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Aromatic and heterocyclic derivatives of phytosterols and/or phytosanols for use in treating or preventing cardiovascular disease

A technology of phytostanols and phytosterols, which is applied in the field of treatment and prevention of cardiovascular diseases and other diseases, can solve the problems of low solubility of phytosterols and complex administration of phytosterols, and achieve the effect of improving solubility

Inactive Publication Date: 2002-09-18
FORBES MEDI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although phytosterols are not only in the treatment of CVD and its underlying conditions (such as hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, thrombosis), but also in the treatment of other diseases such as type II diabetes, dementia, cancer and aging There are clear and now well-known advantages of phytosterols, but the administration of phytosterols and their incorporation into foods, drugs, and other delivery vehicles is complicated by the highly hydrophobic nature of phytosterols (i.e., their low solubility in water).

Method used

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  • Aromatic and heterocyclic derivatives of phytosterols and/or phytosanols for use in treating or preventing cardiovascular disease
  • Aromatic and heterocyclic derivatives of phytosterols and/or phytosanols for use in treating or preventing cardiovascular disease
  • Aromatic and heterocyclic derivatives of phytosterols and/or phytosanols for use in treating or preventing cardiovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0128] Example 1 Preparation of Niacin Stanol Ester

[0129] Nicotinyl chloride (6 g) was suspended in chloroform (150 mL) and a stanol mixture (11 g, campesterol 36.4%; sitostanol 62.3%). The mixture was stirred at room temperature, and anhydrous pyridine (6 ml) was added dropwise to the above-prepared mixture. Stirring was continued for 3 hours. After the addition was complete, the mixture was concentrated, the solvent was removed, and acetone (100 mL) was added to the remaining residue. The resulting white precipitate was collected and recrystallized from acetone:chloroform (2:1). 10 g of white crystals are obtained.

Embodiment 2

[0130] Example 2 Preparation of Niacin Stanol Hydrochloride

[0131] The nicotinic acid stanol ester (2 g) prepared above was dissolved in anhydrous ether (20 ml), and 36% HCl (1 ml) was added thereto at room temperature and stirred. The white precipitate was filtered off, washed with diethyl ether (10 mL), and dried to obtain nicotinic acid stanol hydrochloride (2 g) as a white powder.

Embodiment 3

[0132] Example 3 Preparation of stanol nicotinyloxyacetate

[0133] Step a. Synthesis of stanol monochloroacetate

[0134] A stanol-containing mixture (4 g, campestanol (36.4%) and stanol (62.3%)) in monochloroacetic acid (10 mL) was stirred with heating at 120° C. for 3 hours. After cooling, 50 mL of water was added to the reaction mixture, and the precipitate was collected, washed with 10 mL of water, and dried to give a white solid (4.5 g).

[0135] Step b. Synthesis of stanol nicotinyloxyacetate. Anhydrous DMF (10 ml) containing sodium nicotinate (0.5 g) was added to the stanol chloroacetate (1.5 g) prepared above, and the mixture was heated and stirred at 140° C. for 1 hour. After cooling to room temperature, the mixture was poured into 100 mL of water and an off-white solid was collected, dried and weighed (1.8 g).

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Abstract

Novel phytosterol and / or phytostanol derivatives, including salts thereof, are represented by general formulae (I or II) wherein R is a phytosterol or phytostanol moiety; R2 is oxygen or hydrogen (H2) and R3 is an aromatic or heterocyclic unit. These derivatives are effective in treating and preventing cardiovascular disease and its underlying conditions including hyperlipidemia.

Description

field of invention [0001] The present invention relates to the field of phytosterols and phytostanols and their application in the treatment and prevention of cardiovascular diseases and other diseases. Background of the invention [0002] Although recent scientific and technological advances have contributed to improving the quality of human life and prolonging human longevity, the problem of preventing atherosclerosis, the underlying cause of cardiovascular disease ("CVD"), has not been successfully addressed. Atherosclerosis is a degenerative process caused by the interplay of intrinsic (genetic) and environmental factors such as diet and lifestyle. Research so far suggests that cholesterol may play a role in atherosclerosis, where it forms atherosclerotic plaques in blood vessels that eventually cut off blood supply to the heart muscle or the brain or extremities, depending on where the plaque is in the arterial network (1, 2). It has been observed that a 1% reduction ...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P3/06A61P9/10C07J43/00
CPCC07J43/003A61P3/06A61P9/10
Inventor J·P·库托尼R·K·米拉诺瓦丁岩冰陈宏明
Owner FORBES MEDI TECH
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