Schering Aktiengesellschaft

Other

Robert C Nickolson

Rudolf Wiechert

Ulrich Kerb

Helmut Vorbrueggen

Martin Haberey

Marcel Muller

Leo Alig

Andor Furst

Werner Skuballa

Henry Laurent

Klaus Nickisch

Olaf Loge

Bernd Raduechel

Dieter Bittler

Jorge Casals-Stenzel

Klaus Kieslich

Claus-Steffen Stuerzebecher

Claus S Stuerzebecher

The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,

20-alkyl-7-oxoprostacyclin derivatives useful as pharmaceuticals

Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group,

Novel carbacyclins, process for the preparation thereof, and their use

Certain prostacyclins and their blood-pressure-lowering and

5.beta.-Hydroxy-.DELTA..sup.6 -steroids and process for the preparation

17.alpha.-hyroxy- and 17a.alpha.-hydroxy-D-homoetiocarboxylic acids of the formula ##STR1## wherein n is 1 or 2,

Process for the preparation of 17.alpha.-hydroxy- and

.DELTA..sup.16 -21-HYDROXY-20-KETO STEROIDS OF THE PREGNANE SERIES HAVING AN OTHERWISE UNSUBSTITUTED D-ring and a 13-methyl or -ethyl group, and 21-ethers and -esters thereof, are produced by reaction of a corresponding D-ring saturated 17-keto steroid with a lithium compound of the formula ##STR1## thereby converting the 17-keto group to a 17.beta.-hydroxy-20.alpha.-enol ether in which the 17.alpha.-side chain has the formula ##STR2## wherein R.sub.3 and R.sub.4 have the values given above, and, in any desired sequence, splitting off R.sub.3 and/or R.sub.4 enol ether by hydrolysis; eliminating 17.beta.-hydroxy group, preferably after acylation, with formation of a .DELTA..sup.16 -double bond; and, if desired, splitting off any blocking group.

Process for the preparation of 21-hydroxy-16-pregnen-20-one derivatives

D-Homo-21-carboxylic acids of the formula ##STR1## the   represents a single bond or a double bond; X is a hydrogen atom, a fluorine atom, or methylene;

D-homo steroids

The present disclosure relates to steroid carboxylic acids and derivatives thereof. More particularly, the disclosure is concerned with D-homosteroid carboxylic acids and their derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The instant compounds are active endocrinal agents, especially as antiinflammatory agents.

Steroid carboxylic acids and derivatives

D-homo steroids of the formula ##STR1## wherein X is H, F or CH.sub.3 ; Y is H, F or Cl; Z is CH.sub.2, CO, .beta.-HOCH.sub.2, .beta.-AcOCH.sub.2 or, when Y is Cl, also .beta.-FCH.sub.2 or .beta.-ClCH.sub.2 ; R.sub.1 is H or CH.sub.3, R.sub.2 is H, OH or AcO; and one of R.sub.3 and R.sub.4 is H and the other is OH or alkoxy or both are O, possess anti-inflammatory activity.

Novel D-homo steroids

Growing community of inventors

Berlin, Germany

Robert C Nickolson