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6858589 |
Methods of and compositions for potentiating the action of agents active on cell wall sites of the susceptible bacteria
The invention provides a method of potentiating the activity of antibacterial agents that act on bacterial cell walls, comprising the step of administering to a subject an antibacterial agent and...
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6642365 |
Anti-(retro)viral conjugates of saccharides and acetamidino or guanidino compounds
Conjugates of a saccharide and an acetamidino- or guanidino-compound, of the formula: wherein A is CH 3 or NH 2 ; X is a linear or branched C 1 -C 8 alkyl chain optionally containing hydroxy,...
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6573060 |
Methods and compositions for targeting DNA metabolic processes using aminoglycoside derivatives
Protein targets for disease intervention through inhibition of nucleic acid metabolism are disclosed. Novel polypeptides for one such target, DNA-dependent ATPase A, and novel polynucleotides...
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6403777 |
Metalloligands for cleaving nucleic acids
Transition metal complexes, referred to hereinafter as “metalloligands”, that catalyze the degradation of DNA and the cleavage of RNA at select sites are provided. In one embodiment, the...
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5814488 |
Semisynthetic 1-N-ethylgentamicin C.sub.1a and method for its preparation
This invention relates to the fields of microbiology and antibiotics. Particularly, it relates to a new mutant strain, a method of its mutation breeding, to a monocomponent Gentamicin C 1a ...
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5696244 |
Method for preparing 1-N-ethylsisomicin
1-N-ethylsisomicin represented by the following structural formula I and pharmaceutically acceptable salts thereof are useful antibacterial agents and can be prepared in high yields by a...
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5686588 |
Amine acid salt compounds and process for the production thereof
A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and...
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5679646 |
Solvent for a sparingly soluble gentamicin salt
A solvent for the salt of gentamicin with 3-p-methoxybenzylidene-6-hydroxy-4 '-methoxyflavanone-6-phosphate which is a mixture of from 6 to 9.75 parts by volume of tetrahydrofuran and from 4 to...
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5604208 |
Antibiotic preparation and use of the same in plants
An antibiotic formulation comprising gentamicin, and optionally tetracycline or oxytetracycline, for use in plants.
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5595977 |
Salts of amino glycosides
The present invention relates to novel amino glycoside salts of sucrose-octa-O-sulfonic acid of formula I: ([sucrose-octa-O-sulfonic acid 8 - ]-[R-(NH 3 + ) x ] y -M z n +) ...
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5539121 |
2-formylmercaptobenzothiazole
There is disclosed a novel formylating agent, 2-formylmercaptobenzothiazole.
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5527781 |
4-O-(aminoglycosyl)- or 4,6-di-O-(aminoglycosyl)-2,5-dideoxy-5,5-difluorostreptamine derivatives
As new compounds are now synthetized 5-deoxy-5,5-difluoro derivatives of aminoglycosidic antibiotics of neamine, kanamycin A-series, kanamycin B-series, gentamicin-series and seldomycin-series....
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5523288 |
Method of treating gram-negative bacterial infection by administration of bactericidal/permeability-increasing (BPI) protein product and antibiotic
The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein...
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5442047 |
Process for preparing isepamicin
An improved process for converting gentamicin B to isepamicin comprising forming 3,6'-di-N-formylgentamicin B, acylating the 1-amino group with an N-protected (S)-isoserine compound and removing...
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5079234 |
Inhibitors of aminoglycoside nephrotoxicity
Certain water-soluble polyanionic organic acid polymers in the weight range of from about 1,000 to 30,000 daltons may be use to inhibit aminoglycoside nephrotoxicity. These polyanionic polymers are...
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4975541 |
Aminoglycosides for controlled drug release
The invention disclosed provides a method for preparing spherical-like encapsulated aminoglycosides which may be administered orally to a patient, and which retain antibacterial properties without...
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4937257 |
Flavanone derivatives
New flavanone derivatives of the formula I ##STR1## wherein Ar 1 and Ar 2 are each phenyl which is unsubstituted or monosubstituted to trisubstituted by OH, alkyl, alkoxy, acylamino, halogen,...
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4877775 |
Polymeric aminosaccharides as antihypercholesterolemic agents
Crosslinked copolymers of monomeric aminosaccharides such as aminoglycosidic antibiotics, e.g. neomycin, or of polymeric aminosaccharides, e.g., chitosan, with dialdehydes are useful...
