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Class 536/16.8 - Antibiotics


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which have the capacity to inhibit the growth
No. of patents: 371
Last issue date: 05/03/2011


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NumberTitleIssue Date
4136254Process 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 metal salt complexes of available neighboring amino and h...
01/23/1979
4130709Pleuromutilin glycoside derivatives
Pleuromutilin glycoside derivatives which are useful agents against gram-positive and gram-negative bacteria, anaerobic bacteria, and mycoplasma....
12/19/1978
4129720Aminoeverninomicin and derivatives thereof
Everninomicin B, C or D may be converted to amino derivatives by reductive means. The amino derivatives may, subsequently, be converted to novel N-acyl, N-alkyl or N,N-dialkyl derivatives. Alternatively, everninomicins B, C or D may be converted to N-acyl...
12/12/1978
4129721A-40104 antibiotics and process for production thereof
A-40104 antibiotic complex, comprising active factors A, B, C, and D, produced by submerged aerobic fermentation of Clitopilus pseudo-pinsitus. Individual factors, A, B, and C have been isolated. A-40104 factor C is the known antibiotic pleuromutilin. A-4...
12/12/1978
4117221Aminoacyl derivatives of aminoglycoside antibiotics
Disclosed herein are novel 1-N-X-aminoglycoside anti-bacterial agents produced from antibiotics elaborated by species of the genus Micromonospora wherein X is a member selected from the group consisting of S-3-amino-2-hydroxypropionyl and S-4-amino-2-hydr...
09/26/1978
4107435Process 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 6-dihydroxymethyltetrahydro-1, 3-oxazin-2-one or 5-dihydroxymet...
08/15/1978
4085208Process 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 1-N-substituted aminoglycoside antibacterial agents....
04/18/1978
4078139Process for deoxygenating secondary alcohols
The process for removing a secondary hydroxyl group from an organic compound having at least one secondary hydroxyl group and having any amino groups protected, comprises the reaction of a reactive ester of said secondary hydroxyl group selected from the ...
03/07/1978
4071560Diaminoalditols useful in the preparation of antibacterial antibiotics AM31଱, AM31ଲ, and AM31γ
This disclosure describes a novel class of antibiotics, three of which have been designated AM31଱, AM31ଲ, and AM31γ and are produced in a microbiological fermentation under controlled conditions using a new strain of Streptoverticillium netro...
01/31/1978
40667521-Desamino-1-hydroxy and 1-desamino-1-epi-hydroxy-4,6-di-o-(aminoglycosyl)-1,3-diaminocyclitols; 1-desamino-1-oxo-4,6-di-o-(aminoglycosyl)-1,3-diaminocyclitols, intermediates and use as antibacterial agents
This invention relates to the preparation of novel 1-desamino-1-oxo-aminoglycosides and their use as intermediates in the preparation of novel 1-desamino-1-hydroxy and 1-desamino-1-epi-hydroxyaminoglycoside antibacterial agents....
01/03/1978
4065615Deoxyaminoglycoside antibiotic derivatives
A new deoxystreptamine-containing aminoglycoside antibiotic derivative in which all the amino groups other than the amino group at the 1-position of the deoxystreptamine moiety are formylated is obtained in a high yield by treating a deoxystreptamine-cont...
12/27/1977
4064341Nogalamycinic acid and derivatives thereof
Novel antibiotic, nogalamycinic acid (U-51,205) prepared by the chemical modification of the known antibiotic nogalamycin. Nogalamycinic acid is active against various microorganisms, for example, Mycobacterium avium, Bacillus subtilis, Lactobacillus case...
12/20/1977
4064012Process for producing antibacterial antibiotics AM31଱, AM31ଲ, and AM31γ with Streptoverticillium netropsis
This disclosure describes a novel class of antibiotics, three of which have been designated AM31଱, AM31ଲ, and AM31γ and are produced in a microbiological fermentation under controlled conditions using a new strain of Streptoverticillium netro...
12/20/1977
4064340Nogamycin and process of preparation
Novel antibiotic, nogamycin (U-51,204) prepared chemically from nogalamycinic acid. Nogamycin is active against various microorganisms, for example, Mycobacterium avium, Bacillus subtilis, Lactobacillus casei, Staphylococcus aureus, and Sarcina lutea. Thu...
