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5004738 |
1,1-dioxopenicillanoyl oxymethyl D-6-(α-(methyleneamino) phenylacetamido)-penicillanate and a process for the preparation thereof
A pharmaceutical compound which comprises reacting the sodium penicillanic acid 1,1-dioxides with chloroiodomethane in the presence of a solvent to produce chloromethylpenicillanate 1,1-dioxides,...
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4840944 |
Antibacterial beta-lactams, pharmaceuticals thereof and methods of using them
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R 2 ...
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4826833 |
6-(Substituted)methylene-penicillanic and 6-(substituted)hydroxymethylpenicillanic acids and derivatives thereof
Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X 3 is H or Br, R 1 is H, the...
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4626384 |
Penam derivatives
This invention provides a penam derivative represented by the formula ##STR1## wherein R is hydrogen or methyl and R 1 is (hexahydro-1H-azepin-1-yl)methyleneamino, 2-phenylacetamido,...
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4582829 |
Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds
6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymeth
yl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which...
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4530792 |
Process and intermediates for preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate
A process for the preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate which comprises reacting 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillanate or the...
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4503040 |
6-(Aminoacyloxymethyl)penicillanic acid 1,1-dioxides as beta-lactamase inhibitors
Beta-lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof...
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4488994 |
Bis-esters of methanediol with penicillins and penicillanic acid 1,1-dioxide
6'-Acylaminopenicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. The 6'-aminopenicillanoyloxymethyl ester, halomethyl esters, alkylsulfonyloxymethyl...
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4478748 |
Bis-esters of alkanediols
6-Acylaminopenicillanoyloxymethyl esters and 1-(6-acylaminopenicillanoyloxy)ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carbox
ylic acid 1,1-dioxide are useful as...
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4462934 |
Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides
Antibacterial bis-esters of 1,4-cyclohexanedicarboxylic acids and alkane dicarboxylic acids wherein the ester moieties are derived from different alcohols; one alcohol being...
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4457924 |
1,1-Alkanediol dicarboxylate linked antibacterial agents
Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula ##STR1## where A is the residue of certain...
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4452796 |
6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which...
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4444687 |
2β-Chloromethyl-2α-methylpenam-3α-carboxylic acid sulfone methylene diol mixed esters
2β-Chloromethyl-2α-methylpenam-3α-carboxylic acid sulfone and salts and esters thereof were synthesized and found to be potent inhibitors of β-lactamases.
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4434173 |
Bis-esters of 4,5-di(hydroxymethyl)-2-oxo-1,3-dioxole as antibacterial agents
Derivatives of 4,5-di(hydroxymethyl)-2-oxo-1,3-dioxole in which one hydroxy group has been esterified through the carboxy group of ampicillin or amoxicillin, and the other hydroxy group has been...
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4432987 |
Crystalline benzenesulfonate salts of sultamicillin
Novel benzenesulfonic acid addition salts of sultamicillin of the formula ##STR1## and hydrated forms thereof, where X is hydrogen or chloro, especially the crystalline dihydrate salts, having...
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4407751 |
Processes for preparing β-lactams
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R 2 ...
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4393001 |
Intermediates for production of 1,1-dioxopenicillanoyloxymethyl 6-(2-amino-2-phenylacetamido)penicillanates
Compounds of the formula ##STR1## wherein R 1 is H or HO; Y and Z are each Cl, Br or I, or Y is H and Z is Cl, Br or I; Q is N 3 or NHCO 2 CH 2 C 6 H 4 R 4 where R 4 is H, Cl, Br, NO 2 , CH...
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4381263 |
Process for the preparation of penicillanic acid esters
A process for the preparation of chloromethyl esters of penicillanic acids, using iodochloromethane or bromochloromethane and a tetraalkylammonium salt of the penicillanic acid, and their use in...
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4380512 |
2β-Chloromethyl-2α-methylpenam-3α-carboxylic acid sulfone and salts and esters thereof
2β-Chloromethyl-2α-methylpenam-3α-carboxylic acid sulfone and salts and esters thereof were synthesized and found to be potent inhibitors of β-lactamases.
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4377590 |
Derivatives of ampicillin and amoxicillin with beta-lactamase inhibitors
Certain beta-lactamase inhibitors which have a beta-lactam ring as well as a carboxy group have been linked through their carboxy group to either the amino group of ampicillin, the amino group of...
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4376076 |
Bis-esters of 1,1-alkanediols with 6-beta-hydroxymethylpenicillanic acid 1,1-dioxide
Bis-Esters of 1,1-alkanediols with 6-beta(hydroxymethyl)penicillanic acid 1,1-dioxide and 6-betaacylaminopenicillanic acids are useful as antibacterial agents. Intermediates useful for the...
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4375434 |
Process for 6'-amino-penicillanoyloxymethyl penicillanate 1,1-dioxide
6'-Aminopenicillanoyloxymethyl penicillanate 1,1-dioxide is prepared by a two-step procedure. The first step consists of coupling a salt of a 6-(protected amino)penicillanic acid with a halomethyl,...
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4364957 |
Bis-esters of alkanediols as antibacterial agents
6-Acylaminopenicillanoyloxymethyl esters and 1-(6-acylaminopenicillanoyloxy)ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carbox
ylic acid 1,1-dioxide are useful as...
