Solvay Pharmaceuticals, Gmbh

Abbott Products Gmbh

Solvay Pharmaceuticals, B.v.

Universitaet Des Saarlandes

Josef Messinger

Heinrich-Hubert Thole

Pasi Koskimies

Michael Weske

Bettina Husen

Dieter Ziegler

Dagmar Hoeltje

Lechoslaw Turski

Axel Pahl

Yvan Fischer

Yasmin Karimi-Nejad

Hrissanthi Ikonomidou

Constanze Hoefer

Katrin Michaelis

Uwe Schoen

Lila Pirkkala

Mikko Unkila

Nina Johansson

Bartholomeus Johannes Van Steen

Jochen Antel

Reinhard Brueckner

Rolf Wolfgang Hartmann

Harald Waldeck

Michael Wurl

Dirk Thormaehlen

Mark Stuart Johnson

Tiina Annamaria Salminen

Martin Frotscher

Pekka Lehtovuori

Olli Taneli Pentikaeinen

Leena Hirvelae

Tommi Nyroenen

Pauli Saarenketo

Sandrine Oberwinkler

Frank Gundlach

Ernst Sinner

Erika Ziegler

Gyula Schneider

Johannes Bernardus Everardus Hulshof

Jerzy Adamski

Lila Kallio Nee Pirkkala

Johanna Kiviniemi

Johannes Bernardus Hulshof

Lila Kallio

The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases

Substituted steroid compounds which represent selective inhibitors of 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17&#x3b2;-estradiol concentration.

17-beta HSD1 and STS inhibitors

Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17&#x3b2;-hydroxysteroid dehydrogenase (17&#x3b2;-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds. 

Substituted estratriene derivatives as 17BETA HSD inhibitors

3,15-substituted estrone compounds which act as inhibitors of 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17&#x3b2;-estradiol concentration, as well as the general use of selective 17&#x3b2;-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.

17&#x3b2;-hydroxysteroid dehydrogenase type I inhibitors

Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17&#x3b2;-hydroxysteroid dehydrogenase (17&#x3b2;-HSD) such as 17&#x3b2;-HSD type 1, type 2 or type 3 enzyme. 

Therapeutically active triazoles and their use

The present invention relates to novel substituted steroid derivatives which represent selective inhibitors of the 17&#x3b2;-hydroxysteroid dehydrogenase type I (17&#x3b2;-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17&#x3b2;-estradiol concentration.

17&#x3b2;-HSD1 and STS inhibitors

Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17&#x3b2;-hydroxysteroid dehydrogenase enzymes.

Compounds and their use in therapy

Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R, R, Rand Rhave the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.

Amidomethyl-substituted 1-(carboxyalkyl) cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them

Amidomethyl-substituted 1-(carboxyalkyl)-cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them

Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula 1, wherein the substituents R, R, Rand Rhave the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.

3-phenyl-3,7-diazabicyclo&lsqb;3.3.1&rsqb; nonane compounds, process for preparing them, pharmaceutical compositions containing them and use thereof to inhibit cardiac arrhythmia

The invention relates to a device or equipment as well as to a method for the simultaneous, fractionating operation of a plurality of parallel chromatographic columns. It is particularly advantageous to apply this equipment and method in research, in the framework of organic synthesis for simultaneous, parallel separation, isolation and purification of a plurality of chemical compounds, e.g. of potential new active ingredients for medicaments, particularly also on the semi-preparative scale.

Method and device for parallel chromatography

Compounds with neutral endopeptidase (NEP) inhibitory activity corresponding to the formula I ##STR1## in which R.sup.1 is a lower alkoxy-lower-alkyl group whose lower alkoxy radical is substituted by a lower alkoxy group, or a phenyl-lower-alkyl or phenyloxy-lower-alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or a naphthyl-lower-alkyl group,

Benzazepine-, benzoxazepine- and benzothiazepine-n-acetic acid

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Sehnde, Germany

Josef Messinger