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Compound for treating diseases related to high-frequency ankylosing contraction of uterine smooth muscle

A compound and high-frequency technology, applied in diseases, muscular system diseases, neuromuscular system diseases, etc., can solve the problems of unsustainable curative effect and unsuitable for long-term use, achieve amplitude and vitality inhibition, significant sustained release effect, increase compliance sexual effect

Active Publication Date: 2021-06-08
刘红枚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commonly used uterine smooth muscle relaxants in clinic mainly include cyclooxygenase inhibitors (such as indomethacin), nitric oxide donors (such as nitroglycerin), β2 receptor agonists (such as ritodrine hydrochloride) and Calcium ion channel blockers (such as nifedipine), etc. These drugs can relieve uterine pain symptoms to varying degrees, but have obvious adverse reactions such as digestive tract, heart, liver, kidney, etc., and the curative effect is not long-lasting and should not be taken for a long time. has obvious limitations when using

Method used

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  • Compound for treating diseases related to high-frequency ankylosing contraction of uterine smooth muscle
  • Compound for treating diseases related to high-frequency ankylosing contraction of uterine smooth muscle
  • Compound for treating diseases related to high-frequency ankylosing contraction of uterine smooth muscle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Compound G-01 preparation of

[0026] According to the preparation scheme of Patent Application CN1195353A Example 1, isoamyl nitrite was added to the mixture containing [3aR-(3aα, 4α, 6α, 6aα)]-6-[5-amino-6-chloro-2-(propylthio Base)-4-pyrimidinylamino]-tetrahydro-2,2-dimethyl-4H-cyclopentyl-1,3-dioxol-4-methanol in acetonitrile solution, heated at 70°C for 1h. After cooling, the reaction mixture was concentrated and purified (SiO2, eluent, dichloromethane:ethyl acetate, 4:1) to obtain the compound of formula G-01.

Embodiment 2

[0028] According to the literature method, the isolated rat uterine smooth muscle strips were prepared, and the non-pregnant female rats were injected with 2 mg / kg of estradiol benzoate every day for 5 days before the experiment to make a model. After 5 days, the rats were sacrificed and the uterus was quickly dissected. The two uterine horns were each taken from two uterine segments, which were cut longitudinally along the muscle texture to obtain four 2 cm long uterine muscle strips, which were hung in De- In Jalon solution, one section of the uterine smooth muscle strip was fixed on the T-shaped hook in the bath, and the other section was connected to the muscle tension transducer. The load was 1.0 g before adding the drug, and the temperature was kept at 37°C and incubated with saturated oxygen. The muscle tension transducer records the contraction of the muscle through the Med lab biological signal acquisition and processing system.

[0029] Uterine smooth muscle strips w...

Embodiment 3

[0034] Melt 1000g of Pluronic F-108, weigh another 10g of compound G-01 and dissolve it in 50g of glycerin, pour it into the melted Pluronic F-108, add 10g of L31, magnetically stirred for 2 hours, defoamed, and poured into a plug mold pre-coated with liquid paraffin. Put it at 4°C to cure for 1 hour, take it out, cut off the excess part, absorb the lubricating oil on the surface, and pack it. The average suppository weighs 1 g, and each suppository contains 10 mg of compound G-01. (In vitro adhesion time is 164.62s, 24h cumulative release rate of drug is about 86.2%)

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Abstract

The invention belongs to the field of medicinal chemistry, and provides a compound for treating diseases related to high-frequency ankylosing contraction of uterine smooth muscle, the compound has a remarkable inhibition effect on the frequency, the amplitude and the activity of the uterine smooth muscle ankylosing contraction caused by oxytocin, the prepared suppository can obviously enhance drug release and has a remarkable long-acting sustained-release effect, the administration frequency can be reduced, and the compliance of a patient is improved. Meanwhile, the suppository can be applied to the vagina, and side effects of patients are reduced.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a compound for inducing uterine smooth muscle contraction and a pharmaceutical preparation thereof. Background technique [0002] Excessive contraction of uterine smooth muscle can cause dysmenorrhea in adolescent girls, unmarried and unmarried women without children, and premature birth in pregnant women. It is a common disease in women and seriously affects women's health and work efficiency. At present, the commonly used uterine smooth muscle relaxants in clinic mainly include cyclooxygenase inhibitors (such as indomethacin), nitric oxide donors (such as nitroglycerin), β2 receptor agonists (such as ritodrine hydrochloride) and Calcium ion channel blockers (such as nifedipine), etc. These drugs can relieve uterine pain symptoms to varying degrees, but have obvious adverse reactions such as digestive tract, heart, liver, kidney, etc., and the curative effect is no...

Claims

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Application Information

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IPC IPC(8): A61K9/02A61K31/519A61K47/10A61K47/32A61P15/00A61P21/02
CPCA61K9/02A61K47/10A61K31/519A61K47/32A61P15/00A61P21/02
Inventor 不公告发明人
Owner 刘红枚
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