12/20/1977
4064339Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions
There are disclosed pharmaceutically-active aminoglycosides comprising 4-O-(2',6'-diamino 2',6'-didesoxy ଱,D-glucopyrannosyl) 6-O-(3"-amino 3",4",6"-tridesoxy ଱, D-xylohexopyrannosyl) 2-desoxy streptamine of the formula: ##STR1## and...
12/20/1977
4062947Di-N-alkylaminoglycosides, methods for their manufacture and novel intermediates useful therein, method for their use as antibacterial agents and pharmaceutical compositions useful therefor
1,2'-di-N-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and 1,6'-di-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and their acid addition salts are valuable as antibacterial agents. Also disclosed are 2'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diamin...
12/13/1977
40535915-Deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents and compositions useful therefor
5-Deoxy-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, useful antibacterial agents, are prepared by the reaction of the corresponding 5-O-thioformyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol having all amino functions and all primary and secondary hydr...
10/11/1977
4048430Mercaptopseudotrisaccharides
Novel pseudodisaccharide compounds which are related to neamine are prepared. These compounds have a mercapto group or a derivative thereof at position 3 or 4 of the glucose moiety of neamine. The compounds have antibacterial activity and have utility as ...
09/13/1977
40441236'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their use as antibacterial agents and compositions useful therefor
Described are 6'-N-alkyl derivatives of antibacterially active 4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a primary carbinamine at C-5' of which a preferred group are 6'-N-alkyl derivatives having 2 to 4 carbon atoms of 4-O-aminoglycosyl-6-O-gar...
08/23/1977
4029548Process for producing antibiotics U-50,147 and U-51,738
Microbiological process for preparing the known antibiotics, antibiotic A-396-1 also known as U-50,147 and L-dihydrophenylalanine also known as U-51,748, by use of the new microorganism Streptomyces lemensis, NRRL 8170 using controlled fermentation condit...
06/14/1977
4029882Selective acylation of the C-1 amino group of aminoglycoside antibiotics
A novel process for preparing novel 1-N-acyl-4,6-di-(aminoglycosyl)aminocyclitols is disclosed. The compounds are useful as antibacterial agents....
06/14/1977
4027016Everninomicin antibacterial derivatives, electrochemical method for their manufacture, method for their use as antibacterial agents, and pharmaceutical compositions useful therefor
Everninomicin derivatives devoid of a nitro group and having antibacterial activity are prepared by electrochemically reducing the corresponding everninomicin having a nitro function or salts thereof in an aprotic anhydrous solvent in the absence of carbo...
05/31/1977
4024251Antibiotic FR-02A and therapeutic compositions thereof
This invention relates to a new antibiotic agent which also possesses growth promoting activity. The antibiotic is isolated from the fermentation broth of Streptomyces lactamdurans by solvent extraction and designated Efrotomycin....
05/17/1977
4020269Epiminodeaminodeoxyaminoglycoside antibiotics and intermediates
Deoxyaminoglycoside antibiotics are prepared in a high yield from phosphorylated aminoglycosides by reacting a phosphorylated aminoglycoside (a) with a silylating agent, or (b) successively with (i) a silylating or acylating agent and (ii) a halogenating ...
04/26/1977
4012576Antibiotic complex Bu 2183
A novel aminoglycoside antibiotic complex designated herein as Bu-2183 is produced by fermentation of Pseudomonas sp. strain D946-B83, A.T.C.C. 31086. Complex Bu-2183 is known to consist of at least five components, said components being herein designated...
03/15/1977
4011391Validamycin C, D, E and F antibiotics
Novel antibiotics, termed validamycins C, D, E and F, and acid salts thereof, are prepared by cultivating a validamycin-producing strain of microorganism of the genus Streptomyces, and optionally converting the free base to its acid salt....
03/08/1977
4009328Aminoglycoside 66-40C, method for its manufacture, method for its use as an intermediate in the preparation of known antibiotics and novel antibacterials
Aminoglycoside 66-40C, a minor product produced by the fermentation of Micromonospora inyoensis, is separated from said fermentation mixture, and is used as an intermediate in preparing the known antibiotic, sisomicin, as well as 6' -N-alkylsisomicins hav...
02/22/1977
40082181-N-((S)-଱-substituted-ω-aminoacyl)-neamine or -ribostamycin and the production thereof
An 1-N-((S)-଱-substituted-ω-aminoacyl)-neamine or -ribostamycin of the formula: ##STR1## wherein R is a hydrogen atom or ଲ-D-ribofuranosyl group of the formula ##STR2## and R3 is hydroxyl, amino-NH2 or acy...
