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6833445 |
Guanidinylation, guanidinoglycosides, uses, and methods of assaying their activity
Provided are reagents and methods useful for the synthesis of guanidinylated compounds. Also provided are methods for assaying molecules, including guanidinylated molecules that modulate viral...
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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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5763587 |
Process for the synthesis of amikacin
In the synthesis of amikacin, having the formula: ##STR1## by acylation of a diprotected derivative of kanamycin A with a reactive derivative of L-(-)-4-amino-2-hydroxybutyric acid, the selection...
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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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5656735 |
Process for the preparation of amikacin precursors
Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an...
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5618795 |
Dibekacin derivatives and arbekacin derivatives active against resistant bacteria, and the production thereof
As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin,...
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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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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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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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4985549 |
Process for preparing amikacin
Described is a process for preparing Amikacin wherein 1-N-(L(-)γ-benzyloxycarbonylamino-α-hyroxybutyryl)-3,6'-di
-N-b enzyloxycarbonyl-Kanamycin A suspended in a suitable solvent, is treated with...
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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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4873225 |
1-n-(4-amino-3-fluoro-2-hydroxybutyryl)-kanamycins
As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-2',3'-dideox
ykanamycin A;...
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4845082 |
3'4'-dideoxy-3'-fluorokanamycin B and production thereof
New compound, 3',4'-dideoxy-3'-fluorokanamycin B is now provided, which is useful as antibacterial agent. 3',4'-Dideoxy-3'-fluorokanamycin B is prepared by a process comprising halogenating an...
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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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4661474 |
2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(α-hydroxy-ω-aminoalkanoyl) derivatives thereof
New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(α-hydroxy-ω-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and...
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4656160 |
Aminoglycoside derivatives
Aminoglycoside derivatives and pharmaceutically acceptable salts thereof which are useful as prophylactic and therapeutic agents for infectious diseases caused by pathogenic microorganisms, and a...
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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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4634688 |
3'-fluoro-3'-deoxykanamycin A
A new compound, 3'-fluoro-3'-deoxykanamycin A is now provided, which is active against gram-negative and gram-positive bacteria, including kanamycin-resistant strains of bacteria and is useful as...
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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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4567165 |
N-Methanesulfonic acid derivatives of 3-demethoxyistamycin B
As new semi-synthetic antibiotic derivatives are provided N-methanesulfonic acid derivatives of 3-demethoxyistamycin B which are less toxic than the parent 3-demethoxyistamycin B but retain...
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4547492 |
1-N-(ω-Amino-α-hydroxyalkanoyl-2',3'-dideoxykanamycin A and pharmaceutical composition containing same
1-N-(L-3-amino-2-hydroxypropionyl)-2',-3'-dideoxykanamycin A and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxykanamycin A are now provided which each is a new compound useful as antibacterial...
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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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4455419 |
2'-Modified kanamycins and production thereof
2'-Modified kanamycins, including 2'-deoxykanamycin A, 2'-epikanamycin A and 2'-epikanamycin B, as new compounds are produced starting from kanamycin A by consecutive reaction steps. These new...
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4424343 |
Preparation of 1-N- ω-amino-α-hydroxyalkanoyl!kanamycin polysilylates and products
An improved process for the preparation of 1-N- ω-amino-α-hydroxyalkanoyl!kanamycins comprises acylating a polysilylated kanamycin in a substantially anhydrous organic solvent with an acylating...
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4410516 |
1-N(αHydroxy-ω-aminoalkanoyl) derivatives of 5,3',4'-trideoxy- or 5,3', 4'-trideoxy-6'-N- methyl- or 5, 3', 4',6"-tetradeoxykannamyci B and production thereof
New antibacterial compounds are provided, including a 1-N-(α-hydroxy-ω-aminoalkanoyl)-5,3',4'-trideoxykanamycin B; a 1-N(α-hydroxy-ω-aminoalkanoyl)-5,3',4',641 -tetradeoxykanamycin B; and a...
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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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4359572 |
Process for the production of 3'-deoxykanamycin A and intermediate product
3'-Deoxykanamycin A useful as an antibacterial agent can be produced by a new process comprising reacting a 2',2"-di-O-acylated-3'-O-sulfonylated-tetra-N-protected derivative of kanamycin A with a...
