Abstract: The invention relates to 17?-alkyl-17?-oxy-oestratrienes of the formula (I), to processes for their preparation, to the use of the 17?-alkyl-17?-oxy-oestratrienes for preparing pharmaceuticals and to pharmaceutical preparations comprising these compounds.

Abstract: The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. 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.

Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, 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.

Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, 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.

Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, R3a, R3b, R4, R5, R6, R7, 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.

Abstract: 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.

Abstract: This invention relates to anti-androgenic N-[?-[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.

Abstract: The invention relates to a combination comprising (a) a compound selected from the class of prostaglandins and (b) a compound selected from the class of tubulin/microtubule interfering agents and/or (c) a compound selected from the class of cyclooxygenase inhibitors.

Abstract: A head-tracking system and a method for operating a head-tracking system in which a stationary reference point is detected are provided. A detector for detecting the position of a head is calibrated based on the detected stationary reference point. In one example implementation, the detection of the stationary reference point is used to determine the position of the head.

Abstract: The invention relates to 17?-alkyl-17?-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?-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?-alkyl-17?-oxy-estratrienes for the production of pharmaceutical agents as well as pharmaceutical preparations that contain at least one 17?-alkyl-17?-oxy-estratriene as well as at least one pharmaceutically compatible vehicle.

Abstract: The invention provides methods, kits and compounds for determining the potential responsiveness of a subject suffering from a pathological disorder, including non-small cell lung cancer (NSCLC), to treatment with an epothilone by analyzing the gene expression profile and/or certain molecular markers in a sample obtained from said subject. The invention further relates to methods, compounds and uses of said compounds for treating subjects suffering from said pathologic disorder, optionally in combination with other therapeutic agents. Also provided are genes and/or proteins encoded by them whose expression level have been determined to differ between epothilone responders and epothilone non-responders.

Abstract: The present invention relates to the single use of the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, as well as to a combination comprising the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one pure antiestrogen, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer, endometriosis, myeloma, myoma and meningioma.

Abstract: The present invention relates to the combination of the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one none-steroidal antiestrogen and to the use of said combination for the prophylaxis and treatment of BRCA1- or BRCA2-mediated diseases. None-steroidal antiestrogens which can be combined together with the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one are for example is tamoxifen, raloxifene, droloxifen, toremifen, lasofoxifen, arzoxifen, GW5638, EM-800, idoxifen and basedoxifene.

Abstract: The present invention relates to the combination of the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one lutein-hormone-releasing hormone agonist or antagonist and to the use of said combination for the prophylaxis and treatment of BRCA1- or BRCA2-mediated diseases. Lutein-hormone-releasing hormone agonists and antagonists, which can be combined together with the compound 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2 pentafluoroethyl)-estra-4,9-dien-3-one are for example gonadorelin, goserelin, triptorelin, buserelin, nafarelin, deslorelin, histrelin, antide, ramorelix, cetrorelix, antarelix, ORG30850, abarelix, ganirelix and leuprolin.

Abstract: The present invention relates to the combination of the progesterone-receptor antagonist 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one aromatase inhibitor and to the use of said combination for the prophylaxis and treatment of BRCA1- or BRCA2-mediated diseases. Aromatase inhibitors which can be combined together with the compound 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2 pentafluoroethyl)-estra-4,9-dien-3-one are for example aminoglutethimide, fadrozole, anastrozole, letrozole, vorozole, formestane, exemestane and atamestane.

Abstract: 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?-(4-acetylphenyl)-17?-hydroxy-17?-(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.

Abstract: The present invention relates to methods and uses for preventing or treating hormone-dependent diseases, in particular breast cancer, in a mammal, by a combination of an antiprogestin, in particular the antiprogestin 11?-(4-acetylphenyl)-17?-hydroxy-17?-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, and a pure antiestrogen, in particular a compound of general formula I as defined in the specification, for instance 11?-Fluoro-17?-methyl-7?-{5-[methyl(8,8,9,9,9-pentafluorononyl)amino]pentyl}-estra-1,3,5(10)-triene-3,17?-diol. The invention further relates to pharmaceutical compositions comprising said combination.

Abstract: This invention relates to anti-androgenic N-[?-[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.

Abstract: 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.

Abstract: This invention relates to anti-androgenic N-[?-[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.