Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Bayer Intellectual Property Gmbh

Sterix Limited

Schring Aktiengesellschaft

Jens Hoffmann

Rosemarie Lichtner

Andreas Reichel

Ulrich Klar

Rolf Bohlmann

Arwed Cleve

Werner Skuballa

Gerhard Siemeister

Wolfgang Schwede

Alexander Hillisch

Bernd Buchmann

Volker Schulze

Nikolaus Heinrich

Karsten Parczyk

Dieter Zopf

Jorg Kroll

Gerhard Sauer

Rolf Jautelat

Karl-Heinrich Fritzemeier

Martin Schneider

Orlin Petrov

Christoph Huwe

Walter Elger

Karl-Heinz Schlemmer

Dieter Lang

Ulf Bömer

Adrian Tersteegen

Martin Haberey

Ludwig Zorn

Andrea Rotgeri

Hartmut Schirok

Andreas Steinmeyer

Christa Hegele-Hartung

Mario Lobell

Olaf Peters

Sigfrid Schwarz

Kirstin Petersen

Olaf Prien

Ulrike Fuhrmann

Holger Hess-Stumpp

Herbert Himmel

Alexander Ernst

Eberhard Unger

Gerd Mueller

Klaus Bosslet

Thomas Michel

Martin Kr&uuml;ger

Tobias Neumann

Ina Scherlitz-Hofmann

Helmut Morack

J&ouml;rg Kroll

Michael Brands

Dominik Mumberg

Matthias Renz

Ying Li-Sommer

Ulf BÖMER

This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.

Substituted tricyclic compounds and methods of use thereof

The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.

Antitumor-active 2-alkoxyestradiol sulfamates

This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R, R, R, R, R, R, R, R, R, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described. 

6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations

Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.

Effector conjugates, methods for their preparation and their pharmaceutical use

This invention relates to anti-androgenic N-[&#x3c9;-[3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]alkyl]-substituted pyrrolidines of general formula I, with a strongly pronounced antiproliferative profile of action; process for the production of the compounds of general formula I, pharmaceutical preparations and the use for the production of pharmaceutical agents.

Anti-androgenic pyrrolidines with tumor-inhibiting action

The invention relates to 17&#x3b1;-alkyl-17&#x3b2;-oxy-estra-1,3,5(10)-trienes that have an antiestrogenic action with general formula I. In addition, the invention also relates to 17-oxo-estra-1,3,5(10)-trienes as well as 17&#x3b2;-hydroxy-estra-1,3,5(10)-trienes as intermediate products in the production of the estratrienes according to the invention. The invention also relates to the use of 17&#x3b1;-alkyl-17&#x3b2;-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17&#x3b1;-alkyl-17&#x3b2;-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.

17&#x3b1;-alkyl-17&#x3b2;-oxy-estratrienes and intermediate products for their production, use of the 17&#x3b1;-alkyl-17&#x3b2;-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations

The present invention relates to methods and uses for preventing or treating hormone-dependent disease, in particular breast cancer, in a mammal by antiprogestins, in particular antiprogestin 11&#x3b2;-(4-acetylphenyl)-17&#x3b2;-hydroxy-17&#x3b1;-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof. The invention further relates to pharmaceutical compositions comprising said antiprogestin.

Use of antiprogestins for prophylaxis and treatment of hormone-dependent diseases

This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R, R, R, R, R, R, R, R, R, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.

This invention relates to new 19-nor-17&#x3b1;-pregna-1,3,5(10)-trien-17&#x3b2;-ols with a 21,16&#x3b1;-lactone ring with a long-chain substituent in 11&#x3b2;-position of general formula II in which Rmeans a straight-chain alkyl radical with 6 to 17 carbon atoms, and Rand Rhave the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

11&#x3b2;-long-chain-substituted 19-nor-17&#x3b1;-pregna-1,3,5(10)-trien-17&#x3b2;-ols with a 21,16&#x3b1;-lactone ring

17&#x3b1;-ALKYL-17&#x3b2;-OXY-ESTRATRIENES AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION, USE OF THE 17&#x3b1;-ALKYL-17&#x3b2;-OXY-ESTRATRIENES FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS AS WELL AS PHARMACEUTICAL PREPARATIONS

This invention relates to new 19-nor-17&#x3b1;-pregna-1,3,5(10)-trien-17&#x3b2;-ols with a 21,16&#x3b1;-lactone ring with a long-chain substituent in 11&#x3b2;-position of general formula IIin which Ris a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

11&#x3b2;-Substituted 19-nor-17-&#x3b1;-pregna-1,3,5(10)-trien-17&#x3b2;-ols with a 21,16&#x3b1;-lactone ring

This invention relates to new piperazine derivatives of general formula I,in which V, W, n, R, R', i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.

Piperazine derivatives that destabilize androgen receptors

This invention describes a 11&bgr;-long-chain-substituted estratriene of general formula (I), in which R is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the terminal position with a perfluoroalkyl group or an optionally substituted arly radical. The compound can have antiestrogenic or tissue-selective estrogenic properties and be suitable for the production of pharmaceutical agents.

11&bgr; LONG-CHAIN SUBSTITUTED ESTRATRIENES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11&bgr; LONG-CHAIN SUBSTITUTED ESTATRIENES, AND THEIR USE FOR PRODUCING MEDICAMENTS

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Muehlenbeck, Germany

Jens Hoffmann