153121-88-1Relevant academic research and scientific papers
Mononucleoside Phosphotriester Derivatives with S-Acyl-2-thioethyl Bioreversible Phospate-Protecting Groups: Interacellular Delivery of 3'-Azido-2',3'-dideoxythymidine 5'-Monophosphate
Lefebvre, Isabelle,Perigaud, Christian,Pompon, Alain,Aubertin, Anne-Marie,Girardet, Jean-Luc,et al.
, p. 3941 - 3950 (1995)
The synthesis, in vitro anti-HIV-1 activity, and decomposition pathways of several mononucleoside phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) incorporating a new kind of carboxylate esterase-labile transient phosphate-protecting group, namely S-acyl-2-thioethyl, are reported.All the described compounds showed marked antiviral activity in thymidine kinase-deficient CEM cells in which AZT was virtually inactive.The results strongly support the hypothesis that such pronucleotides exert their biological effects via intracellular delivery of the 5'-mononucleotide of AZT.This point was corroborated by decomposition studies in cell extracts and culture medium.
CYCLOPENTENYL PURINE DERIVATIVE OR SALT THEREOF
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Paragraph 0373-0375, (2021/05/28)
An object of the present invention is to provide a compound exhibiting an excellent drug efficacy as an anti-adenoviral agent, and an anti-adenoviral agent. The present invention provides an anti-adenoviral agent including a compound represented by General Formula [1] (in the formula, R1 represents a hydrogen atom, a halogen atom, an amino group which may be substituted, a monocyclic nitrogen-containing heterocyclic ring group which may be substituted (provided that a nitrogen atom forming the ring is bonded to a carbon atom to which R1 is bonded), a monocyclic nitrogen- and oxygen-containing heterocyclic ring group which may be substituted (provided that a nitrogen atom forming the ring is bonded to a carbon atom to which R1 is bonded), a C1-6 alkoxy group which may be substituted, a hydroxyl group which may be protected, or the like; R2 represents a hydrogen atom or an amino protecting group; R3 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; R4 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; and X represents an oxygen atom or a sulfur atom) or a salt thereof.
CYCLOBUTYL PURINE DERIVATIVE OR SALT THEREOF
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Paragraph 0297-0299, (2021/05/21)
An object of the present invention is to provide a compound exhibiting an excellent drug efficacy as an anti-adenoviral agent, and an anti-adenoviral agent. The present invention provides a compound represented by General Formula [1] (in the formula, R1 represents a halogen atom, an amino group which may be substituted, a C1-6 alkoxy group which may be substituted, a hydroxyl group which may be protected, or the like; R2 represents a hydrogen atom or an amino protecting group; R3 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; R4 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like); or a salt thereof.
CYCLIC DINUCLEOTIDE PRODRUG MOLECULE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0065-0068, (2021/11/04)
Disclosed are a cyclic dinucleotide prodrug molecule, a preparation method therefor and an application thereof relating to the field of pharmaceuticals. The cyclic dinucleotide prodrug molecule has a structure shown in formula I, II, or III, can freely cr
PHOSPHORODIAMIDATES AND OTHER PHOSPHORUS DERIVATIVES OF FINGOLIMOD AND RELATED S1 P RECEPTOR MODULATORS
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Page/Page column 57, (2019/04/26)
Compounds of general formula (I): (Formula I)) wherein R1, Q, R3, R4, R5, R6, R7 and Ar1 are as defined herein are inhibitors of class I histone deacetylases and are of use in th
THIONUCLEOSIDE DERIVATIVE OR SALT THEREOF, AND PHARMACEUTICAL COMPOSITION
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Paragraph 0479-0482, (2017/12/27)
Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General Formula [1] (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.
PYRROLO[1,2-f][1,2,4]TRIAZINES USEFUL FOR TREATING RESPIRATORY SYNCITIAL VIRUS INFECTIONS
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Paragraph 0430; 0431, (2015/05/26)
Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.
TRANSDUCIBLE DELIVERY OF NUCLEIC ACIDS BY REVERSIBLE PHOSPHOTRIESTER CHARGE NEUTRALIZATION PROTECTING GROUPS
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Page/Page column 56, (2008/06/13)
This disclosure relates to nucleic acid constructs modified to have a reduced net anionic charge. In some aspects the constructs comprise phosphodiester and/or phosphothioate protecting groups. The disclosure also provide methods of making and using such
Cell permeation of a Trypanosoma brucei aldolase inhibitor: Evaluation of different enzyme-labile phosphate protecting groups
Azema, Laurent,Lherbet, Christian,Baudoin, Cecile,Blonski, Casimir
, p. 3440 - 3443 (2007/10/03)
A series of four prodrugs directed against Trypanosoma brucei aldolase bearing various transient enzyme-labile phosphate protecting groups was developed. Herein, we describe the synthesis and evaluation of cell permeation of these prodrugs. The oxymethyl
Nucleotide mimics and their prodrugs
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Page 45, (2008/06/13)
The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.
