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Combination of dihydroporphin derivative and ultrasound medical system

Pending Publication Date: 2021-08-03
于波
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The sonosensing agents reported so far show a large difference in selectivity for tumor cells, a narrow therapeutic window, poor solubility under physiological conditions, and a slow clearance rate in the body, making it difficult to reflect clinical value.
In addition, in the current sonodynamic therapy, the treatment system used is single in structure and small in size, which can only act on the patient's local area, but cannot treat the patient in an all-round way, and cannot effectively kill the current medical equipment and instruments. Detectable extremely small malignant tumors that have already occurred in the human body
Therefore, for patients whose malignant tumors have metastasized throughout the body, or for patients whose malignant tumors are undergoing systemic metastases after cancer surgery, the existing treatment system cannot treat them in a timely and effective manner
Since the existing ultrasonic therapy systems are all single-head transducers, and for lesions in different parts of the same patient, doctors cannot treat them at the same time and select ultrasonic transducers according to the needs of treatment.
Moreover, using a single-head ultrasonic transducer to treat the patient's whole body requires dozens of hours of continuous work to complete, thus greatly increasing the workload of the doctor, causing unbearable treatment time for the patient and missing the best treatment opportunity

Method used

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  • Combination of dihydroporphin derivative and ultrasound medical system
  • Combination of dihydroporphin derivative and ultrasound medical system
  • Combination of dihydroporphin derivative and ultrasound medical system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0199] The preparation of embodiment 1. compound 8-BA and 9-BA (Pd)

[0200] The synthetic route of compound 8-BA and 9-BA (Pd) is as follows:

[0201]

[0202] Each step in the above-mentioned synthetic route is specifically as follows:

[0203] Dissolve 541 mg of compound 1 in 5% sulfuric acid methanol solution, concentration 0.1 M, react for 10 hours, concentrate under reduced pressure, dilute the obtained acid with an equal volume of dichloromethane (DCM), wash with water, collect the organic phase, and concentrate to obtain compound 2 , directly used in the next reaction without separation.

[0204]Dissolve compound 2, the product of the previous step, in dimethylformamide (DMF) at a concentration of 0.1M, add 435 mg of benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate (HBTU ) and 189 μL N,N-diisopropylethylamine (DIEA), after stirring for 0.5-1 hour, add 417 mg β-alanine tert-butyl ester hydrochloride and 379 μL DIEA successively, continue to react for ...

Embodiment 2

[0211] Embodiment 2. The impact of compound 9-BA (Pd) on breast cancer and breast cancer metastasis

[0212] Using the water-soluble chlorin derivative 9-BA (Pd) synthesized in Example 1 as a sonosensitizer (abbreviated as a sonosensitizer), the ultrasonic medical system provided in Example 7 was used to treat tumor-bearing mice with lung metastasis of breast cancer. The sonodynamic therapy was evaluated.

[0213] The water-soluble chlorin derivative 9-BA(Pd) is dissolved in physiological saline to prepare a drug solution for administration. 4T1 mouse breast cancer cells were inoculated directly under the second pair of nipples on the left side of Balb / c (female, 18-22 g) mice to construct a mouse breast cancer lung metastasis model, and the tumor volume and mouse tumor volume were recorded on the 7th day after inoculation. Body weight was measured every other day. The tumor-bearing mice were randomly divided into 4 groups: (1) a control group (normal saline alone), (2) b ul...

Embodiment 3

[0218] Embodiment 3. The preparation of compound 17-MPA and 18-MPA (Pd)

[0219] The synthetic route of compound 17-MPA and 18-MPA (Pd) is as follows:

[0220]

[0221] Each step in the above-mentioned synthetic route is specifically as follows:

[0222] 1000mg of compound 1-chlorin e6 was dissolved in dimethylformamide (DMF) at a concentration of 0.1M, added 1043μL of iodomethane and 4633mg of anhydrous potassium carbonate, stirred for 2 hours, and diluted with dichloromethane (DCM) The reaction solution was washed with water, the collected organic phase was concentrated, and 200-300 mesh silica gel column chromatography was eluted with ethyl acetate / dichloromethane=1:100 to obtain 962 mg of compound 10 with a yield of 90%.

[0223] Dissolve 800 mg of compound 10 and 675 μL of p-methoxystyrene in dichloromethane (DCM) at a concentration of 0.03 M, add 319 mg of Grubbs catalyst, and then reflux for 20 hours. After the reaction solution is filtered, the filtrate is transfer...

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Abstract

The present invention relates to a combination of a chlorin derivative or a pharmaceutically acceptable salt thereof having a structure represented by formula (I) and an ultrasonic medical system comprising a transducer acoustic bed and a contact agent, wherein the transducer acoustic bed comprises a bottom and a wall extending upwardly from the bottom; the bottom is provided with at least one ultrasonic transducer at the positions corresponding to the head, the trunk and the four limbs of the target respectively, and the ultrasonic transducers are used for transmitting ultrasonic waves to the target located above the ultrasonic transducers; the wall part is provided with at least one ultrasonic transducer at the position corresponding to the head and the four limbs of the target so as to transmit ultrasonic waves to the target; the contact agent is used for transmitting ultrasonic waves between the target and the ultrasonic transducer. The invention also relates to a method for preparing the chlorin derivative or the medicinal salt thereof.

Description

technical field [0001] The invention belongs to the field of biomedicine; more specifically, the invention relates to a combination of a chlorin derivative or a pharmaceutically acceptable salt thereof and an ultrasonic medical system for comprehensive treatment of patients. Background technique [0002] Photodynamic therapy (PDT) and sonodynamic therapy (SDT) are to trigger a chemical reaction to kill the Modern medical technology of tumor cells. [0003] Photodynamic therapy (PDT) is a new method of treating tumors or diseases with photosensitizers and laser activation. It uses photosensitizers to generate singlet oxygen ( 1 o 2 ) react with free radicals to kill tumor cells. Compared with traditional treatment methods such as surgery, chemotherapy, and radiotherapy, PDT has the advantages of less side effects on the body and no damage to internal organs, etc., but it is ineffective in the treatment of deep tumors in the body. At present, some photosensitive compounds ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61N7/00A61K41/00A61P35/00C07D487/22
CPCA61N7/00A61K41/0033A61P35/00C07D487/22
Inventor 苏江安赵伟杰Q·李王夏青于波
Owner 于波
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