Benzoazacyclo compound and application thereof

A compound and drug technology, applied in the field of medicine, can solve problems such as inability to effectively reverse liver fibrosis in patients, failure to develop anti-hepatic fibrosis drugs, etc.

Active Publication Date: 2019-12-20
NANHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the existing antiviral drugs for hepatitis such as lamivudine, interferon, adefovir dipivoxil and sofosbuvir cannot effectively reverse the Hepatic fibrosis, so far no specific anti-hepatic fibrosis drug targeting a single link or target has been developed clinically

Method used

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  • Benzoazacyclo compound and application thereof
  • Benzoazacyclo compound and application thereof
  • Benzoazacyclo compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The synthesis of embodiment 1 benzazeterocyclic compounds

[0036]

Embodiment 2

[0037] Example 2 Left middle common bile duct ligation (LMBDL) induced liver fibrosis in mice

[0038] Experimental materials: C57L / 6 mice, 3% sodium pentobarbital solution, surgical instruments.

[0039] Experimental method: LMBDL group: 12-week-old male C57BL / 6 mice were anesthetized by intraperitoneal injection of 3% pentobarbital sodium solution, cut the abdominal skin and muscle layer, freed the common bile duct, ligated the left middle common bile duct, and sutured the abdominal cavity.

[0040] Sham-operated group: 12-week-old male C57BL / 6 mice were anesthetized by intraperitoneal injection of 3% pentobarbital sodium solution, the skin and muscle layer of the abdominal cavity were incised, the common bile duct was freed, and the abdominal cavity was sutured.

[0041]Treatment group: get through LMBDL operation (postoperative 24 hours) mouse, calculate according to 25mg / kg / d, 0.25mg / 10g body weight, calculate with every mouse 20g, get 0.5mg, be 20 μ l and formula (I ) d...

Embodiment 3

[0043] Example 3 HE staining and Sirius Red Staining (Sirius Red Staining) observation of benzazepine compounds shown in formula (I) (R1=Ts, R2=Ph, R3=Bn) on common bile duct ligation-induced mouse liver fibrosis influence

[0044] Experimental materials: camera, tissue section making, microscope.

[0045] Experimental method: The mouse liver tissue was fixed with paraformaldehyde, dehydrated, transparent, and soaked in wax, and then embedded in paraffin with an embedding machine. After the wax block solidified, it was stored in a refrigerator at 4°C. The wax blocks were then made into paraffin sections for HE staining and Sirius red staining.

[0046] HE staining: dewaxed by xylene I and II for 10 minutes each; put the sections in 100%, 95%, 85%, 75% alcohol solutions of various levels for 10 minutes each, rinse with tap water for 5 minutes, 1×PBS 5 Minutes; 0.3% H2O2 37 ℃ warm bath for 30 minutes, 1 × PBS washed again for 5 minutes; staining: hematoxylin dipping for 2 minu...

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Abstract

The invention discloses a compound represented by a formula (I) or a salt thereof. The invention further provides an application of the compound represented by the formula (I) or the salt thereof in preparation of drugs for preventing or treating hepatic fibrosis diseases. The invention provides a new benzoazacyclo compound or a salt thereof, and it is found that the benzoazacyclo compound has anobvious anti-hepatic fibrosis effect for the first time, and thus a new application of the benzoazacyclo compound in preparation of drugs for preventing hepatic fibrosis diseases or treating hepatic fibrosis diseases is found out.

Description

technical field [0001] The application relates to the technical field of medicine, in particular to benzoazepine heterocyclic compounds and applications thereof. Background technique [0002] Liver fibrosis (Liver Fibrosis) is a chronic liver disease, which is caused by many factors, such as inflammatory response, oxidative stress, autophagy, cytokines, anticoagulant therapy, etc., and its formation is also the result of the interweaving of many factors. The essence of liver fibrosis is that the synthesis of collagen-based extracellular matrix (ECM) is far greater than its degradation, resulting in a large amount of ECM deposition. A large number of studies have confirmed that the activation of hepatic stellate cells (HSC) plays a pivotal role in the development of liver fibrosis. Under physiological conditions, ECM is mainly synthesized by HSC; when liver tissue is damaged, HSC is activated and becomes myofibroblast (MFB) to secrete and synthesize ECM. fibrosis. [0003]...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D273/06A61P1/16A61P3/00A61P37/06A61K31/553
CPCC07D273/06A61P1/16A61P3/00A61P37/06
Inventor 谢伟全涂剑张素君李玲娇周芊芊李子涵
Owner NANHUA UNIV
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