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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

[0031] Preparation Example 1 (compound A is the preparation of compound A11)

[0032] Compound A1 and A2 are combined to generate compound A3, A3 is brominated to obtain compound A4, benzene is substituted for bromine to generate compound A5, deaminated to generate compound A6, nitro is substituted to generate compound A7, nitro is reduced to generate compound A8, under the protection of Boc, The unprotected amino group of A8 is activated to generate compound A9, the de-Boc of trifluoroacetic acid is generated to generate A10, and the cycloalkylamino group is activated to generate A11.

[0033]

preparation Embodiment 2

[0034] Preparation Example 2 (compound B is the preparation of compound B11)

[0035] Compound B1 and B2 are combined to generate compound B3, B3 is brominated to obtain compound B4, benzene is substituted for bromine to generate compound B5, deaminated to generate compound B6, nitro is substituted to generate compound B7, nitro is reduced to generate compound B8, under the protection of Boc, The unprotected amino group of B8 is activated to generate compound B9, the de-Boc of trifluoroacetic acid generates B10, and the cycloalkylamino group is activated to generate B11.

[0036]

preparation Embodiment 3

[0037] Preparation Example 3 (Preparation of Compound C, Compound C11)

[0038] Compound C1 and C2 are combined to generate compound C3, C3 is brominated to obtain compound C4, benzene is substituted for bromine to generate compound C5, deaminated to generate compound C6, nitro is substituted to generate compound C7, nitro is reduced to generate compound C8, under the protection of Boc, C8 The amino group not protected by Boc is activated to generate compound C9, the de-Boc of trifluoroacetic acid is generated to generate C10, and the cycloalkylamino group is activated to generate C11.

[0039]

[0040] Preparation of injection containing compound A:

[0041] 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 dissolve them;

[0042] ② After mixing and dissolving, after stabilization, first use a 0.45um microporous membrane for coarse f...

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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 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): C07D401/12A61K31/454A61K31/5377A61P27/02
CPCC07D401/12
Inventor 韩冰邢瑞娟
Owner 韩冰
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