Schering Aktiengesellschaft

Bayer Intellectual Property Gmbh

Bayer Schering Pharma Ag

Other

Bayer Pharma Aktiengesellschaft

Schering Akitengesellschaft

Hans-Peter Muhn

Rolf Bohlmann

Joachim Kuhnke

Karl-Heinrich Fritzemeier

Rolf Krattenmacher

Katja Prelle

Steffen Borden

Frederik Menges

Ulrich Klar

Thomas Frenzel

Sven Ring

Wolfgang Schwede

Peter Strehlke

Nikolaus Heinrich

Wolfgang Halfbrodt

Manfred Lehmann

Klaus Schollkopf

Jan Hübner

Klaus Schoellkopf

Hermann Kuenzer

Jan Huebner

Norbert Gallus

Alexander Hillisch

Ludwig Zorn

Dieter Bittler

Olaf Peters

Ulrike Fuhrmann

Peter Esperling

Reinhard Nubbemeyer

Margit Richter

Nico Braeuer

Ina Thieme

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

This invention relates to 8&#x3b2;-vinyl-11&#x3b2;-(&#x3c9;-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ER&#x3b2;-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.

8&#x3b2;-vinyl-11&#x3b2;-(&#x3c9;-substituted)alkyl-estra-1,3,5(10)-trienes

A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction. The meanings of R, R, R, R, Rand Ras well as of the grouping U&#x2014;V&#x2014;W&#x2014;X&#x2014;Y&#x2014;Z are indicated in the claims 

Microbiological process for the production of 7-substituted 11-hydroxy steroids, 7,17-substituted 11-Halogen steroids and uses thereof

Nonsteroidal gestagens

This invention describes the new, nonsteroidal gestagens of general formula I

Described are 14,17-C.sub.2 -bridged steroids of the formula (I) defined in the specification. The compounds are available, even after peroral administration, with high gestagenic action and are suitable for the production of pharmaceutical agents.

14-.alpha., 17-.alpha.-C.sub.2 bridged norprogesterone derivatives

The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are in contrast, with the disclaimed compound, the new compounds are available even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.

14-.alpha.,17-.alpha.-C.sub.2 -bridged norprogesterone derivatives

The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are, in contrast with the disclaimed compound 14,17-ethano-19-norpregn-4-ene-3,20-dione bioavailable even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.

14.alpha., 17.alpha.-C.sub.2 -bridged norprogesterone derivatives

Growing community of inventors

Berlin, Germany

Hans-Peter Muhn