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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...
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...
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.
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...
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 ...
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.
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,...
7145017 Preparation of Aztreonam  
The invention relates to a process for the synthesis of Aztreonam. Specifically, the process entails hydrolyzing...
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...
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 ...
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...
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.
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.
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...
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 ...
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 ...
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...
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...
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...
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...
5760219 Pyridyl substituted B-lactam compounds  
Pyridyl substituted β-lactam compounds used in preparing taxane derivatives having a 3' pyridyl substituted C13 side chain.
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...
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...
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...
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...
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...
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,...
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...
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...
5120729 Beta-lactams as antihypercholesterolemics  
This application relates to compounds of formula (I), which are useful as antihypercholesterolemic agents. ##STR1##
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...
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...
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,...
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...
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 ...
4983597 Beta-lactams as anticholesterolemic agents  
Compounds of formula (I), which are useful as antihypercholesterolemic agents, are disclosed. ##STR1##
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.
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.
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...
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...
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...
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.
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...
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...
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,...
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...
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...
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.
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...
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...
Matches 1 - 50 out of 108 1 2 3 >