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Pharmaceutical composition and application thereof using anophylline derivatives as active ingredients

A kind of technology of fenugreek, derivative, applied in the pharmaceutical composition and application field of fenutraline derivative as active ingredient, can solve problems such as unreported

Active Publication Date: 2020-08-11
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no report on the medicines of the anophylline derivatives (1-6) provided by the present invention as melatonin and 5-hydroxytryptamine receptor agonists and active ingredients for antipsychotic diseases, and its derivatives or pharmaceutical compositions thereof are used as Melatonin and serotonin receptor agonists have not been reported in the preparation or treatment of antipsychotic drugs

Method used

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  • Pharmaceutical composition and application thereof using anophylline derivatives as active ingredients
  • Pharmaceutical composition and application thereof using anophylline derivatives as active ingredients
  • Pharmaceutical composition and application thereof using anophylline derivatives as active ingredients

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0021] Anophylline (2mmol) was dissolved in 10mL anhydrous toluene with ethylamine, pyrrole, piperidine, N-isopropylpiperazine, N-methylhomopiperazine and homopiperazine (2-10mmol) respectively, and refluxed at 110°C To the end of the reaction, the solvent was recovered under reduced pressure to prepare a crude product, which was purified by silica gel column chromatography (diethylamine / methanol / chloroform, v / v / v, 2 / 4 / 94~3 / 5 / 92) to obtain the target compound ( 1‐6):

[0022] Compound 1‐6 structure determination data:

[0023] N,N‐Diethyl‐3‐indolylmethylamine (N,N‐Diethyl‐3‐indolylmethylamine, 1): white powder, yield 97%. 1 H NMR (400MHz, CDCl 3 )δ H :8.93(s,1H,NH),7.78‐7.00(m,5H,H‐2,4,5,6,7),3.87(s,2H,‐CH 2 N),2.69‐2.65(m,4H,

[0024] N‐Pyrrolyl‐3‐indolylmethylamine (N‐Pyrrolyl‐3‐indolylmethylamine, 2): white powder, yield 96%. 1 H NMR (400MHz, CDCl 3 )δ H :9.27(s,1H,NH),7.75‐7.00(m,5H,H‐2,4,5,6,7),3.91(s,2H,CH 2 N),2.68(m,4H,H‐2',5'), Piperazinyl‐3‐indolylmethyl...

Embodiment 1

[0043] The anophylline derivative 1-6 prepared according to the method of Preparation Example 1 was dissolved in a small amount of DMSO separately or mixed, and then added with water for injection as usual, finely filtered, potted and sterilized to make an injection.

Embodiment 2

[0045] According to the method of Preparation Example 1, firstly prepare the stephanine derivatives 1-6, separately or mixed, after dissolving with a small amount of DMSO, dissolve it in sterile water for injection, stir to dissolve, and use a sterile suction filter funnel Filtration, and then aseptic fine filtration, sub-package in ampoules, freeze-drying at low temperature and then aseptically melt-seal to obtain powder injection.

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Abstract

The invention provides pharmaceutical compositions taking gramine derivatives (1-6) as active ingredients, application of the derivatives and the pharmaceutical compositions prepared from the derivatives as agonist for melatonin and a serotonin receptor, and application of the derivatives and the pharmaceutical compositions prepared from the derivatives in preparation of medicines for treating or relieving central nervous system diseases related to the melatonin and the serotonin receptor.

Description

technical field [0001] The present invention belongs to the technical field of medicines, in particular, it relates to a pharmaceutical composition with the anophylline derivatives shown in structural formulas 1-6 as active ingredients, their preparation methods, and the use of such derivatives and their pharmaceutical compositions as catharpine derivatives. Melatonin and serotonin receptor agonists, and their application in the preparation of medicines for treating or improving central nervous system diseases related to melatonin and serotonin receptors. Background technique [0002] Melatonin receptor is a neuroendocrine hormone secreted by the pineal gland. It is controlled by the suprachiasmatic nucleus of the hypothalamus and can regulate the circadian rhythm. This rhythmic fluctuation shows that it reaches a peak at night and drops to a valley during the day. McCord and Allan discovered in 1917 that the bovine pineal gland can regulate changes in the skin of Rana pipie...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/551A61K31/496A61K31/404A61K31/4045A61K31/454A61P25/00A61P25/28
CPCA61K31/404A61K31/4045A61K31/454A61K31/496A61K31/551A61K2300/00
Inventor 陈纪军尹秀娟马云保黄晓燕耿长安张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI