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Anticoagulant compound, composition and application thereof

A compound and composition technology, applied in the field of new coumarin derivatives, can solve the problems of fast dissociation speed, unsatisfactory bioavailability, short half-life and the like

Active Publication Date: 2010-02-24
SHANGHAI SINE PHARMA LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral platelet membrane II b / IIIa receptor antagonists have suboptimal bioavailability, short half-life, and rapid dissociation from the receptor

Method used

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  • Anticoagulant compound, composition and application thereof
  • Anticoagulant compound, composition and application thereof
  • Anticoagulant compound, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] 1. Preparation of 4-phenyl-3-butene-2-one (7)

[0079]

[0080] Benzaldehyde (6)

[0081] Dissolve 120g sodium hydroxide in 1.08L distilled water to make a 10% sodium hydroxide aqueous solution, cool to 5℃ in an ice bath, add 30.5ml benzaldehyde and 88ml acetone, stir at 5-10℃ for 4 hours, thin layer chromatography Show that the reaction is complete. The reaction solution was extracted three times with dichloromethane, and the organic layers were combined, then washed with saturated ammonium chloride aqueous solution until neutral, and dried with anhydrous sodium sulfate overnight. After filtration, the filtrate was concentrated under reduced pressure to obtain a yellow oil. The crude product was distilled under reduced pressure, and the fraction at 106-108°C (under 3mmHg) was collected and placed in the refrigerator for a while to form a solid. Finally, 32 g of a light yellow solid (compound (7)) was obtained, yield: 74 %.

[0082] 2. Preparation of compound (2)

[008...

Embodiment 2

[0087] Take SD rats into random groups, 10 in each group, half male and half male. Set up a negative control group. Warfarin sodium is the positive control drug. 37 hours before the experiment, the rats were given by intragastric administration, the tails of the rats were cut off and blood was collected, and the clotting time was measured.

[0088] The test drug was dissolved in 0.5% CMC solution, the dosage of compound (2) obtained in Example 1 was 1 mg / kg, 3 mg / kg, 10 mg / kg, 30 mg / kg, 100 mg / kg; the dosage of the positive control drug was 1 mg / kg. kg, 3mg / kg, 10mg / kg, 30mg / kg, gavage volume is 10ml / kg, single gavage administration. The negative control group was given an equal volume of solvent.

[0089] Using clotting time as an indicator, a t test was performed to compare the significance of differences between groups.

[0090] Table 1 shows the results of rat coagulation time of compound (2) obtained in the examples.

[0091] The results of the rat clotting time of the positi...

Embodiment 3

[0100] Take SD rats into random groups, 4 in each group, half male and half male. Set up a negative control group. Warfarin sodium is the positive control drug. 37 hours before the experiment, the rats were given by intragastric administration, the tails of the rats were cut off and blood was collected, and the clotting time was measured.

[0101] The test drug was dissolved in 0.5% CMC solution, the dosage of compound (2) obtained in Example 1 and the positive control drug were both 10 mg / kg, the gavage volume was 10 ml / kg, and single gavage was administered. The negative control group was given an equal volume of solvent.

[0102] Using clotting time as an indicator, a t test was performed to compare the significance of differences between groups.

[0103] See Table 3 for the results of rat clotting time of the tested drug.

[0104] Table 3 Experimental results of coagulation time of rat tail docking

[0105]

[0106] *p<0.05 **p<0.01 Comparison between each group and the negative...

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PUM

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Abstract

The invention discloses a compound represented by a formula I or pharmaceutically acceptable salt thereof, a composition comprising the compound or the pharmaceutically acceptable salt thereof, and application of the compound or the pharmaceutically acceptable salt thereof and the composition in anti-coagulation medicaments.

Description

Technical field [0001] The invention relates to an anticoagulant compound, in particular to a new coumarin derivatives. Background technique [0002] Disorders of blood coagulation can lead to diseases such as stroke, myocardial infarction and peripheral arterial obstructive diseases that seriously endanger human health. Although there are currently drugs such as heparin and oral coumarin that can be used for anticoagulation, the side effects of these drugs themselves have always been a headache for clinical doctors. With the continuous advancement of basic medical research, people have gradually deepened their understanding of the various enzymes, active factors and related receptors involved in the coagulation process. [0003] The following are several commonly used drugs for anticoagulant effects. [0004] Thrombin inhibitors. Thrombin is a serine protease, which is a key enzyme in the coagulation cascade. Thrombin can convert soluble fibrinogen into insoluble fibrin, and can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/48A61K31/4035A61P7/02
Inventor 陈良戴健张跃良沈康宁
Owner SHANGHAI SINE PHARMA LAB
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