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Amino acid phenoxy ethers

Inactive Publication Date: 2005-05-05
BEXEL PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015] The compounds of the present invention are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels and are useful in the treatment and / or prophylaxis of diabetes. The compounds of the present invention are effective in treatment of obesity, inflammation, autoimmune diseases such as such as multiple sclerosis and rheumatoid arthritis. Surprisingly, these compounds increase the leptin level and have no liver toxicity.

Problems solved by technology

However, in inflammatory diseases such as rheumatoid arthritis, pathologic inflammatory processes can lead to morbidity and mortality.
All of these therapies have limited efficacy, limited tolerability and significant mechanism-based side effects.
Several current treatments for type II diabetes are associated with episodes of hypoglycemia, and few of the available therapies adequately address underlying defects such as obesity and a phenomenon known as insulin resistance.
Many patients who respond to sulfonylureas initially become refractory to the treatment over time (secondary failure).

Method used

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  • Amino acid phenoxy ethers
  • Amino acid phenoxy ethers
  • Amino acid phenoxy ethers

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzyl]-thiazolidin-2,4-dione hydrochloride salt

[0215]

Step (i)

Preparation of methyl-2-[(t-butoxycarbonyl)amino]-3-[-(4-formylphenoxy)phenyl]propanoate

[0216] To a suspension of fresh sodium hydride (0.813 g, 33.9 mmol) in dry DMF (20 ml) under nitrogen atmosphere was added the solution of methyl-2-[(t-butoxycarbonyl)amino]-3-(4-hydroxyphenyl)propanoate (10 g, 33.9 mmol) in DMF (20 ml) slowly. The mixture was stirred for 15 minutes. 4-Fluorobenzaldehyde (4.20 g, 33.9 mmol) was added and the mixture was heated to 80° C. After completion of the reaction, the solvent was removed by high vacuum and the mixture was quenched with addition of saturated aqueous ammonium chloride. The mixture was extracted with ethyl acetate (3×50 ml). After washing with brine and dried on anhydrous sodium sulfate, the solvent was evaporated and the product was purified with flash column from eluent of hexanes: ethyl ether; 12 / 30 to 12 / 22 to aff...

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Abstract

Novel amino acid phenyl ethers are provided which exhibit activity for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases and diabetes.

Description

[0001] This application claims priority of U.S. patent application Ser. No. 10 / 356,113, filed Sep. 21, 2004, and the benefit of the earlier filing date of U.S. Provisional Application No. 60 / 440,772 filed Jan. 17, 2003, both of which are incorporated herein by reference.FIELD OF THE INVENTION [0002] The present invention relates to novel amino acid phenyl ethers for the treatment of immunological diseases, inflammation, obesity, hyperlipidemia, hypertension, neurological diseases and diabetes. BACKGROUND OF THE INVENTION [0003] The principal elements of the immune system are macrophages or antigen-presenting cells, T cells and B cells. The role of other immune cells such as NK cells, basophils, mast cells and dendritic cells are known, but their role in primary immunologic disorders is uncertain. Macrophages are important mediators of both inflammation and providing the necessary “help” for T cell stimulation and proliferation. Most importantly macrophages make IL 1, IL 12 and TNF-α...

Claims

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Application Information

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IPC IPC(8): C07D263/44C07D277/34
CPCA61K31/421A61K31/422C07D277/34A61K31/427C07D263/44A61K31/426A61P19/00A61P19/02A61P25/00A61P29/00A61P3/00A61P3/04A61P3/06A61P3/08A61P37/00A61P37/02A61P37/06A61P43/00A61P9/12A61P3/10
Inventor NAG, BISHWAJITNAG, ABHIJEETDEY, DEBENDRANATHAGARWAL, SHIV KUMAR
Owner BEXEL PHARMA INC
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