Abstract: The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred herein.

Abstract: The invention relates to new compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.

Abstract: The present patent application relates to 11?-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of formula I bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.

Abstract: This invention relates to 17?-substituted 4-(3-oxoestra-4,9-dien-11?-yl)-benzoic acids and derivatives thereof, a process for the production of these compounds, the use of the compounds for the production of pharmaceutical agents as well as pharmaceutical compositions that contain these compounds.

Abstract: The invention relates to a process for the production of 4-(17?-methyl-substituted 3-oxoestra-4,9-dien-11?-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1 radical, whereby n is 1, 2 or 3, R2 is a C1-4-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC1-6-alkyl group, an SC1-6-alkyl group or an OCH2CnF2+1 group, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity

Abstract: The present invention relates to carbazoles/fluorenes, to processes for their preparation and to their use for preparing pharmaceutical agents for the treatment of disorders connected to the EP2 receptor.

Abstract: The novel glucocorticoid receptor antagonists are 11?-substituted steroid compounds of formula (I): wherein R1 denotes a methyl group, a methoxy group, or an ethoxy group; wherein R2 denotes a tert.-butyl group, a 1-hydroxy-1-methylethyl group, a 1-methoxy-1-methylethyl group, an ethyl isocrotonate group, or a substituted phenyl group. The method of treating an individual suffering from glucocorticoid-mediated hypogonadism, sexual dysfunctions, and/or infertility includes administering a daily dosage consisting of an effective amount of one of these 11?-substituted steroid compounds.

Abstract: The present patent application relates to 11?-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of formula I bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.

Abstract: The invention relates to a method for the production of 4-(17? substituted 3-oxoestra-4,9-dien-11?-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R1?H, C1-6 alkyl or a CnF2n+1 group; R2?C1-4 alkyl, X=E- or Z-OH; and Y?O—C1-6 alkyl, S—C1-6 alkyl or O—CH2CnF2n+1, where n=1, 2 or 3, which produces the target compounds of formula (I) with high yield and selectivity.

Abstract: This invention relates to a process for the production of 4-(17?-alkoxymethyl-17?-substituted-3-oxoestra-4,9-dien-11?-yl)benzaldehyde-(1E)-oxime derivatives of general formula (I) in which R means an amino group, an O—C1-7-alkyl- or O-aryl radical, an S—C1-7-alkyl- or S-aryl radical, an NH—C1-7-alkyl- or NH-aryl radical or an N-di-C1-7-alkyl radical, and R1 means a hydrogen atom or a C1-6-alkyl radical, which yields the target compounds of formula (I) with high yield and selectivity.

Abstract: The invention relates to new compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.

Abstract: The present invention discloses the use of ER?-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER?-agonists are used for treatment of infertility and ER?-antagonists for contraception.

Abstract: Compounds of general formula I as well as their pharmaceutically compatible salts are described, in which R1 stands for hydrogen, C1- to C6-alkyl, COR4, COOR4, COSR4 or CONHR5, in which R4 is C1- to C6-alkyl or unsubstituted or substituted aryl and in which R5 is hydrogen, C1- to C6-alkyl or unsubstituted or substituted aryl, in which R2 also stands for hydrogen, C1- to C6-alkyl or C1- to C6-acyl, and R3 stands for a CnF2n+1 group, in which n=1, 2 or 3, or a CH2O(CH2)mCnF2n+1 group, in which m=0 or 1 and n=1, 2 or 3. In addition, a process for the production of the compounds with general formula I is indicated. The compounds can be used for the production of pharmaceutical agents.

Abstract: The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.

Abstract: The present invention relates to novel glucocorticoid receptor antagonists for producing a drug for the prophylaxis and therapy of glucocorticoid-mediated hypogonadism, sexual dysfunctions and/or infertility.

Abstract: Compounds of general formula I as well as their pharmaceutically compatible salts are described, in which R1 stands for hydrogen, C1- to C6-alkyl, COR4, COOR4, COSR4 or CONHR5, in which R4 is C1- to C6-alkyl or unsubstituted or substituted aryl and in which R5 is hydrogen, C1- to C6-alkyl or unsubstituted or substituted aryl, in which R2 also stands for hydrogen, C1- to C6-alkyl or C1- to C6-acyl, and R3 stands for a CnF2n+1 group, in which n=1, 2 or 3, or a CH2O(CH2)mCnF2n+1 group, in which m=0 or 1 and n=1, 2 or 3. In addition, a process for the production of the compounds with general formula I is indicated. The compounds can be used for the production of pharmaceutical agents.

Abstract: The invention relates to a process for the production of 4-(17&agr;-methyl-substituted 3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1 radical, whereby n is 1, 2 or 3, R2 is a C1-4-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC1-6-alkyl group, an SC1-6-alkyl group or an OCH2CnF2+1 group, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity.

Abstract: This invention relates to a process for the production of 4-(17&agr;-alkoxymethyl-17&bgr;-substituted-3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyde-(1E)-oxime derivatives of general formula (I) 1

Abstract: The invention relates to a method for the production of 4-(17&agr; substituted 3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R1═H, C1-6 alkyl or a CnF2n+1 group; R2═C1-4 alkyl, X=E- or Z-OH; and Y═O—C1-6 alkyl, S—C1-6 alkyl or O—CH2CnF2n+1, where n=1, 2 or 3, which produces the target compounds of formula (I) with high yield and selectivity.

Abstract: The method of treating or preventing a disease in a human male or a male animal caused by a decreased production of androgens, such as testosterone, in the human male or male animal includes administering an effective amount of a glucocorticoid receptor antagonist to the human male or the male animal in order to increase production of the androgens. These diseases include male sexual dysfunction, infertility and hypogonadism. Novel androgen receptor antagonist compounds and methods of synthesis are also described.