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Phenoxazine compounds, its pharmaceutical compositions and medical use

A technology for compounds and prodrugs, applied to phenoxazine compounds and their pharmaceutical compositions and their medical application fields, can solve problems such as aberrations

Inactive Publication Date: 2002-08-28
陆鑑青
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, labeling amyloid deposits with antibiotics, serum amyloid P protein, or other detection molecules provides some resolution of the periphery of the body tissue, but poorly visualizes the interior of the body tissue

Method used

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  • Phenoxazine compounds, its pharmaceutical compositions and medical use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] 3-Nitro-12H-benzo[b]phenoxazine-1-carboxylic acid Preparation Step A: 2-3-Hydroxy-naphthalen-2-yl-amino)-3,5-dinitro-benzoic acid preparation of

[0094] 3-Amino-naphthalene-2-ol (4.65 g, 0.029 mol), 2-chloro-3,5-dinitro-benzoic acid (7.20 g, 0.029 mol), water (30 ml) and 2N sodium acetate (15 mL) was stirred and heated at reflux for 15 minutes. To the resulting thick viscous solution was added 2N sodium hydroxide (15 mL), and the mixture was stirred and heated for 15 minutes. The resulting purple-black sodium salt was washed with cold brine. The filtered precipitated aqueous solution was then acidified with dilute hydrochloric acid. The free acid forms a black precipitate. The precipitate was dissolved in 10% MeOH-H 2 Grinding in the boiling liquid of O, then filtering, with 10% MeOH-H 2 Rinse with cold solution of O and dry overnight in a vacuum oven at room temperature to obtain 9.00 g (0.024 mol, 84%) of the desired product as a brown solid with a melti...

Embodiment 2

[0097] 3-Nitro-8-phenyl-10H-phenoxazine-1-carboxylic acid Preparation Step A: 2-(4-Hydroxy-biphenyl-3-yl-amino)-3,5-dinitro- Preparation of benzoic acid

[0098] The title compound was prepared with 3-amino-biphenyl-4-ol (5.59 g, 0.03 mol), 2-chloro-3,5-dinitro-benzoic acid (7.45 g, 0.03 mol), water (30 mL), 2N sodium acetate (15 mL) and 2N-sodium hydroxide (15 mL) were prepared by the method of step A of Example 1. The desired product was obtained as 9.37 g (0.023 mol, 78%) of a red solid with a melting point of 215-217°C. Elemental Analysis C 19 h 13 N 3 o 7 1.13H 2 O: Calculated: Carbon, 54.90; Hydrogen, 3.70; Nitrogen, 10.11; Found: Carbon, 54.51; Hydrogen, 3.57; Nitrogen, 9.84. Step B: Preparation of 3-nitro-8-phenyl-10H-phenoxazine-1-carboxylic acid

[0099] The title compound was prepared with 2-(4-hydroxy-biphenyl-3-ylamino)-3,5-dinitro-benzoic acid (8.82 g, 0.022 mol), water (50 ml), 10N-hydrogen Sodium oxide (10 ml) was prepared by the method in step B...

Embodiment 3

[0101] Preparation of 3-nitro-10H-phenoxazine-1-carboxylic acid Step A: Preparation of 2-(4-hydroxyphen-3-yl-amino)-3,5-dinitro-benzoic acid

[0102] The title compound was prepared with 3-aminobenzene-4-ol (3.27 g, 0.03 mol), 2-chloro-3,5-dinitro-benzoic acid (7.45 g, 0.03 mol), water (30 ml) , 2N sodium acetate (15 ml) and 2N sodium hydroxide (15 ml) were prepared by the method of step A of Example 1. The desired product was obtained as 9.37 g (0.023 mol, 78%) of a red solid with a melting point of 210-212°C. Elemental Analysis C 13 h 9 N 3 o 7 : Calculated: Carbon, 48.91; Hydrogen, 2.84; Nitrogen, 13.16; Oxygen, 35.08; Found: Carbon, 48.71; Hydrogen, 3.02; Nitrogen, 13.22. Step B: Preparation of 3-nitro-10H-phenoxazine-1-carboxylic acid

[0103] The title compound was prepared with 2-(4-hydroxyphen-3-ylamino)-3,5-dinitro-benzoic acid (5.98 g, 0.022 mol), water (50 ml), 10N sodium hydroxide ( 10 ml) prepared by the method of step B of Example 1 to obtain the...

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Abstract

The invention relates to the phenoxazine compounds of formulae I, and the pharmaceutical acceptable salts, esters, amides and prodrugs thereof, to the pharmaceutical compositions containing them, to the use of the preparation of the medicines for inhibiting the starchy protein coagulate. The definitions of R1, R2 and R in formulae I are described in the specification.

Description

technical field [0001] The present invention relates to a class of phenoxazine compounds and their pharmaceutically acceptable salts, esters, amides and prodrugs, and pharmaceutical compositions containing them, which are used in the preparation for inhibiting amyloid aggregation and / or amyloid deposition Pharmaceutical applications of imaging methods. Background technique [0002] The cause of amyloidosis is the accumulation of various insoluble fibrin deposits in the tissues of the patient's body. The fibrous protein that forms deposits is called amyloid. There are various forms of specific proteins or polypeptides found within deposits. Many kinds of amyloid have fibrous type and a large amount of β-sheet secondary structure (β-sheet secondary structure). Aggregated amyloid plus amyloid or amyloid continues to aggregate to form amyloid deposits. [0003] Amyloid deposits are found in many diseases, each caused by its specific protein, such as Medi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/536A61P25/28A61P43/00C07D265/34C07D265/38
CPCA61P25/28A61P43/00C07D265/34C07D265/38
Inventor 陆鑑青
Owner 陆鑑青
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