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Freeze-dried powder of antitumor drug and preparation method thereof

A technology of anti-tumor drugs and freeze-dried powders, which is applied in the direction of anti-tumor drugs, drug combinations, freeze-dried delivery, etc., and can solve the problems of low dependence of tumors on angiogenesis, adverse reactions, and drug resistance

Active Publication Date: 2021-09-24
江西润泽药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these tumor angiogenesis inhibitors have great advantages, there are still some problems in practical application, such as the dependence of some tumors on angiogenesis, drug resistance, adverse reactions and toxicity caused by mutation and compensatory tumor signal transduction.

Method used

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  • Freeze-dried powder of antitumor drug and preparation method thereof
  • Freeze-dried powder of antitumor drug and preparation method thereof
  • Freeze-dried powder of antitumor drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0044] The preparation method of the 1,4-diaminonaphthalene derivative shown in formula (I) can comprise the following steps:

[0045] (a) making the compound shown in formula (1) carry out dealkylation reaction, obtain the compound shown in formula (2);

[0046] (b) making the compound shown in formula (2) carry out nucleophilic substitution reaction, obtain the compound shown in formula (3);

[0047] (c) In the presence of tert-butanol hydroperoxide and potassium hydroxide, a hydroxyl group is introduced into the compound shown in formula (3) to obtain a compound shown in formula (4);

[0048] (d) Substituting the compound shown in formula (4) to obtain the compound shown in formula (5);

[0049] (e) making the compound shown in formula (5) undergo an affinity substitution reaction with an amino substituent to obtain a compound shown in formula (6);

[0050] (f) making the compound shown in formula (6) undergo a hydrogenation reduction reaction to obtain the target compoun...

preparation example 1

[0073] (1) Preparation of 3-methoxy-5-nitro-2-naphthol

[0074]

[0075] Dissolve 6,7-dimethoxy-1-nitronaphthalene (4.66g, 20mmol) and L-methionine (2.98g, 20mmol) in 38.4g of methanesulfonic acid (400mmol), and reflux the oil bath at 90°C Stir the reaction under heating conditions for 8 hours, after TLC detects that the reaction is complete, neutralize the reaction with a saturated sodium bicarbonate solution until no bubbles emerge, the pH test paper detects that it is neutral or weakly alkaline, and then extract the aqueous phase 3 times with ethyl acetate, The ethyl acetate phases were combined, washed three times with saturated sodium chloride, dried over anhydrous magnesium sulfate, filtered, evaporated to dryness under reduced pressure, and separated by column chromatography to obtain a yellow powdery solid (1.18 g, yield: 27%).

[0076] (2) Preparation of 4-(3-((3-methoxy-5-nitronaphthalene-2-) oxygen) propyl) morpholine

[0077]

[0078] Dissolve 3-methoxy-5...

Embodiment 1

[0109] Under a sterile environment, accurately weigh 0.5g of compound 1 and 0.5g of mannitol, place them in a clean preparation container, add 4ml of water for injection, stir until completely dissolved, then add water for injection to 5ml, and stir evenly to obtain frozen Dry stock solution.

[0110] Fill the lyophilized stock solution into a 10ml control glass bottle, stopper halfway, and transfer it to a freeze dryer for freezing treatment. The specific freeze-drying process is as follows: the lyophilized stock solution is quickly frozen to -25°C for 2 hours, and then vacuumed to 15Pa. Raise the temperature to -5°C at a rate of 2°C per hour, sublimate and dry for 12 hours, then raise the temperature to 20°C at a rate of 8°C per hour, analyze and dry for 8 hours, fully stopper, and cap to obtain the antineoplastic drug jelly Dry powder A1.

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Abstract

The invention relates to the field of medicinal chemistry, and discloses a freeze-dried powder of an antitumor drug and a preparation method thereof. The freeze-dried powder of the antitumor drug contains a pharmaceutically active component and an excipient, and the mass ratio of the pharmaceutically active component to the excipient is 1:0.5-8, wherein the pharmaceutically active component is 1,4-diaminonaphthalene derivatives represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The freeze-dried powder of the antitumor drug can inhibit VEGF, can be used for treating and / or preventing diseases related to epidermal growth factor receptor tyrosine kinase in mammals, and can also be used for treating tumor diseases.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a freeze-dried powder of an antitumor drug and a preparation method thereof. Background technique [0002] The results of clinical and basic medical research in recent years have confirmed that the occurrence, development and metastasis of tumors depend on the formation of new blood vessels. Tumor angiogenesis is the result of the interaction between tumor cells, vascular endothelial cells, and vascular extracellular matrix. Among them, the biological function of vascular endothelial growth factor VEFG (vascular endothelial growth factor) plays a key role in angiogenesis. [0003] Most cell growth factor receptors contain peptide sequences of tyrosine kinases, and overexpression or activation of different tyrosine kinase receptors can be seen in many tumors. According to the similarity of the peptide chain sequence and its structural characteristics, these receptors are divid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/136A61K47/10A61K47/26A61P35/00A61K31/40A61K31/4453A61K31/5375
CPCA61K9/19A61K31/136A61K31/40A61K31/4453A61K31/5375A61K47/10A61K47/26A61P35/00
Inventor 廖年生胡贤德徐海军
Owner 江西润泽药业有限公司
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