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Eflornithine prodrug and conjugate and using method thereof

A kind of eflunomine, drug technology, applied in the field of eflunomine prodrugs and conjugates

Inactive Publication Date: 2010-12-01
徐锋
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the complex nature of each condition, treatment with a single agent often has limited success

Method used

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  • Eflornithine prodrug and conjugate and using method thereof
  • Eflornithine prodrug and conjugate and using method thereof
  • Eflornithine prodrug and conjugate and using method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153] Example 1: Synthesis of Eflornithine-Aspirin Conjugate

[0154] The invention provides a method for synthesizing an eflornithine-NSAID conjugate. The examples shown below generally describe the synthesis of eflornithine analog-NSAID conjugates, and more specifically the synthesis of eflornithine-aspirin conjugates.

[0155]

Embodiment 2

[0156] Embodiment 2: Synthesis of Eflornithine Prodrug

[0157] This example generally provides the preparation method of eflornithine prodrug, more specifically phosphoramidate prodrug.

[0158]

Embodiment 3

[0159] Example 3: In Vitro Test of Caco-2 Cell Permeability of Eflornithine Conjugates or Eflornithine Prodrugs

[0160] Passive permeation of the eflornithine-NSAID conjugates or eflornithine prodrugs of the present invention is performed in vitro using methods well known in the art (see, e.g., Stewart, et al., Pharm. Res. ., 1995, 12, 693). For example, passive permeability is determined by testing the flux of eflornithine-NSAID conjugates or eflornithine prodrugs through cultured polarized cell monolayers (eg, Caco-2 cells). Caco-2 cells obtained through continuous culture (less than 28 passages) were transferred to Transwell polycarbonate filter at high concentration. Cells were stored in DMEM / 10% fetal bovine serum + 0.1 mM non-essential amino acids + 2 mM L-Gln, 5% CO2 / 95% O2, 37°C until the day of the experiment. Permeability studies were performed at pH 6.5 apically (in 50 mM MES buffer containing 1 mM CaCl2, 1 mM MgCl2, 150 mM NaCl, 3 mM KCl, 1 mM NaH2PO4, 5 mM gluc...

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Abstract

On one hand, the invention provides a composition of a covalent conjugate of an eflornithine analogue and an anti-inflammatory. On the other hand, the invention provides an eflornithine prodrug composition. In addition, the invention provides a method for treating or preventing cancer by using the conjugate of the eflornithine analogue or the eflornithine prodrug.

Description

technical field [0001] The present invention relates to eflornithine prodrugs and conjugates and methods of use thereof. Background technique [0002] Cancer, also known as malignancy, is a strongly proliferative disorder characterized by abnormal growth of cells manifested by uncontrolled cell division, invasion, and destruction of adjacent tissues, sometimes metastasizing to other parts of the body. There are more than 100 types of cancer, including breast, skin, lung, colon, prostate, and lymphoma. Cancer can affect people of all ages, even unborn babies, but the risk of most cancers increases with age. Cancer can infect all animals. [0003] Cancer is affected by multiple molecular mechanisms. Due to the complex nature of each pathology, treatment with single agents has often had limited success. Therefore, combination administration is often used in the treatment of cancer. A strong correlation has been reported between the number of agents administered and the cu...

Claims

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Application Information

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IPC IPC(8): C07C271/22C07F9/24C07C229/26A61K31/664A61K31/621A61P35/00A61P35/02
Inventor 徐锋
Owner 徐锋
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