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Use of phthalimide derivative in preparation of medicament for resisting angiogenesis

A new angiogenesis and use technology, applied in anti-tumor drugs, drug combinations, cardiovascular system diseases, etc., can solve the problems of unpublished, poor water solubility, and high medicinal toxicity, and achieve the effect of inhibiting the proliferation of vascular endothelial cells

Inactive Publication Date: 2007-05-16
北京恩华医药研究院有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the disadvantages of thalidomide and its derivatives disclosed in the prior art are poor water solubility and high toxicity as a medicine
In the existing literature, the composition containing the phthalimide water-soluble derivatives of the present invention and the use of the phthalimide water-soluble derivatives of the present invention for the prevention and treatment of new diseases have not been disclosed so far. Uses for Angiogenesis

Method used

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  • Use of phthalimide derivative in preparation of medicament for resisting angiogenesis
  • Use of phthalimide derivative in preparation of medicament for resisting angiogenesis
  • Use of phthalimide derivative in preparation of medicament for resisting angiogenesis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: Preparation of phthalimide derivatives (TD-1 to TD-18) of general formula I

[0047] Secondary amines (0.05 mol) were dissolved in 10 ml of dry benzene, and slowly dropped into dry benzene containing N-(bromoalkyl)-phthalimide (0.01 mol). After dripping, stir and reflux for 24h. 50ml of water was added to the reaction solution, and the layers were shaken, the benzene layer was separated, 10% hydrochloric acid was added, the water layer was separated and extracted with benzene (20ml×3). The aqueous layer was neutralized with 1N sodium hydroxide solution to pH 11, extracted with ether, combined with ether solution, washed with saturated sodium chloride solution and water in turn until neutral, dried overnight with anhydrous sodium sulfate, filtered, and hydrochloric acid was added to the filtrate After diethyl ether solution, a large amount of white precipitates were formed immediately. After filtration, the white precipitates were recrystallized (ethanol: ...

Embodiment 2

[0049] Example 2: (±)-N-(2-dimethylamino-ethyl)-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H )-Diketone hydrochloride (TD-19) preparation.

[0050] Take 2g of 1-chloro-2-dimethylamino-ethane hydrochloride, add 5ml of water to dissolve, ice bath, add 10% sodium hydroxide solution, adjust the pH value to 11, extract with ether (10ml×3), and combine the extracts , dried over night with anhydrous sodium sulfate, filtered, ether solution was removed under reduced pressure and low temperature (20-25°C), during this process, a small amount of solid appeared, which was the self-reaction product of 1-chloro-2-dimethylamino-ethane, Filter off the solid, add 20ml of dioxane, (±)-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione ( Lilidomide) 0.26g, anhydrous potassium carbonate 0.27g, stirred and refluxed for 2h, filtered, added 20ml of water in the filtrate, after shaking and layering, separated the dioxane layer, added 20ml of 10% hydrochloric acid, separated the aqueous layer...

Embodiment 3

[0051] Example 3: (±)-N-(2-diethylamino-ethyl)-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H ) - Preparation of diketone hydrochloride (TD-20).

[0052] Take 3g of 1-chloro-2-diethylamino-ethane hydrochloride and add 5ml of water to dissolve it. The solution is lavender red, put it in ice bath, add 10% sodium hydroxide solution, adjust the pH value to 11, extract with ether (10ml× 3), combine the extracts, dry overnight with anhydrous sodium sulfate, filter, the filtrate is light yellow, ether solution is removed under reduced pressure and low temperature (20-25°C), during this process, a small amount of white solid appears, which is 1-chloro- 2-Diethylamino-ethane self-reaction product, filter out the solid, add 20ml of dioxane, (±)-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole- 0.26g of 1,3(2H)-diketone (thalidomide) and 0.27g of anhydrous potassium carbonate were stirred and refluxed for 2h. The purification method is the same as TD-19. A large amount of white precipitate w...

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Abstract

The invention relates to the action of phthalimide derivatives of formula I and II in the preparation of medicament against angiogenesis, wherein the definitions of each substituent group are described in the specification.

Description

technical field [0001] The invention relates to the use of phthalimide derivatives in the preparation of medicines for treating neovascularization. Background technique [0002] Angiogenesis refers to the process of generating new blood vessels from the existing vascular bed. Under normal circumstances, angiogenesis is strictly controlled by certain transient and specific physiological processes, such as: reproductive process, development process and wound The healing process etc. Sustained angiogenesis is a characteristic of certain diseases such as malignant growth of tumor tissue, diabetic retinopathy, arthritis and bone hyperplasia. [0003] Tumor metastasis refers to the process of malignant tumor cells moving from the original site to other parts of the body and forming new lesions. Studies have found that a tumor with a volume of 1-2 mm can obtain nutrients from the surrounding tissue through osmosis to maintain its own survival, but its further growth depends on th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4035A61K31/454A61P35/00A61P3/10A61P9/10A61P19/10
Inventor 汪海杨永林王林刘静霞包存刚
Owner 北京恩华医药研究院有限公司
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