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4831123 |
Process for preparing netilmicin
A high yielding process for converting 3,2',6'-tri-N-acetyl sisomicin to netilmicin comprising the step of silylating the starting material at the 5,2' positions, and optionally at the 4' position,...
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4816391 |
Amine stabilized aminoglycoside formulations
Novel formulations are provided containing conjugated or unconjugated aminoglycosides, particularly labeled glycosides, a small amount of a polyamine, and additional additives, such as buffer,...
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4645760 |
Activated aminoglycosides and aminoglycoside-aminocyclitols pharmaceutical compositions and method of use
Aminoglycosides and aminoglycoside-aminocyclitols which have been oxygen-radical activated show a broad spectrum of antibacterial activity. The activated compounds are able to penetrate the cell...
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4593089 |
Fluorescent polarization immunoassay utilizing substituted triazinylaminofluorescein aminoglycosides
This disclosure relates to a method and reagents for determining ligands in biological fluids such as serum, plasma, spinal fluid, amnionic fluid and urine. In particular, this disclosure relates...
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4550163 |
Ligand analog-irreversible enzyme inhibitor conjugates
The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding...
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4503046 |
1-Nitro-aminoglycoside derivatives, pharmaceutical compositions containing them and such derivatives for use as pharmaceuticals
Hydroxymethylated aminoglycoside derivatives which are useful, in particular as anti-bacterially active antibiotics.
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4486419 |
5,2',3',4',4",6"-Hexadeoxykanamycin and its 1-N-acylated derivative
5,2',3',4',4",6"-Hexadeoxykanamycin and 1-N-[(S)-4-amino-2-hydroxybutyryl]-5,2',3',4',4",6"-hexadeox
ykanamycin are now provided, which are each a new compound useful as antibacterial agent. The...
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4468512 |
1-N-Acylated and 1-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides
Zinc salts are used to effect the regio-selective acylation and alkylation of the 1-amino group of 4-O-substituted-2-deoxystreptamine-containing aminoglycosides. The 1-N-substituted derivatives of...
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4424344 |
2-N-Acylated and 2-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides and process
Nickel salts are used to effect the regio-selective acylation and alkylation of the 2'-amino group of 4-O-substituted-2-deoxystreptamine containing aminoglycosides. The 2'-N-substituted derivatives...
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4412068 |
Novel compounds of the gentamicin class
5-Deoxygentamicin C 2b and 6'-N-methyl-2-hydroxy- and 6'-N-methyl-5-deoxygentamicins C 2b are prepared, as the major fermentation products, by culturing a nutrient medium containing...
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4404366 |
Beta-galactosyl-umbelliferone-labeled hapten conjugates
An improved specific binding assay method and reagent for determining a ligand in a liquid medium employing, as an enzyme-cleavable substrate label, a residue having the formula: G--D--R wherein...
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4396609 |
Aminocyclitol antibiotics, pharmaceutical compositions and method of using same
Aminocyclitol analogs of gentamicin C 1 , C 2 and C 1a and the corresponding compounds acylated on the 1-, 3- and 2'-amino groups with an ω-amino-α-hydroxy-lower-alkanoyl group are prepared by...
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4393051 |
1-N(Aminopolyhydroxyalkyl)aminoglycoside antibiotics and method of use
The invention relates to pseudotrisaccharides of Formula (I) as defined above, methods for preparing them, compositions containing them and methods for the use of said compounds and compositions.
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4387219 |
2-Hydroxy gentamicin compounds
2-Hydroxygentamicins B, B 1 and A 3 and 2-hydroxy antibiotics JI-20A and JI-20B are prepared as fermentation products by culturing a nutrient medium containing carbohydrates, a source of...
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4380625 |
Process for the preparation of purified aminoglycoside antibiotics
The invention relates to an improved process for the isolation and purification of aminoglycoside antibiotics of Formula (I) as defined herein combining selective lipophilization of the compound of...
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4337335 |
Transition metal salt complexes of polyamino organic compounds
Described are transition metal salt complexes of available neighboring amino and hydroxyl group pairs in polyamino organic compounds, their preparation, and use as intermediates in the preparation...
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4331590 |
β-Galactosyl-umbelliferone-labeled protein and polypeptide conjugates
An improved specific binding assay method and reagent for determining a ligand in a liquid medium employing, as an enzyme-cleavable substrate label, a residue having the formula: G-D-R wherein G...
