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5880111 |
Therapeutic derivations of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by...
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5874571 |
Process for the recovery of cephalexin
The disclosed process is for the recovery of cephalexin from a mixture containing cephalexin and 7-aminodesacetoxy cephalosporanic acid (7-ADCA), wherein a mixture of cephalexin and 7-ADCA, with a...
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5854227 |
Therapeutic derivatives of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are...
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5847116 |
Process for the preparation of intermediates useful in the synthesis of cephalosporins
A process is described for preparing 3-exomethylene cephalosporanic acid derivatives for use in the synthesis of cephalosporin antibiotics such as ceftibuten. The process comprises electrochemical...
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5824801 |
Process for sterospecific synthesis of keto-enol tautomeric mixture of p nitrobenzyl (1R, 6R, 7R)-7-phenoxyacetamido-3-oxo-3-cepham-4-(R/S)-carboxylate-1-oxide and p-nitrobenzyl (1R, 6R, 7R)-7-phenoxyacteamido-3-hydroxy-3-cephem-4-carboxylate-1-oxide
A process for the stereospecific synthesis of keto-enol tautomeric mixture of p-nitrobenzyl (1R,6R,7R)-7-phenoxyacetamido-3-oxo-3-cepham-4-(R/S)-carboxy
late-1-oxide and p-nitrobenzyl...
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5801242 |
Process for making quinolonyl lactam antimicrobials and novel intermediate compounds
The present invention provides processes for making compounds of the structure (Q--L 1 )--L--(L 2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L 1 ,...
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5777104 |
Cephem derivatives as anti-metastatic agents
The present invention relates to the use of known cephem derivatives of the formula: ##STR1## wherein n is zero, one or two; R 1 is hydrogen or an organic radical, R 2 represents halo or an...
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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...
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5750683 |
Process for the stereospecific synthesis of keto-enol tautomeric mixture of p-nitrobenzyl (1R,6R,7R)-7-phenoxyactamido-3-oxo-cepham-4-(R/S)-carboxylate-1-oxide and p-nitrobenzyl (1R,6R,7R)-7-phenoxyacetamido-3-hydroxy-3-cephem-4-carboxylate-1-oxide
A process for the stereospecific synthesis of keto-enol tautomeric mixture of p-nitrobenzyl(1R,6R,7R)-7-phenoxyacetamido-3-oxo-3-cepham-4-
(R/S)-carboxyl ate-1-oxide and...
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5741902 |
7-acyl-3-(substituted carbamoyloxy) cephem compounds and process for their preparation
A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH or --N group; R 1 denotes a hydroxyl, lower alkoxyl,...
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5693790 |
Crystalline form of a cephalosporin antibiotic
The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and...
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5686604 |
Cephalosporines
The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of...
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5677443 |
Bioavailable crystalline form of cefuroxime axetil
A bioavailable crystalline form of cefuroxime axetil, obtained by treating known crystalline or amorphous cefuroxime axetil with water or with a water-miscible organic solvent or with a mixture...
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5663330 |
Process for the selective sulfoxide reduction of 3-hydroxy cephem and 3-methylene cepham compounds
Process for selectively reducing cephalosporin sulfoxides of 3-hydroxy cephem and 3-methylene cepham compounds by treatment with a chlorinating agent in the presence of a solvent and a base, which...
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5656754 |
Process for preparing cephem compounds
The present invention provides a process for preparing a cephem compound represented by the general formula (3) characterized in that an allenyl-β-lactam compound represented by the general...
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5656755 |
Process for preparation on 3-substituted cephem compound
An object of the invention is to provide a process for preparing a 3-substituted cephem compound from an allenyl-β-lactam compound which can be easily produced from an inexpensive penicillin...
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5631366 |
Process for making 3-formylcephem derivatives
The present invention is concerned with a novel process for the making of a compound of formula I ##STR1## by oxidizing the corresponding 3-hydroxymethyl-cephem derivative with an inorganic...
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5597914 |
Process for the production of cephalosporins
A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate.
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5580865 |
2,2-disubstituted cephem sulphones
The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R 1 is hydrogen,...
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5580976 |
Preparation of β-lactam compounds, and intermediates therefor
A process for preparing a β-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R 1 is hydrogen,...
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5578721 |
Process for preparation of 3-exomethylene cepham sulfoxide esters
A process for the manufacture of 3-exomethylene cepham sulfoxide ester of the formula ##STR1## wherein R is hydrogen, C 1 -C 3 alkyl, halomethyl, phenyl, substituted phenyl cyanomethyl, phenoxy,...
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5574153 |
Oxime derivatives of cephalosporanic structure
The invention relates to oxime derivatives of cephalosporanic structure, possessing antibacterial activity.
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5565445 |
3-thioheteroaryl 1-carba-1-dethiacephalosporin compounds, compositions and methods of use
1-Carba-1-dethiacephalosporin compounds of the formula I ##STR1## are disclosed. The compounds are useful against MRSA/MRCNS. Compositions and methods of use are also included.
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5563264 |
Preparation of βlactam compounds
A process for preparing a β-lactam compound of the formula (I): ##STR1## which comprises cyclization, in the presence of a catalyst, of an azetidinone derivative of the formula: ##STR2## is...
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5539102 |
Production method for sulfamide
The method for producing a sulfamide according to the present invention includes the step of reacting an alcohol and an oxycarbonylsulfamide compound in the presence of a trivalent phosphorus...
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5536830 |
Process for P-nitrobenzyl ester cleavage in cephalosporin
A process for converting cephalosporin p-nitrobenzyl ester (Formula I) to the corresponding cephalosporin free acid (Formula II) comprising treating the cephalosporin p-nitrobenzyl ester with a...
