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Application of chiral spiro indole-pyran pyrimidine base compound in preparation of anti-inflammatory drugs
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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: 2014-03-12
LANZHOU UNIVERSITY
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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 kineticsin vivo.
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Embodiment 1
[0032] Embodiment 1, the preparation of tablet
[0033] Formula: JP-8g (purity greater than 95%) 20.0g
[0055] Process: According to the conventional process for preparing injections, a total of 1000 2ml injections were prepared, each containing 100 mg of JP-8g.
[0056] Usage and dosage: twice a day, 1~2 sticks each time.
[0057] 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-pyranpyrimidine base compound, particularly application of the compound in preparation of anti-inflammatory drugs. An in vitrocyclooxygenase (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 present invention is a new pharmaceutical purpose involving a new pharmaceutical use of a handiculum-pipidine alkaline compound, especially the handiculum-pipidine alkaline compounds are preparing for anti-inflammatory drugs.Application. Background technique [0002] Handicated drugs are composed of hand -active compounds with pharmacological activity. It plays a therapeutic effect through hand -matching and recognition between the human body.Although the physical and chemical properties of the in vitro of the heterogeneous structure are basically the same, the receptor or target of the drug molecules acts is amino acids, nucleosides, membranes and other hand proteins and nucleic acid macromolecules.They have certain requirements for the three -dimensional structure of the spatial composition of the pharmaceutical molecules, so they often show a large difference in pharmaceuticals and metabolism in the body.At the end of the twentieth century, as people...
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