KR-102964078-B1 - Composition for treating allergic disease comprising an arylethene derivative as an active ingredient

Abstract

The present invention relates to a pharmaceutical composition for treating or preventing one or more allergic diseases selected from the group consisting of hypersensitivity, allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, contact dermatitis, and urticaria, comprising as an active ingredient a compound selected from arylethene derivative compounds, pharmaceutically acceptable salts thereof, solvates thereof, or stereoisomers thereof. It has been confirmed that the compound inhibits the degranulation of mast cells and inhibits the elution of Evan Blue, reduces ear thickness, and inhibits the release of prostaglandin D2 in an animal model of cutaneous anaphylaxis, thereby making it useful as a treatment for allergic diseases.

Inventors

• 전소연
• 전용현

Assignees

• 재단법인 대구경북첨단의료산업진흥재단

Dates

Publication Date

20260513

Application Date

20231218

Claims (9)

1. A pharmaceutical composition for the treatment or prevention of allergic diseases comprising, as an active ingredient, a compound selected from an arylethene derivative compound represented by the following chemical formula 2, a pharmaceutically acceptable salt thereof, a solvate thereof, or a stereoisomer thereof, A pharmaceutical composition characterized in that the above allergic disease is one or more selected from the group consisting of hypersensitivity, allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, contact dermatitis, and urticaria: [Chemical Formula 2]
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4. In claim 1, The above composition is a pharmaceutical composition characterized by inhibiting the degranulation of mast cells.
5. In claim 1, The above composition is a pharmaceutical composition characterized by inhibiting the release of prostaglandin D2 .
6. A cosmetic composition for improving or preventing allergic diseases comprising, as an active ingredient, a compound selected from an arylethene derivative compound represented by the following chemical formula 2, a pharmaceutically acceptable salt thereof, a solvate thereof, or a stereoisomer thereof, wherein A cosmetic composition characterized in that the above allergic disease is one or more selected from the group consisting of hypersensitivity, allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, contact dermatitis, and urticaria: [Chemical Formula 2]
7. A health functional food composition for improving or preventing allergic diseases comprising, as an active ingredient, a compound selected from an arylethene derivative compound represented by the following chemical formula 2, a food-grade acceptable salt thereof, a solvate thereof, or a stereoisomer thereof, A health functional food composition characterized in that the above allergic disease is one or more selected from the group consisting of hypersensitivity, allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, contact dermatitis, and urticaria: [Chemical Formula 2]
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Description

Composition for treating allergic disease comprising an arylethene derivative as an active ingredient The present invention provides a composition for treating allergic diseases comprising an arylethene derivative as an active ingredient. Mast cells (MCs) are immune cells derived from hematopoietic precursors that play a major role in immediate-allergic reactions. Aggregation of high-affinity IgE receptors (FcεRI) and stimulation by neuropeptides in mast cells trigger the release of mediators such as histamine, proteases, and newly synthesized inflammatory mediators (e.g., prostaglandin D2 (PGD2), leukotriene C4 (LTC4), and various cytokines). Mast cells are the only cells that store formed tumor necrosis factor (TNF), which is rapidly released and influences the collection and activation of T-cells. The ability of mast cells to release multiple mediators facilitates active interactions with other cells in the surrounding environment, enabling them to participate in the development of mast cell-related diseases. Ultimately, mast cell activation can lead to various diseases that are life-threatening or directly cause allergic reactions, such as anaphylaxis, asthma, rhinitis, and atopic dermatitis. Therefore, inhibiting mast cell activation is strongly suggested as a potential treatment. Figure 1 shows the results of confirming the inhibitory effect on mast cell degranulation and cytotoxicity according to arylethene derivative compounds. Figure 2 shows the results of confirming the inhibitory effect on degranulation and cytotoxicity of bone marrow-derived mast cells according to arylethene derivative compounds. Figure 3 shows a schematic diagram of an experiment to confirm the drug treatment effect through animal testing. Figure 4 shows the results of confirming whether Evans blue leaked extravascularly due to an arylethene derivative compound. Figure 5 shows the results of confirming the change in ear thickness according to arylethene derivative compounds. Figure 6 shows the results of confirming the change in the release of prostaglandin D2 according to arylethene derivative compounds. The present invention will be described in more detail below. The present invention provides a pharmaceutical composition for treating or preventing allergic diseases, comprising as an active ingredient a compound selected from an arylethene derivative compound represented by the following chemical formula 1, a pharmaceutically acceptable salt thereof, a solvate thereof, or a stereoisomer thereof, wherein the allergic disease is one or more selected from the group consisting of hypersensitivity, allergic rhinitis, asthma, allergic conjunctivitis, allergic dermatitis, contact dermatitis, and urticaria. [Chemical Formula 1] In the above chemical formula 1, n is one of 0 to 5, and R1 to R3 may each be the same or different and may be one of hydrogen, hydroxy, and (C1-C10)alkyl, preferably in the above formula 1, n is one of 2 to 4, R1 and R2 are hydroxy, and R3 may be (C1-C5)alkyl. The arylethene derivative compound represented by the above chemical formula 1 may be DN200434 of the following chemical formula 2. [Chemical Formula 2] The above composition can inhibit the degranulation of mast cells. The above composition can inhibit the release of prostaglandin D2 . In another embodiment of the present invention, the pharmaceutical composition may further comprise one or more additives selected from the group consisting of suitable carriers, excipients, disintegrants, sweeteners, coating agents, leavening agents, lubricants, lubricants, flavoring agents, antioxidants, buffers, bacteriostatic agents, diluents, dispersants, surfactants, binders, and lubricants commonly used in the manufacture of pharmaceutical compositions. Specifically, the carrier, excipient, and diluent may be lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia gum, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil. Solid dosage forms for oral administration include tablets, pills, powders, granules, capsules, etc. These solid dosage forms may be prepared by mixing at least one excipient, for example, starch, calcium carbonate, sucrose or lactose, gelatin, etc., with the above composition. In addition, lubricants such as magnesium stearate and talc may also be used in addition to simple excipients. Liquid preparations for oral administration include suspensions, oral liquids, emulsions, and syrups, and may contain various excipients, such as humectants, sweeteners, flavorings, and preservatives, in addition to commonly used simple diluents like water and liquid paraffin. Preparations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, and suppositories. Propylen