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2,4,5-trisubstituted selenazole compounds and preparation method, compositions and application thereof

A compound, selenazole technology, applied in the field of methods and methods, can solve problems such as reducing HDL levels and hindering plasma phospholipid transfer

Active Publication Date: 2011-09-21
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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Problems solved by technology

Feeding a high-fat diet to PLTP-null mice did not induce plasma lipoprotein abnormalities, but blocked the transfer of all major plasma phospholipids from VLDL to HDL, significantly reducing HDL levels (Jiang, X.C.; Bruce, C.; Mar, J. et al. J. Clin. Invest. 1999, 103, 907-914.)

Method used

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  • 2,4,5-trisubstituted selenazole compounds and preparation method, compositions and application thereof
  • 2,4,5-trisubstituted selenazole compounds and preparation method, compositions and application thereof
  • 2,4,5-trisubstituted selenazole compounds and preparation method, compositions and application thereof

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Abstract

The invention relates to 2,4,5-trisubstituted selenazole compounds and a preparation method, a composition and application thereof, in particular to compounds in a formula (I), or all possible isomers, predrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein each substituent is shown as the description. The invention also relates to a method for preparing the compounds in the formula (I), medicinal compositions comprising the compounds in the formula (I), and application of the compounds in the formula (I) or the medicinal compositions in preparation of medicines for treating and / or preventing phospholipid transfer protein (PLTP) activity increase and / or diseases or syndromes related with the phospholipid transfer protein activity increase. The compounds in the formula (I) have good effect of inhibiting the PLTP activity and / or cholesteryl ester transfer protein (CETP) activity of blood plasma, and can be used for treating diseases on the basis.

Description

2,4,5-trisubstituted selenazole compound and its preparation method, composition and use technical field The present invention relates to 2,4,5-trisubstituted selenazole compounds as phospholipid transfer protein (PLTP) inhibitors and / or cholesterol ester transfer protein (Cholesteryl ester transfer protein (CETP)) inhibitors, and Their preparation method and use in the medical field, especially the treatment and prophylaxis of various diseases associated with the increase of plasma PLTP activity and / or with the increase of plasma CETP activity, said diseases include atherosclerosis, cardiac Vascular disease and peripheral vascular disease etc. Background technique Diseases caused by atherosclerosis are the number one cause of death in developed countries. In my country, with the development of social economy and the aging of population, the incidence and mortality of cardiovascular and cerebrovascular diseases have also increased significantly in recent years. The etiol...

Claims

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Application Information

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IPC IPC(8): C07D293/06A61K31/41A61P9/10A61P9/00A61P3/06A61P9/12A61P3/10A61P3/04A61P7/00
Inventor 李松钟武凌翠郑志兵肖军海蒋宪成谢云德
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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