Pfizer Corporation

Memory Pharmaceuticals Corporation

Hans-Jurgen E Hess

Thomas K Schaaf

Jasjit S Bindra

Michael Ross Johnson

James F Eggler

Leonard J Czuba

Ashok Tehim

Saul B Kadin

Allen T Hopper

Thomas H Althuis

Ruiping Liu

Praful K Shah

Erik Mikal Kuester

Yajing Rong

Richard A Schumacher

Robert F Dunn

Timothy H Cronin

Axel Unterbeck

Roger P Nelson

William Frederick Brubaker, Jr

Mike De Vivo

Gerald George De Angelis

PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R, R, Rand Rare as defined herein.

Phosphodiesterase 4 inhibitors, including N-substituted aniline and diphenylamine analogs

PDE4 inhibition is achieved by novel compounds of the Formula I: wherein Rand Rare as defined herein.

Phosphodiesterase 4 inhibitors

Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I:wherein R, R, and Rare as defined herein.

15-Substituted-.omega.-pentanorprostaglandin C-1 tetrazoles, imides and sulfonimides. Their use as anti-secretory agents or as agents for the control of fertility.

15-Substituted-.omega.-pentanorprostaglandin derivatives

2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such than when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;

Chloro- and alkoxy-substituted-2,4-diaminoquinazolines

2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;

Chloro- and alkoxy-substituted-2-chloro-4-aminodquinazolines

2-Descarboxy-2-(tetrazol-5-yl)-16,16-dimethyl-17-(

Alkoxy-substituted-6-chloro-quinazoline-2,4-diones

The invention discloses certain novel 13,14-dihydro-15-alkenyl prostaglandins and 13,14-dihydro-15-alkynyl prostaglandins and analogs of each as well as the novel intermediates employed in their preparation. The 9-oxo compounds of this novel series demonstrate selective bronchodilator activity, certain of these are also useful as antisecretory agents.

Bronchodialation with 13,14-dihydro-15-alkenyl prostaglandins

13,14-Dihydro-15-alkenyl- and 13,14-dihydro-15-alkynyl prostaglandins

The 15 aryl substituted-.omega.-pentanorprostaglandins and various intermediates empolyed in their preparation. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins, but exhibit a greater tissue specificity of action.

15-Substituted-omega-pentanorprostaglandins

N-alkylsulfonyl, N-alkanoyl and N-benzoyl 16,16-dimethyl-17-oxaprostaglandin E.sub.2 and E.sub.1 carboxamides having antisecretory biological activity as well as intermediates for their synthesis are disclosed.

Antisecretory 16,16-dimethyl-17-oxaprostaglandins

11-DESOXY-15-SUBSTITUTED-.omega.-PENTANORPROSTAGLANDINS AND VARIOUS INTERMEDIATES EMPLOYED IN THEIR PREPARATION. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins, but exhibit a greater tissue specificity of action.

11-Desoxy-15-substituted-.omega.-pentanor prostaglandins

The 15-substituted-.omega.-pentanorprostaglandins and various intermediates employed in their preparation. The novel prostaglandins of this invention have been found to have activity profiles comparable to the parent prostaglandins, but exhibit a greater tissue specificity of action.

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Old Lyme, CT, United States of America

Hans-Jurgen E Hess