30 results about "Y nucleoside" patented technology

The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.

The present invention relates to 2′-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I):As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related β-D and β-L-nucleoside derivatives.

The present invention relates to 2′-allene-substituted nucleoside derivatives of the general formula (I):As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related β-D and β-L-nucleoside derivatives.

The present invention relates to 2′-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I):As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related β-D and β-L-nucleoside derivatives.

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.

[Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose.[Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.

Therapeutic oligonucleotide analogues which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligomers with four atom linking groups forms unique di- and poly-nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

[Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose.[Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.

Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. The reactive portions preferably comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with or without intervening intercalating moieties. Therapeutics, diagnostics and research methods also are disclosed, as are synthetic nucleosides and nucleoside fragments that can be elaborated into oligonucleotides.

This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

Disclosed are bridged nucleosides and nucleotides. The nucleosides of the present invention have a 2′,4′-bridged structure and are represented by formula I below:An oligonucleotide containing a 2′,4′-bridged artificial nucleotide of the present invention has a binding affinity for single-stranded RNA comparable to that of known 2′,4′-BNA / LNA and higher nuclease resistance than LNA. In particular, since the oligonucleotide has a much higher binding affinity for single-stranded RNA than S-oligo, it is expected that the oligonucleotide is applicable to nucleic acid drugs.

This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, wherein the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

The invention discloses a method for measuring the contents of alkaloids, lignans and nucleosides in the isatis root or preparation thereof by using a quantitative analysis single-maker method. With low-cost stable-structure avaible alkaloids compound (R,S)-epigoitrin as a reference, relative correction factors with lignans compound clemastanin B and nucleoside compounds cytidine, uridine, vernine, and adenosine are established. Therefore, the contents of another five kinds of lignan and nucleoside contents with high content rates are calculated by using the correction factors only by measuring the content of the(R,S)-epigoitrin of the isatis root or preparation, thereby carrying out multi-indicator quality evaluation on the isatis root or preparation simply, conveniently, comprehensivelyand accurately. The quality controllability and curative effect stability of the product can be guaranteed; and the detection cost and time can be saved.

The invention belongs to the technical field of biological medicine and nucleoside compound preparation, and particularly relates to an N4-hydroxy cytidine lipid prodrug as well as a preparation method and application thereof. The N4-hydroxy cytidine lipid prodrug is selected from a compound shown in the following formula I, and n is an integer from 0 to 20; x is independently selected from CH2, O, S or NH; r is independently selected from hydrogen, deuterium, fluorine, chlorine, alkenyl, alkynyl, fluoromethyl, difluoromethyl, trifluoromethyl, dichloromethyl, trichloromethyl, hydroxymethyl, alkoxy, azido, cyano, aryl or heterocyclic radical. Tests prove that the prepared compound, namely the N4-hydroxy cytidine lipid prodrug, has higher anti-new coronavirus activity, so that the N4-hydroxy cytidine lipid prodrug can be used for preparing anti-new coronavirus drugs. In addition, compared with the existing nucleotide drugs, the compound provided by the invention has the advantages that the preparation process is shorter, the yield is higher, and the compound is suitable for industrial large-scale production and has a good application prospect.

The compositions of the present invention comprise one or more palladium bound ligands that are covalently bonded to inorganic or organic solid supports. These palladium bound ligands bonded to solid supports can be used for single heterocyclic amine base separation, or can be used to separate nucleotide chain containing specific sequences from other nucleotides or nucleotide chains. In one aspect of the invention, each ligand present is individually complexed to a single Pd(II) ion. If there are from 2 to 4 ligands present in the composition, then each ligand present must be separated from the other ligands by at least 3 atoms, preferably from 3 to 20 carbon atoms or equivalent spacing.

The invention discloses a method for extracting nucleotide and polypeptide from animal viscera. The method comprises the following steps of: taking fresh animal viscera, performing cleaning, draining,chopping and mashing, and adding deionized water to obtain a mixed solution; adding a guanidinium isothiocyanate solution into the mixed solution, vibrating the solution to mix the substances uniformly, and then performing standing; adding a carrier containing silicon dioxide into the solution, performing vibration and mixing the substances uniformly, then conducting standing, cracking cells by guanidinium isothiocyanate, and binding nucleotide released from the cells to silicon dioxide; taking out the carrier containing silicon dioxide, leaving the remaining solution for later use, carryingout adsorption and desorption on the carrier by an eluent, and conducting separation to obtain purified nucleotide. The invention has the beneficial effects that: the polypeptide and nucleotide can beextracted in sequence, nucleotide is extracted in a silicon dioxide adsorption mode, the carrier only has high adsorption capacity and affinity to nucleotide and does not adsorb other biochemical components like polysaccharide, and meanwhile the problem that mutual reaction between biochemical reagents when the biochemical reagents are added for extraction can be avoided.

