Inflazyme Pharmaceuticals Ltd.

Aquinox Pharmaceuticals Inc.

Biolipox Ab

Yuanlin Zhou

Yaping Shen

David L Burgoyne

Ronald W Lauener

Patrick J Rebstein

Jeffery R Raymond

James Gee Ken Yee

Yuehua He

Kang Han

Bradley Noren

Lloyd Mackenzie

Nicholas D Paschalides

Gueijun Ji

Eugene W Kelleher

Kishore Ramachandran

Samuel D M Abraham

Indene derivatives as pharmaceutical agents

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

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &#x3b1;,&#x3b2;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &#x3b1;,&#x3b2;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process improvements in steroid chemistry

&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

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr;,&bgr;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &agr;,&bgr;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process for the production of 6,7-diols of steroidal compounds

&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

Growing community of inventors

Richmond, CA, United States of America

Yuanlin Zhou