Tenofovir bis-l-amino acid ester and preparation method thereof

A tenofovir and amino acid ester technology, applied in the field of medicinal chemistry, can solve the problems of maintaining sufficient drug concentration at the infection site and poor membrane permeability
CN108948084BActive Publication Date: 2020-10-20ZHEJIANG STARRY PHARMA +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG STARRY PHARMA
Publication Date
2020-10-20

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Abstract

The invention relates to a tenofovir bis-L-amino acid ester compound as shown in a formula (I), a preparation method and medical application of the compound, and an anti-hepatitis B medicine composition taking the compound as an effective component. More specifically, the invention relates to a 9-[2-(phosphonylmethoxy)propyl]adenine bis-L-amino acid ester compound, wherein R represents isopropyl,isobutyl, sec-butyl or benzyl, X represents oxygen or sulfur, and n represents a number selected from 1-3.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and relates to tenofovir bis-L-amino acid ester compounds with anti-hepatitis B virus (HBV) activity, a preparation method thereof, and an anti-hepatitis B pharmaceutical composition containing them; more specifically, the present invention The invention relates to 9-[2-(phosphonomethoxy)propyl]adenine bis-L-amino acid ester compounds and 9-[2-(phosphonomethoxy)propyl]adenine bis-L-thio Amino acid ester compounds. Background technique

[0002] Nucleoside compounds are an important class of clinical antiviral (HIV, HBV, HCV, influenza virus, herpes virus, etc.) drugs, but their drug resistance is increasing year by year, and has become a major public health and social problem of global concern. Compared with cyclic nucleoside reverse transcriptase inhibitors, non-cyclic nucleoside drug tenofovir [(R)-PMPA] has significant advantages in the prevention and treatment of viral drug resistance. For...

Claims

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