Inflazyme Pharmaceuticals Ltd.

Biolipox Ab

Patrick J Rebstein

Yaping Shen

David L Burgoyne

Yuanlin Zhou

Ronald W Lauener

Lloyd Mackenzie

Samuel D M Abraham

Samuel D Abraham

The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.

Benzylated PDE4 inhibitors

&ggr;-Phenyl-substituted &Dgr;-lactams are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.

Substituted &ggr;-phenyl-&Dgr;-lactams and uses related thereto

&ggr;-Phenyl-substituted &Dgr;-lactones and analogs thereof, including lactams, are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.

Substituted &ggr;-phenyl-&Dgr;-lactones and analogs thereof and uses related thereto

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Vancouver, Canada

Patrick J Rebstein