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Intraocular tension reducing compound and preparation method and use thereof

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

Inactive Publication Date: 2015-02-25
韩冰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 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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  • Intraocular tension reducing compound and preparation method and use thereof
  • Intraocular tension reducing compound and preparation method and use thereof
  • Intraocular tension reducing compound and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0033] Preparation Example 1 (compound A is the preparation of compound A13)

[0034] Compound A1 in CH 3 NO 2 Catalyzed in AcOH / NH 4 In OAc solution at 120 degrees and amino condensation reaction to obtain compound A2, in LiAlH 4 And trifluoroacetic acid, reacted under the condition of feeding nitrogen to obtain compound J (for use).

[0035] Compound A3 and a1 were reacted under the catalysis of tetrahydrofuran to obtain compound A4. Under the catalysis of a2, compound A4 was reacted in a mixed solution of dichloromethane and dimethyl sulfoxide at minus 50 degrees for 2 hours, and in an aqueous solution of triethylamine. Compound A5 was obtained by reacting at 50°C for 2 hours, compound A6 was obtained overnight at room temperature under the catalysis of bromine and tetrachloromethane, compound A7 was generated at 100°C under the catalysis of a3 in aqueous solution of dioxane, 4-dimethylaminopyridine, acetonitrile solution , add di-tert-butyl dicarbonate, and reflux for ...

preparation Embodiment 2

[0037] Compound (B) was prepared in the same manner as in Preparation Example 1.

[0038]

preparation Embodiment 3

[0040] Compound (C) was prepared in the same manner as in Preparation Example 1.

[0041]

[0042]

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Abstract

The invention discloses a compound and a pharmaceutical composition and a preparation method and use thereof, the use is the use of the compound in preparation of intraocular tension reducing drugs, and the compound has very obvious intraocular tension reducing effects.

Description

technical field [0001] The present invention relates to a class of compounds for reducing intraocular pressure and their preparation methods and uses, pharmaceutical compositions prepared from the above compounds and their pharmaceutically acceptable salts and analogs thereof, and the compounds or their pharmaceutically acceptable salts and their analogues Use of a substance in the preparation of a medicament for reducing intraocular pressure. [0002] Background technique [0003] 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. [0004] At present, the scientific community is still inconclusive about the cause of lowering intraocular pressure. It is generally believed that ...

Claims

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Application Information

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IPC IPC(8): C07D498/04A61K31/519A61P27/02
CPCC07D491/048
Inventor 韩冰杨逢源王斓
Owner 韩冰
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