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5683996 |
4-thia-1-aza-bicyclo 4,2,0!oct-2-ene antibiotics
A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and R b --NH--, Ra is an organic radical, Ri and Rj...
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5672711 |
Process for manufacturing cephem derivatives
The objective of this invention is to provide a process of manufacturing cephem derivatives expressed by the following formula (1), wherein the compound (2) is reacted with an condensing agent of...
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5661144 |
Cephem derivatives with 3-substituted bis heterocycles
Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted 3-(imidazo[5,1-b]thiazolium-6-yl)-1-propenyl as a substituent at the 3-position...
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5656623 |
Antimicrobial lactam-quinolones
Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A 1 , A 2 , A 3 , R 1 , R 4 and R 6 generally...
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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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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...
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5648346 |
Antimicrobial carbacephem-quinolones
A substantially flat collapsed plastic bag with an evacuation form unit insert positioned therein as manufactured to serve as a form about which the filled bag will collapse as it is emptied. The...
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5644052 |
Process for the production of cephalosporines and novel intermediates in this process
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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5639877 |
Intermediates in the synthesis of cephalosporins
Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of...
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5637580 |
Antimicrobial penem-quinolones
Compounds of structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzables esters, and hydrates thereof, are effective antiinfective agents, useful in treating and...
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5631367 |
E-rotamers of 3-hydroy cephem derivatives
A process for the manufacture of 7-acylamino-3-hydroxy-cephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with...
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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...
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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...
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5602117 |
Cephalosporin compounds
β-lactam antibiotics of formula (I) or a salt thereof, wherein R 1 is hydrogen, methoxy of formamido; R 2 is an acyl group, in particular that of an antibacterially active cephalosporin; CO 2 R...
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5594131 |
Process for preparing cephalosporin intermediates
The present invention provides a process for the preparation of stable, crystalline cephalosporin intermediates of the formula ##STR1## wherein X is HI, HCl or H 2 SO 4 which are substantially...
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5593984 |
Cephalosporin derivatives
The present invention relates to novel cephalosporin derivatives or pharmaceutically acceptable non-toxic salts thereof useful as antibiotics and to processes for the preparation thereof. ##STR1##...
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5594129 |
Process for the preparation of a cephalosporin antibiotic
The present invention provides an anhydrous acylation process for the preparation of antibiotic, cefepime dihydrochloride hydrate which is substantially free of the anti-isomer and the Δ 2 isomer...
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5594130 |
Preparation of a cephalosporin antibiotic using the syn-isomer of a thiazolyl intermediate
The present invention provides an aqueous acylation process for the preparation of antibiotic, cefepime dihydrochloride hydrate which is substantially free of the anti-isomer and the Δ 2 isomer...
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5583217 |
Fluorogenic and chromogenic β-lactamase substrates
Chromogenic and fluorogenic substrates for β-lactamase, methods for synthesis thereof and methods for detecting β-lactamase in a sample are provided. The substrates are substantially colorless or...
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5583216 |
Methods for the manufacture of cephems
Provided is a process for preparing a cephem compound of the formula: ##STR1## wherein R 3 is hydrogen or methoxy, R 4 is hydrogen or a residue of a nucleophilic compound, R 5 is hydroxyl or a...
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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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5574153 |
Oxime derivatives of cephalosporanic structure
The invention relates to oxime derivatives of cephalosporanic structure, possessing antibacterial activity.
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5574154 |
Process for the preparation of cephalosporanic compounds
The invention relates to a process for the preparation of a compound of the formula I or salts thereof ##STR1## wherein R 1 is hydrogen or trityl, R 2 is hydrogen, trityl, NOCH 3 , NOCH...
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5571909 |
Cephalosporin compounds and processes for preparing thereof
Quaternary ammoniocephalosporins of formula(I) wherein QCH or N, Phydroxylated amine or hydroxylated heterocyclylamines including N-methyl-bis(2-hydroxyethyl)amine,...
