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6110897 |
Antiinflammatory cell adhesion inhibitors
The invention relates to compounds of formula Ix and Ia: ##STR1## wherein (Ix) comprises the regioisomeric form sLe X and (Ia) comprises the regioisomeric form sLe A , and R 1 is a lipophilic...
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6103884 |
Glycosylated analogs of fusidic acid
Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient...
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6100240 |
Macrolide derivatives
The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , Q, X, Y and Z are as defined herein. The invention also...
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6100391 |
Method for making an alkyl glycoside
A process for preparing alkyl polyglycosides by reacting a fatty alcohol with a saccharide in a glycosidation reaction under acidic condition wherein a water-containing emulsion is drawn off from...
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6084079 |
Process for preparing N-demethyl-N-alkyl erythromycin derivatives
The claimed invention relates to a novel process of preparing N-demethyl-N-alkyl-4"-deoxy erythromycin A and B. The process comprises protecting the 2'-hydroxy or the 2'- and 11-hydroxy of a...
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6077945 |
Process for making alkylpolyglycosides
A novel process for making an alkylpolyglycoside comprises reacting a monosaccharide with an alcohol in the presence of a binary sulfate catalyst under heat. The particular binary sulfate catalyst...
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6077944 |
Secomacrolides from class of erythromycins and process for their preparation
The invention relates to novel secomacrolides from the class of erythromycin A, potential intermediates for preparation of novel macrolide antibiotics general formula ##STR1## and its...
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6075135 |
3,4-di-O,N-Protected-4-amino-2,4,6-trideoxy-2-fluoro-L-manno-pyranosyl halide and a process for its preparation
7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-α-L-mannopyranosyl)-da
unomycinon e or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1##...
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6071886 |
β,β-distributed derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A
The present invention relates to β,β-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I)...
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6069238 |
Spirocyclic C-glycosides
An improved and a new synthetic route for the reparation of spirocyclic C-glycoside compounds having the following general structure are described. ##STR1## Novel derivatives of spirocyclic...
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6063752 |
Acylated carboxyl alkyl saccharides, method for manufacture and use thereof in detergents
Acylated carbohydrates with at least one carboxyalkyl group etherified with the carbohydrate of the following general formula KH(--O--CHR 1 --(CH 2 ) p --(COOH or COO - )) n (--O--CO--R 2 ) m...
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6054435 |
6-O-substituted macrolides having antibacterial activity
The instant invention provides novel macrolide compounds and compositions useful in treating bacterial infections. Also provided are processes for preparing same.
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6051695 |
Process for preparing erythromycin derivative, such as roxithromycin, from the corresponding oxime
A process for preparing an erythromycin derivative, such as roxithromycin, from the corresponding oxime is disclosed. The oxime is reacted with a metal alkoxide and results in improvements over...
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6046171 |
6,11-bridged erythromycin derivatives
Novel 6,11-bridged erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions comprising a therapeutically...
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6043227 |
C11 carbamates of macrolide antibacterials
This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that may be used to treat...
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6043226 |
3,6-ketal and enol ether macrolide antibiotics
This invention relates to compounds of formulas 1 and 2 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein X, X 1 , R 1 , R 2 , R 7 , R 17 and R 19 are as defined...
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6040433 |
Sulfinyl hexose derivatives useful for glycosylation
Hexose derivatives are described which facilitate control over the stereochemistry of the glycosyl bond formed in the course of a solid phase glycosylation reaction. Methods for their use are also...
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6037151 |
Process for the preparation of long-chain alkyl glycosides
The invention provides a process for the preparation of long-chain alkyl glycosides, comprising reacting a glucose-containing reactant and a C 8 -C 18 fatty alcohol in the presence of a...
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6037467 |
Methods for preparing carbohydrate-containing hydrophilic polymers
Carbohydrate-containing polymers which can have an HLB* of from about 10 to about 20 are disclosed. The compounds comprise a hydrophilic polymer portion, a carbohydrate portion comprising from 1 to...
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6034055 |
Glycosyl-amides of 2-aminoacylamino-2-deoxy-sugars
The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the...
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6034069 |
3-'N-modified 6-O-substituted erythromycin ketolide derivatives having antibacterial activity
Novel 3'-N-modified 6-O-substituted erythromycin ketolide compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## compositions...
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6030815 |
Enzymatic synthesis of oligosaccharides
The present invention provides improved methods for the preparation of sialyl galactosides. The methods use sialyl transferase cycle in which the reaction conditions are optimized to provide...
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6027733 |
Method for generating saccharide fragments
A method for depolymerizing polysaccharides containing into saccharide fragments using ozonolysis is described.
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6022965 |
Method for isomerising the 10-methyl radical of erythromycin derivatives
An isomerization method wherein a compound of formula ##STR1## wherein X and y together form a 3-oxo radical, or X is a hydrogen atom and Y is either a radical a ##STR2## where R 2 is OH or...
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6020316 |
Glutaraldehyde modified chemotherapeutic agents and methods of use thereof
Clinical utility of chemotherapy agents is limited by dose-dependent systemic toxicity and emergence of resistant tumor cell lines. The present invention provides derivatives of chemotherapeutic...
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6020472 |
Process for preparing α-D-glucopyranosido-1,6-mannitol and-sorbitol from α-D-glucopyranosido-1,6-fruetose
The sugar alcohols mentioned as title compounds can be prepared from the corresponding sugar in equimolar amounts by catalytic hydrogenation with hydrogen in aqueous solution, the hydrogenation...
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6017753 |
Process for the manufacture of methyl glucoside having low color and low sugar content
A process for decolorizing an aqueous solution of methyl glucoside, the solution containing at least one color component and at least one sugar component, is disclosed. The process comprises the...