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5532353 |
Process for the preparation of halogenated β-lactam compounds
There is described the preparation of halogenated β-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting...
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5470972 |
Process for preparing examethylenecephem compounds
The object of the invention is to provide a β-lactam compound and a 2-substituted methyl-3-cephem compound, both of which are of value as intermediates for the synthesis of cephem antibiotics. The...
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5453504 |
Bicyclic β-lactams intermediates having a new amino protecting group
A method for preparing a new class of protected amino intermediates is provided which utilizes reaction of an imido protected primary amine with a secondary amine. The intermediates thus provided...
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5451675 |
Process for the preparatuon of 3-alkoxymethyl cephalosporin derivatives
A compound of formula (I): ##STR1## or a salt thereof, is prepared by reacting 7-aminocephalosporanic acid or a salt thereof, with a solution comprising a compound of formula ROSO 3 H in a...
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5442058 |
Conversion of penicillins and cephalosporins to 1-(S)-sulfoxides
The present application discloses a process for the conversion of penicillin-1-(R)-sulfoxide(s) and/or cephalosporin-1-(R)-sulfoxides in solution, to their corresponding 1-(S)-sulfoxides comprising...
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5439904 |
2-spiro(2'-spirocycloalkyl)cyclopropyl cephalosporin sulfones as antiinflammatory and antigenerative agents
2-spiro (2'-spirocycloalkyl) cyclopropyl cephalosporin sulfone compounds, methods of treating patients for elastase inhibition, and processes for preparing such compounds.
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5434259 |
Process for isolation of cefaclor after enzymatic acylation
Provided is a process for isolating cefaclor from an acylation reaction mixture by adding anthraquinone-1,5-disulfonic acid to the mixture. The acid highly selectively precipitates with cefaclor so...
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5412094 |
Bicyclic beta-lactam/paraben complexes
The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH 3 , Z is O; is 0-5; Y is phenyl or 1,4-cyclohexadien-1-yl; R 1 and R 2 are...
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5410042 |
Process for the cleavage of cephalosporin prodrug esters to 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid
The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their...
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5405955 |
Method for producing azetidinone and cephalosporin derivatives
New compounds are disclosed having the general formulas (1) and (2): ##STR1## Also described is a process for preparing the compounds of formulas (1) and (2). Further described is a process for...
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5401841 |
Process for the production of cephalosporines
The invention relates to a new, economical and simple process for the production of 3-vinylcephalosporin compounds of formula ##STR1## wherein R 1 and R 2 may be the same or different and denote...
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5397780 |
Pyrroloazepine derivative
This invention provides a pyrroloazepine derivative represented by the following formula (I): ##STR1## where the substituents are defined in the specification. The pyrroloazepine derivatives...
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5352782 |
Process for preparing crystalline β-lactam monohydrate
The invention provides a process for the preparation of the crystalline monohydrate form of the compound of the formula (I) ##STR1## which comprises the step of mixing a form of loracarbef, other...
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5350845 |
Process for preparing 7-substituted-amino-3-hydroxy-3-cephem-4-protected carboxy-sulfoxide esters
A process for the conversion of a 4-chlorosulfonyl azetidinone (a) to a 3-hydroxy-3-cephem-sulfoxide ester (d) by subjecting an intermediate comprising a tin containing Lewis acid-type...
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5329001 |
Substantially anhydrous crystalline cefadroxil and method for producing it
The invention relates to a substantially anhydrous crystalline cefadroxil having a water content between about 0.8% and 3.9%. Such cefadroxil is obtained slurrying a cefadroxil solvate of...
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5304641 |
Process for the synthesis of exomethylenecephams
The present invention relates to a process for the preparation of exomethylene cephams, which are useful intermediates in the production of many useful β-lactam antibiotics. More particularly...
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5302711 |
Ester cleavage process for use with β-lactams
The present invention provides a novel ester cleavage process for use with β-lactams. The process is useful because of mild conditions necessary to complete the reaction, such conditions being...
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5281703 |
Process for making antimicrobial quinolonyl lactams
The present invention provides methods of making compounds of the structure [Q-L 1 ]-L-[L 2 -B[ wherein (I) Q is a quinolone moiety; (II) B is a beta-lactam moiety; (III) L, L 1 , and...
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5266691 |
Processes for making cephems from allenylazetidinone derivatives
This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In...
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5254680 |
Process for the preparation of 7 alpha-alkoxycephem derivatives
There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R 1 is an organic residue, R 2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group,...
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5252731 |
Cephalosporin intermediates
Intermediates of the following formula are disclosed: ##STR1## wherein R 1 is aryl; R 2 is carboxy or protected carboxy; ZCHCH 2 , CH 2 --X 2 , --CH 2 --P + (R 7 ) 3 .X 3 or CH P(R...
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5229509 |
Process for the preparation of 3-chloro-cefem compounds
The process comprises a series of stages essentially comprising the protection of the functional groups of the side chain of Ampicillin, esterification of the acid group, oxidation to sulphoxide,...
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5221739 |
Acetylation of 3-hydroxymethyl cephalosporins
Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.
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5206360 |
Intermediates for cyclobutenedione substituted (1-carba)cephalosporin compounds
A compound of formula I ##STR1## wherein X is sulfur or CH 2 ; R 1 is hydrogen, hydroxy, amino, C 1 -6 alkyl, C 2 -6 alkenyl, C 2 -6 alkynyl, phenyl optionally substituted with one to three C...
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