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5567813 |
Process for preparing cephalosporin compounds from reactive organic acid derivatives
The present invention provides a process for preparing cephem derivatives having the following general formula (I): ##STR1## in which R 1 represents a carboxy group or a protected carboxy group...
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5559225 |
7-acyl-3-(substituted carbamoyloxy) cephem compound
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 or protected...
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5541176 |
3-thioheteroaryl cephalosporin compounds, compositions and methods of use
Cephalosporin 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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5541177 |
3-aryl or heteroaryl-7-heteroaralkylamido cephalosporin compounds, compositions and methods of use
A compound of the formula I is disclosed. ##STR1## R 13 represents hydrogen, NH 2 , C1-4 alkyl, C1-4 alkylamino or di(C1-4)alkylamino-; Y represents CH or N; Y" represents (a) CR y ' R z '...
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5541175 |
Cephalosporin antibiotics
The present invention relates to a cephalosporin compound represented by the following general formula (I): ##STR1## its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable...
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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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5532354 |
Intermediates for cephem compounds
Compounds of the formula: ##STR1## wherein R is a group of the formula: ##STR2## in which R 3 and R 4 are each lower alkyl or R 3 and R 4 are linked together to form C 3 -C 6 alkylene, A is...
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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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5530116 |
Antimicrobial quinolonyl lactams
Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A 1 , A 2 , A 3 , R 1 , and R 4 generally form...
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5523400 |
Cephalosporin antibiotics
The present invention relates to compounds of the formula ##STR1## wherein R 1 is an acyl group derived from a carboxylic acid, hydrogen, or an amino protecting group; R 2 is hydrogen,...
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5516902 |
Process for preparing cephalosporin compounds
Chromogenic and fluorogenic substrates for β-lactamase, methods for synthesis thereof and methods for detecting β-lactamase in a sample are provided. The substrates are substantially colorless or...
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5498787 |
Method for preparing cephalosporin derivatives
A method for preparing cephalosporm derivatives by reacting cephalosporin alkaline metal salts with organic halide in the presence of quaternary ammonium salts catalyst is disclosed. Δ 3 ➝Δ 2 ...
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5480879 |
Quinolonecarboxylic acids
The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a β-lactam antibiotic, to their salts, to processes for their...
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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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5446037 |
2-[(substituted) methylene]cephalosporin sulfones as antiinflammatory, antidegenerative and antithrombin agents
This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as...
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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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5438052 |
Cephalosporin derivatives
Cephalosporin derivatives have the formula ##STR1## wherein Z 1 , Z 2 , X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and...
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5434147 |
Antimicrobial quinolonyl lactam esters
Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1##...
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5412093 |
3-heterocyclic thiomethyl cephalosporins
Cephalosporin compounds having a 3-position substituent of the formula (I) are described: --CH 2 --S--Q--(Y) n --P wherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring...
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5409918 |
Crystalline cephem acid addition salts and process for their preparation
Crystalline cephem acid addition salts of the general formula II ##STR1## pharmaceutical preparations effective against bacterial infections which contain such cephem derivatives, processes for the...
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5409919 |
Pharmaceutically acceptable salt of 7B-[2-(5-amino-1,2,4-thio-diazol-3-yl)-2(Z)-metho-xyiminoacetamido]-3-[( imidazo[1,2-b]pyridazinium-1-yl)methyl]-3-cephem-4-carboxylate and composition comprising same
A compound of the formula: ##STR1## wherein R 1 is an amino group which may be protected, R 3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S➝O, O or CH 2 , R 4 ...
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5410044 |
Process for preparing Z and E-rotamers of 3-hydroxy cephem derivatives
A process for the manufacture of 7-acylamino-3-hydroxycephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with...
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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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5401842 |
Injectable compositions of a cephalosporin dihydrate salt
The present invention provides physical admixtures of a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime with a pharmaceutically acceptable non-toxic organic...
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