New compound with radiation protection function, preparation method and pharmaceutical application thereof

Abstract

The invention provides a new compound with a radiation protection function, and pharmaceutically acceptable salt, pro-drug and solvate. The compound and the pharmaceutically acceptable salt, pro-drug and solvate are as shown in formula (I): a chemical formula is shown in the original PDF, wherein W is selected from carbonyl, sulfoxide and sulfonyl; R<1> is selected from substituted or un-substituted aromatic ring or aromatic heterocycle: chemical formulae are shown in the original PDF; X is selected from carbon and nitrogen; R<4> is selected from hydrogen, halogen, cyan, substituted or un-substituted C1-3 alkyl or alkoxy, methyl, trifluoromethyl, methoxyl, and trifluoromethoxy; R<2> is selected from the following perssad: chemical formulae are shown in the original PDF; R<3> is selected from hydrogen, methyl, vinyl and the like; when the W is selected from the sulfonyl, and the R<1> is selected from 4-fluorophenyl, 4-chlorophenyl, 4-iodophenyl and 4-trifluoromethoxy phenyl, the R<2> cannot be selected from 4-carboxyphenyl and 4-carboxyphenyl sodium, and the R<3> cannot be selected from the hydrogen; and when the W is selected from the sulfoxide and the R<1> is selected from 4-fluorophenyl, 4-chlorophenyl, and 4-iodophenyl, the R<2> cannot be selected from 4-carboxyphenyl and 4-carboxyphenyl sodium, and the R<3> cannot be selected from the hydrogen.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the aspect of ionizing radiation damage protection, in particular to a class of new compounds with radiation protection effect. [0002] The present invention also relates to the preparation method of the compound. [0003] The present invention also relates to the application of the compound in the prevention and treatment of related damage and disease treatment caused by ionizing radiation. Background technique [0004] With the vigorous development of the global nuclear industry, nuclear technology has been widely used in various fields such as nuclear power plants, aerospace, national defense, and biomedicine. Human beings are more likely to be exposed to ionizing radiation and cause damage. The hidden dangers of nuclear war and nuclear terrorism, the protection and treatment of body damage caused by ionizing radiation (referred to as radiation damage) are receiving more and more att...

AI Technical Summary

Problems solved by technology

[0005] On the other hand, the incidence of malignant tumors and the number of patients have been on the rise in recent years. Radiation therapy, as one of the main treatment methods, plays an indispensable role, but high-dose radiation exposure will inevitably lead to normal Acute radiation damage to tissues, organs and even the whole body, the side effects caused by radiation damage seriously limit the wide application of radiation therapy in tumor treatment, and also significantly affect the curative effect of radiation therapy and the quality of life of cancer patients after treatment

[0006] At present, the existing drugs related to the treatment of radiation damage mainly include: sulfur-containing compounds, hormones, cytokines, and Chinese herbal medicines, etc., which have their own inherent defects: for example, sulfur-containing compounds generally have relatively large side effects, and amifostine (also known as amifostine ) as the representative of this type of compound is currently recognized as the compound with the best protective effect, and is the first selective broad-spectrum cytoprotective agent passed by the international regulatory agency, but the half-life is extremely short (7 minutes) and expensive (domestic The medical market price is 400-500 yuan / branch) which limits its application; while the prevention and treatment of hormonal drugs to radiation damage is mainly to bone marrow nucleated cells, hematopoietic stem cells and progenitor cells, and the impact of such drugs on sexual organs and reproductive system It limits its wide use; cytokine drugs such as interleukins and colony-stimulating factor drugs can alleviate and treat the damage to the bone marrow hematopoietic function system caused by radiation, but its radiation protection effect is closely related to the time of administration (used for prevention and In the medical practice of rescue and treatment, such drugs require high levels of medical testing and attention), have obvious inflammatory effects, are expensive, and are difficult to store at room temperature; anti-radiation components of Chinese herbal medicines mainly include phenols, polysaccharides, natural Flavonoids have the characteristics of unclear active ingredients and low toxicity. After years of research, there are no similar drugs on the market or to be listed

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