Hoechst Aktiengesellschaft

Glycorex Ab

Hoeschst Aktiengesellschaft

Hoescht Aktiengesellschaft

Gerhard Kretzschmar

Susanne Grabley

Eckart Bartnik

Peter Hammann

Manfred Schudok

Dirk Seiffge

Wolfgang Schmidt

Alexander Toepfer

Johannes Meiwes

Ulrich Lerch

Michael Ahlers

Horst Kunz

Ulrich Sprengard

Eugen Uhlmann

Anuschirwan Peyman

Axel Walch

Rudolf Schleyerbach

Dieter Duwel

Irvin Winkler

Wilhelm Stahl

Matthias Helsberg

Matthias Mag

Christoph Huls

Brigitte Hoersch

Eckhart Bartnik

Bernward Scholkens

Gerhard Seibert

Klaus Kuhlein

Gerhard Wohner

Rudiger Marquardt

Hartmut Voelskow

Carlo Giani

Gerd Fulling

Brigitte Horsch

Robert Klein

Carlo Unverzagt

Ruediger Marquardt

Andreas Seiffert-Stoeriko

Dick Seiffge

Peter Hamann

Peter Klemm

Gregor Kuznik

The invention relates to novel mimetics of the tetrasaccharides sialyl-Lewis-X and sialyl-Lewis-A having an improved action as inhibitors of cell adhesion, to a process for the preparation of these compounds and to their use as pharmacological active compounds and diagnostic agents.

Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity

A process for preparing polyvalent, physiologically degradable carbohydrate-containing polymers by enzymatic glycosylation reactions is described. The carbohydrate-containing polymers thus prepared may be used for preparing carbohydrate building blocks. The polyvalent carbohydrate-containing polymers of the invention cause no intolerance reactions in vivo, either in their intact form or in the form of degradation products. The carbohydrate side chain of the carbohydrate-containing polymer is assembled by enzymatic glycosylation reactions in homogeneous aqueous buffer systems directly on a biodegradable polymer. The yields of the glycosylation reaction are significantly improved over known processes, and are often quantitative. This also provides a significant increase in the loading densities. A process for preparing free oligosaccharides by means of the carbohydrate-containing polymers of the invention is also described.

Process for preparing polyvalent and physiologically degradable carbohydrate-containing polymers by enzymatic glycosylation reactions and the use thereof for preparing carbohydrate building blocks

The invention relates to novel stabilized oligonucleotides in which at least one non-terminal pyrimidine nucleoside is modified, and to their use as a diagnostic or pharamaceutical for the treatment of viral infections, cancer or diseases in which integrins or cell-cell adhesion receptors are active.

Stabilized oligonucleotides and their use

The invention relates to novel mimetics of the tetrasaccharides sialyl- Lewis-X (SLeX) and sialyl- Lewis-A (SLeA) having an improved action as inhibitors of cell adhesion, specifically a compound of the formula I

Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity prepared therefrom

The invention relates to carbohydrate mimetics, which inhibit the binding of selectin to carbohydrate ligands, of the formula I ##STR1## excluding the compounds sialyl-Lewis-X and -A and their derivatives which, instead of an N-acetyl group, carry the substituents N.sub.3, NH.sub.2 or OH or which, instead of fucose, carry glycerol, and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.

Carbohydrate mimetics having antiadhesive properties

The invention relates to compounds of formula Ix and Ia: ##STR1## wherein (Ix) comprises the regioisomeric form sLe.sup.X and (Ia) comprises the regioisomeric form sLe.sup.A, and R.sup.1 is a lipophilic radical formed from aliphatic or cycloaliphatic units, or a sugar residue which is capped by a .beta.1-O-linked aliphatic or cycloaliphatic unit at the reducing end of the terminal sugar. The compounds of the present invention are useful as inhibitors of increased cell-cell adhesion as well as useful in treating diseases associated with increased cell-cell-adhesion. The compounds of the present invention are also incorporated into pharmaceutical compositions.

