Biolipox Ab

Inflazyme Pharmaceuticals Ltd.

Aquinox Pharmaceuticals Inc.

Lloyd Mackenzie

Yaping Shen

David L Burgoyne

Yuanlin Zhou

Ronald W Lauener

Patrick J Rebstein

Curtis Harwig

Jeremy D Pettigrew

Vladimir Khlebnikov

Rudong Shan

Paul Bird

Sam Place

Tom MacRury

Noor Aini Bhatti

Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R, R, R, R, R, Rand Rare as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

SHIP1 modulators and methods related thereto

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

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Surrey, Canada

Lloyd Mackenzie