The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 02, 2008

Filed:

Mar. 08, 2007
Applicants:

Ronald W. Lauener, New Westminster, CA;

David L. Burgoyne, Delta, CA;

Patrick J. Rebstein, Vancouver, CA;

Lloyd F. Mackenzie, Surrey, CA;

Yuanlin Zhou, Richmond, CA;

Yaping Shen, Port Coquitlam, CA;

Inventors:

Ronald W. Lauener, New Westminster, CA;

David L. Burgoyne, Delta, CA;

Patrick J. Rebstein, Vancouver, CA;

Lloyd F. Mackenzie, Surrey, CA;

Yuanlin Zhou, Richmond, CA;

Yaping Shen, Port Coquitlam, CA;

Assignee:

Biolipox AB, Solna, SE;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 31/38 (2006.01); C07D 207/12 (2006.01);
U.S. Cl.
CPC ...
Abstract

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.


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