Schering Aktiengesellschaft

Joachim-Friedrich Kapp

Henry Laurent

Rudolf Wiechert

Hans Wendt

Klaus Annen

Helmut Biere

Clemens Rufer

Eberhard Schroder

Irmgard Bottcher

Helmut Hofmeister

Karl Petzoldt

Alfred Weber

Gerald Kirsch

Mario Kennecke

Helmut Dahl

Peter Esperling

Klaus Kieslich

Henning Koch

Hanns Ahrens

Ernst Schottle

Pyrido[2,1-b]quinazolinones of the formula ##STR1## wherein X is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl, carboxy, carboxy in the form of a salt thereof with a physiologically compatible base, carboxy esterified with a physiologically acceptable alcohol or carboxy amidated with a physiologically acceptable amine;

Pyrido[2,1-b]quinazolinone derivatives and the preparation and use

Phenylacetic acid derivatives of the formula ##STR1## wherein n is an integer of 2 to 5; ##STR2## R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R.sub.2 and R.sub.3 each independently is hydrogen or lower alkyl; or together form an ethylene group;

Novel phenylacetic acid derivatives

Corticoid 21-sulfopropionates of the formula ##STR1## wherein St is a steroid nucleus of a corticoid having anti-inflammatory activity, and the salts thereof with physiologically acceptable bases, simultaneously form stable, sterilizable and storable solutions and also are very rapidly cleaved after i.v. administration, yielding the free corticoids as the cleavage product.

Corticoid 21-sulfopropionates and the salts thereof, a process for the

Corticoids of the formula ##STR1## wherein X is fluorine, chlorine and

Novel corticoids, the preparation thereof and the use thereof

Indanyl derivatives of the formula ##STR1## wherein AR is phenyl, pyridyl, or phenyl or pyridyl substituted by halogen, alkyl of 1-4 carbon atoms or trifluoromethyl; X is oxygen or a sulfur; R.sub.1 is alkyl of 1-4 carbon atoms or alkyl of 1-4 carbon atoms substituted by fluorine or chlorine; A is ##STR2## Y is oxo, oximino, C.sub.1-4 -alkoximino of 1-4 carbon atoms, phenylhydrazono or p-toluenesulfonylhydrazono; n is 0, 1 or 2; R.sub.2 is alkyl of 1-4 carbon atoms, phenyl or phenyl substituted by halogen, alkyl of 1-4 carbon atoms, nitro or carboxy; Z is hydroxy, acyloxy of 1 to 6 carbon atoms, R.sub.1 SO.sub.3 -- amino, acylamino of 1 to 6 carbon atoms, R.sub.1 SO.sub.2 NH-- or cyano, and V is hydrogen, acyl of 1 to 6 carbon atoms or R.sub.1 SO.sub.2 --, and the salts thereof with physiologically acceptable bases or acids have valuable pharmacological and herbicidal activity.

Indanyl derivatives and their use

Corticoids of the formula ##STR1## wherein represents a single bond or a double bond;

Novel 17-substituted 11 .beta.-hydroxy steroids of the pregnane series,

Compounds of the formula ##STR1## wherein X is .beta.-CH.sub.2 OH or CO and R.sub.2 is F, Cl or CH.sub.3, and their physiologically acceptable 21-esters are useful for the treatment of allergic diseases of the respiratory tract and for the treatment of topical and systemic inflammatory conditions.

Novel corticoids

Novel corticoids of formula I ##STR1## wherein X is .beta.-hydroxymethylene, .beta.-fluoromethylene or carbonyl; Y is fluorine, chlorine, hydroxy, or acyloxy of 1-10 carbon atoms; and R.sub.1 is acyloxy of 1-10 carbon atoms, possess strong anti-inflammatory activity when administered topically and display only minor systemic side effects.

Pyrazole compounds of the formula ##STR1## wherein n is 1, 2, 3, or 4; R.sub.1, R.sub.2, R.sub.3, and R.sub.4, which can be in the ortho, meta or para position, each are hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, nitro or amino; X is cyano, aminocarbonyl, lower alkoxycarbonyl, carboxy and physiologically acceptable salts thereof, have anti-inflammatory activity.

Growing community of inventors

Berlin, Germany

Joachim-Friedrich Kapp