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Use of compounds for the prevention of drug-induced cell toxicity

A compound and application technology, applied in the field of cytotoxic therapy, can solve the problems of reducing cytotoxicity, not disclosed, etc.

Inactive Publication Date: 2007-11-21
RECEPTICON
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This document does not disclose cytotoxicity-reducing compounds or drugs that bind to cubilin and / or megalin receptors and / or co-receptors of megalin and cubilin

Method used

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  • Use of compounds for the prevention of drug-induced cell toxicity
  • Use of compounds for the prevention of drug-induced cell toxicity
  • Use of compounds for the prevention of drug-induced cell toxicity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0113] Preferred embodiment of X

[0114] In a preferred use embodiment of the present invention, X is an aromatic, carbocyclic, heterocyclic or heteroaromatic structure having 1-3 rings, each ring having 3-8 ring members and 0-3 heteroatoms, wherein each ring may be substituted at least once, wherein said substituent is selected from O, OH, phenyl, halogen, alkyl, alkenyl or alkynyl, substituted lower alkyl, substituted lower alkenyl or alkyne Base, aryl, heterocyclyl, heteroaryl, aryl-(C 1-4 )-Alkyl, Heteroaryl-(C 1-4 )-Alkyl, Heterocyclyl-(C 1-4 )-alkyl, cycloalkylalkyl, cycloalkyl, alkoxy, carboxy, trifluoromethyl, cyano, amino, nitro, O-alkyl, O-acyl, aminoalkyl and aminodioxane base.

[0115] In other more preferred embodiments, wherein X is an aromatic, carbocyclic, heterocyclic or heteroaromatic structure having 1-3 rings, with 5-6 ring members and 1 or 2 heteroatoms in each ring , wherein each ring may be substituted at least once, wherein said substituent is sel...

Embodiment 1

[0301] in vitro test

[0302] The inhibitory effect of p-xylylenediamine on the binding of gentamicin to immobilized megalin was assessed by proton surface resonance (SPR) analysis on a Biacore 2000 instrument. Megalin was purified from rabbit kidneys at 28-40 fmol / mm as described by Birn et al. 2 concentration is fixed. Sample dissolved in 10mM Hepes, 150mM NaCl, 1.5mM CaCl 2 , 1 mM EGTA, 0.005% Tween-20pH 7.4. The same buffer was used as running buffer. At time 0, the indicated concentrations of p-xylylenediamine (Figure 3) were applied to the chip and binding was expressed in relative response units (RU), i.e. the measured response between megalin and the control flow cell. difference. After 700 s, 1 mM gentamycin was injected together with buffer alone or various concentrations of p-xylylenediamine. Inhibition of gentamicin binding was scored using the difference in RU units obtained by injection of gentamicin alone and in the presence of antagonist. After each anal...

Embodiment 2

[0306] The in vivo effects of p-xylylenediamine (RC043 / B5) were tested. Gentamicin uptake in the mouse kidneys was measured after intraperitoneal (i.p.) administration of the compounds. Inject 50 μg / kg of tritiated gentamicin, using different concentrations of the inhibitor in each mouse. This corresponds to a clinical dose of gentamicin used in 1% of patients.

[0307] The results are shown in Figure 4.

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PUM

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Abstract

The present invention relates to the use of compounds for the manufacture of a medicament for the prophylaxis and / or treatment of induced cell toxicity, such as nephewrotoxicity and ototoxicity, in particular where the cell toxicity is induced by a medical treatment. In a preferred embodiment, the compounds have at least two nitrogen atoms, more preferably at least two amino groups. The compounds according to the invention are capable of docking binding of cell toxic compounds to the megalin receptor, and thereby inhibiting uptake of the cell toxic compounds into cells. The invention further relates to novel compounds for use in said treatment, as well as a method for reducing the cell toxicity of cell toxic compounds.

Description

[0001] All patent and non-patent references cited in this application are hereby incorporated by reference in their entirety. field of invention [0002] The present invention relates to the technical field of cytotoxic therapy and discloses compounds and combination medicaments for the above-mentioned therapy. Background of the invention [0003] The present invention relates to compounds for the prevention of organ damage, particularly kidney and inner ear organ damage resulting from the administration of therapeutic agents. [0004] Many drugs in clinical use are toxic to organs such as the kidneys and inner ear. Among the well-known drugs are cisplatin, ifosfamide, cyclosporine, amphotericin B, valproate, polymyxin B and therapeutic antibodies. Of particular importance, however, are the aminoglycosides, which are among the most important antibiotics for the treatment of severe bacterial infections. They are preferred agents against Gram-negative bacteria. At present, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P43/00A61K31/132A61K31/137A61K31/14A61K31/444A61K31/435A61K31/439A61K31/15A61K31/155A61K31/4035A61K31/495A61K31/34A61K31/351
CPCA61K31/132A61K31/495A61K31/137A61K31/444A61K31/351A61K31/14A61K31/4035A61K31/439A61K31/435A61K31/34A61K31/155A61K31/15A61P13/12A61P27/16A61P43/00Y02A50/30
Inventor 安德斯·尼科耶尔
Owner RECEPTICON
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