GlaxoSmithKline’s CCR3 chemokine receptor antagonists

Abstract

A series of nine closely related applications claiming various acyl and urea derivatives of 2-aminomethyl-4-benzylmorpholine are considered. These claim CCR3 chemokine receptor antagonists, some of which have affinities in the 10 – 100 pM range. They are claimed to be useful in the treatment of asthma, allergic rhinitis and other inflammatory diseases. One of the applications (WO03082292) claims inter alia 766994, a clinical development candidate, currently in Phase II studies for the treatment of asthma and allergic rhinitis.

• 766994
• allergic rhinitis
• asthma
• CCR3
• CCR3 antagonist
• chemokine
• eotaxin