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6018033 |
Hydrophilic, hydrophobic, and thermoreversible saccharide gels and forms, and methods for producing same
Polymerizable saccharide monomers are made by the reaction of a saccharose and a (meth)acrylate. Hydrophilic, hydrophobic and thermoreversible gels and foams are formed upon polymerization of the...
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6018034 |
Process for the production of 2-keto-D-glusonic acid
This process for the production of 2-keto-D-gluconic acid starts from D-glucose. D-glucose is catalytically oxidised using molecular oxygen in a one-pot process. The oxidation is performed in the...
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6013779 |
Process for preparation of glycosides of tumor-associated carbohydrate antigens
Glycoconjugate antigens are prepared by preparing a hapten glycoside, especially an alpha glycoside prepared by the Fischer method, with an olefinic aglycon moiety, especially one having a...
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6008333 |
Preparation of glucosaminyl muramic acid derivatives
The present invention provides a method for the preparation of disaccharides, such as glucosaminyl muramic acids peptides and derivatives. The method includes condensing a protected muramic acid...
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6004938 |
Inositolglycans having insulin-like action
The invention relates to inositolglycans having insulin-like action. Specific compounds are provided having the formula I A--Z--R (I) where A is...
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5998594 |
Self-assembling, chromogenic receptors for the recognition of medically important substrates and their method of use
A chromogenic receptor comprises a self-assembled chromogenic compound having at least one intrinsic binding site. The chromogenic compound is characterized by the property of producing a...
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5998595 |
Azidohalogenobenzyl derivatives, sugar compounds and protection of hydroxy groups
Azidohalogenobenzyl derivatives of the formula (I) ##STR1## wherein A is a halogen atom, B is a halogen atom or a hydrogen atom, and X is a group reactive with a hydroxy group, methods of...
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5994520 |
p-Nitrophenyl 2-acetylamino-4-O-(2-amino-2-deoxy-β-D-glucopyranosyl)-2-deoxy-β -D-Glucopyranoside and its salts, and method for producing them
Disclosed is p-nitrophenyl 2-acetylamino-4-O-(2-amino-2-deoxy-β-D-glucopyranosyl)-2-de
oxy-β -D-glucopyranoside of formula (1) and its acid-addition salts. ##STR1## The compound of formula (1) is...
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5986089 |
Process for the preparation of moenomycin A
Moenomycin A can be prepared by fermentation of a moenomycin-producing microorganism and subsequent separation of moenomycin A from the other components of the culture filtrate by chromatography,...
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5981710 |
Therapeutic hemoglobin composition having isotropically increased size
Novel polysaccharide compounds are disclosed for decorating biomolecular surfaces to increase isotropic size and mask antigenicity. The oligosaccharides may be synthesized as repeating disaccharide...
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5977080 |
Sulfated disaccharide inhibitors of selectins, methods for synthesis and therapeutic use
Sulfated disaccharides characterized by the ability to inhibit the binding of selectin to its physiologically-relevant ligand are disclosed. Included are efficient and inexpensive methods for...
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5977327 |
Synthesis of annamycin
An improved method for synthesis of Annamycin is described. The synthesis relies upon a method of selectively deacetylating the Annamycin precursor and purification of the deacetylated product by a...
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5977329 |
Methods of synthesizing GM3
The invention describes an improved method for making monosialoganglioside GM3 and its intermediates. Following reaction of a neuraminic acid donor and a lactose acceptor in the presence of an acid...
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5972898 |
3',3-N-bis-substituted macrolide LHRH antagonists
Disclosed are 3',3'-N-bisdesmethyl-3',3'-N-bis-substituted-6-O-methyl-11-d
eoxy-11,12-cyc lic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone...
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5965719 |
Combinatorial synthesis of carbohydrate libraries
Disclosed are methods for synthesizing very large collections of diverse thiosaccharide derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccharide...
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5962244 |
High-throughput in vitro assays for modulators of peptidyl transferase
High-throughput in vitro assays are provided for identifying modulators of peptidyl transferase. New solid-phase assays, related compositions, apparatus and integrated systems are provided.
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5962659 |
Anthelmintic milbemycins and avermectins
Novel compounds of formula (I): ##STR1## wherein R 1 is hydrogen or optionally protected hydroxy; R 2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R 3 is...
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5958889 |
Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2-fluoro-mannopyranosyl group
7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-α-L-mannopyranosyl)dau
nomycinone or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1##...
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5959088 |
Process for producing erythromycin derivatives
A process for the preparation of fumaric acid salts of compounds of general formula (II) (wherein R 1 is lower alkyl; and R 2 is lower alkyl), is characterized by reacting a compound, which is...
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5955440 |
Macrolide LHRH antagonists
Disclosed are 3'-N-desmethyl-3'-N-substituted-6-O-methyl-11-deoxy-11,12-cy
clic carbamate erythromycin A derivatives which are antagonists of lutenizing hormone-releasing hormone (LHRH). Also...
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5955587 |
Process for preparing alkyl oligoglucosides with a high degree of oligomerization
A process for producing alkyl oligoglucosides having a high degree of polymerization involving: (a) providing a fatty alcohol; (b) providing a glucose component; (c) mixing the fatty alcohol and...
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5945405 |
Crystal form O of clarithromycin
The present invention concerns the novel antiobiotic 6-O-methylerythromycin A form O solvate, a process for its preparation, pharmaceutical compositions comprising this compound and a method of use...
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5945519 |
Process for the preparation of sucrose fatty acid esters
The invention relates to a process for the solvent-free preparation of sucrose fatty acid esters, their mixtures with nonsugar polyol fatty acid esters, and in particular of sucrose glycerides. In...
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