02/15/1977
40083621-N-((S)-଱-substituted-ω-aminoacyl)-neamine or -ribostamycin and the production thereof
An 1-N-((S)-଱-substituted-ω-aminoacyl)-neamine or -ribostamycin of the formula ##STR1## wherein R is a hydrogen atom or ଲ-D-ribofuranosyl group of the formula ##STR2## and R3 is hydroxyl, amino-NH2 or acyl...
02/15/1977
4006225Method of using reduction products of everninomicins as antibacterial agents and pharmaceutical compositions useful therefor
Everninomicin antibiotics having a nitro function, e.g. everninomicin B, everninomicin C, and everninomicin D, upon treatment with aluminum amalgam in aqueous alkanol are converted to a mixture of at least two reduction products having antibacterial activ...
02/01/1977
40027421-N-alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, methods for their use as antibacterial agents, and compositions useful therefor
1-N-Alkyl-4,6-di-(aminoglycosyl)-1,3-diaminocyclitols, valuable as antibacterial agents, are prepared by treating an acid addition salt of a 4,6-di-(aminoglycosyl)-1,3-diamonocyclitol antibacterial agent in an inert solvent, preferably a protic solvent co...
01/11/1977
4001209Antibiotic G-52 and method for the production thereof
A novel actinomycete herein designated Micromonospora zionensis elaborates a product having substantial antibacterial activity, said activity being due to sisomicin and the novel antibiotic substance coproduced therewith. The disclosure sets forth methods...
01/04/1977
40012081-N-[(S)-଱-hydroxy-ω-aminoacyl]
A new and useful 1-N-[(S)-଱-hydroxy-ω-aminoacyl]derivative of an aminoglycosidic antiobiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine, 3',4'-dideoxyribostamycin or 3', 4'-dideoxykanamycin B is now ...
01/04/1977
40002625-Epi-amino and 5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines 1-N-alkyl-5-epi-amino and 1-N-alkyl-5-epi-azido-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines
5-Epi-azido- and 5-epi-amino-4,6-di-O-(aminoglycosyl)-2,5-dideoxystreptamines and 1-N-alkyl derivatives thereof, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,6-di...
12/28/1976
40002615-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, methods for their manufacture and intermediates useful therein, methods for their use as antibacterial agents and compositions useful therefor
5-Epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines and 1-N-alkyl-5-epi-4,6-di-O-(aminoglycosyl)-2-deoxystreptamines, valuable as antibacterial agents, are prepared from the corresponding 5-O-hydrocarbonsulfonyl (or substituted hydrocarbonsulfonyl)-4,...
12/28/1976
3998708Electrochemical process for preparing hydroxylaminoeverninomicins
Hydroxylaminoeverninomicins having antibacterial activity are prepared by electrochemically reducing the corresponding everninomicin having a nitro function or the corresponding nitrosoeverninomicin in an aqueous miscible organic solvent under an inert at...
12/21/1976
3997403Antibiotic G-418 and the production thereof
A novel actinomycete herein designated Micromonospora rhodorangea elaborates a product having substantial antibacterial activity, said activity being due primarily to a novel antibiotic herein designated Antibiotic G-418. The disclosure sets forth methods...
12/14/1976
3997524Process for the manufacture of 6'-N-alkyl derivatives of sisomicin and verdamicin; novel intermediates useful therein, and novel 6'-N-alkylverdamicins prepared thereby
1,3,2',3"-tetra-N-acyl-5'-deaminomethyl-5'-formylsisomicin and 1,3,2',3"-tetra-N-acyl-5'-de-଱-aminoethyl-5'-acetylverdamicin are prepared from the 1,3,2',3"-tetra-N-acyl-6'-N-(2,4-dinitrophenyl) derivatives of sisomicin and verdamicin, respectively,...
12/14/1976
3996205Aminoglycoside antibiotics and intermediates
6-0- AND 3'-0-D-glycosyl analogs of neamine, 6-0- and 3'-0-D-glycosyl ortho esters of neamine, novel aminoglycoside antibiotics, and novel intermediates are prepared by a new chemical process. The compounds have utility as antibacterial agents or as inter...
12/07/1976
3988316Antibiotics sisomicin and verdamicin I and complex containing same
A novel composition having antibiotic activity is produced by fermentation of the new species of microorganism, Micromonospora grisea. The antibiotic complex is composed of four components, Verdamicin I, sisomicin, Antibiotic G-418, and gentamicin A, of w...
10/26/1976
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