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A kind of compound for reducing intraocular pressure and preparation method and use thereof

A technology for compounds and uses, applied in the field of preparing medicines for reducing intraocular pressure, can solve problems such as unsatisfactory treatment effects

Active Publication Date: 2018-03-13
韩冰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the scientific community is still inconclusive about the cause of lowering intraocular pressure. It is recognized that it is caused by a variety of reasons. At present, the therapeutic effect of drugs for lowering intraocular pressure is not very satisfactory.

Method used

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  • A kind of compound for reducing intraocular pressure and preparation method and use thereof
  • A kind of compound for reducing intraocular pressure and preparation method and use thereof
  • A kind of compound for reducing intraocular pressure and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0028] Preparation Example 1 (compound A is the preparation of compound A9)

[0029] Compound A1 was catalyzed by di-tert-butyl dicarbonate to generate A2, and under the catalysis of oxalyl chloride and diisopropylethylamine, under ultra-low temperature conditions, the reaction in a mixture of dimethyl sulfoxide and dichloromethane generated A3, and then in Under the catalysis of a1 and a2, reflux in the ethanol solution of hydrochloric acid generates A4, A4 generates A5 at normal temperature in the ethanol solution of sodium hydroxide, and generates A6 in the ethanol solution of sodium borohydride at normal temperature, in dichloromethane, a3, 1-Hydroxybenzotriazole, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide catalyzed to generate A7, generate A8 in dichloromethane of trifluoroacetic acid, under the catalysis of a4, A9 was formed in dichloromethane.

[0030]

preparation Embodiment 2

[0031] Preparation Example 2 (compound B is the preparation of compound B9)

[0032] Compound B1 is catalyzed by di-tert-butyl dicarbonate to generate B2, and under the catalysis of oxalyl chloride and diisopropylethylamine, under ultra-low temperature conditions, reacts in a mixture of dimethyl sulfoxide and dichloromethane to generate B3, and then in Under the catalysis of b1 and b2, reflux in the ethanol solution of hydrochloric acid generates B4, B4 generates B5 at normal temperature in the ethanol solution of sodium hydroxide, refluxes in the ethanol solution of sodium borohydride at normal temperature to generate B6, in dichloromethane, b3, 1-Hydroxybenzotriazole, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide catalyzed to generate B7, generate B8 in dichloromethane of trifluoroacetic acid, under the catalysis of b4, Formation of B9 in dichloromethane.

[0033]

preparation Embodiment 3

[0034] Preparation Example 3 (compound C is the preparation of compound C9)

[0035] Compound C1 is catalyzed by di-tert-butyl dicarbonate to generate C2, and under the catalysis of oxalyl chloride and diisopropylethylamine, under ultra-low temperature conditions, the reaction in a mixture of dimethyl sulfoxide and dichloromethane generates C3, and then in Under the catalysis of c1 and c2, reflux in the ethanol solution of hydrochloric acid generates C4, C4 generates C5 in the ethanol solution of sodium hydroxide at room temperature, and generates C6 in the ethanol solution of sodium borohydride at room temperature, and in dichloromethane, c3, 1-Hydroxybenzotriazole and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide catalyze C7, generate C8 in dichloromethane of trifluoroacetic acid, and under C4 catalysis, Formation of C9 in dichloromethane.

[0036]

[0037] Preparation of injection containing compound A:

[0038] ① Take mannitol, phospholipids, glycerol, cyclodextrin de...

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PUM

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Abstract

The invention discloses a class of compound and its pharmaceutical composition as well as its preparation method and application. The application is the application in the preparation of medicine for reducing intraocular pressure. The effect of the above-mentioned compound on lowering intraocular pressure is very remarkable.

Description

technical field [0001] The present invention relates to a class of compounds for reducing intraocular pressure, pharmaceutically acceptable salts and analogs thereof, pharmaceutical compositions prepared from the compounds, pharmaceutically acceptable salts and analogs thereof, and the compounds or pharmaceutically acceptable salts thereof Use of salts and analogues thereof for the preparation of a medicament for reducing intraocular pressure. Background technique [0002] The increase of intraocular pressure (IOP) due to various reasons is an eye disease that endangers human health all over the world. The main manifestation of patients is short-term or long-term increase of intraocular pressure. This is a very serious blinding eye disease due to the irreversible loss of vision caused by elevated intraocular pressure. [0003] At present, the scientific community is still inconclusive about the cause of lowering intraocular pressure. It is generally believed that it is caus...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P27/02
CPCY02P20/55
Inventor 韩冰王爽王斓
Owner 韩冰