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4359472 |
Bis-hydroxymethyl carbonate bridged antibacterial agents
Antibacterial agents in which a penicillin and a beta-lactamase inhibitor are linked by means of a bis-hydroxymethyl carbonate bridge are of the formula: ##STR1## and pharmaceutically acceptable...
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4356174 |
Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxides and intermediates therefor
Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5R)penam-3-alpha-carboxyl
ic acid 1,1-dioxides and esters thereof, wherein the 2-beta-substituent is cyano, acetyl, alkoxycarbonyl,...
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4351840 |
Antibacterial esters of resorcinol with ampicillin and penicillanic acid 1,1-dioxide derivatives
Bis-esters of resorcinol (1,3-dihydroxybenzene) with ampicillin or amoxicillin and penicillanic acid 1,1-dioxide or 6-beta-(hydroxymethyl)penicillanic acid 1,1-dioxide, having utility as...
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4345071 |
Derivatives of penicillanic acid
Novel intermediates useful for the preparation of substituted 6-β-amidinopenicillanic acids.
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4342772 |
β-Lactam compounds, antibacterial compositions thereof and method of use
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R 2 ...
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4340539 |
Derivatives of 6-bromo penicillanic acid
2β-Chloromethyl-2α-methylpenam-3α-carboxylic acid sulfone and salts and esters thereof were synthesized and found to be potent inhibitors of β-lactamases.
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4325960 |
6-Amidinopenicillanic acid derivatives including the radical of a β-lactamase inhibitor
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a five- to ten-membered azacycloalkyl or azabicycloalkyl residue attached via...
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4323499 |
6-(2-Aryl-2-(1,1-dioxopenicillanoyloxy-methoxycarbonyl)acetamido penicillanic acids
6-[2-(1,1-Dioxopenicillanoyloxymethoxycarbonyl)-2-phenylacet
amido]penicilla nic acid, 6-[2-(1,1-dioxopenicillanoyl=oxymethoxycarbonyl)-2-(3-thieny
l)acetamido]-p enicillanic acid and salts thereof...
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4321196 |
Bis-esters of methanediol with acetonides of ampicillin or amoxicillin and penicillanic acid 1,1-dioxide
Bis-esters of methanediol wherein one hydroxy group of the methanediol is esterified with the carboxy group of hetacillin (or of the p-hydroxy analog of hetacillin) and the other hydroxy group of...
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4309347 |
Penicillanoyloxymethyl penicillanate 1,1,1',1'-tetraoxide
Penicillanoyloxymethyl penicillanate 1,1,1',1'-tetraoxide; a method of treating a bacterial infection in a mammalian subject using penicillanoyloxymethyl penicillanate 1,1,1',1'-tetraoxide and a...
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4181659 |
Bis-penicillanoyloxy-alkanes
The present invention relates to hitherto unknown esters of the below formula I, to salts of the esters of formula I with pharmaceutically acceptable acids, to methods for producing said new...
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4072676 |
Process for preparation of 6-aminopenicillanic acid derivatives
A process for the preparation of 6-aminopenicillanic acid is described which comprises reacting a natural penicillin with a phosphorus halide to protect the carboxyl group of the natural penicillin...
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4067858 |
Acid derivative immobilized cephalosporin carboxylic carrying polymer
There are provided cephalosporin and penicillin carboxylic acid derivatives which comprise polymers carrying a plurality of molecules of said acid, the carboxyl groups of which are blocked by...
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3981865 |
Bis-type penicillins and process for producing the same
Novel bis-type penicillins containing a (thio)acylureido group in the molecule, which are valuable antibacterial compounds for use in mammals including a human being. This disclosure relates to...
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3928595 |
Dipenicillin and dicephalosporin ester antibiotics
Compounds containing penicillanic and cephalosporanic acid moieties, of the general formula ##EQU1## wherein R 1 is --H, --CH 3 or --C 2 H 5 and R 2 is ##EQU2## or ##EQU3## wherein R 3 is an...
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3896110 |
Process for preparation of 6-aminopenicillanic acid
A process for the preparation of 6-aminopenicillanic acid is described which comprises reacting a natural penicillin with a phosphorus halide to protect the carboxyl group of the natural penicillin...
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3887542 |
Polyisocyanate and polyisothiocyanate derivatives of 6-aminopenicillanic acid
Derivatives of polyfunctional compounds such as diisocyanates or diisothiocyanates wherein each functional group is reacted with 6-aminopenicillanic acid possess antibacterial activity.
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3869449 |
New penicillin esters, salts thereof, and methods for their preparation
The invention relates to a new series of penicillin esters and salts thereof, to methods of their preparation and to intermediates in the production of the esters of the general formula ##SPC1## in...
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3862932 |
Thallium (I) Penicillanates
Thallium (I) penicillanates are uniquely adaptable for synthetic production of penicillanic acid anhydrides of mixed and symmetrical derivation. The penicillanic acid anhydrides are valuable as...
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3678037 |
PROCESS FOR PRODUCING α-AMINO PENICILLIN INTERMEDIATES
A method for preparing organosilane derivatives of α-amino penicillins comprising preparation of an amine base salt of 6-aminopenicillanic acid by reacting the latter with a strong amine in an...
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3362959 |
Production of (-)-2-dehydroemetine and intermediates employed therein
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3303185 |
Bis (6-acylpenicillanyl) disulfides
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2880203 |
Process for the preparation of penicillin derivatives
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3838152 |
Title is not available
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3654266 |
Title is not available
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