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NO donor-type hydrocortisone derivative, its preparing method and antiphlogistic use

A technology for hydrocortisone and uses, which is applied in the direction of anti-inflammatory agents, steroids, and medical preparations containing active ingredients, which can solve problems such as inducing osteoporosis, achieve overcoming side effects, good therapeutic effects, and excellent anti-inflammatory effects. The effect of inflammatory activity

Inactive Publication Date: 2007-08-08
JIANGSU YUNYANG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Hydrocortisone is widely used clinically because of its powerful pharmacological effects, but long-term medication can cause many adverse reactions such as hypertension and osteoporosis

Method used

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  • NO donor-type hydrocortisone derivative, its preparing method and antiphlogistic use
  • NO donor-type hydrocortisone derivative, its preparing method and antiphlogistic use
  • NO donor-type hydrocortisone derivative, its preparing method and antiphlogistic use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Synthesis of 4-(hydrocortisone-21-oxo-)-4-oxo-butyric acid (2)

[0053] Get a 100ml eggplant-shaped bottle, dissolve 5.43g (15mmol) hydrocortisone (1) in 75ml pyridine, add 3g (30mmol) succinic anhydride, heat and reflux for 8 hours to stop the reaction, pour into 100ml ice water after cooling, 5% HCl was used to adjust the pH to 5.0-5.5, and a white solid was precipitated, which was filtered and washed with water to obtain 5.95 g of the product, with a yield of 86%. IR (v, cm -1 ): 3428vs, 1730vs, 1711vs; ESI-MS: [M+H] + = 463; 1 H-NMR (300MHz, CDCl 3 ): δ=0.96[s, 3H, C(19)-CH 3 ], 1.00-1.05[m, 1H, C(9)-H], 1.10-1.26[m, 2H, C(6)-H b , C(15)-H b ], 1.44[s, 3H, C(18)-CH 3 ], 1.47-1.61 [m, 4H, C(12)-H b , C(14)-H, C(15)-H a , C(16)-H b ], 1.66-1.81 [m, 2H, C(12)-H a , C(1)-H b ], 1.83-1.95[m, 3H, C(1)-H a , C(1)-H, C(6)-H a ], 1.91-2.15[m, 4H, C(7)-H, C(2)-H b , C(2)-H a , C(16)-H a ], 2.16-2.27[m, 2H, C(5)-H a , C(5)-H b ], 2.27-2.39 [m, 2H, C(24)-CH ...

Embodiment 2

[0063] Mix 50 mg of Compound I of the present invention with 100 mg of starch and 100 mg of lactose, use an appropriate amount of 5% polyvinylpyrrolidone as a wetting agent to make a soft material, granulate in a conventional manner, dry, add 3 mg of magnesium stearate and mix to make a tablet.

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PUM

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Abstract

The invention discloses hydrogenated cortisone derivant from NO as compound I in the medical chemical domain, which reserves or reinforces anti-inflammatory action and lessens the bad reaction of elevation of blood pressure and osteoporosis.

Description

technical field [0001] The invention relates to the field of pharmaceutical compounds, in particular to a NO donor hydrocortisone derivative. The invention also discloses a preparation method of the derivative and its use as an anti-inflammatory drug. Background technique [0002] Hydrocortisone is widely used clinically because of its powerful pharmacological effects, but long-term medication can cause many adverse reactions such as hypertension and osteoporosis. [0003] Nitric oxide (NO) participates in the regulation of many physiological functions in the body, and is closely related to the cardiovascular system, nervous system, immune system, bone metabolism system, etc. It is a small molecule compound that has been studied in depth. In recent years, NO-donating drugs have developed significantly in both basic and applied research. NO is linked to certain drugs, which can enhance drug efficacy and / or reduce toxic side effects. Contents of the invention [0004] The ...

Claims

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Application Information

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IPC IPC(8): C07J5/00A61K31/573A61P29/00A61P19/02A61P19/04
Inventor 张奕华房雷季晖丁大勇彭司勋
Owner JIANGSU YUNYANG PHARMA GRP
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