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4357466 |
Processes for the production of 3'-deoxykanamycin A and intermediates
3'-Deoxykanamycin A useful as antibacterial agent is produced from a protected kanamycin A derivative either by a process comprising imidazolylthiocarbonylation of the 3'- and 2"-hydroxyl groups of...
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4357465 |
3',4'-Diedeoxykanamycin B derivatives
New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a...
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4349666 |
Process for the production of kanomycin B derivatives and products obtained therefrom
3'-Deoxykanamycin B, namely tobramycin is produced in an improved yield with a reduced reaction time under moderate reaction conditions, starting from a penta-N-protected 3'-mono-O-alkyl-, aralkyl-...
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4348516 |
Microbiological methylation of aminoglycosyl-aminoglycosides
The microorganisms Micromonospora inyoensis 1550F-1G and M. purpurea strain 1124 each microbiologically convert tobramycin, kanamycin A, kanamycin B and dibekacin to their respective 3"-N-methyl...
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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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4332794 |
6"-Deoxydibekacin, 4",6"-dideoxydibekacin and 1-N-aminoacyl derivatives thereof, and the production of these new compounds
New compounds, 6"-deoxydibekacin, 4", 6"-dideoxydibekacin, 1-N-(L-4-amino-2-hydroxybutyryl)-6"-deoxydibekacin and 1-N-(L-4-amino-2-hydroxybutyryl)-4",6"-dideoxydibekacin are now produced...
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4298727 |
3',4'-Dideoxykanamycin A and 1-N-(S)-α-hydroxy-ω-aminoalkanoyl) derivatives thereof
3',4'-Dideoxy derivative and 1-N-((S)-α-hydroxy-ω-aminoalkanoyl)-3',4'-dideoxy derivative of kanamycin A are now synthetized from kanamycin A and show a wider and/or higher antibacterial activity...
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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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4273923 |
Process for preparing aminoglycoside derivatives
Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety and 4',5'-unsaturation effective in treatment and prevention of infectious diseases caused by gram-positive and...
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4268505 |
Pharmaceutical composition comprising a nitrogen-containing polysaccharide and an antibiotic agent, and a method of treating an infectious disease therewith
A nitrogen-containing polysaccharide, which is obtainable by extracting mycelia of a fungus belonging to the genus Coriolus of Polyporaceae of Basidiomycetes with an aqueous solvent, is effectively...
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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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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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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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4217446 |
ωAmino-2-hydroxyalkyl derivatives of aminoglycoside antibiotics
Certain novel 2-deoxystreptamine aminoglycoside derivatives which have an ω-amino-2-hydroxyalkyl group attached to the 1-amino group of the 2-deoxystreptamine ring, and which are useful as...
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4214074 |
Hydroxyalkyl derivatives of aminoglycoside antibiotics
Certain 2-deoxystreptamine aminoglycoside antibiotics, substituted on the 1-amino group by an alkyl group bearing one or more hydroxy groups, are useful antibacterial agents. The 2-deoxystreptamine...
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4212859 |
2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents, and compositions useful therefor
2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminoc
yclitols having a 6'-amino function exhibit antibacterial activity and are prepared by reaction of the corresponding N-protected (except...
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4209511 |
Aminoglycoside antibiotics and process for production thereof
Aminoglycoside antibiotics biochemically transformed from Kanamycin A or Kanamycin B, which are represented by the formula ##STR1## wherein R 1 represents a hydrogen atom or a methyl group and R 2...
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4208531 |
Synthetic aminoglycosides
Novel pseudotrisaccharides based on 2-deoxy- and 2,5-dideoxystreptamine are described. The compounds of the invention can be considered as modified Kanamycin, Gentamycin and Apramycin compounds. In...
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4199572 |
N-Substituted amino glycoside compounds, their production, and their use as medicaments
The invention relates to new derivatives, substituted on one or more nitrogen atoms, of 4,6-di-(amino-glycosyl)-1,3-diamino-cyclitols, which include the gentamycins, sisomicin, verdamycin,...
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4195170 |
3',4'-Episulfido kanamycin B compounds
New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a...
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4171356 |
2-Unsubstituted derivatives of 4,6-di-o-(aminoglycosyl)-1,3-diaminocyclitois, methods for their use as antibacterial agents and compositions useful therefor
The preparation of novel 2'-unsubstituted derivatives of 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, useful as antibacterial agents, is described.
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