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Class 540/228 - Alkyl, hydroxyalkyl, alkoxyalkyl or alkanoyloxyalkyl bonded directly to 3 position


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which have -alkyl, -alkyl-OH, -alkyl-O-alkyl,
No. of patents: 505
Last issue date: 04/08/2008


1                      
NumberTitleIssue Date
7355040Process 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
7339055Process 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
7273935Process 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
7091355Chiral 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
7071329Process 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
7045618Cefpodixime 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
6949641Crystalline 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
6825344Process 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
6683176Intermediates 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
6642377Process 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
6639068Method 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
6610845Thioester 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
6602999Amorphous 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
6552186ଲ-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
6504025Process 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
6489470Process 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
6407091ଲ-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
6388070Thioester 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
6384212Process 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
63035927-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
6255480Aminothiazole 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
6232305Substituted 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
6107481De-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
6100393Process 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
5998611Process 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
5945532Method 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
5922861De-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
5869649Process 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
5831086Production 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
5763617Cephalosporins
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
5760027Use 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
5710146Cephem 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
5654425Method 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
56293067-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
56209687-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
5614623Diastereomers 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
5594133Crystalline 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
55941327-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
5589594Process 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
5583216Methods 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
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