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8110678 |
Antibiotic-bound poly(caprolactone) polymer
This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After...
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7846920 |
Heterosubstituted N-thiolated beta-lactam compounds and methods of use
The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth...
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7601832 |
Process for making aztreonam
A simplified process for the one-pot preparation of aztreonam, using azetidine and TAEM as starting materials, without the intermediary separation of t-butyl-aztreonam is provided.
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7501404 |
Substituted azetidinones
Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd′ are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor X...
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7452991 |
Aztreonam β polymorph with very low residual solvent content
The invention relates to the β polymorph of Aztreonam, which contains less than 2.5% by weight residual solvent and to a process of making said polymorph. In the process of the invention, a ...
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7262293 |
Aztreonam L-lysine and methods for the preparation thereof
The present invention relates to the L-lysine salt of aztreonam and methods for making the L-lysine salt of aztreonam.
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7214364 |
Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections
A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae,...
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7145017 |
Preparation of Aztreonam
The invention relates to a process for the synthesis of Aztreonam. Specifically, the process entails hydrolyzing...
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7026472 |
Methods for preventing and treating cancer using N-thiolated β-lactam compounds and analogs thereof
The subject invention concerns N-thiolated β-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1–8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, al...
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6946458 |
N-thiolated beta-lactams: novel antibacterial agents for methicillin-resistant Staphylococcus aureus
The invention relates generally to novel N-thiolated β-lactams. More specially, the invention relates to the use of these novel antibacterial agents in the treatment or inhibition of ...
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6916803 |
3-(Heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids derivatives as antibacterial agents
The present invention relates to novel Syn isomers of racemates and optical isomers of 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids of the following formula: and their use in treating...
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6617451 |
Enantioselective acylation of cis racemic azetidinones
Cis-β-lactam compounds having structure (II) are described herein which are prepared by enantioselective acylation of the free amine in the presence of Penicillin G Amidase.
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6562962 |
Preparation of substituted isoserine esters using metal alkoxides and β-lactams
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a β-lactam.
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6495568 |
Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents...
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6476015 |
N-thiolated β-lactam antibiotics
Substituted monocyclic β-lactam compounds that are N-1-thiolated monolactams, and which exhibit wide-ranging antibacterial activities, having a single 4-membered azetidinone ring in which: the N-1 ...
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6437119 |
Compounds formed from two or three antibiotics and their processes of preparation
Processes for preparing compounds having two or three antibiotic functionalities using quinolone derivatives, β-lactams and vancomycin and the like as the starting materials and chloride linking ...
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6335324 |
Beta lactam compounds and their use as inhibitors of tryptase
Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents...
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5994340 |
Azetidinone derivatives as β-lactamase inhibitors
New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These...
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5986108 |
4-substitued-3-[1 or 2 amino acid residue]-azetidin-2-one derivatives useful as cysteine proteinase inhibitor
Disclosed herein are azetidin-2-one compounds which exhibit excellent cysteine proteinase inhibitory activity. The compounds are 4-substituted-3-{1 or 2 amino acid residue}-azetidin-2-ones of...
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5888998 |
2-oxo-1-azetidine sulfonic acid derivatives as potent β-lactamase inhibitors
A compound of formula (I) ##STR1## wherein R1 is selected from the group consisting of 2-thienyl, 2-furyl, 2-pyrrolyl, 1-methyl-2-pyrrolyl, 2-amino-1-thiazolyl and 5-isothiazolyl; R2 is selected...
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5760219 |
Pyridyl substituted B-lactam compounds
Pyridyl substituted β-lactam compounds used in preparing taxane derivatives having a 3' pyridyl substituted C13 side chain.
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5670638 |
2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines, and preparation
The azetidines of the present invention have the formula I ##STR1## wherein R1 is hydrogen or bromine, R2 is hydrogen or bromine, wherein at least one of R1 or R2 is bromine, R3 is hydrogen; Me2...
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5318963 |
Heterocyclic hydrazide derivatives of monocyclic β-lactam antibiotics
Antibacterial activity has been found in compounds of the formula.Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: A is a bond or alkylene; Q completes...
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5290929 |
Heteroaryl derivatives of monocyclic beta-lactam antibiotics
Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R1, R2, and M are as defined herein and X is --(CH2)n -- wherein n is 0, 1, 2, 3 or 4 or CR3 R4 wherein R3...
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5254681 |
Process for preparing monobactames and their intermediate product
There is described a process for preparing monobactames of formula: ##STR1## where R=acyl, and their pharmaceutically acceptable salts, starting from ethyl (S)-3-hydroxybutanoate through the...
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5250676 |
Process for the preparation of 3-substituted-2-azetidinones
Provided is a process for diastereoselectively preparing compounds of the formula ##STR1## which includes the step of subjecting a compound of the formula ##STR2## to a salt whose anion is a...
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5250525 |
4-oxo-azetidine-2-sulfonic acids and their salts, processes for the preparation thereof and their use
The invention relates to novel 4-oxo-azetidine-2-sulfonic acids and their salts or the formula I ##STR1## wherein: R1 =hydrogen, halogen, phenylacetamido; R2 =hydrogen, halogen, phenylacetamido,...
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5237059 |
Compounds capable of generating an acid by light irradiation
A compound capable of generating an acid by light irradiation selected from the group consisting of oxime sulfonic acid esters of formula (I): ##STR1## wherein R1 is an alkyl group, each of R2 and...
