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Imaging agents of fibrotic diseases

A technology for fibrotic diseases and imaging agents, which can be used in the digestive system, in vivo radioactive agents, general/multifunctional contrast agents, etc., and can solve problems such as undescribed

Inactive Publication Date: 2011-09-21
NITTO DENKO CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of these methods are satisfactory and further diagnostic techniques need to be developed
[0007] Furthermore, JP, A, 2009-518372 discloses the synthesis of retinoyl-PEG(12)-Lys-OH, which is suitable for diagnostic imaging of fibrosis as a diagnostic contrast agent, but does not describe the true nature of this substance suitable for use as a contrast agent

Method used

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  • Imaging agents of fibrotic diseases
  • Imaging agents of fibrotic diseases
  • Imaging agents of fibrotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0323] Retinoid-PGA-DOTA Synthesis

[0324] according to figure 1 The general scheme shown was to prepare the retinoid-PGA-DOTA polymer conjugate as follows: PGA (150 mg) was dissolved in DMF (15 mL). Retinol (10 mg), EDC (50 mg) and DMAP (50 mg) were added. The mixture was stirred for 24 hours. Then pNH2-Bn-DOTA (10 mg), EDC (50 mg) and DMAP (50 mg) were added. The resulting mixture was stirred for 24 hours. Dilute HCl solution (0.2M) was then added to induce precipitation. The mixture was stirred for 2 minutes and centrifuged at 10000 rpm for 15 minutes. The solid precipitate was collected, washed with water, and redissolved with sodium bicarbonate solution (0.5M). The mixture was dialyzed against water for 24 hours. The product retinoid-PGA-DOTA polymer conjugate was lyophilized. The product is identified by 1 H-MR confirmed.

Embodiment 2

[0326] Synthesis of Retinoid-PGA-DTPA

[0327] according to figure 2 The general scheme shown was to prepare the retinoid-PGA-DTPA polymer conjugate as follows: PGA (150 mg) was dissolved in DMF (15 mL). Retinol (10 mg), EDC (50 mg) and DMAP (50 mg) were added. The mixture was stirred for 24 hours. Then add pNH 2 - Bn-DTPA (10 mg), EDC (50 mg) and DMAP (50 mg). The resulting mixture was stirred for 24 hours. Dilute HCl solution (0.2M) was then added to induce precipitation. The mixture was stirred for 2 minutes and centrifuged at 10000 rpm for 15 minutes. The solid precipitate was collected, washed with water, and redissolved with sodium bicarbonate solution (0.5M). The mixture was dialyzed against water for 24 hours. The product retinoid-PGA-DTPA polymer conjugate was lyophilized. The product is identified by 1 Confirmed by H-NMR.

Embodiment 3

[0329] Synthesis of Retinoid-PGGA-DOTA

[0330] according to image 3 The general scheme shown was to prepare the retinoid-PGGA-DOTA polymer conjugate as follows: poly(L-γ-glutamylglutamine) (PGGA, 150 mg) was dissolved in DMF (15 mL). Retinol (10 mg), EDC (50 mg) and DMAP (50 mg) were added. The mixture was stirred for 24 hours. Then add pNH 2 - Bn-DOTA (10 mg), EDC (50 mg) and DMAP (50 mg). The resulting mixture was stirred for 24 hours. Dilute HCl solution (0.2M) was then added to induce precipitation. The mixture was stirred for 2 minutes and centrifuged at 10000 rpm for 15 minutes. The solid precipitate was collected, washed with water, and redissolved with sodium bicarbonate solution (0.5M). The mixture was dialyzed against water for 24 hours. The product retinoid-PGGA-DOTA polymer conjugate was lyophilized. The product is identified by 1 Confirmed by H-NMR.

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Abstract

Agents and methods for imaging a cell and / or a portion of tissue characterized by fibrosis, as well as to agents and methods for determining and / or diagnosing fibrotic diseases are disclosed herein. Also disclosed herein are polymer conjugates that can include a detectable label, a retinoid and a polymer. The polymer conjugates can be used to image a portion of tissue, deliver a detectable label to a portion of tissue or a cell and / or diagnosis a condition or disease.

Description

technical field [0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Patent Application Serial No. 61 / 096488, filed September 12, 2008, and Japanese Patent Application No. 2009-184806, filed August 7, 2009, all of which The contents are incorporated herein by reference. [0003] Compositions and methods relating to the fields of organic chemistry, medicinal chemistry, biochemistry, molecular biology and medicine are disclosed herein. Embodiments disclosed herein are particularly directed to reagents and methods for imaging cells and / or a portion of tissue (eg, cells and / or tissue characteristic of fibrosis), and to reagents and methods for determining and / or diagnosing fibrotic diseases. Background technique [0004] Fibrosis, or excess production of fibrous connective tissue in the body, is associated with many diseases or disorders, such as liver fibrosis, pancreatic fibrosis, vocal cord scarring, and various form...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/10A61K49/00C08G69/48
CPCA61K49/0041C08G69/10A61K49/0054A61K49/0052A61K51/065C08G69/48A61K49/128A61K49/085A61K49/0002A61P1/16A61P43/00
Inventor 新津洋司郎俞磊赵刚S·万王兴河刘健S·库马尔达什田中康进梶原庆子高桥博一宫崎美代乃
Owner NITTO DENKO CORP
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