Behringwerke Aktiengesellschaft

Hoechst Aktiengesellschaft

Laboratoires Hoechst S/a

Aventis Pharma Deutschland, Gmbh

Laboratories Hoechst S.a.

Dieter Hoffmann

Klaus Bosslet

Cenek Kolar

Jean-Claude Jacquesy

Claude Monneret

Michel Koch

Jorg Czech

Jean-Pierre Gesson

Jean-Claude Florent

Francedillaois Tillequin

Michel Azoulay

Peter Hermentin

Hans P Kraemer

Manfred Gerken

Michael Paal

Hans G Berscheid

Dirk Bottger

Ernst Raab

Klaus-Dieter Hammer

Hans-Harald Sedlacek

Axel Walch

Gerhard Seemann

Ulrich Stache

Michael Magerstadt

Volker Krone

Joerg Czech

Wolfgang Heinrich

Erich Schuierer

J Org Czech

Albrecht Groner

Roland Hoos

J&ouml;rg Czech

Reiner Straub

Monika Grimm

Seigfried Billenstein

Heinz Brecht

Provided herein are carbohydrate complement-modified bifunctional glycoproteins, and their use in tumor-selective therapy. The bifunctional glycoproteins comprise a first component that specifically binds to a tumor-specific antigen and a second component having enzymatic activity by means of which a non-toxic prodrug is cleaved into a cytotoxic drug. The carbohydrate complement comprises at least one exposed carbohydrate residue selected from the group consisting of mannose, galactose, N-acetylglucosamine, N-acetyllactose, glucose and fucose. The modified carbohydrate complement contributes to increased relative concentration of the glycoproteins at the site of the tumor, and enhanced clearance from the general circulation and non-tumor sites.

Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy

The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.

Glycosyl-etoposide prodrugs, a process for preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates

Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.

Prodrugs, their preparation and use as pharmaceuticals

Prodrugs their preparation and use as pharmaceuticals

Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.

Pro-prodrugs, their production and use

The invention relates to a combination of substances (component I) inducing necrosis in tumors or inflamed tissue with other nontoxic substances ('prodrugs', component II). The enzymes set free by necrotic processes then cleave the nontoxic 'prodrug' into the toxic 'drug', which leads to massive tumor cell death and/or remission of inflammation.

Combination of necrosis-inducing substances with substances which are

The invention relates to a pharmacological composition comprising a polyelectrolyte complex, in particular a polyacid with an average particle size of less than 15 .mu.m and an active agent, among which are active peptides, proteins, enzymes, enzyme inhibitors, antigens, cytostatics, antiinflamatory agents, antibiotics and vaccines. The said composition ensures that the active agent is converted in a non-deleterious manner into a form which can be administered. In addition, the biodistribution, bioavailability and absorption of the pharmaceutical are beneficially affected.

Pharmacological composition containing polyelectrolyte complexes in

Enzymatically clearable prodrugs with reduced Michaelis-Menten constant (Km) are described.

Prodrugs for enzyme mediated activation

Semisynthetic diastereomerically pure N-glycidylanthracyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics. The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, ##STR1## in which R.sup.1 is hydrogen or a hydroxyl group,

Semisynthetic diastereomerically pure N-glycidylanthracyclines, a

The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.7 is an organic substituent which has 2 to 6 carbon atoms and which contains at least one oxygen, nitrogen or sulfur atom or a C--C double bond or a C--C triple bond, it being possible for the double bond also to be a constituent of a heteroaromatic system and for the oxygen, nitrogen or sulfur atom to be a constituent of an open-chain or heterocyclic system, to a process for the preparation thereof and to the use thereof in a pharmaceutical.

Anthracycline derivatives having cytostatic activity

The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, which are optionally in the form of a salt of an inorganic or organic acid, ##STR1## in which the substituents have the following meaning: R.sup.1 is hydrogen or a hydroxyl group,

The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## in which the radicals R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen or a hydroxyl group or a structure of the formula II, and R.sup.3 is a hydroxyl group or a structure of the formula II ##STR2## in which R.sup.4 is an aliphatic or aromatic acyl group, with the proviso that at least one of the radicals R.sup.2 and R.sup.3 has a structure of the formula II, which are optionally in the form of a salt of an inorganic or organic acid, as well as to the process for the preparation thereof, and to the use thereof in pharmaceuticals.

Addition products of water-soluble sulfites or disulfites to maleic acid mono- or diesters of partially fluorinated alkanols or the mono-, di- or triethyleneglycol ethers of these alcohols are useful as surface active agents, especially as wetting agents, as levelling agents in wax emulsions or as dispersants.

Fluorinated sulfosuccinates

An aqueous composition containing (A) an aminoplast precondensate, (B) a polymeric ethylene imine, the monomer of which is a reaction product of toluenediisocyanate a fluorinated alkanol and ethylene imine, which polymer is dispersed by means of a dispersant obtained by reacting said fluorinated alkanol, toluenediisocyanate and a polyethylene glycol, (C) a long-chain alkyl urea and (D) a cross-linking catalyst is useful for rendering a velvety suede-like polyurethane structure oil- and water-repellant.

Aqueous aminoplast coating composition with polymers of fluorinated

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Marburg-Elnhausen, Germany

Dieter Hoffmann