Jenapharm Gmbh & Co. Kg

Schering Aktiengesellschaft

Jenapharm Gmbh

Sterix Limited

Sigfrid Schwarz

Walter Elger

Birgitt Schneider

Gudrun Reddersen

Michael Oettel

Sven Ring

Bernd Undeutsch

Ina Thieme

Alexander Hillisch

Olaf Peters

Gunter Kaufmann

Lothar Sobek

Wolfgang Roemer

Margit Richter

Thomas Michel

G&uuml;nter Kaufmann

Ina Scherlitz-Hofmann

Dirk Kosemund

Jens Hoffmann

Gerd Schubert

Bernd Menzenbach

Peter Droescher

Matti Lehtinen

Guenter Kaufmann

Klaus Schollkopf

Vladimir Patchev

Eberhard Unger

Bernd Erhart

Doris Hubler

Wolfgang Romer

Jens Schroder

Holger Zimmermann

Gerd Muller

Gerd M&uuml;ller

Rolf-Dieter Hesch

Peter Moellmann

Tobias Neumann

Gerhard Teichmuller

Harald Raethe

Annemarie Hedden

Hans-Joachim Siemann

By Margit Lucas, Heir

Hans-Joachim Siemann, Deceased

By Frank Siemann, Heir

Gisela Weber

Gerhard Teichmueller

Hans-Joachim Palme

Carmen Pfeiffer

Pekka Lähteenmäki

Harry Henkel

Ronald Gebuhr

Christel Siemann

The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein 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.

Antitumor-active 2-alkoxyestradiol sulfamates

The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula &#x2014;SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high 'first path' effect, to be administered orally effectively or significantly improve the oral activity thereof.

Compounds with sulphonamide group and pharmaceutical compositions containing these compounds

The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.

Use of biogenic estrogen sulfamates for hormone replacement therapy

The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formulaR&#x2014;SO&#x2014;O&#x2014; The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives

14, 15-.&agr;.-methylene equilenine derivatives, methods for producing the same and medicaments containing them

C13-substituted estra-1,3,5,(10)-trien-3-yl sulfamates, methods of preparing same, and pharmaceutical compositions containing these compounds

Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.

Unsaturated 14, 15-cyclopropanoandrostanes, method for the production thereof and pharmaceutical preparations containing said 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

Pharmaceutical preparations containing selected steroid compounds and methods of treating estrogen deficiency in the central nervous system (CNS) without influencing other organs or systems are described. These steroids have selective neurotropic estrogen-like transcription action in contrast to the systemically acting natural and synthetic estrogen compounds, such as 17&agr;-estradiol. The selected steroids surprisingly have a selective influence on the transcription estrogen-dependent gene in the CNS and cause changes of physiological parameters as well as CNS-specific transcription effects in the dosages used with no biological effects in reproductive system tissues. They have CNS specific transcription effects at those dosages at which neither 17 &bgr;-estradiol nor 17&agr;-estradiol had any action and the transcription estrogen-dependent gene in the CNS is not influenced by secondarily formed 17&bgr;-estradiol.

Pharmaceutical preparations for treatment of estrogen deficiency in the central nervous system

Estra-1,3,5(10)-trien derivatives, processes for their preparation and

The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.

17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutical

The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel). Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.

Steroid intermediate products and method of their production

Androgens and anabolic agents

The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.

Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for

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Jena, Germany

Sigfrid Schwarz