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4307085 |
Antibiotic AR-5 complex, antibiotics coproduced therewith and derivatives thereof
The Antibiotic AR-5 complex is elaborated by a novel species of the Micromonospora; namely, Micromonospora polytrota. The microorganism also elaborates a number of minor components including the...
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4297485 |
Production of a selectively protected N-acylated derivative of an aminoglycosidic antibiotic
Aminoglycosidic antibiotic comprising a 6-0-(3"-aminoglycosyl)-2-deoxystreptamine optionally having a 4-0-(aminogycosyl) group, such as kanamycins, gentamicins, sisomicin, forms reversible complex...
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4284764 |
Process for the preparation of 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and novel 5-fluoro-5-deoxy and 5-epi-fluoro-5-deoxy derivatives produced thereby
A novel process whereby 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols are reacted with a dialkylaminosulfur trifluoride to produce novel 5-fluoro-5-deoxy and...
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4283528 |
1-N-aminohydroxyacyl derivatives of gentamicin B
1-N-(R-β-amino-α-hydroxypropionyl) gentamicin B, 1-N-(R-γ-amino-α-hydroxybutyryl) gentamicin B, 1-N-(R-δ-amino-α-hydroxyvaleryl) gentamicin B and the corresponding diastereoisomers derived...
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4282350 |
Selective 3"-N-acylation of 1,3"-di-N-unprotected-poly-N-protected-4,6-di-O-(aminoglycosyl)-1,3-diam inocyclitols
This invention describes a novel process whereby 1,3"-di-N-unprotected-poly-N-protected-4,6-di-O-(aminoglycos
yl)-1,3-diamin ocyclitols are selectively acylated at the 3"-N-position with...
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4256876 |
Process for precipitating aminoglycosides
A highly efficient process for the precipitation of an amorphous (non-crystalline) aminoglycoside antibiotic salt during the purification process. Illustratively, there are disclosed processes for...
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4252971 |
Chromatographic process
A chromatographic process for separation of an aminoglycoside antibiotic from impurities. Illustratively, there is disclosed a chromatographic process for separation of the gentamicin complex (C 1...
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4248865 |
Novel aminoglycoside derivatives
Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is modified with a group represented by the formula: ##STR1## (wherein R is...
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4243801 |
6"-Amino derivatives of 4-0-aminoglycosyl-6-0-garosaminyl-1,3-diaminocyclitols
Novel 6"-amino derivatives of 4-0-aminoglycosyl-6-0-garosaminyl-1,3-diaminocyclitols, useful as antibacterial agents, are described.
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4242331 |
Aminoglycosides and method of use
Novel aminoglycoside derivatives of desoxystreptamines of the formula ##STR1## wherein R 1 and R 2 are selected from the group consisting of hydrogen and hydroxyl with at least one of them being...
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4234572 |
1-N-4,6-di-O-(Aminoglycosyl)-1,3-diamino-cyclitol derivatives, processes for their preparation and their use
The invention relates to 1-N-4,6-di-O-(aminoglycosyl)-1,3-diamino-cyclitol derivatives useful as antimicrobial agents. Also included in the invention are methods for preparing said derivatives, the...
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4231945 |
S-5-(Azidomethyl or aminomethyl)-2-lower-alkoxytetrahydrofurans
4-O-(2,3,5-Trideoxy-5-amino-α-D-pentofuranosyl)-6-O-aminogl
ycosyl-1,3 -diaminocyclitols and 1-N-substituted derivatives thereof are described together with methods for their preparation and their...
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4230847 |
Aminoglycoside antibiotic compounds
Selective blocking of some amino groups in a polyamino organic compound having at least one pair of available neighboring hydroxyl and amino groups is effected by first preparing in situ transition...
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4226978 |
β-Galactosyl-umbelliferone-labeled aminoglycoside antibiotics and intermediates in their preparation
β-Galactosyl-umbelliferone labeled aminoglycoside antibiotics, e.g., gentamicin, useful in homogeneous and heterogeneous specific binding assays for such antibiotics in liquid media such as serum....
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4224315 |
Pseudotrisaccharides and their medicinal use
The invention includes, as novel compounds, aminoglycoside antibiotics of the 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols which are 3-N"-substituted. Also included in the invention are...
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