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Adefovir dipivoxil ester colalin derivatives as well as preparation method and uses thereof

A technology for adefovir dipivoxil and its derivatives, which is applied in the field of adefovir dipivoxil cholic acid derivatives and its preparation, and can solve problems that do not involve adefovir dipivoxil cholic acid derivatives

Inactive Publication Date: 2008-05-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

None of the above patents involved adefovir dipivoxil cholic acid derivatives, nor did they mention that adefovir dipivoxil cholic acid derivatives have the characteristics of liver targeting

Method used

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  • Adefovir dipivoxil ester colalin derivatives as well as preparation method and uses thereof
  • Adefovir dipivoxil ester colalin derivatives as well as preparation method and uses thereof
  • Adefovir dipivoxil ester colalin derivatives as well as preparation method and uses thereof

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Experimental program
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Embodiment 1

[0058] Embodiment 1 The structural formula of adefovir dipivoxil bile acid conjugates

[0059] Formula 9:

[0060]

[0061] where R 1 , R 2 , R 3 and R 4 are a hydrogen atom or a hydroxyl group, respectively.

Embodiment 2

[0062] The structural formula of embodiment 2 adefovir dipivoxil bile acid salts

[0063] Formula 10:

[0064]

[0065] Where X is -OH, -NH-(CH 2 ) n SO 3 H,, -NH-(CH 2 ) n -CO 2 H (wherein n is an integer of 1-3).

Embodiment 3

[0066] The structural formula of embodiment 3 adefovir dipivoxil bile acid salts

[0067] Formula 11:

[0068]

[0069]where R 1 , R 2 , R 3 and R 4 Respectively hydrogen atom or hydroxyl; Wherein X is -OH, -NH-(CH 2 ) n SO 3 H,, -NH-(CH 2 ) n -CO 2 H (wherein n is an integer of 1-3).

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Abstract

The present invention discloses an adefovir dipivoxil cholic acid class derivative and also relates to a preparation method and applications thereof at the medical aspect. The adefovir dipivoxil cholic acid class derivative is a hepatic targeting precursor drug of adefovir; compared with the adefovir dipivoxil, the adefovir dipivoxil cholic acid class derivative can improve the concentration of the adefovir in liver after being taken orally, and the adefovir dipivoxil cholic acid class derivative can be used as a preferential drug for the treatment of resisting virus and especially resisting hepatitis virus.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically adefovir dipivoxil cholic acid derivatives, a preparation method and application thereof. Background technique: [0002] Adefovir dipivoxil chemical name: 9-[2-[bis(pivaloyloxymethoxy)phosphorylmethoxy]ethyl]adenine, CA accession number is [142340-99- 6], molecular formula: C 20 h 32 N 5 o 8 P, its structural formula is as formula 1: [0003] [0004] Adefovir dipivoxil is the prodrug of adefovir, which is a purine derivative. It can be taken orally and hydrolyzed into adefovir after oral administration. It has antiviral effect without phosphorylation. This product can inhibit the activity of HBV DNA polymerase, and can penetrate into the DNA of hepatitis B virus to inhibit the replication of the virus. It has a strong inhibitory effect on HBV virus strains resistant to lamivudine and famciclovir. It is used clinically Hepatitis treatment. [0005] The earliest compound p...

Claims

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Application Information

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IPC IPC(8): C07F9/6561C07J9/00A61K47/48A61K31/675A61P1/16A61K47/54
Inventor 周建平张振海吕慧侠张磊谢俊郭伟程玉钏张辉李悦恒吴益平
Owner CHINA PHARM UNIV
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