Schering Aktiengesellschaft

Schering Aktiengesellscaft

Josef Heindl

Werner Skuballa

Bernd Buchmann

Roland Ekerdt

Claudia Giesen

Wolfgang Frohlich

Gerhard Sauer

Helmut Wachtel

Rolf Bohlmann

Helmut Hofmeister

Dieter Bittler

Yukishige Nishino

Martin Schneider

Christa Hegele-Hartung

Rosemarie Lichtner

Nikolaus Heinrich

Karsten Parczyk

Thomas Brumby

Jonathan Turner

Hermann Kunzer

Gertrud Schroeder

Gerhard Kuhne

Wolfgang Fr Ohlich

Olaf Loge

Hermann K&uuml;nzer

Rolalnd Ederdt

Wolfgang Fro/ Hlich

This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I

7&agr;-(xi-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7&agr;-(xi-aminoalkyl-estratrienes as well as their use for the production of pharmaceutical agents

This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids. The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.

7.alpha.-(.xi.-aminoalkyl)-estratrienes, process for their production,

Leukotriene B4 derivatives, process for their production and their use

Leukotriene-B4 derivatives, process for their production and their use

Pyridine compounds which are useful as leukotriene-B.sub.4 -antagonists

Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,

Leukotriene-B.sub.4 antagonists, process for their production and their

New leukotriene-B4 Antagonists and their use as pharmaceutical agents

Leukotriene-B.sub.4 derivatives, process for their production and their

The present invention relates to a leukotriene-B.sub.4 analog according to formula I ##STR1## in which R.sup.1 is a COOR.sup.2 group, wherein R.sup.2 is a C.sub.2-4 -alkyl group;

Leukotriene-B.sub.4 derivatives of formula I ##STR1## are described, in which R.sup.1 means CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5, CONR.sup.6 R.sup.7, or R.sup.1 together with R.sup.2 means a carbonyl group, R.sup.4 symbolizes H, C.sub.1 -C.sub.10 alkyl optionally substituted, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.10 aryl radical optionally substituted, or a 5-6-membered aromatic heterocyclic ring, A symbolizes a trans, trans-CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group, B symbolizes a C.sub.1 -C.sub.10 alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sup.6 or together with B can also mean a direct bond, their salts with physiologically compatible bases and their cyclodextrin clathrates.

New leukotriene-B.sub.4 derivatives, process for their production and

1. Leukotriene-B.sub.4 antagonists of formula I ##STR1## are described, in which X is a CH.sub.2 group or an oxygen atom,

Leukotriene-B.sub.4 antagonist compounds and their use as pharmaceutical

##STR1## Compounds of formula (I) in which the residues have the following meanings: a is (II) or (III); R.sup.1 is CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5 with R.sup.5 or, A is a trans, trans--CH.dbd.CH--CH.dbd.CH--or tetramethylene group; B is an alkylene group with up to 10 C atoms; D is a direct bond, oxygen, sulphur, a --C.tbd.C--group or a --CH.dbd.CR.sup.7 --group, or (IV); B and D together are a direct bond; R.sup.2 and R.sup.3 are the same or different and denote hydrogen or an organic acid residue with 1 to 15 C atoms, R.sup.1 and R.sup.2 together are a carbonyl group; R.sup.4 is a hydrogen atom or C.sub.1-10 alkyl, and if R.sup.5 denotes a hydrogen atom, their salts with physiologically acceptable bases and their cyclodextrin clathrates.

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Berlin, Germany

Josef Heindl