Schering Aktiengesellschaft

Bayer Schering Pharma Ag

Jenapharm Gmbh & Co. Kg

Jenapharm Gmbh

Gerd Schubert

Sven Ring

Walter Elger

Anatoli Kurischko

Lothar Sobek

Birgitt Schneider

Alexander Hillisch

Michael Oettel

Bernd Menzenbach

Kurt Ponsold

Guenter Kaufmann

Vladimir Patchev

Helmut Kasch

Gerd Mueller

Bernd Erhart

Ingo Tornus

Gudrun Bertram

Heidemarie Rohrig

Lothar Sobeck

Dirk Kosemund

Karl-Heinrich Fritzemeier

Ulrich Bothe

Kristof Chwalisz

Christa Hegele-Hartung

Olaf Peters

Sigfrid Schwarz

Gudrun Reddersen

G&uuml;nter Kaufmann

Hiroshi Yamanouchi

Birgit Schneider

Guenther Kaufmann

G Unther Kaufmann

Gunther Kaufmann

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.

Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT)

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.

Progesterone receptor modulators with increased antigonadotropic activity for female birth control and hormone replacement therapy

The present patent application relates to 11&#x3b2;-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein 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.

11&#x3b2;-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones

The invention relates to a process for the production of 4-(17&#x3b1;-methyl-substituted 3-oxoestra-4,9-dien-11&#x3b2;-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which Ris a hydrogen atom, a C-alkyl radical or a CFradical, whereby n is 1, 2 or 3, Ris a C-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC-alkyl group, an SC-alkyl group or an OCHCFgroup, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity 

Method for the production of 4-(17$g(a)-methyl substituted 3-oxoestra-4 9-dien-11$g(b)-yl)benzaldehyd-(1e or 1z)-oximes

The novel glucocorticoid receptor antagonists are 11&#x3b2;-substituted steroid compounds of formula (I): wherein Rdenotes a methyl group, a methoxy group, or an ethoxy group; wherein Rdenotes 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&#x3b2;-substituted steroid compounds.

Glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility

The invention relates to a method for the production of 4-(17&#x3b1; substituted 3-oxoestra-4,9-dien-11&#x3b2;-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R&#x2550;H, Calkyl or a CFgroup; R&#x2550;Calkyl, X=E- or Z-OH; and Y&#x2550;O&#x2014;Calkyl, S&#x2014;Calkyl or O&#x2014;CHCF, where n=1, 2 or 3, which produces the target compounds of formula (I) with high yield and selectivity.

Method for the production of 4-(17&#x3b1;-substituted-3-oxoestra-4,9-dien-11&#x3b2;-yl)benzaldehyde-(1E)-oximes

This invention relates to a process for the production of 4-(17&#x3b1;-alkoxymethyl-17&#x3b2;-substituted-3-oxoestra-4,9-dien-11&#x3b2;-yl)benzaldehyde-(1E)-oxime derivatives of general formula (I) in which R means an amino group, an O&#x2014;C-alkyl- or O-aryl radical, an S&#x2014;C-alkyl- or S-aryl radical, an NH&#x2014;C-alkyl- or NH-aryl radical or an N-di-C-alkyl radical, and Rmeans a hydrogen atom or a C-alkyl radical, which yields the target compounds of formula (I) with high yield and selectivity.

Process for the production of 4-(17&#x3b1;-alkoxymethyl-17&#x3b2;-substituted 3-oxoestra-4,9-dien-11&#x3b2;-yl) benzaldehyde-(1E)-oxime derivatives

Compounds of general formula I as well as their pharmaceutically compatible salts are described, in which R stands for hydrogen, C - to C -alkyl, COR , COOR , COSR or CONHR , in which R is C - to C -alkyl or unsubstituted or substituted aryl and in which R is hydrogen, C - to C -alkyl or unsubstituted or substituted aryl, in which R also stands for hydrogen, C - to C -alkyl or C - to C -acyl, and R stands for a C F group, in which n&equals;1, 2 or 3, or a CH O(CH ) C F group, in which m&equals;0 or 1 and n&equals;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.

17&agr;-fluoroalkyl-11&bgr;-benzaldoxime steroids, process for their production, pharmaceutical preparations that contain these steroids as well as their use for the production of pharmaceutical agents

Use of ER&bgr;-selective ligands for regulating fertility and compounds useful therefor

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.

Methods and compositions for treating diseases due to androgen deficiency with glucocorticoid receptor antagonist compounds and new compounds

Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.

14,15-cyclopropano steroids of the 19-norandrostane series, method for the production thereof and pharmaceutical preparations containing said compounds

S-substitute 11&bgr;-benzaldoxime-estra-4, 9-diene-carbonic acid thiolesters, method for the production thereof and pharmaceutical preparations containing these compounds

The invention relates to 11.beta.-aryl-gona-4,9-dienes of formula I ##STR1## wherein the variables are defined in the specification. The compounds are progesterone synthesis inhibitors and are suitable for inducing labor or an abortion, and for treating endometriosis, dysmenorrhea, and endocrine hormone-dependent tumors.

11 Beta-aryl-gona-4, 9-dien-3-ones

This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## and their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.

11-benzaldoxime-estra-diene derivatives, methods for their production

This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## wherein Z is --CO--CH.sub.3, --CO--O--C.sub.2 H.sub.5, --CO--NH-phenyl, --CO--NH--C.sub.2 H.sub.5, --CO--C.sub.2 H.sub.5, --CH.sub.3, or --CO-phenyl and their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds of the general formula I are produced by esterifying or etherizing a compound of the general formula II ##STR2## The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.

11-benzaldoxime-17.beta.-methoxy-17.alpha.-methoxymethyl-estrasdiene

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Jena, Germany

Gerd Schubert