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6288028 |
BPC peptide salts with organo-protective activity, the process for their preparation and their use in therapy
The present invention discloses new pharmaceutical compositions useful for the treatment of various human and animal diseases. These pharmaceutical compositions contain one or more peptides.
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6077822 |
Drug salts
It has been found that sugar acid salts represent beneficial controlled release forms for basic organic drug compounds. Examples of appropriate salts include mono, di, oligo and polysaccharide...
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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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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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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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5122601 |
Synthesis of 2,3,3',4,4'-penta-o-methylsucrose
A process for manipulating any polyhydroxy compound bearing two or more primary and secondary hydroxyl groups to expose only the primary hydroxyl groups, while blocking all interfering secondary...
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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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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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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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4855287 |
Aminoglycoside compounds, processes for production thereof, and pharamaceutical composition containing the same
An aminoglycoside compound represented by the following formula (I) ##STR1## wherein one of R 1 and R 2 represents a hydrogen atom, and the other represents a methyl group, R 3 represents 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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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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4617293 |
Flavonoid phosphate salts of aminoglycoside antibiotics
Flavonoid phosphates of aminoglycoside antibiotics are useful sparingly soluble salts, e.g., for achieving a depot effect.
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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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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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4337336 |
Derivative of kanamycin A and a process for the preparation thereof
There are provided new compounds, 3',4'-anhydro-4'-epi derivatives of kanamycin A of the formula: ##STR1## wherein R represents an alkyl, aralkyl or aryl group and Y represents an alkylidene,...
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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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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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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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4268664 |
Process for the preparation of 1-N-isoseryl- or 1-N-(L-4-amino-2-hydroxybutyryl)-3',4'-dideoxykanamycin B and intermediates thereof
1-N-Isoseryl- or 1-N-(L-4-amino-2-hydroxybutyryl)-3',4'-dideoxykanamycin B is prepared through a new route starting from 3',4'-dideoxy-3',4'-didehydrokanamycin B, which comprises the steps of...
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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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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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4199570 |
1-N-Hetero containing aminoglycoside derivatives
Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is acylated by a group represented by the formula: ##STR1## wherein R is hydrogen,...
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4181797 |
1-N-(ω-amino-α-hydroxyalkanoyl) derivatives of 4'-deoxy-6'-N-methylkanamycin A
1-N-(ω-Amino-α-hydroxyalkanoyl) derivatives of 4'-deoxy-6'-N-methylkanamycin A are prepared by multi-step processes beginning with 1,3-ureidokanamycin A. The compounds are potent antibacterial...
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4180565 |
1-N-substituted derivatives of 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols
Novel 1-N-aminoalkyl (oxycarbonyl or carboxamido or thiocarboxamido) derivatives of 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, useful as antibacterial agents, are described.
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4178437 |
1-N-Kanamycin derivatives
3-N-formyl derivatives of 3",6'-di-N-acyl-kanamycin A and 2',3",6'-tri-N-acyl-kanamycin B, process for their preparation, and their use as intermediates for production of antibacterially active...
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4170642 |
Derivatives of kanamycin A
Novel derivatives of kanamycin, 1-N-(L-4-amino-2-hydroxy butyryl)-6'-N-alkylkanamycins, have been prepared which possess improved antibacterial activity against gram-positive and gram-negative...
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4169939 |
Processes for the production of 3',4'-dideoxykanamycin B
A clinically valuable antibiotic, 3',4'-dideoxykanamycin B is now produced by a reduced number of consecutive steps in an improved overall yield by new processes starting from kanamycin B via...
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4166114 |
Aminoglycoside antibiotic derivatives and method of use
Novel aminoglycoside antibiotic derivatives and their salts containing a 2-deoxystreptamine moiety of which the 1-amino group is substituted by a group represented by the formula: ##STR1## [wherein...
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4160082 |
Intermediates for aminoglycoside antibiotics
Derivatives of kanamycin A, which have an acyl protecting group on the C-3" and C-6' amino groups, and optionally have a benzyl protecting group on the C-3 amino group, are useful intermediates for...
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4147861 |
1N-(α-Hydroxy-ω-aminoalkanoyl)- 6'N-methyl-3',4'-dideoxykanamycin B and the production thereof
A number of 1N-(α-hydroxy-ω-aminoalkanoyl)-6'N-methyl-3',4'-dideoxykan
amyc in B derivatives have been found to possess excellent antibacterial activity against most kanamycin susceptible and...
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4140849 |
Kanamycin C derivatives
1-N-(L-4-amino-2-hydroxybutyryl) derivatives of kanamycin C, 3'-deoxykanamycin C and 3',4'-dideoxykanamycin C have been prepared which possess high antibacterial activity against a wide variety of...
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4136254 |
Process of selectively blocking amino functions in aminoglycosides using transition metal salts and intermediates used thereby
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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4107435 |
Process for ω-amino-2-hydroxyalkyl derivatives of aminoglycoside antibiotics
1-N-(ω-Amino-2-hydroxyalkyl) derivatives of aminoglycoside antibiotics are prepared by reductive alkylation of the parent antibiotic, or a partially protected derivative thereof, with a...
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4107424 |
1-N-[(S)-α-hydroxy-ω-aminoacyl] derivatives of 3',4'-dideoxykanamycin B and 3'-deoxykanamycin B antibiotics
A new and useful 1-N-[(S)-α-hydroxy-ω-aminoacyl] derivative of an aminoglycosidic antibiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine,...
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4104372 |
1-N-(α-hydroxy-ω-aminoalkanoyl) derivatives of 3'-deoxykanamycin A and the production thereof
1-N-(α-hydroxy-ω-aminoalkanoyl)-derivatives of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A are provided as new and useful compounds which are active against gram-negative and...
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4085208 |
Process for preparing 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and novel 1-epimers and 1-N-alkyl derivatives produced thereby; methods for the use of the 1-epimer derivatives as antibacterial agents and compositions useful therefor
This invention relates to the preparation of novel 1-epi-aminoglycosides, useful as antibacterial agents, and also relates to the process for the preparation of known as well as novel...
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