Schering Aktiengesellschaft

Veb Jenapharm

Jenapharm Gmbh & Co. Kg

Jenapharm Gmbh

Kurt Ponsold

Bernd Menzenbach

Helmut Kasch

Michael Oettel

Peter Droescher

Bernd Undeutsch

Gunter Kaufmann

Anatoli Kurischko

Gudrun Bertram

Gerd Schubert

Jens Schroder

Wolfgang Romer

Michael Hubner

Heidemarie Rohrig

Jens Schroeder

Reimar Krieg

Richard Prousa

Herbert Hoffmann

Wolfgang R&ouml;mer

Joachim Strecke

Michael Oettell

Anatoil Kurischko

The method of prophylaxis and therapy of radical-mediated cell damage includes administering an effective amount of at least one steroid and at least one pharmaceutical adjuvant to a human being. The at least one steroid is selected from the group consisting of ent-estradiol, 17&agr;-estradiol, 8-dehydro-estradiol, 8-dehydro-17&agr;-estradiol, 8(14)-dehydroestradiol, 6,8-didehydro-17&agr;-estradiol, 6-dehydroestriol, 9(11)-dehydroestriol, 20-hydroxymethyl-3-hydroxy-19-norpregna-1,3,5(10)-triene, 14&agr;, 15&agr;-methylene-8-dehydroestradiol, 14&agr;, 15&agr;-methylene-estradiol, 2-hydroxy-estradiol-3-methyl ether, 3-hydroxy-1,3,5(10)-estratriene-17S-spirooxirane, 3-hydroxy-1,3,5(10),9(11)-estratetraene-17S-spirooxirane, and 14&bgr;,15&bgr;-methylene-8-dehydroestradiol. This method strongly inhibits changes in cells and tissues, such as lipid peroxidation and oxidation of low-density lipoprotein (LDL) cholesterol, triggered by reaction oxygen species, free oxygen radicals and other forms of radicals and thus reduces attendant irreversible membrane and endothelial damage.

Pharmaceutical compositions and method for prophylaxis and therapy of radical-mediated cell damage

Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.

Steroids with radical-attracting aromatic substituents, process for the

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 11.beta.-aryl-gona-4,9-dienes of the general formula I ##STR1## wherein the variables are defined in the specification. The compounds are progesterone antagonists and are suitable for inducing labor or an abortion.

11.beta.-aryl-gona-4,9-dien-3-ones

11.sym.-Aryl-16.alpha.,17.alpha.-cyclohexano-estra-4,9-dienes of formula ##STR1## wherein R.sup.1 is H or a methyl group;

11.beta.-aryl-16.alpha.,17.alpha.-cyclohexano-estra-4,9-dienes

11.beta.-substituted-16.alpha., 17.alpha.-methylene-estra-4,9-dien-3-ones of formula I ##STR1## wherein R.sup.1 is a methyl or ethyl group;

11.beta.-substituted 16.alpha., 17.alpha.-methylene-estra-4,9-dien-3-ones

New gona-4,9(10)-dienes of formula I ##STR1## where R is alkyl of 1 to 3 carbon atoms and X is Cl, Br, F, N.sub.3, SCN, CN, OH, OR'(R'-alkyl), NH.sub.2, a substituted amino group or a heterocyclic compound including nitrogen in the ring. The compounds have valuable biological properties, especially hormonal and antihormonal effects, and can be used to advantage in pharmaceutical preparation, for the treatment of endocrinopathies and for reproduction control in human beings and livestock. The invention also embraces a process for making the compounds by converting 3-methoxy-13.beta.-R-gona-2,5(10)-diene-17.beta.-spiro-1,`2`-ox iranes to 17.beta.-hydroxy-17.alpha.-CH.sub.2 -13.beta.-R-gona-4,9(10)-diene-3-ones to the 17.alpha.-CH.sub.2 X-14.beta.-ols which are hydrolyzed to the 17.beta.-OH which latter are then converted to the compounds of formula I.

Gona-4,9(10)-dienes and process of producing the same

Compounds of the general formula ##STR1## in which R' is hydrogen or a methyl radical; R is a hydroxyl, acetoxy, arylaminocarbonyloxy, alkylaminocarbonyloxy radical;

14,15-Methylene derivatives of the estrane series and methods for

New gona-4,9(10)-dienes of formula I ##STR1## where R is alkyl of 1 to 3 carbon atoms and X is Cl, Br, F, N.sub.3, SCN, CN, OH, OR'(R'=alkyl), NH.sub.2, a substituted amino group or a heterocyclic compound including nitrogen in the ring. The compounds have valuable biological properties, especially hormonal and antihormonal effects, and can be used to advantage in pharmaceutical preparations for the treatment of endocrinopathies and for reproduction control in human beings and livestock. The invention also embraces a process for making the compounds by converting 3-methyoxy-13.beta.-R-gona-2,5(10)-diene-17.beta.-spiro-1',2'-o xiranes first to 17.beta.-hydroxy-17.alpha.-CH.sub.2 X-13.beta.-R-gon-5(10)-en-3-one, then to the 17.beta.-hydroxy-17.alpha.-CH.sub.2 X-13.beta.-R-gona-4,9(10)-diene-3-ones of formula I.

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Jena, Germany

Kurt Ponsold