Euro-celtique S.a.

The Purdue Frederick Company

Peter Hofer

Mark Chasin

David J Cavalla

Andre Gehrig

Peter Wintergerst

Bola V Shetty

Arthur McFadden

Lloyd Jay Dolby

Stewart Thomas Leslie

Alfred Halpern

John David Cavalla

Anddre Gehrig

Peter Wintergest

Ronald B Miller

Aryl isoguanines

Purine derivatives having phosphodiesterase iv inhibition activity

Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.

Benzoxazoles

6,5-fused aromatic ring systems having enhanced phosphodiesterase IV inhibitory activity

Purine derivatives having phosphodiesterase IV inhibition activity

Hypoxathine compounds

Disclosed is a compound selected from the group consisting of 1,3,8-triethyl-2,6-dithioxanthine; 1,3,8-triethyl-2-thioxanthine; 8-cyclopropyl-1-ethyl-3-(2-methyl-butyl)-6-thioxanthine; 1,3-diethyl-8-isopropyl-6-thioxanthine; 8-cyclopropyl-1,3-dipropyl-6-thioxanthine; 8-isopropyl-1,3-dipropyl-6-thioxanthine; 1,3-diethyl-8-cyclopropyl-2,6-dithioxanthine; 1-(4-chlorobenzyl)-3-ethyl-8-isopropyl-6-thioxanthine; and 8-cyclopropyl-1,3-diethyl-6-thioxanthine. Also disclosed is a pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and a compound selected from the group above. Also disclosed is a method of effecting PDE IV inhibition which comprises administering to a patient suffering from a disease or disorder selected from the group consisting of asthma, allergies, PDE IV modulated inflammation, and depression, a therapeutically effective amount of a compound selected from the group above.

Trisubstituted thioxanthines

With the above and other objects in view, the present invention comprises compounds having the general formula (I):

3-(arylalkyl) xanthines

Disclosed are compounds of the formula (I):

The present invention comprises compounds having the general formula I:

Methods of Synthesing Purine Compounds Having PDE Iv Inhibitory Activity

Disclosed are compounds having the formulae: ##STR1## wherein: Q.sub.3,Q.sub.6a,Q.sub.6b and Q.sub.8 are independently a bond, C.sub.1-8 alkylene, C.sub.2-8 alkenylene and C.sub.2-6 alkynylene, and

Aryl thioxanthines

Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. The present invention includes compounds of Formula I: ##STR1##

6,5-fused aromatic ring systems having enhanced phosphodiesterase IV

The present invention comprises methods of synthesizing compounds having the formula I: ##STR1## wherein: Y.sub.1, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein, which comprises the steps of

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Liestal, Switzerland

Peter Hofer