Abstract: The invention refers to 8?-substituted estra-1,3,5(10)-triene derivatives of general formula I their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.

Abstract: The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z=O, H2, ?NOR or ?NNHSO2R, where R=H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R4=H, halogen, methyl or trifluoromethyl, R6 and/or R7 can be ?- or ?-positioned and independently=branched- or straight-chain 1-4 or 3-4 alkyl, or R6=H and R7=a- or ?-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R6 and R7=H, or R6 and R7 together=a- or ?-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.

Abstract: The present invention relates to arylmethylen substituted N-acyl-Y-aminoalcohols of the general formula I in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH modulators and can be used for example for fertility regulation in men or in women.

Abstract: The present invention relates to 2,3,4,9-tetrahydro-1H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: The present invention relates to acyltryptophanols of the general formula I, in which Q, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: The present invention relates to acyltryptophanols of the general formula I, in which Q, V, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: This invention describes the new 9?-substituted estratrienes of general formula I in which R3, R7, R7?, R13, R16 as well as R17 and R17? have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

Abstract: The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which Z is an oxygen atom, two hydrogen atoms, a group ?NOR or ?NNHSO2R, where R is a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom or a trifluoromethyl group, and R6 and/or R7 may have a or a configuration, and R6 and R7 are independently of one another a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 4 or 3 to 4 carbon atoms or a straight- or branched-chain alkenyl group having 2 to 4 or 3 to 4 carbon atoms or a saturated cycloalkyl group having 3 to 5 carbon atoms or together are a methylene group or a double bond. The novel compounds have progestational and antimineralocorticoid activity.

Abstract: The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

Abstract: This invention describes the new 9?-substituted estratrienes of general formula I in which R3, R7, R7?, R13, R16 as well as R17 and R17? have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

Abstract: The invention relates to new quinoline, isoquinoline and phthalazine derivatives as antagonists of the gonadotropin-releasing hormone.

Abstract: This invention relates to 8?-vinyl-11?-(?-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ER?-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.

Abstract: A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction. The meanings of R7, R10, R11, R13, R17 and R17? as well as of the grouping U—V—W—X—Y-Z are indicated in the claims.

Abstract: The invention relates to a pharmaceutical combined preparation of LHRH analogues and anti-oestrogens having tissue-selective oestrogen activity and also to its use for the treatment of gynaecological disorders, especially for the treatment of endometrioses and myomas.

Abstract: A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction.

Abstract: The present patent application relates to acyltryptophanols of the general formula I, in which Q, X, Y, W, R1, R2, R3, R4, R5, R8 have the meanings stated in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

Abstract: This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ?NOR or ?NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in ?- or ?-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an ?- or ?-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an ?- or ?-position methylene group or an additional bond.

Abstract: This invention provides new tetrahydrocarbazole derivatives that act as ligands for G-protein-coupled receptors (GPCR), especially as antagonists of the gonadotropin-releasing hormone (GnRH). A pharmaceutical composition that contains these new tetrahydrocarbazole derivatives as well as a process for the production of the new tetrahydrocarbazole derivatives are also provided. Moreover, this invention relates to the administration of tetrahydrocarbazole derivatives for treating pathologic conditions that are mediated by GPCR, especially for inhibiting GnRH, in mammals, especially humans, who require such an administration, as well as the use of tetrahydrocarbazole derivatives for the production of a pharmaceutical agent for treating GPCR-mediated pathologic conditions, especially for inhibiting GnRH.

Abstract: A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction. The meanings of R7, R10, R11, R13, R17 and R17? as well as of the grouping U-V-W-X-Y-Z are indicated in the claims.