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Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs

A technology of pyrimidine bases and anti-inflammatory drugs, applied in the field of biochemistry, can solve problems such as differences in pharmacodynamics and metabolic kinetics

Active Publication Date: 2014-12-10
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the physical and chemical properties of enantiomeric drugs are basically the same in vitro, because the receptors or targets that drug molecules act on are chiral proteins and nucleic acid macromolecules composed of amino acids, nucleosides, membranes, etc., They have certain requirements for the three-dimensional configuration of the drug molecules bound to them. Therefore, enantiomeric drugs often show great differences in pharmacodynamics and metabolic kinetics in vivo.

Method used

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  • Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs
  • Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs
  • Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1, the preparation of tablet

[0031] Formula: JP-8g (purity greater than 95%) 20.0g

[0032] Filler 180.0g

[0033] Disintegrant 10.0g

[0034] Adhesive 6.0g

[0035] Lubricant 3.0g

[0036] Total 200.0g

[0037] Process: 1000 tablets were made according to the conventional process for preparing tablets, each containing 20 mg of JP-8g.

[0038] Usage and dosage: twice a day, 2~3 tablets each time.

Embodiment 2

[0039] Embodiment 2: the preparation of soft capsule

[0040] Formula: JP-8g (purity greater than 95%) 50.0g

[0041] Filler 85.0g

[0042] Adhesive 5.0g

[0043] Lubricant 10.0g

[0044] Total 200.0g

[0045] Process: According to the conventional process for preparing capsules, 1000 capsules are made, and each capsule contains 50 mg of JP-8g.

[0046] Usage and dosage: twice a day, 2~3 capsules each time.

Embodiment 3

[0047] Embodiment 3, the preparation of injection

[0048] Formula: JP-8g (purity greater than 95%) 100.0g

[0049] Citric acid 1.0g

[0050] Sodium citrate 0.5g

[0051] Sodium chloride 18.0g

[0052] Water for injection 2000ml

[0053] Process: According to the conventional process for preparing injections, a total of 1000 2ml injections were prepared, each containing 100 mg of JP-8g.

[0054] Usage and dosage: twice a day, 1~2 sticks each time.

[0055] The fillers, disintegrants, binders, lubricants and other auxiliary materials in the above-mentioned embodiments are the most conventional auxiliary materials in pharmacy.

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Abstract

The invention provides a new medical application of a chiral spiro indole-pyran pyrimidine base compound, particularly application of the compound in preparation of anti-inflammatory drugs. An in vitro cyclooxygenase (COX) activity inhibiting experiment, an experiment of inhibiting generation of an inflammatory molecule (nitric oxide) in primary mice macrophage and inhibition test on an ear swelling and paw edema model in mice, show that the chiral compound has an obvious anti-inflammatory effect and has extremely low gastrointestinal injury effect; therefore, the chiral compound, as an active ingredient, can be prepared into anti-inflammatory drugs in various dosage forms through pharmaceutically acceptable technologies and auxiliary materials, so that the chiral compound has an excellent medical application prospect.

Description

technical field [0001] The invention belongs to the technical field of biochemistry, and relates to a new medical application of a chiral spirocyclic indole-pyranyrimidine base compound, in particular to the use of a chiral spirocyclic indole-pyranyrimidine base compound in the preparation of anti-inflammatory drugs in the application. Background technique [0002] Chiral drugs are composed of chiral compounds with pharmacological activity, which play a therapeutic role in the human body through chiral matching and recognition with biomacromolecules. Although the physical and chemical properties of enantiomeric drugs are basically the same in vitro, because the receptors or targets that drug molecules act on are chiral proteins and nucleic acid macromolecules composed of amino acids, nucleosides, membranes, etc., They have certain requirements on the three-dimensional configuration of the drug molecules bound to them. Therefore, enantiomeric drugs often show great differenc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/527A61P29/00
Inventor 王锐蒋先兴孙瑜隆
Owner LANZHOU UNIVERSITY