Application of N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative in preparing drug for treating glaucoma

A technology of benzodioxane and amide derivatives is applied in the field of preparation of medicines for the treatment of glaucoma, can solve the problems of incurable medicines and the like, and achieve the effects of protecting ganglion cells and optic nerve

Inactive Publication Date: 2010-11-10
四川爱森生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the use of drugs or surgery to lower intraocular pressure is the only clinical treatment for glaucoma, and there is no curable drug

Method used

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  • Application of N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative in preparing drug for treating glaucoma
  • Application of N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative in preparing drug for treating glaucoma
  • Application of N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative in preparing drug for treating glaucoma

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0020] Experimental example 1N-(2-(2-(dimethylamino)ethoxy)-4-(1H-pyrazole-4-)phenyl)-2,3-dihydro-1,4-benzo The hypotensive effect of dioxane-2-amide (ROCK001)

[0021] 1. Experimental animal feeding and management

[0022] Barrier system Spragμe-Dawley rats 15 (10 females, 5 males), weighing 180-220 grams, aged 6-7 weeks, no obvious crooked neck, transparent cornea, clear iris blood vessels, etc. Round, sensitive to light reflection.

[0023] Before entering the room, the rats were adapted to the environment and quarantined for one week, and healthy (female must not be pregnant) animals were selected as the test animals. The quarantine content: whether it was consistent with the quality indicators required at the time of order; body temperature, food intake, blood biochemistry, electrolytes; animal General status; whether the animal's weight reaches the range required by the test.

[0024] The room temperature is air-conditioned to maintain 22-24°C (daily temperature diffe...

experiment example 2R

[0086] Experimental Example 2 The protective effect of ROCK001 on ganglion cells

[0087] Animals and Anesthesia

[0088] 1.Spragμe-Dawley rats

[0089] Barrier system Spragμe-Dawley rats 8 (4 females, 4 males), weighing 180-220 grams, aged 6-7 weeks, no obvious crooked neck, transparent cornea, clear iris blood vessels, pupil size, etc. Round, sensitive to light reflection.

[0090] General anesthesia: intraperitoneal injection, anesthetized with 10% chloral hydrate (0.3ml / 100g body weight).

[0091] Eye anesthesia: 0.4% Obuvacaine hydrochloride eye drops (Benuoxi) was instilled into the conjunctival sac 2 to 3 times for surface anesthesia of the cornea. Preoperative preparation: 0.3% levofloxacin eye drops (Helen) was instilled into the conjunctival sac 3 times for eye preparation, and iodophor was used to disinfect the operation area of ​​the eye.

[0092] intravitreal drug delivery

[0093] Two Hamilton-10 μl microsyringes were used to extract 15 μl of NMDA+ROCK00 and...

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Abstract

The invention belongs to the field of organic synthesis and medicines, in particular to application of an N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative in preparing a drug for treating glaucoma. In the invention, experiments prove that the N-[4-(monohydro-pyrazol-4-) phenyl]-2,3-dihydro-1,4-benzdioxan-2-amide derivative shown by a formula I has better action of lowering intraocular pressure and protecting ganglion cells, can take the dual effects of protecting optic nerves and RGC (Retinal Ganglion Cells) while lowering the intraocular pressure and provides a new selection for preparing the drug for treating the glaucoma.

Description

technical field [0001] The invention belongs to the field of organic synthesis and medicine, in particular to N-(4-(1 hydrogen-pyrazole-4-)phenyl)-2,3-dihydro-1,4-benzodioxane-2-amide Use of the derivative in the preparation of medicine for treating glaucoma. Background technique [0002] Glaucoma is one of the most common blinding eye diseases in China and even in the world. Currently, 1-1.5% of the Chinese population suffers from glaucoma, among which 4% are people over the age of 60. Statistics from the 4th International Glaucoma Conference in 2003 showed that the blinding rate of glaucoma in the world ranks second among blinding eye diseases. There are about 12 million glaucoma patients in China and about 3 million glaucoma patients in the United States. In the international medical community, the pathogenic mechanism of glaucoma is still unclear, but increased intraocular pressure is an important factor for glaucoma. Increased intraocular pressure can lead to the dea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4155A61P27/06A61P27/02
Inventor 张康
Owner 四川爱森生物科技有限公司
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