Composition and application thereof to medicines for preventing or treating pancreatic fibrosis

A technology of pancreatic fibrosis and composition, which is applied in the fields of organic synthesis and medicinal chemistry, and can solve the problems of high toxicity and low safety

Inactive Publication Date: 2016-02-03
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of pancreatic fibrosis have the problems of high toxicity and low safety. It is most important to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs with high efficiency and low toxicity.

Method used

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  • Composition and application thereof to medicines for preventing or treating pancreatic fibrosis
  • Composition and application thereof to medicines for preventing or treating pancreatic fibrosis
  • Composition and application thereof to medicines for preventing or treating pancreatic fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Example 1 Preparation of compound SalviskinoneA

[0011] The preparation method of the compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsakietal., 2011. Salviskinone A, aditerpene with a new skeleton from Salvia przewalskii. Tetrahedron Letters 52 (2011) 1375-1377).

[0012]

Embodiment 2

[0013] Example 2 Synthesis of O-bromoethyl derivative (II) of SalviskinoneA

[0014] Compound I (312mg, 1.00mmol) was dissolved in 15mL of benzene, tetrabutylammonium bromide (TBAB) (0.08g), 1,2-dibromoethane (3.760g, 20.00mmol) and 6mL of benzene were added to the solution 50% sodium hydroxide solution. The mixture was stirred at 35 degrees Celsius for 12 h. After 12h, the reaction solution was poured into ice water, immediately extracted twice with dichloromethane, and the organic phase solutions were combined. Then the organic phase solution was washed 4 times with water and saturated brine in turn, and then dried over anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain the crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain the brown powder of compo...

Embodiment 3

[0019] Example 3 Synthesis of O-(tetrahydropyrrolyl) ethyl derivative (III) of SalviskinoneA

[0020] Compound II (209 mg, 0.5 mmol) was dissolved in 20 mL of acetonitrile, and anhydrous potassium carbonate (345 mg, 2.5 mmol), potassium iodide (84 mg, 0.5 mmol) and pyrrolidine (1420 mg, 20 mmol) were added thereto, and the mixture was heated to reflux for 8 h. After the reaction, the reaction solution was poured into ice water, extracted with the same amount of dichloromethane three times, and the organic phases were combined. The combined organic phase was washed with water and saturated brine in turn, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.0, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain the yellow powder of compound III (131.6mg, 6...

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PUM

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry and in particular relates to a composition, a preparation method and an application of the composition to preparation of medicines for preventing or treating pancreatic fibrosis. The invention discloses the composition and the preparation method thereof. Pharmacological experiments show that the composition has the function of preventing or treating pancreatic fibrosis and has the value in developing the medicines for preventing or treating pancreatic fibrosis.

Description

Technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to compositions, preparation methods and uses thereof. Background technique [0002] Pancreatic fibrosis is a common feature of chronic pancreatitis caused by various reasons, and it is also the accompanying histopathological characteristics, which is manifested as a large number of fibroblast proliferation and extracellular matrix rich in connecting tissues. It is the result of the repair of pancreatic damage caused by various reasons. Recently, it has been discovered that pancreatic stellate cells and various cytokines are related to pancreatic fibrosis. The current incidence of pancreatic fibrosis is increasing. There is an urgent need to develop highly effective and low-toxic anti-pancreatic fibrosis drugs. . [0003] Treatment of pancreatic fibrosis The existing drugs have the problems of high toxicity and low safety. It is most important to find compounds or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4453A61P1/18A61K31/40
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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