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5143913 |
[3S(Z)]-3-[[(2-amino-4- thiazolyl)[[2-(hydroxyamino)-2-oxoethoxy]imino]acetyl]amino]-2,2-dimethyl -4-oxo-1-azetidinyl sulfate
The compound [3S(Z)]-3-[[(2-amino-4-thiazolyl)[[2-(hydroxyamino)-2-oxoeth
oxy]imino]acet yl]amino]-2,2-dimethyl-4-oxo-1-azetidinyl sulfate has gram-positive and gram-negative activity and good oral...
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5120729 |
Beta-lactams as antihypercholesterolemics
This application relates to compounds of formula (I), which are useful as antihypercholesterolemic agents. ##STR1##
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5112968 |
Monobactam hydrazide derivatives
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof which possess antibacterial activity. Rs is a substituted hydroxy pyridone of the formulae: ##STR2## wherein Y1...
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5106968 |
Process for bicyclic β-lactams diazo-β-keto-butyrate-intermediates for bicyclic β-lactams
1-Carbapenam-2-one-3-carboxylic acid and 1-carba-3-hydroxy-3-cephem-4-carboxylic acid and esters thereof are provided by a process comprising a rhodium C2 -C10 carboxylate catalyzed cyclization of...
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5057512 |
3-amino-2-oxo-azetidine-1-sulfonic acids
Novel syn isomers of reacemates and optical isomers of 3-amino-2-oxo-azetidine-1-sulfonic acids of the formula ##STR1## wherein R is difluoromethyl, R1 is --(CH2)n --X, n is an integer from 1 to 4,...
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5051502 |
Rhodium catalyzed cyclization process for bicyclic β-lactams
1-Carbapenam-2-one-3-carboxylic acid and 1-carba-3-hydroxy-3-cephem-4-carboxylic acid and esters thereof are provided by a process comprising a rhodium C2 -C10 carboxylate catalyzed cyclization of...
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4992544 |
Monocyclic beta-lactams and process for the preparation thereof
Monocyclic β-lactam compounds represented by the formula ##STR1## wherein R1 is H, NH2, acylamino, C1 -C4 alkyl, etc.; R2 is e.g. C1 -C4 alkyl, hydroxyalkyl, aminoalkyl, carboxy, esterified ...
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4983597 |
Beta-lactams as anticholesterolemic agents
Compounds of formula (I), which are useful as antihypercholesterolemic agents, are disclosed. ##STR1##
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4946838 |
Crystalline anhydrous aztreonam
The crystalline anhydrous form of [3S-[3α(Z), 4β]]-3-[[(2-amino-4-thiazolyl) [(1-carboxy-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-ox
o-1-azetidines ulfonic acid is prepared.
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4939253 |
2-oxoazetidin-1-yloxy acetic acids and analogs
Antibiotic activity is exhibited by β-lactams having an ##STR1## substituent (and analogs thereof) in the 1-position and an acylamino substituent in the 3-position.
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4885275 |
Vancomycin-HCL solutions and the lyophilization thereof
Gel-free concentrated aqueous formulations of vancomycin hydrochloride are provided which comprise the antibiotic salt at a concentration between about 12% and about 50% w/v and a gel-inhibiting...
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4883869 |
Novel beta-lactams containing amino acid substituents
An antimicrobially active compound of the formula ##STR1## and pharmaceutically acceptable salts thereof: wherein R1 is hydrogen, --OCH3, or --NH--CHO; R2 is an acyl group derived from a carboxylic...
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4837318 |
Carbonate substituted monobactams as antibiotics
This invention concerns 2-oxoazetidine analogs (monobactams) having antimicrobial activity, novel processes and novel intermediates useful to make monobactams. The compounds of this invention...
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4826973 |
Delta form of aztreonam and preparation thereof
The crystalline delta(δ)-form of [3S-[3α(Z),-4β]]-3-[[(2-amino-4-thiazolyl) [(1-carboxy-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-ox
o-1-azetidines ulfonic acid is prepared.
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4822790 |
1-Sulfo-2-oxoazetidine derivatives and their production
Disclosed are compounds of the general formula: ##STR1## wherein R1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R4 where R is an...
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4822788 |
1-sulfo-2-oxozetidine derivatives and their product ion
Disclosed are compounds of the general formula: ##STR1## wherein R1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R4 wherein R is an...
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4816582 |
Antimicrobial 2-oxo-1-azetidinesulphonic acids
Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula ##STR1## in which H2 N ##STR2## represents an amino-substituted thiazolyl group, R1 is lower alkyl which is substituted by carbamoyl,...
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4812564 |
Process for preparing 4,4-dialkyl-2-azetidinones utilizing a pyridine (or substituted pyridine) sulfur trioxide complex
Disclosed herein is a process for preparing a compound having the formula ##STR1## which comprises sulfonating a compound having the formula ##STR2## with a complex having the formula ##STR3## and...
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4794108 |
1-carboxymethoxy acetidinones and their production
A 2-azetidinone derivative having a group of the formula ##STR1## wherein R1 and R2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a...
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4775670 |
2-oxo-1-azetidinesulfonic acid salts
Antibacterial activity is exhibited by β-lactams having a sulfonic acid salt substituent in the 1-position and an amino or acylamino substituent in the 3-position.
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4771045 |
2-oxozetidinone derivatives, their production and use
Novel 1-sulfo-2-oxoazetidine derivatives and their production and use.These 1-sulfo-2-oxoazetidine derivatives exhibit excellent antimicrobial activity against gram-positive and gram-negative...
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4751296 |
Process for 4-halomethyl-azetidinones by cyclization of O-acylhydroxamates
A process for 4-halomethylazetidin-2-ones is provided which comprises mixing in an inert solvent a positive halogen reagent in the presence of a weak base with a β,γ-unsaturated O-acylhydroxamate o...
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