Bayer Intellectual Property Gmbh

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Bayer Pharma Aktiengesellschaft

Bayer Schering Pharma Ag

Steffen Borden

Rolf Bohlmann

Joachim Kuhnke

Frederik Menges

Hans-Peter Muhn

Ulrich Klar

Thomas Frenzel

Ludwig Zorn

Katja Prelle

Sven Ring

Jan Hübner

Jan Huebner

Dieter Bittler

Karl-Heinrich Fritzemeier

Ulrike Fuhrmann

Peter Esperling

Hermann Kuenzer

Norbert Gallus

Hans Peter Muhn

The invention relates to 17-(1'-propenyl)-17-3&#x2032;-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R, R, R, R, R, R, Rand Rhave the meanings stated in Claim, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action. 

17-(1'propenyl)-17-3&#x2032;-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative

The 15&#x3b1;,16&#x3b1;-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid &#x3b3;-lactone derivatives of the present invention possess progestational efficacy. They have the general chemical formula I, in which Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSOR, where R is hydrogen, C-C-alkyl, aryl or C-C-aralkyl, Ris hydrogen or halogen, and moreover either: R, Rtogether form methylene or 1,2-ethanediyl or Ris hydrogen and Ris selected from the group comprising hydrogen, C-C-alkyl, C-C-alkenyl or C-C-alkynyl, and Ris selected from the group comprising hydrogen, C-C-alkyl, C-C-cycloalkyl, C-C-alkenyl or C-C-alkynyl, or: Ris hydrogen and Rand R, together, denote a bond, an oxygen or form methylene, Rrepresents hydrogen or C-C-alkyl and in addition include their solvates, hydrates, stereoisomers and salts. 

19-nor-steroid derivatives with a 15&#x3b1;,16&#x3b1;-methylene group and a saturated 17,17-spirolactone ring, use thereof, and medicaments containing said derivatives

The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid &#x3b3;-lactone derivatives with the chemical formula I, where R, R, R, R, R, R, R, Rand Z have the meanings stated in claim, and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action. 

17-hydroxy-19-nor-21-carboxylic acid-steroid &#x3b3;-lactone derivative, use thereof, and medicament containing the derivative

The invention relates to 15,16-methylene-17-(1'-propenyl)-17-3&#x2032;-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the Z, R, R, R, Rand Rhave the meanings stated in claim, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity. 

15, 16-methylene-17-(1'-propenyl)-17,3&#x2032;-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative

A 18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactone of general formula I 

18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones, as well as pharmaceutical preparations that contain the latter

The 17&#x3b2;-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSOR, in which R is hydrogen or C-C-alkyl, Ris hydrogen or halogen, furthermore either: R, Rtogether form methylene or 1,2-ethanediyl or Ris hydrogen and Ris selected from the group comprising hydrogen, methyl and hydroxymethylene, and Ris selected from the group comprising hydrogen, C-C-alkyl, C-C-alkenyl and cyclopropyl, or: Ris hydrogen and Rand Rtogether form methylene or are omitted with formation of a double bond between Cand C, R, Rare hydrogen or are omitted with formation of a double bond between Cand C, R, Rare hydrogen or together form methylene, Ris selected from the group comprising hydrogen, C-C-alkyl and allyl, where at least one of the substituents R, R, R, R, R, Rand Ris unequal to hydrogen or Rand Rare omitted with formation of a double bond between Cand C, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts. 

17&#x3b2;-cyano-19-nor-androst-4-ene derivative, its use and medicaments comprising the derivative

The present invention describes the novel 18-methyl-19-norandrost-4-ene 17,17-spiro ethers of the general formula I in which The novel compounds have progestational and antimineralocorticoid activity.

18-Methyl-19-norandrost-4-ene 17, 17-spiro ether (18-methyl-19-nor-20-spirox-4-en-3-one), and pharmaceutical products comprising the same

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Berlin, Germany

Steffen Borden