16/2001 |
| 6255480 | Aminothiazole derivatives useful in the preparation of ଲ-lactam antibiotics Aminothiazole derivatives having the carboxyl activated by means of thioesters, said derivatives being condensable with ଲ-lactam nuclei to yield ଲ-lactam antibiotics... | 07/03/2001 |
| 6232305 | Substituted amino bicyclic-ଲ-lactam penam and cepham derivatives as cysteine protease inhibitors The present invention provides substituted amino bicyclic-ଲ-lactam penam derivatives and substituted amino bicyclic-ଲ-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of... | 05/15/2001 |
| 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 corresponding 4-methoxybenzyl ester of a 3-substituted (6R,... | 08/22/2000 |
| 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 molecular weights over 10,000 Dalton and preferably over 2000 Dalt... | 08/08/2000 |
| 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 R1 means either group represented by the foll... | 12/07/1999 |
| 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 well as to use thereof in the manufacture of... | 08/31/1999 |
| 5922861 | De-esterification process An efficient process for de-esterification has been provided for by application of special tetrahalogenides. By applying this process a new compound, viz. cefesone, and especially the E-isomer thereof, has been prepared.... | 07/13/1999 |
| 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 2-mercapto-5-methyl-1,3,4-thiadiazolyl-(Z)-2-(2-aminothiazol-4-yl)... | 02/09/1999 |
| 5831086 | Production of cefotaxime and new sodium salts A process for the production of cefotaxime in acetone/water and its use in the production of a sodium salt of cefotaxime and a crystalline sodium salt of cefotaxime in the form of rounded agglomerates and in the form of needles.... | 11/03/1998 |
| 5763617 | Cephalosporins A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherei... | 06/09/1998 |
| 5760027 | Use of 7-alkylidene cephalosporins to inhibit elastase activity The present invention relates to the use of 7-alkylidene derivatives of cephalosporin esters, such as sulfides, sulfoxides, and sulfones, as inhibitors of human leukocyte elastase. These materials are therefore useful as anti-inflammatory and anti-degener... | 06/02/1998 |
| 5710146 | Cephem derivatives and processes for their manufacture Cephem derivatives of the general formula ##STR1## in which the R2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.... | 01/20/1998 |
| 5654425 | Method for the acylation of the 7-amino group of the cephalosporanic ring A method for the acylation of the 7-amino group of the cephalosporanic ring, according to which a 7-ACA amino thiazolyl protected adduct is prepared by acylating said amino group by an aminothiazolyl acetic acid whose amino group has been protected by a p... | 08/05/1997 |
| 5629306 | 7-alkylidene cephalosporanic acid derivatives and methods of using the same Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of ଲ-lactamase enzymes.... | 05/13/1997 |
| 5620968 | 7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above comp... | 04/15/1997 |
| 5614623 | Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate and processes for their preparation Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxyme thyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and ... | 03/25/1997 |
| 5594133 | Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropinonyloxy)-ethyl-3-cephem-4-carboxylate Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate The invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carbox... | 01/14/1997 |
| 5594132 | 7-acylamino-3-substituted cephalosporanic acid derivatives A compound of the formula: ##STR1## in which R2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl, R3 is carboxy or a protected carboxy group, A5 is lower alkylene which may have a group of the formul... | 01/14/1997 |
| 5589594 | Process for the preparation of cephem prodrug esters The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R1 is C1 -C5 -alkanoyloxy-C1 -C3 -alkyl or C1 -C5 -alkoxyca... | 12/31/1996 |
| 5583216 | Methods for the manufacture of cephems Provided is a process for preparing a cephem compound of the formula: ##STR1## wherein R3 is hydrogen or methoxy, R4 is hydrogen or a residue of a nucleophilic compound, R5 is hydroxyl or a protected hydroxyl, and R | 12/10/1996 |