Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Bayer Schering Pharma Ag

Evestra, Inc.

Jenapharm Gmbh

Other

Bayer Pharma Aktiengesellschaft

Sterix Limited

Shering Ag

Entec Gesellschaft Fuer Endokrinologische Technologie M.b.h.

Walter Elger

Sybille Beier

Olaf Loge

Werner Skuballa

Eckhard Ottow

Rudolf Wiechert

Birgitt Schneider

Helmut Vorbruggen

Gunter Neef

Helmut Vorbrueggen

Alexander Hillisch

Bernd Raduechel

Krzysztof Chwalisz

Henry Laurent

Bernd Raduchel

David A Henderson

Norbert Schwarz

Sven Ring

Sigfrid Schwarz

Gudrun Reddersen

Gerd Schubert

Guenter Neef

Karl Petzoldt

Ekkehard Schillinger

Wolfgang Losert

Guenter Kaufmann

Klaus Nickisch

Karl-Heinrich Fritzemeier

Olaf Peters

Peter Droescher

Karin Schmidt-Gollwitzer

Michael-Harold Town

Eckehard Schillinger

Helmut Hofmeister

Klaus Annen

Arwed Cleve

Michael Oettel

Bernd Menzenbach

Hermann Steinbeck

Ralph Rohde

James R Bull

Bindu Santhamma

Ralf Wyrwa

Stefan Scholz

Krzystof Chwalisz

Christian Gege

Dieter Bittler

Martin Schneider

Marianne Fahnrich

Hareesh Nair

Jerzy Adamski

Hans-Udo Schweikert

Wilko Regenhardt

Gabriele Moeller

Cornelius Scheidges

Michael John Reed

Barry Victor Lloyd Potter

Dirk Kosemund

Wolfgang Schwede

Bernd Buchmann

Karl-Heinz Thierauch

Gerald Kirsch

Ulrich Bothe

Kristof Chwalisz

Peter Esperling

Rolf Krattenmacher

Claus-Steffen Stuerzebecher

Claus-Steffen Sturzebecher

Anatoli Kurischko

Lothar Sobek

Ina Thieme

Uwe Kollenkirchen

Gulzar Ahmed

Margit Richter

Frederick Meece

Dominga Deluca

Gerd M&uuml;ller

G&uuml;nter Kaufmann

Syed Hamiduddin Hasan

Rolf Bohlmann

Gerhard Sauer

Yukishige Nishino

Michael Dittgen

Christa Hegele-Hartung

Jens Hoffmann

Matti Lehtinen

Michael Topert

Gunter Kaufmann

Klaus Schollkopf

Vladimir Patchev

Klaus Schoellkopf

Harald Von Keyserlingk

Paul E Schulze

Holger Zimmermann

Gerd Muller

Ingo Tornus

Wolfgang Roemer

Kunhard Pollow

Thomas Michel

Doris Hubler

Various prodrug compounds having the general structure: Active agent&#x2014;(acid)-(linker)&#x2014;SONRRare described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.

Pro-drug forming compounds

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

Combination of estrogens plus antiprogestins with significant partial agonistic effect as an effective treatment of menopausal symptoms and for prevention of the occurrence of breast cancer

Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SONRRare described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.

Described herein are imidazolyl compounds which either act as pure antiprogestins and methods of using such pure antagonists for gynecological indications and breast cancer.

Imidazolyl progesterone antagonists

This present invention disclosed the use of mesoprogestins, a new class of progesterone receptor modulators (PRMs), for the treatment and prevention of benign hormone dependent gynecological disorders: a) for the treatment of gynecological disorder such as endometriosis, uterine fibroids, postoperative peritoneal adhesions, dysfunctional bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; b) for the prevention of gynecological disorders such as postoperative, peritoneal adhesions, dysfunctional uterine bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; and c) a method of treatment and prevention of the above mentioned disorders in a female, preferably in a human female, in need of treatment or prevention of one or more of these disorders, with an effective amount of a mesoprogestin. 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. The daily dose of mesoprogestin is 0.5 to 100 mg, preferably 5.0 to 50 mg and most preferably 10 to 25 mg. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.

Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders

The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which

2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17&#x3b2;-hydroxy steroid dehydrogenase type 1

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 invention relates to estradiol prodrugs of general formula (I), in which group Z is bonded to the steroid, process for their production, pharmaceutical compositions that contain these compounds, as well as their use for the production of pharmaceutical agents with estrogenic action.

Estradiol prodrugs

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 new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17&#x3b2;-hydroxy steroid dehydrogenase type 1.

2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17&#x3b2;-hydroxy steroid dehydrogenase type 1

The invention relates to &#x394;-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.

[object Object]

This invention describes the new 8&#x3b2;-substituted estratrienes of general formula I in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rand Rhave the meanings that are indicated in the description, and Rmeans a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8&#x3b2;-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.

8&#x3b2;-hydrocarbyl-substituted estratrienes for use as selective estrogens

There is provided a pharmaceutical composition comprising (i) a compound of the formula wherein: X is a hydrocarbyl ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rs is a sulphamate group; (ii) optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant, wherein the compound is present in an amount to provide a dosage of no greater than 200 &#x3bc;g/day.

Composition

Growing community of inventors

Berlin, Germany

Walter Elger