Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Rosemarie Lichtner

Rolf Bohlmann

Yukishige Nishino

Nikolaus Heinrich

Karsten Parczyk

Jorg Kroll

Christa Hegele-Hartung

Jens Hoffmann

Monika Lessl

Ulrich Klar

Gerhard Sauer

Martin Schneider

Karl-Heinrich Fritzemeier

Helmut Hofmeister

Dieter Bittler

Werner Skuballa

Wolfgang Schwede

Bernd Buchmann

Josef Heindl

Hermann Kuenzer

Hermann Kunzer

Ludwig Zorn

Rolf Jautelat

Orlin Petrov

Andreas Reichel

Gerhard Siemeister

Ulrike Fuhrmann

Christa Hegelehartung

Hermann K&uuml;nzer

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

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

Benzocycloheptenes of formula (I), in which R, Rand Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis: 

Benzocycloheptenes, process for their production, pharmaceutical preparations that contain that latter as well as their use for the production of pharmaceutical agents

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 antiestrogens of the general formulain which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

Antiestrogens, process for their production and their pharmaceutical use

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 describes the new benzocycloheptenes of general formula Iin which

Benzocycloheptenes, process for their production, pharmaceutical preparations that contain the latter as well as their use for the production of pharmaceutical agents

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

11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES, PROCESS FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS THAT CONTAIN THESE 11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES AS WELL AS THEIR USE FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS

Antiestrogens, process for their protection and their pharmaceutical use

This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I

7 &agr;-(5-methylaminopentyl)-estratrienes, process for their production, pharmaceutical preparations that contain these 7 &agr;(5-methylaminopentyl)-estratrienes as well as their use for the production of pharmaceutical agents

This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I

7&agr;-(xi-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7&agr;-(xi-aminoalkyl-estratrienes as well as their use for the production of pharmaceutical agents

Growing community of inventors

Berlin, Germany

Rosemarie Lichtner