Antiinflammatory cell adhesion inhibitors

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 about 20 naturally occurring, identical or different, monosaccharide units, at least one bifunctional spacer coupling the carbohydrate portion to the hydrophilic polymer portion, and a potentiator moiety. The potentiator moiety can be is a crosslinking moiety located within the hydrophilic polymer or a hydrophobic, hydrophilic or ionic moiety. Processes for the preparation and use of such polymers are also disclosed.

Methods for preparing carbohydrate-containing hydrophilic polymers

The invention relates to novel conjugates of tetrasaccharides, preferably of sialyl-Lewis X (SLeX) and sialyl-Lewis A (SLeA), having improved activity as inhibitors of cell adhesion, a process for the preparation of these compounds, and their use as pharmacological active compounds and as diagnostics and pharmaceuticals which contain these conjugates.

Carbohydrate conjugates as inhibitors of cell adhesion

Polymer-conjugated malonic acid derivatives and their use as medicaments

The invention relates to multiply fucosylated dicarboxylic acid derivatives possessing antiadhesive properties, to a process for preparing them, to their use, and to pharmaceuticals and diagnostic agents which are prepared from these derivatives. These multiply fucosylated dicarboxylic acid derivatives are suitable for preparing pharmaceuticals or diagnostic agents for diseases which are associated with an excessive, selectin receptor-mediated cell adhesion in the tissue which is affected by the disease.

Multiply fucosylated dicarboxylic acids possessing antiadhesive

The present invention relates to an improved process for isolating and purifying sugar nucleotides, in particular cytidine monophosphate-activated N-acetylneuraminic acid (CMP-Nana), from biological sources. The sugar nucleotides can be obtained from a sugar nucleotide-containing solution, which has been freed of proteins by alcoholic precipitation, by means of an improved column-chromatographic method which uses silica gel as the stationary phase, and at a purity level which requires only a subsequent desalting step to obtain a substantially pure product.

Process for isolating and purifying nucleotide-activated sugars from

Process for the biotechnological preparation of L-thienylalanines in enantiomerically pure form from 2-hydroxy-3-thienylacrylic acids, and their use. L-Thienylalanines are prepared via the hydantoin or the azlactone route. The starting substances used for the biotransformation are 2-hydroxy-3-thienylacrylic acids. The innovative step consists in the transamination of the enol form of the 2-hydroxy-3-thienylacrylic acids to give L-thienylalanines with the aid of biotransformation. The transaminiation is carried out in the presence of L-aspartic acid or L-glutamic acid as amino donor.

Process for the biotechnological preparation of L-thienylalanines in

Methods for the enzyme catalyzed acylation of primary and secondary alcohols using an enol ester as the acyl donor are described. The acylation occurs in organic media, and is enantioselective for racemic or prochiral alcohols. The reaction is irreversible, and produces unreactive by-products.

Process for enzymatic acylation of alcohols with alkoxyvinyl acetates by

The invention relates to conjugates which consist of mono- or polycarboxylated piperidine or pyrrolidine derivatives and pyranoses, furanoses or polyalcohols linked via a chain or a cyclic system. The carboxyl groups of the piperidine derivatives can either be located directly on the ring or linked to the ring via a short chain. The invention additionally relates to the preparation of these compounds and to their use for the production of pharmaceuticals and diagnostics.

Antiadhesive piperidine-and pyrrolidinecarboxylic acids

A process for the stereospecific synthesis of .beta.-glycosidically linked N-acetylglucosamine derivatives is provided, wherein a protected .alpha.-(N-acetyl-2-amino-2-deoxy)-.beta.-pyranosyl halide is coupled to a glycosyl acceptor using zinc chloride and a 4,4'-dialkoxytriphenylmethyl halide as catalysts.

Process for the specific synthesis of .beta.-glycosidically linked

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Eschborn, Germany

Gerhard Kretzschmar