Application of compound XL-001 in preparation of medicines for treating chronic kidney disease

A technology for chronic kidney disease and compounds, applied in the field of preparation of drugs for the treatment of chronic kidney disease, to achieve the effect of delaying and inhibiting progress

Active Publication Date: 2015-05-27
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still no effective drugs to delay the progression of CKD clinically.

Method used

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  • Application of compound XL-001 in preparation of medicines for treating chronic kidney disease
  • Application of compound XL-001 in preparation of medicines for treating chronic kidney disease
  • Application of compound XL-001 in preparation of medicines for treating chronic kidney disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Inhibition of XL-001 on renal fibrosis in UUO mice

[0021] 1. Experimental animals: BALB / c mice, male, weighing 20-22g, SPF grade. The animals were first weighed and numbered, and 18 healthy mice weighing 20-22 g were selected and randomly divided into 3 groups, 6 in each group. Including sham operation group, model control group and medication group.

[0022] XL-001 [N-(4-diethylamino-benzyl)-4-methoxy-N-p-tolyl-benzenesulfonamide; molecular formula C 25 h 30 N 2 o 3 S; molecular weight is 438.58] is a small molecular compound synthesized by the inventor's laboratory. The molecular structure of XL-001 is shown in the following formula:

[0023]

[0024] N-(4-Diethylamino-benzyl)-4-methoxy-N-p-tolyl-benzosulfonamide

[0025] 2. Treatment of each group

[0026] 1) Sham-operated group: After mice were anesthetized with 3% pentobarbital sodium at room temperature and 1ml / kg body weight, an incision was selected 1-2 cm below the left dorsal costal mar...

Embodiment 2

[0040] Example 2: Inhibition of XL-001 on renal fibrosis in UIRI mice

[0041] 1. Experimental animals: BABL / c mice, male, weighing 20-22g, SPF grade. The animals were first weighed and numbered, and 18 healthy mice weighing 20-22 g were selected and randomly divided into 3 groups, 6 in each group. Including sham operation group, model control group and medication group.

[0042] XL-001 (molecular formula C 25 h 30 N 2 o 3 S; molecular weight is 438.58) was synthesized by our laboratory.

[0043] 2. Treatment of each group

[0044] 1) Model control group: After mice were anesthetized with 3% pentobarbital sodium at room temperature and 1ml / kg body weight, the incision was made 1-2 cm below the left ventral costal margin; the skin, subcutaneous layer, muscle layer and peritoneum were cut layer by layer After the left kidney was found, the left renal artery was clamped with a vascular-arterial clip. During this period, the mouse was placed on a 37°C constant temperature inc...

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Abstract

The invention relates to a novel application of a small molecule compound XL-001, in particular to an application of a compound XL-001 in preparation of medicines for treating a chronic kidney disease (CKD), and provides an application of the XL-001 in treatment of the CKD. The compound XL-001 is significant in curative effect, and free of an obvious toxic or side effect, so that the compound XL-001 provided by the invention can be prepared into a medicinal preparation for treating the CKD.

Description

technical field [0001] The present invention relates to small molecular compound XL-001 [N-(4-diethylamino-benzyl)-4-methoxy-N-p-tolyl-benzenesulfonamide; an inverse agonist of cannabinoid receptors (Inverse agonist)], specifically relates to the use of compound XL-001 in the preparation of drugs for the treatment of chronic kidney disease (CKD). Background technique [0002] Chronic kidney disease (CKD) is becoming a "public health problem", which seriously endangers human health and consumes a lot of health resources. However, currently there are no drugs that can effectively delay the progression of CKD clinically. Aiming at the pathogenesis of CKD, finding drugs that can effectively inhibit or delay the progress of CKD is undoubtedly an urgent task in the field of nephrology, and it has become one of the strategic priorities that need to be overcome. [0003] Cannabinoid receptors are a group of G protein-coupled receptors (Front Biosci, 2009, 14:944), involved in appe...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K31/18A61P13/12
Inventor刘友华解昭骏周丽丽杨鹏
OwnerNANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV