Hoechst Aktiengesellschaft

Behringwerke Aktiengesellschaft

Roussel Uclaf

Laboratoires Hoechst S/a

Heochst Aktiengesellschaft

Laboratories Hoechst S.a.

Behrinwerke Aktiengesellschaft

Jorg Czech

Klaus Bosslet

Claude Monneret

Dieter Hoffmann

Jean-Claude Florent

Jean-Claude Jacquesy

Michel Koch

Jean-Pierre Gesson

Francedillaois Tillequin

Michel Azoulay

Wilfried Schwab

Cenek Kolar

Manfred Gerken

Rainer Straub

Klaus Boslett

Lucien Nedelec

Rudolf Matusch

Hans-Harald Sedlacek

Jacques Guillaume

Hans H Sedlacek

Mathias Gehrmann

Christian Marchandeau

Roland Hoos

Gerhard Seeman

Matthias Blumrich

Manfred Hunz

Frederic Schmidt

The invention relates to compounds which contain an antigen binding region which is bound to at least one enzyme which is able to metabolize a compound (prodrug) which has little or no cytotoxicity to a cytotoxic compound (drug), where the antigen binding region is composed of a single polypeptide chain. It is advantageous for covalently bonded carbohydrates to be present on the polypeptide chain.

Fusion proteins for prodrug activation

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

Prodrugs, their preparation and use as pharmaceuticals

A preparation having increased in vivo tolerability comprising a glycosyl-Y[--C(.dbd.Y)--X--].sub.p --W(R).sub.n --X--C(.dbd.Y)-active compound, sugar or sugar alcohol and, optionally divalent ions, and a pharmaceutically tolerable carrier.

Preparation having increased in vivo tolerability

The compound of the formula I or II ##STR1## is suitable for the production of a pharmaceutical for the treatment of carcinomatous disorders, where R.sup.1 is (C.sub.3 -C.sub.5)-cycloalkyl, (C.sub.2 -C.sub.6)-alkenyl or (C.sub.2 -C.sub.6)-alkynyl, R.sup.2 is CF.sub.3, OCF.sub.3, SCF.sub.3, OH, NO.sub.2, halogen, benzyl, phenyl, CN or O-phenyl, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, halogen or a hydrogen atom and X is a --CH group or a nitrogen atom.

Use of isoxazole and crotonamide derivatives for the treatment of

Prodrugs their preparation and use as pharmaceuticals

Prodrugs for the therapy of tumors and inflammatory disorders

The use of isoxazole and crotonamide derivatives for the treatment of carcinomatous disorders The compound of the formula I or II ##STR1## is suitable for the production of a pharmaceutical for the treatment of carcinomatous disorders, where R.sup.1 is (C.sub.3 -C.sub.5)-cycloalkyl, (C.sub.2 -C.sub.6)-alkenyl or (C.sub.2 -C.sub.6)-alkynyl, R.sup.2 is CF.sub.3, OCF.sub.3, SCF.sub.3, OH, NO.sub.2, halogen, benzyl, phenyl, CN or O-phenyl, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, halogen or a hydrogen atom and X is a --CH group or a nitrogen atom.

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

Compounds of the formulae I and II ##STR1## are suitable for the suppression of tumor growth and of tumor metastasis.

Inhibitors of .beta.-glucuronidase and their use in the treatment of

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

Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.

Substituted phenols and their use for the treatment of disorders caused

Use of derivatives of 9,10-dihydrophenanthrene for the preparation of an

Growing community of inventors

Marburg, Germany

Jorg Czech