Photosensitizers and MRI enhancers

A diagnostic agent, the technology of SARS virus, which is used in the treatment of the above diseases, can solve the problems of inefficiency, high toxicity, chemical and photochemical instability of photosensitizers in photoactive treatment of tumor cells, etc.

Inactive Publication Date: 2008-08-06
PHOTO DIAGNOSTIC DEVICES PDD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the photosensitizer disclosed in RU-2183956 has low selectivity to tumor tissue, high toxicity to normal organs and tissues, and low efficacy of photoactive treatment of tumor cells
Furthermore, these photosensitizers are chemically and photochemically unstable, and are very slowly metabolized and cleared from normal tissues

Method used

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  • Photosensitizers and MRI enhancers
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  • Photosensitizers and MRI enhancers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0173]Ammonia is added to the water until the pH of the solution is not less than 9. Chlorin e6 (0.1 g) was dissolved in the aqueous solution. An equimolar amount of zinc acetate (0.22 g) was added, and the reaction mixture was stirred at about 20°C for 15 minutes to obtain a complex formation reaction. The process and completion of the complex formation reaction are monitored by a spectrophotometer. Upon completion of the complex formation reaction, human serum albumin (SHA) (71 g) was added as a fixative to the reaction mixture. Once the immobilization reaction is completed (monitored by a spectrophotometer), the reaction product, the Zn-chlorin-e6 complex immobilized on the SHA, is purified by dialysis.

[0174] Figure 1 shows the (1) raw material chlorin e6 (λ max =656nm), (2) Zn-chlorin e6 complex (λ max =632nm) and (3) Zn-chlorin e6 complex immobilized on SHA (λ max =636nm) in the long-wave region of the visible light absorption spectrum.

[0175] Figure 1 shows that the for...

Embodiment 2

[0178] The synthesis process of the immobilized Zn-chlorin-e6 complex was carried out as shown in Example 1, but polyvinylpyrrolidone (PVP) (62g) was used as the immobilizer instead of human serum albumin (SHA).

[0179] As shown in Figure 4, (1) the raw material Chlorin-e6 (λ max =656nm), (2) Zn-chlorin e6 complex (λ max =632nm) and (3) Zn-chlorin e6 complex immobilized on PVP (λ max =638nm) is actually the same as the visible absorption spectrum shown in FIG. 1. When the metal complex is formed, an obvious 24nm shortwave shift of the long wave peak is observed, and a small 6nm longwave shift when immobilized on the polymer PVP. When the Zn-chlorin e6 complex is formed, the chlorin-e6 is at λ max The moderate intensity peak at 502nm almost disappeared. All these changes indicate the completion of the reaction and the purity and homogeneity of the product obtained.

Embodiment 3

[0181] Ammonia is added to the water until the pH of the solution is not lower than 9. Then, chlorin e6 (1.0 g) was dissolved in the aqueous solution, an equimolar amount of SHA (71 g) was added, and the reaction mixture was stirred at about 20° C. for 17 minutes to immobilize the chlorin e6 on the SHA. Then an equimolar amount of zinc acetate (0.22 g) was added, and the reaction mixture was stirred at room temperature to complex the zinc with chlorin e6, which was monitored by a spectrophotometer. The reaction product Zn-chlorin-e6 complex immobilized on SHA was purified by dialysis.

[0182] Figure 3 shows (1) the raw material chlorin-e6(λ max =656nm), (2) Chlorin e6(λ max =662nm) and (3) Zn-chlorin e6 complex immobilized on SHA (λ max =636nm) in the long-wave region of the visible absorption spectrum. Different from the first synthesis method (see Example 1), when the chlorin-e6 immobilized on the protein is formed, the 6nm long-wave shift of the absorption peak first appears, ...

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Abstract

The present invention relates to the use of a compound of formula 3 or a salt thereof for preparing a medicament or a phototherapeutic agent for the treatment of the following diseases, including: acne; AIDS; viral hepatitis; diabetic retinopathy; atypical pneumonia virus infection; coronary Arterial stenosis; carotid artery stenosis; intermittent claudication; Asian (chicken) avian influenza virus infection; cervical dysplasia or various cancers including: blood cancer, cervical cancer, nasopharyngeal cancer, tracheal cancer, laryngeal cancer, bronchial cancer , bronchiolar cancer, bladder cancer, esophagus cancer, stomach cancer, rectal cancer, colon cancer, prostate cancer, hollow organ cancer, bile duct cancer, urinary duct cancer, kidney cancer, uterine cancer, vaginal cancer and other gynecological adnexal cancers. The present invention also relates to methods of treating the above diseases. The present invention further relates to the use of a compound of formula 3 or a salt thereof for the preparation of a photodiagnostic agent for the detection of the above-mentioned diseases and diseases including: atherosclerosis, multiple sclerosis, diabetes, arthritis, rheumatism Arthritis, fungal infection, viral infection, chlamydia infection, bacterial infection, or parasitic infection, HIV infection, hepatitis, herpes simplex, shingles, psoriasis, cardiovascular disease and skin disease. The present invention also relates to methods of detecting the above diseases using photodiagnostic agents. The present invention further relates to a method of cryogenically sterilizing a surgical device or other device, comprising the steps of: providing a compound of formula 3 or a salt thereof on the device; subjecting the device to radiation treatment or sonication. The present invention further relates to a compound of formula 3 or a salt thereof linked or attached to a magnetic element. This compound acts as an MRI enhancer. The present invention also relates to the use of such MRI enhancers for performing MRI scans.

Description

Technical field [0001] The present invention relates to the use of a compound of formula 3 or its salt to produce a medicament or optical therapeutic agent for the treatment of the following diseases, the diseases including: acne; AIDS; viral hepatitis; diabetic retinopathy; atypical pneumonia virus infection; Coronary artery stenosis; carotid artery stenosis; intermittent claudication; Asian (chicken) avian influenza virus infection; cervical dysplasia or various cancers, including: blood cancer, cervical cancer, nasopharyngeal cancer, tracheal cancer, laryngeal cancer, bronchus Cancer, bronchiolar cancer, bladder cancer, esophageal cancer, stomach cancer, rectal cancer, colon cancer, prostate cancer, hollow organ cancer, bile duct cancer, urinary duct cancer, kidney cancer, uterine cancer, vagina cancer and other gynecological accessory cancers. The present invention also relates to methods of treating the above diseases. [0002] The present invention also relates to the use of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K49/10
Inventor M·艾尔波特W·H·艾尔波特A·E·奥夫钦尼科夫
Owner PHOTO DIAGNOSTIC DEVICES PDD
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