Application of pyrrolyl-substituted indole compounds in the treatment of glaucoma

A compound and glaucoma technology, applied in medical preparations containing active ingredients, organic chemistry, sensory diseases, etc., can solve problems such as allergic reactions, worsening uveitis, and reduction of adverse reactions, so as to improve the quality of life, reduce side effects, The effect of reducing the blinding rate

Active Publication Date: 2015-11-25
杨子娇
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current clinical situation is: the operation is performed according to the symptoms, the symptoms are not cured, the pain is great and the recurrence is easy, and the drug treatment has little damage, but the treatment effect is not good
[0008] Currently, there are the following methods for the drug treatment of glaucoma, all of which not only have poor therapeutic effects but also have adverse reactions:
[0009] Receptor agonists, adverse reactions and disadvantages: blurred vision, forehead pain, myopia, poor night vision
[0011] Carbonic anhydrase inhibitors (oral or intravenous injection), side effects and disadvantages: after use, it will cause anorexia, fatigue, taste change, depression, paresthesia, kidney stones, blood disorders and other side effects
[0012] Carbonic anhydrase inhibitor (topical application), the adverse reactions caused are significantly reduced, but it will cause bad taste in the mouth
[0013] Nonselective adrenergic agonists (topical), often used with miotics, are less reliable than selective adrenergic agonists and cause allergic and toxic reactions (eg, hypertension, tachycardia speed) is more likely to
[0014] α2-selective adrenergic receptor agonist (topical), disadvantages: systemic reactions (eg) are less obvious than non-selective, aclonidine can easily cause allergic reactions, brimonidine can easily cause dry mouth
[0016] Prostaglandin analogs (topical), Insufficient: Increases iris and skin pigmentation, may worsen uveitis
[0018] At present, the existing glaucoma treatment drugs all have different side effects, and the most important thing is that the treatment effect is not satisfactory. No matter what kind of drugs, they can't produce better treatment effects now, resulting in glaucoma regardless of the various causes. There are more and more patients, and the incidence is getting worse, which seriously threatens the vision of patients

Method used

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  • Application of pyrrolyl-substituted indole compounds in the treatment of glaucoma
  • Application of pyrrolyl-substituted indole compounds in the treatment of glaucoma
  • Application of pyrrolyl-substituted indole compounds in the treatment of glaucoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] ① Take gelatin to prepare empty capsules;

[0055] ② Fill in glycerin as an auxiliary material plasticizer, fill in agar and sodium carboxymethylcellulose to enhance viscosity and plasticity;

[0056] ③Add N-[2-(diethylamino)ethyl]-5-(5-fluoro-2-oxo-1,2-dihydroindoline-3-ylidenemethyl)-2,4- Add dimethyl-1H-pyrrole-3-carboxamide powder into empty capsules to obtain hard capsules for oral administration.

Embodiment 2

[0058] ① Take N-[2-(diethylamino)ethyl]-5-(5-fluoro-2-oxo-1,2-dihydroindoline-3-ylidenemethyl)-2,4- Dimethyl-1H-pyrrole-3-carboxamide powder is dissolved in the solution;

[0059] ②Fill carboxymethylcellulose sodium and mannitol into ①;

[0060] ③ Freeze-dried vested ordinary intraocular powder injection.

Embodiment 3

[0062] ①Weigh 5g meglumine and dissolve it in 1000ml water for injection;

[0063] ②Add N-[2-(diethylamino)ethyl]-5-(5-fluoro-2-oxo-1,2-dihydroindoline-3-ylidenemethyl)-2,4- Dimethyl-1H-pyrrole-3-carboxamide 5g is dissolved;

[0064] ③Add 10g boric acid, 8g borax and 3g sodium chloride to it;

[0065] ④ Adjust the pH value to be suitable for eye use;

[0066] ⑤ Sterile filtration to obtain N-[2-(diethylamino)ethyl]-5-(5-fluoro-2-oxo-1,2-dihydroindoline-3-ylidenemethyl)- 2,4-Dimethyl-1H-pyrrole-3-carboxamide eye drops.

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Abstract

The invention discloses application of pyrryl-substituted indole compound in curing glaucoma. The pyrryl-substituted indole compound can cure glaucoma through small-dose multiple intraocular injection medicine administration and eye drop multiple medicine administration. Furthermore, after the pyrryl-substituted indole compound is coated by lipidosome or is prepared into high-polymer-coated nanometer medicine, micro-ball drug medicine and hydrogel medicine, glaucoma can be cured continuously after intraocular medicine injection to achieve obvious medicine effects.

Description

technical field [0001] The invention relates to the application of a pyrrolyl-substituted indole compound in the treatment of glaucoma. Background technique [0002] Glaucoma is a kind of eye disease characterized by progressive optic nerve damage. It can be divided into primary glaucoma, secondary glaucoma and congenital glaucoma. Angle glaucoma, regardless of the type of glaucoma, the main manifestation of the patient is increased intraocular pressure (IOP). Glaucoma can lead to irreversible vision loss. There are currently about 1.4 billion glaucoma patients in the world, but about half of them are unaware of the existence of this disease. The World Health Organization lists it as the second most common blindness disease. In China, the incidence of glaucoma is about 0.12% to 1.64%, accounting for about 14.36% of eye diseases. According to epidemiological studies, by 2020, the number of glaucoma patients in China will reach 6 million. [0003] Causes of Glaucoma [000...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/404C07D403/06A61P27/06
Inventor 杨子娇王淑霞
Owner 杨子娇
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