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Composition based on benzimidazole carboxylic acid compound and application thereof

A technology of benimidazole carboxylic acid and compound, applied in the field of medicine, can solve problems such as low yield, achieve the effects of high yield, easy operation and reducing congestion

Inactive Publication Date: 2020-09-29
嘉兴市爵拓科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing (1-4-piperidinyl)benzimidazole derivatives are used to treat nasal congestion, but the yield in the preparation process of the derivatives is low

Method used

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  • Composition based on benzimidazole carboxylic acid compound and application thereof
  • Composition based on benzimidazole carboxylic acid compound and application thereof
  • Composition based on benzimidazole carboxylic acid compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1: A kind of pharmaceutical composition for preventing and / or treating nasal congestion:

[0059] The present embodiment provides a pharmaceutical composition for preventing and / or treating nasal congestion, the main component of which is the benzoimidazole carboxylic acid compound, which is prepared by a method comprising the following steps:

[0060] 1) Dissolve 1.15 mol of benzoimidazole in 500 mL of DMF solution, add 1.47 mol of triethylamine in batches at 0°C, and continue to stir the resulting mixture at 50°C for 2 hours; then cool the solution to -5°C , and dropwise added 1.25mol of benzyl bromide at this temperature, after the dropwise addition was complete, stirred overnight at room temperature; added sufficient water and ethyl acetate into the solution, separated the organic phase, and extracted the aqueous phase with ethyl acetate (3×500mL ); the organic layers were combined and washed with saturated brine, anhydrous Na 2 SO 4 Dry and concentrate...

Embodiment 2

[0068] Embodiment 2: another kind of pharmaceutical composition for preventing and / or treating nasal congestion:

[0069] This embodiment provides another pharmaceutical composition for the prevention and / or treatment of nasal congestion, which differs from Example 1 only in that the main component of the pharmaceutical composition described in this embodiment is the bemimidazole carboxylic acid compound Prepared via a process comprising the following steps:

[0070] 1) Dissolve 1.15 mol of benzoimidazole in 500 mL of DMF solution, add 1.47 mol of triethylamine in batches at 0°C, and continue to stir the resulting mixture at 50°C for 2 hours; then cool the solution to -5°C , and dropwise added 1.25mol of benzyl bromide at this temperature, after the dropwise addition was complete, stirred overnight at room temperature; added sufficient water and ethyl acetate into the solution, separated the organic phase, and extracted the aqueous phase with ethyl acetate (3×500mL ); the org...

Embodiment 3

[0075] Example 3: Another pharmaceutical composition for preventing and / or treating nasal congestion:

[0076] Embodiment 3 is substantially the same as Example 1, and its difference is that in embodiment 3, the ethyl bromoacetate in step 2) is replaced by methyl o-bromobenzoate (96.3% yield), and its structural formula is as follows (5 ) as shown in:

[0077]

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PUM

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Abstract

The invention belongs to the field of medicine and pharmacology, and particularly relates to a pharmaceutical composition taking benzimidazole carboxylic acid and pharmaceutically acceptable salt thereof as active ingredients. The pharmaceutical composition taking the benzimidazole carboxylic acid and pharmaceutically acceptable salt thereof as main active ingredients is used for preventing and / ortreating respiratory tract reaction and nasal congestion caused by allergic reaction, nasal congestion caused by other reasons and other symptoms, and can realize immediate and / or lasting alleviationof congestion. The invention also provides a method of treating and / or alleviating and / or preventing nasal congestion in a patient, the method comprising administering to a patient in need thereof aneffective amount of the pharmaceutical composition of the benzimidazole carboxylic acid or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a bemimidazole carboxylic acid compound and an application thereof. Background technique [0002] Respiratory diseases are a common and important cause of illness and death worldwide. In general, respiratory diseases include pathological conditions affecting the organs and tissues that enable gas exchange in mammals. The respiratory tract can be divided into upper and lower respiratory tracts. The upper airway can refer to the part of the respiratory system located above the sternal angle (outside the chest cavity), above the glottis (vocal cords), or above the cricoid cartilage. It consists of the nasal cavity and paranasal sinuses, the pharynx (nasopharynx, oropharynx, and pharynx), and sometimes the larynx. Exposure to potentially toxic or pathogenic agents present in the environment is increased compared to the rest of the body due to gas exchange with the environment i...

Claims

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Application Information

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IPC IPC(8): C07D401/10C07D235/18C07D235/16A61K31/4439A61K31/4184A61P11/00A61P11/02
CPCA61P11/00A61P11/02C07D235/16C07D235/18C07D401/10
Inventor 不公告发明人
Owner 嘉兴市爵拓科技有限公司
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