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Composition and application thereof to chronic obstructive pulmonary disease (COPD) resistant medicines

A chronic obstructive, composition technology, applied in the directions of drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of slow progress in drug treatment research, different pathogenesis, and difficulty in obtaining satisfactory curative effects.

Inactive Publication Date: 2016-02-03
南京海澳斯生物医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is no drug that can curb the progressive development of COPD, and the research progress of its drug treatment is quite slow. At present, the drug for treating asthma is often used in clinical practice to treat COPD. Because the pathogenesis of COPD is different from that of asthma, it is difficult to obtain satisfactory curative effect.

Method used

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  • Composition and application thereof to chronic obstructive pulmonary disease (COPD) resistant medicines
  • Composition and application thereof to chronic obstructive pulmonary disease (COPD) resistant medicines
  • Composition and application thereof to chronic obstructive pulmonary disease (COPD) resistant medicines

Examples

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Embodiment 1

[0012] The preparation of embodiment 1 compound Artalbicacid

[0013] The preparation method of compound Artalbicacid (I) refers to the method published by Antonella Maggio et al. (Antonella Maggio et al., 2011. Artalbicacid, asesquiterpenewithanunusualskeletonfromArtemisiaalba (Asteraceae) fromSicily.TetrahedronLetters, 52 (2011) 4543-4545).

[0014]

Embodiment 2

[0015] The synthesis of the O-bromoethyl derivative (II) of embodiment 2 Artalbicacid

[0016] Compound I (266 mg, 1.00 mmol) was dissolved in 10 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 40 °C for 16 h. After 16 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine for 5 times successively, then dried with anhydrous sodium sulfate, and finally 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 a brown powder of Compound II (272mg, 73%...

Embodiment 3

[0021] Synthesis of O-(piperazinyl) ethyl derivative (III) of embodiment 3 Artalbicacid

[0022] Compound II (187mg, 0.5mmol) was dissolved in 25mL of acetonitrile, anhydrous potassium carbonate (345mg, 2.5mmol), potassium iodide (84mg, 0.5mmol) and anhydrous piperazine (3446mg, 40mmol) were added thereto, and the mixture was heated to reflux 4h. After the reaction was completed, the reaction solution was poured into 20 mL of ice water, extracted twice with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, 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=100:1.5, v / v), the light brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of compoun...

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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 chronic obstructive pulmonary disease (COPD) resistant medicines. The invention discloses the composition and the preparation method thereof. Pharmacological experiments show that the composition has the function of resisting COPD and has the value in developing the COPD resistant medicines.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Chronic obstructive pulmonary disease (chronic obstructive pulmonary disease, COPD) is a common chronic disease worldwide, currently ranking fourth in the global cause of death, according to the World Health Organization forecast, by 2020, COPD will rank fifth in the incidence of global diseases , ranking third among the causes of death. [0003] COPD is a disease characterized by not fully reversible airflow limitation associated with an abnormal inflammatory response of the lungs to noxious gases or noxious particles, with chronic inflammation throughout the airways, lung parenchyma, and pulmonary vessels. The cells involved in COPD include inflammatory cells such as neutrophils, T lymphocytes, and macrophages. When the cells are activated, they release variou...

Claims

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Application Information

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IPC IPC(8): A61K31/495A61P11/00C07D295/088C07D233/60A61K31/4164
Inventor 丁秋菊
Owner 南京海澳斯生物医药科技有限公司
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