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Medicine tromantadine with adamantane structure, anti-tumor application of derivates and analogs thereof having new indications

A kind of technology of tramandamide and derivatives, applied in the application field of disease medicine

Inactive Publication Date: 2011-05-25
LIAONING LIFENG SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Systematic search of domestic and foreign patents and articles, the research on the anti-tumor activity of the above-mentioned drugs and the application of new anti-tumor indications have not been reported yet

Method used

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  • Medicine tromantadine with adamantane structure, anti-tumor application of derivates and analogs thereof having new indications
  • Medicine tromantadine with adamantane structure, anti-tumor application of derivates and analogs thereof having new indications
  • Medicine tromantadine with adamantane structure, anti-tumor application of derivates and analogs thereof having new indications

Examples

Experimental program
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Effect test

preparation example Construction

[0024] 3. Preparation of salts of test compounds

[0025] Take a certain amount of this product, and dissolve it quantitatively in methanol, acetone, 4-hydrofuran or 1,4-dioxane. If the dissolution is not good, you can properly heat it on the basis of keeping the compound stable to make it a true solution. Cool in an ice-water bath and stir at this temperature to slowly feed dried hydrogen chloride gas until it is completely saturated, and then keep feeding it for 5 minutes. Keep the salt-forming reaction for 1-2 hours, and detect the reaction by thin-layer chromatography until all the salts are formed. Evaporate the solvent under reduced pressure and dry under reduced pressure.

[0026] Pharmaceutically acceptable salts of the compounds of the present invention are also within the scope of the present invention, and their acids can be salted by reacting with bases, such as sodium carbonate, sodium hydride, potassium hydroxide, ammonium hydroxide and the like. Containing a n...

Embodiment 1

[0032] Embodiment 1. Structural identification of tromantine

[0033] 1 H NMR (CDCl 3 )δ6.78(s, 1H), 3.83(s, 2H), 3.75(m, 2H), 2.51(m, 2H), 2.28(s, 6H), 2.07(s, 3H), 2.02(m, 6H ), 1.68 (m, 6H); MS / e: 281 (M+1).

Embodiment 2

[0035] Anti-tumor preparation: Weigh 8.0g tromantine, add 50ml DMSO, stir to dissolve, add 500ml 1,2-propanediol and 100ml Tween 80 after dissolving, stir and mix evenly, add water for injection to a total volume of 5000ml, use 0.22μm Membrane filtration, packaging, autoclaving at 100°C for 30 minutes, leak detection, full inspection, packaging, that is, 8mg / 5ml (ammonia bottle), a total of 1000 pieces.

[0036] In vitro anti-tumor experiment example

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Abstract

The invention discloses a medicine tromantadine with an adamantane structure, and adamantane derivates and analogs of the tromantadine, wherein the tromantadine and the adamantane derivates and analogs of the tromantadine have new activity and new indications. The invention further relates to the application of the compounds serving as anti-tumor medicines. The medicine tromantadine has a structure as shown in the specification; and the derivates and analogs generated through the structure, various compounds having the same / or the different structure as the mother nucleus structure of the compound or having similarity or correlation with the compound in the aspect of bioactivity, inorganic acid salts, organic acid salts, inorganic alkali salts, organic alkali salts or compound salts of the adamantane derivates and analogs and prodrugs of inorganic acid salts, organic acid salts, inorganic alkali salts, organic alkali salts or compound salts, are included. The derivates and analogs have the anti-tumor pharmacological activity and are applied as antitumor medicines and used in combination with other know anti-tumor medicines. The derivates and analogs are accompanied with the tumor treatment application when used in the treatment of tumor related diseases or other diseases, the application includes the treatment of diseases caused by virus, bacteria and fungi, nerve system diseases, endocrine system diseases, immune system diseases and the like, and the derivates and analogs are matched with other medicines for application.

Description

technical field [0001] The present invention relates to tromantine, a drug with an adamantane structure, and its derivatives and analogues, which have new anti-tumor activities and new indications, and also relates to the application of such compounds as anti-tumor and other disease drugs. Background technique [0002] Tromantadine (Tromantadine, see chemical structure for chemical structure) has been used clinically for many years as an antiviral drug, a drug for treating acne, and a drug for treating tuberculosis. In terms of literature and patents at home and abroad, after a systematic search of literature, it is found that in addition to the original indications of the above-mentioned drugs, there are a large number of researches and inventions of new indications and applications at home and abroad. These domestic and foreign literature reports and patent inventions mainly focus on In the application of anti-new virus, the activity and neuroprotection of the nervous syst...

Claims

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Application Information

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IPC IPC(8): C07C235/14A61K31/16A61P35/00A61P35/02A61P31/12A61P31/04A61P31/10
CPCA61K31/16C07C2103/74C07C235/14A61P31/04A61P31/10A61P31/12A61P35/00A61P35/02C07C2603/74A61K2300/00
Inventor 徐利锋
Owner LIAONING LIFENG SCI & TECH DEV
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