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Di- and triphosphate prodrugs

A technology of compounds and medicinal salts, applied in the field of diphosphate and triphosphate prodrugs, to avoid side effects and improve the effect of actual use

Inactive Publication Date: 2017-05-10
UNIV OF HAMBURG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the β-cyanoethyl mask can only undergo chemical and non-enzymatic cleavage, which is necessary for use as a drug

Method used

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  • Di- and triphosphate prodrugs
  • Di- and triphosphate prodrugs
  • Di- and triphosphate prodrugs

Examples

Experimental program
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Embodiment

[0127] A schematic diagram of an example of a process for the preparation of compound I of the invention is shown below. The first benzyl alcohol derivative II A with phosphorus trichloride (PCl 3 ) to prepare compound 100, which reacts with N,N-diisopropylamine (NH(iPr) 2 ) react to form the corresponding phosphoramidite compound III. Compound III and the second benzyl alcohol derivative II B The reaction takes place to synthesize the phosphoramidite compound IV. It can then be combined with a mono- or diphosphate compound V, such as nucleoside monophosphate or nucleoside monophosphate analogs (both here abbreviated as NMP), or nucleoside diphosphate or nucleoside diphosphate analogs (both here Abbreviated as NDP) coupling, thereby obtaining compound I. The NDP or NTP compounds of the present invention (including nucleoside analogs containing compounds) may also be referred to herein as DiPPro nucleotides or TriPPPro nucleotides for short.

[0128]

[0129]For the pr...

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Abstract

The invention relates to compounds which can be used as prodrugs, in particular nucleoside diphosphate and triphosphate prodrugs, and to a method for producing said compounds. The aim of the invention is to provide improved di- and / or triphosphate prodrugs, in particular nucleotide or nucleotide analog prodrugs. This is achieved in one aspect by providing bioreversibly and asymmetrically masked di- and triphosphate compounds, in particular nucleoside diphosphate and nucleoside triphosphate compounds or the analogs thereof. The masking only occurs at the terminal phosphate, i.e. at the Beta- or Gamma-phosphate, whereas the masking of the internal phosphate is omitted.

Description

technical field [0001] The present invention relates to compounds useful as prodrugs, particularly nucleoside diphosphate and triphosphate prodrugs, and processes for the preparation of such compounds. Background technique [0002] Nucleoside analogs that can penetrate into DNA can be used in the treatment of viral infectious diseases such as herpes or hepatitis, or immunodeficiency diseases such as AIDS (Acquired Immunodeficiency Syndrome = acquired immunodeficiency syndrome), and cancer. After infiltration is complete, nucleoside analogs tend to act as chain terminators, that is, elongation no longer occurs in the 3' direction (J. Balzarini, P. Herdewijn, E. De Clercq; 2',3'-dide Differential patterns of intracellular metabolism of hydrogen-2′,3′-dideoxythymidine and 3′-azido-2′,3′-dideoxythymidine, two potent anti-human immunodeficiency virus compounds; Journal of Biochemistry 1989, 264, 6127-6133). However, nucleoside analogs must act as triphosphates (NTPs) to allow t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/00A61K31/7072A61P31/18A61P31/14A61P31/16
CPCC07H1/00C07H19/10A61P7/04A61P29/00A61P31/14A61P31/16A61P31/18C07F9/65586
Inventor 克里斯·梅尔特里斯坦·高耐斯特托拜厄斯·内科丽娜·魏因申克
Owner UNIV OF HAMBURG
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