Bayer Pharma Aktiengesellschaft

Bayer Schering Pharma Ag

Michael Sander

Danja Grossbach

Gabriele Winter

Wolfgang Beckmann

Christian Dinter

Tilo Haag

Klaus Bartel

William J Guilford

Detlef Grawe

Sabine Gliesing

Hagen Gerecke

Peter Hoesel

Bernd Erhart

Uwe Mueller

Thomas Michel

Robert Eilers

Ulf Tilstam

Ulf Bohlmann

Dieter Wehmeier

Uwe Knabe

Michael Mosebach

David Voigtlaender

Jürgen Jacke

Klaus Bahl

The present invention relates to a method for the reliable and reproducible preparation of 4-[17&#x3b2;-methoxy-17&#x3b1;-methoxymethyl-3-oxoestra-4,9-dien-11&#x3b2;-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

Method for preparing 4-[17&#x3b2;-methoxy-17&#x3b1;-methoxymethyl-3-oxoestra-4,9-dien-11&#x3b2;-yl]benzaldehyde (E)-oxime (asoprisnil)

This invention is directed to the crystalline potassium salt of a lipoxin Aanalog of Formula (I): processes for preparing the crystalline potassium salts, methods for using them to treat disease-states characterized by inflammation, and pharmaceutical compositions comprising such crystalline potassium salts.

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This invention is directed to compounds useful as intermediates in the synthesis of lipoxin Aanalogs of the following formulas (I) and (II): wherein R, R, R, Rand Rare described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

Crystalline potassium salt of lipoxin A4 analogs

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Frechen, Germany

Michael Sander