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Use of derivatives with C-O-P bonds in patients with renal failure

A kidney function and application technology, applied in the direction of medical preparations containing active ingredients, drug combinations, drug delivery, etc.

Pending Publication Date: 2022-02-08
SANIFIT THERAPEUTICS SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Within this large family containing C-O-P bonds, some compounds have been found to inhibit various types of calcification, but these treatments have not been proven useful in the presence of renal damage, as known studies are either related to normal renal function, or In the case of uremia, the compound was not found to be effective

Method used

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  • Use of derivatives with C-O-P bonds in patients with renal failure
  • Use of derivatives with C-O-P bonds in patients with renal failure
  • Use of derivatives with C-O-P bonds in patients with renal failure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0136] Example 2. In vitro determination of the affinity of IP6 for hydroxyapatite (HAP).

[0137] Purpose: The purpose of this study is to analyze the affinity of IP6 to its target, thereby obtaining the affinity curve of IP6 to HAP.

[0138] Assay: 4 different amounts of HAP were incubated with increasing concentrations of IP6 for 4 hours at 37°C, pH 7.4, with constant agitation. The total amount of IP6 bound to the surface of the target (HAP) was quantified.

[0139] Results: A dose-dependent adsorption curve was obtained and saturated at a concentration of 7.6 μM or higher. The maximum adsorption of IP6 on the HAP surface ranged from 4.8 mg when using 300 mg of target to 6.42 mg when using 25 mg of HAP, and was achieved in the presence of 7.6 μM IP6 over 8 hours. To characterize the binding behavior of IP6, the EC of its adsorption on HAP was calculated 50 and E max . Calculations were performed using a nonlinear regression model (Log[agonist] versus response-slope va...

Embodiment 3

[0141] Example 3. In vitro determination of the binding kinetics of IP6 to HAP.

[0142] Objective: To analyze the binding rate of IP6 and HAP.

[0143] Test: 130 mg HAP was incubated with 7.6 μM IP6 (3 replicates) for different time intervals at 37° C., pH 7.4, with constant agitation.

[0144] Results and Discussion: Rapid binding of IP6 to HAP was observed ( figure 2 ), and reached the adsorption maximum at 60 min. Approximately 80% of maximum binding was achieved after 5 minutes.

Embodiment 4

[0145] Example 4. In vitro affinity of IP6 for HAP. Release research.

[0146] Objective: To analyze the release rate of IP6 from HAP.

[0147] Test: 130 mg HAP was incubated with 7.6 μM IP6 for different time intervals at 37° C., pH 7.4, with constant agitation. Subsequently, the HAP with adsorbed IP6 was placed in a solution without IP6, and the amount of IP6 released from the surface of the HAP was evaluated at different time points.

[0148] Results and Discussion: A relatively slow release of IP6 from the surface of HAP was observed ( image 3 ). After 2 days of incubation, 80% of IP6 remained bound to the surface of HAP.

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Abstract

The invention provides the use of a derivative with C-O-P bonds in the form of controlled release for the treatment of patients with renal failure. The invention also relates to the use of the derivative together with other active substances, that can particularly be selected from the list comprising a calcimimetic, a vitamin, a phosphorus chelator, thiosulfate, biphosphonate, pyrophosphate, citrate, a diuretic, an antihypertensive and an anticholesterolemic agent.

Description

[0001] This application is a divisional application of an invention patent application with an application date of March 14, 2014, an application number of 201480021589.1, and an invention title of "Use of Derivatives Containing C-O-P Bonds in Patients Suffering from Renal Failure". technical field [0002] The present invention relates to the use of a long-acting form of a compound comprising a C-O-P bond for the treatment of a disease in a patient suffering from renal failure, irrespective of whether the compound is being treated otherwise. Background technique [0003] Renal failure (also known as renal impairment or kidney disease) is a condition that results in a progressive loss of kidney function with a reduction in the glomerular filtration rate (GFR) or index. Although the initial stages of renal injury can be asymptomatic, as the disease progresses, uremia presents. Uremia is a concept that describes the contamination of the blood caused by the kidneys not properly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/6615A61K45/06A61P13/12A61P3/14A61P13/04A61P9/00A61P19/10A61P35/00A61P19/06A61P29/00A61P17/00A61P19/02A61P19/08
CPCA61K45/06A61K31/6615A61P13/12A61P17/00A61P19/02A61P19/06A61P19/08A61P19/10A61P21/00A61P29/00A61P3/14A61P9/00A61K2300/00A61K9/00A61K9/20A61K45/00
Inventor J·皮瑞罗佰斯塔德C·萨尔塞多罗卡M·D·费勒瑞尼斯B·艾森阿门瓜尔P·H·朱伯特
Owner SANIFIT THERAPEUTICS SA
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