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Intraocular tension reducing compound and preparation method and use thereof

A technology of compounds and analogues, which is applied in the field of preparing drugs for reducing intraocular pressure, and can solve problems such as unsatisfactory therapeutic 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

[0027] Preparation Example 1 (compound A is the preparation of compound A6)

[0028] Compounds A1 and a1,K 2 CO 3 , CH 3 COCH 3 Reflux to generate compound A2, A2 and a2, a3 are placed in the distillation flask together in triethylamine, reflux in ethanol to generate compound A3, compound A3 reacts at normal temperature in ethanol aqueous solution of sodium hydroxide for 12 hours to generate compound A4, compound A4 in Under the catalysis of sodium borohydride, compound A5 is generated at normal temperature in ethanol solution, and compound A5 and a4 are mixed in 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 1-hydroxybenzotri A6 is generated under the catalysis of azole.

preparation Embodiment 2

[0029] Preparation Example 2 (compound B is the preparation of compound B6)

[0030] Compounds B1 and b1,K 2 CO 3 , CH 3 COCH 3 Reflux to generate compound B2, B2 and b2, b3 are placed in the distillation flask together in triethylamine, reflux in ethanol to generate compound B3, compound B3 is reacted at normal temperature in ethanol aqueous solution of sodium hydroxide for 12 hours to generate compound B4, compound B4 is in Under the catalysis of sodium borohydride, compound B5 is generated at normal temperature in ethanol solution, and compound B5 and b4 are synthesized in 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 1-hydroxybenzotri B6 is generated under the catalysis of azole.

[0031]

[0032] Preparation of injection containing compound A:

[0033] ① Take mannitol, phospholipids, glycerol, cyclodextrin derivatives, dimethyl sulfoxide and poloxamer, 50mg and 100mg of the compound of formula (A), mix them in water for injection and disso...

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PUM

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Abstract

The invention discloses an intraocular tension reducing compound, a pharmaceutically acceptable salt and an analogue thereof, a pharmaceutical composition prepared from the intraocular tension reducing compound, the pharmaceutically acceptable salt and the analogue, and use of the intraocular tension reducing compound, the pharmaceutically acceptable salt and the analogue in preparation of intraocular tension reducing drugs, the invention discloses a preparation method and use of the intraocular tension reducing compound and the pharmaceutical composition, the intraocular tension reducing animal experiment of the intraocular tension reducing compound is performed, 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, 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. [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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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P27/02
CPCC07D487/04
Inventor 韩冰王爽王斓
Owner 韩冰
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