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Benzimidazole derivatives as modulators of IgE

A technology of immunoglobulin and drugs, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2005-09-21
AVANIR PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] No current treatment eliminates excess circulating IgE

Method used

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  • Benzimidazole derivatives as modulators of IgE
  • Benzimidazole derivatives as modulators of IgE
  • Benzimidazole derivatives as modulators of IgE

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0046] The present invention relates to small molecule IgE inhibitors (synthesis and / or release) useful in the treatment of allergy and / or asthma or any other disease in which IgE is the causative agent. Specific compounds disclosed herein are identified by their ability to inhibit IgE levels in in vitro and in vivo assays. By reference to the in vitro and in vivo assays described below, one skilled in the art can understand the evolution and optimization of clinical treatment regimens.

[0047] In vitro analysis

[0048] The assay begins with in vivo antigen priming and the secondary antibody response is measured in vitro. The basic protocol has been documented and has been optimized for a range of parameters including: antigen dose and length of priming, number of cells cultured in vitro, eliciting secondary IgE (and other Ig) responses in vitro antigen concentration, fetal bovine serum (FBS) batches to optimize IgE in vitro responses, the importance of priming CD4+ T cel...

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PUM

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Abstract

This invention relates to a family of diacyl benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and / or asthma or any diseases where IgE is pathogenic.

Description

technical field [0001] The present invention relates to small molecule inhibitors of allergen-responsive IgE, which inhibitors are useful in the treatment of allergy and / or asthma or other diseases in which IgE is the causative agent. Background technique [0002] An estimated 10 million people in the United States suffer from asthma, accounting for about 5 percent of the population. The estimated cost of asthma in the United States exceeds six billion dollars. About 25% of asthma patients who request emergency care require hospitalization, and the largest single direct medical expense for asthma is inpatient hospital services (emergency care), which cost >$16 billion. Spending on prescription drug therapy increased 54% from 1985 to 1990, to nearly $1.1 billion (Kelly, Pharmacotherapy 12: 13S-21S (1997)). [0003] According to the National Ambulatory Medical Care Survey, asthma accounts for 1% of all ambulatory care visits, and the disease continues to be a leading caus...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D235/14A61K31/00A61K31/166A61K31/167A61K31/18A61K31/337A61K31/357A61K31/382A61K31/397A61K31/403A61K31/4035A61K31/404A61K31/4045A61K31/415A61K31/4184A61K31/42A61K31/423A61K31/4427A61K31/443A61K31/4433A61K31/4439A61K31/445A61K31/451A61K31/454A61K31/4545A61K31/53A61K45/06A61P11/06A61P37/08A61P43/00C07D205/04C07D209/16C07D209/48C07D211/46C07D211/52C07D235/18C07D251/70C07D261/12C07D319/18C07D401/12C07D401/14C07D403/14C07D405/04C07D405/12C07D409/12C07D409/14C07D413/04
CPCA61K31/00A61K31/4545A61K31/415A61K31/4184A61K45/06A61P11/06A61P37/00A61P37/08A61P43/00A61K2300/00
Inventor J·西尔卡M·L·里查兹M·G·坎贝尔M·W·马约尔
Owner AVANIR PHARMA INC
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