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J Med Chem. 2004 Dec 16;47(26):6451-4.

Novel 2-(substituted phenyl)benzimidazole derivatives with potent activity against IgE, cytokines, and CD23 for the treatment of allergy and asthma.

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  • 1Avanir Pharmaceuticals, 11388 Sorrento Valley Road, San Diego, California 92121, USA. mrichards@avanir.com

Abstract

The effectiveness of the injectable anti-IgE antibody omalizumab has validated IgE as an important target for allergic diseases, thus spawning the development of small-molecule IgE inhibitors. Herein, a brief SAR is described for novel phenylbenzimidazole compounds that potently suppress IgE responses. In addition to IgE, these agents inhibit other targets critical for allergic response. The profile of orally active AVP-13358, the lead compound of this series currently in clinical trials, is described.

PMID:
15588078
DOI:
10.1021/jm049288j
[PubMed - indexed for MEDLINE]
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