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Anti-hepatoma-virus agent

A technology for liver tumors and viral agents, applied in the field of new therapeutic agents, can solve problems such as undocumented infectious diseases

Active Publication Date: 2018-10-26
KAGOSHIMA UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Patent Document 1 only discloses an anti-HBV test as an actual antiviral test, and there is no description that 2'-fluoro-6'-methylene carbocyclic nucleosides can be used to treat infection by both viruses, HBV and HCV. disease

Method used

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Examples

Experimental program
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Effect test

no. 1 approach

[0066] As the first embodiment of the present invention, the active ingredient contained in the anti-hepatic tumor virus agent of the present invention against both HBV and HCV (hereinafter referred to as "the anti-hepatic tumor virus agent of the first embodiment of the present invention") is called 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl) adenine of clofarabine (in the compound of the above general formula (I), R 1 is fluorine) or a pharmaceutically acceptable salt thereof.

[0067] The chemical structural formulas of cladribine and fludarabine used in clofarabine and following examples are as follows:

[0068] [Chem 3]

[0069]

[0070] As shown in the following examples, the present inventors have no anti-HBV activity based on the cladribine formed by replacing the F at the ribose 2 position of clofarabine with H, thus finding that in the anti-HBV activity of clofarabine, clofarabine The F at position 2 of the ribose sugar is very important. In addition, al...

Embodiment approach

[0085] On the other hand, as the second embodiment of the present invention, the active ingredient contained in the anti-hepatic tumor virus agent against HCV of the present invention (hereinafter referred to as "the anti-hepatic tumor virus agent of the second embodiment of the present invention") is called 2-Chloro-9-(2-deoxy-β-D-arabinofuranosyl) adenine of cladribine (in the compound of the above general formula (I), R1 is hydrogen) or a pharmaceutically acceptable salt thereof .

[0086] In addition, according to the anti-hepatic tumor virus agent according to the second embodiment of the present invention, HCV infection can be prevented or treated, and HCV-related diseases can also be prevented or treated. Therefore, the anti-hepatic tumor virus agent of the second embodiment of the present invention can also be called a preventive or therapeutic agent for HCV-related diseases. Herein, HCV-related diseases refer to diseases caused by HCV infection, and examples thereof ...

Embodiment

[0091] The present invention will be described in more detail below using examples, but the technical scope of the present invention is not limited to these examples.

[0092] Anti-HBV activity and anti-HCV activity of clofarabine, and anti-HCV activity of cladribine

[0093] 1. Materials and Methods

[0094] 1-1. Measurement of anti-HBV activity

[0095] The evaluation of anti-HBV activity is to introduce the gene of 2 times the length of the HBV genome into the human liver cancer cell line HepG2 to form the HBV-producing cell line HepG2.2.15, and use this cell line to evaluate the intracellular activity on the 7th day after adding the drug by quantitative PCR. The amount of HBV DNA or the amount of HBV DNA in the culture supernatant. PCR of HBV DNA using forward primer (HBV-S190F; 5'-GCT CGT GTT ACA GGC GGG-3': SEQ ID NO:1) and reverse primer (HBV-S703R; 5'-GAACCA CTG AAC AAA TGG CAC TAG TA-3': SEQ ID NO: 2). "95°C for 10 seconds-62°C for 10 seconds-72°C for 30 seconds" ...

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Abstract

The purpose of the present invention is to provide a novel therapeutic agent against hepatoma viruses. Specifically, the present invention pertains to an anti-hepatoma-virus agent containing, as an active ingredient, a compound represented by a general formula (I) shown in the specification or a pharmacologically acceptable salt thereof, with R1 in the formula being fluorine or hydrogen.

Description

technical field [0001] The present invention relates to a novel therapeutic agent against eg liver tumor virus. Background technique [0002] In the case of viral infections, prevention of infection was only possible after the discovery of the smallpox vaccine treatment created by Jenner. However, for viruses without vaccines, when infected with the virus, the only option is to clear the virus through individual immunity and symptomatic treatment. The history of developing antiviral agents against viruses began in 1977 with aciclovir, a herpes simplex virus therapeutic agent developed by Elion et al. In 1985, Full House et al. discovered the therapeutic agent zidovudine for human immunodeficiency virus 1 (HIV-1). The development of antiviral agents has progressed for some viruses such as HIV-1, hepatitis B virus (HBV), hepatitis C virus (HCV), and influenza virus, but currently there are no antiviral agents for most viruses. [0003] HCV and HBV are liver tumor viruses th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7076A61P1/16A61P31/14A61P31/20A61P35/00
CPCA61K31/7076A61P1/16A61P31/20A61P31/14A61P35/00
Inventor 池田正德武田绿马场昌范加藤宣之
Owner KAGOSHIMA UNIV