The invention discloses alkaline xanthine dehydrogenase and application thereof in detection kits. A protein disclosed by the invention comprises a xanthine dehydrogenase large subunit and xanthine dehydrogenase small subunit. The alkaline xanthine dehydrogenase provided by the invention is reported for the first time, is acinetobacter baumannii xanthine dehydrogenase confirmed by experiments and is applicable to samples at alkali determination conditions. Compared with existing reports, the alkaline xanthine dehydrogenase has relatively high substrate affinity and the highest catalytic efficiency, is capable of sensitively degrading and detecting hypoxanthine / xanthine, PNP enzyme and 5'-nucleotidase and can be combined with PNP enzyme for detecting inorganic phosphate and adenosine deaminase, so that the catalytic efficiency is improved, the cost is lowered, and the industrial application process is benefited. The invention further provides a method for detecting the content of xanthine / hypoxanthine in samples including serum and urine by virtue the xanthine dehydrogenase. The invention further provides a detection kit for detecting the content of xanthine / hypoxanthine in the samples. The detection method and the detection kit are not influenced by dissolved oxygen in the samples; compared with the prior art, the alkaline xanthine dehydrogenase has the advantages that the detection range is relatively wide, the sensitivity is relatively high, and the detection method and the detection kit are suitable for popularization and application.

Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.

Disclosed is an RNA aptamer, a synthetic oligonucleotide of 2′-fluoro-modified A, U, and C nucleotides, with improved stability compared to its unmodified counterpart. Like the unmodified aptamer, however, the modified version is a potent glutamate receptor antagonist. Additionally, the RNA aptamers described herein are water soluble by nature, and generally exhibit nano- to micromolar potency making them potential therapeutic agents for the treatment of neurological disorders involving glutamate receptor activity.

The invention discloses a method for determining the content of alkaloids, lignans and nucleosides in Radix isatidis or its preparation by adopting a one-measurement multi-evaluation method. , S)-Yichun is used as a reference to establish its relative correction factor with the lignan compound tetracycline B and the nucleoside compounds cytidine, uridine, guanosine, and adenosine, to achieve by measuring only The content of (R,S)-report Yichun of Radix Isatidis or its preparations, the content of the other 5 kinds of lignans and nucleosides with higher content was calculated by the correction factor, so as to be simple, quick, comprehensive and accurate. The multi-index quality evaluation of its preparation is helpful to ensure the quality of the product is controllable and the curative effect is stable, while saving the testing cost and time.

The invention discloses a novel unsaturated nucleoside analogue, particularly relates to a 3 ', 4'-unsaturated-C-ribonucleoside analogue as well as a preparation method and application thereof, and belongs to the field of nucleoside chemistry and medicinal chemistry. The compound has a structure as shown in a general formula 1, wherein R represents H and CN groups; the compound has antiviral activity, can be used as an antiviral agent or a primer of an antiviral drug, and has a good development prospect.

The invention discloses rare-earth nucleoside fluorescent hydrogel as well as a preparation method and application thereof in fluorescent encoding. The preparation method of the rare-earth nucleosidefluorescent hydrogel comprises the following steps: (1) preparing a soluble rare-earth nitrate water solution and a nucleoside water solution; (2) uniformly mixing the soluble rare-earth nitrate watersolution and the nucleoside water solution and regulating the pH (Potential of Hydrogen) value to 7 to 9; raising the temperature to 55 to 95 DEG C and standing and reacting for 10 to 20min; coolingto room temperature and standing for 1 to 4h to obtain the rare-earth nucleoside fluorescent hydrogel with different fluorescent colors. The rare-earth nucleoside fluorescent hydrogel disclosed by theinvention has the advantages of environment-friendly and safe raw materials, simplicity in operation, low cost and good repeatability; the rare-earth nucleoside fluorescent hydrogel disclosed by theinvention keeps characteristic of emission fluorescent light of rare-earth ions and also has characteristics of good biocompatibility of biological small molecular nucleoside, biodegradability, no toxicity and the like. The obtained fluorescent hydrogel is regulated and controlled to obtain various fluorescent colors and can be used as a fluorescent encoding material; the fluorescent hydrogel canbe used for fluorescent biological detection, cell culture and tissue engineering.

Methods for forming 2-bromo, 2-fluoro ribofuranose intermediates and 2-chloro, 2-fluoro ribofuranose intermediates for use in preparing antiviral nucleosides are disclosed. Methods for forming nucleosides, and nucleoside prodrugs, using the intermediates, are also disclosed. The methods all produce intermediates, and the resulting nucleosides and prodrugs thereof, wherein the chirality of the carbon at the 2-position is controlled. In some embodiments, the chemistry involves using chiral auxiliaries, such as (R)-2,2-dimethyl-1,3-dioxolane-4-carbaldehyde, and in other embodiments, the chemistry involves using chiral starting materials, such as D-xylose.

The present invention pertains to: an alkoxyphenyl derivative with which oligonucleotides can by synthesized by a liquid-phase synthesis method easier and faster than conventional methods; a nucleoside protector and a nucleotide protector to which the alkoxyphenyl derivative binds; a method for producing an oligonucleotide using same; and a method for selectively removing the alkoxyphenyl derivative moiety. Provided is a compound represented by general formula (1) or a derivative thereof. (In the formula, each R independently represents a C10-40 alkyl group which may be substituted or unsubstituted. m represents an integer of 1-5. When m is 2 or more, the plurality of RO's may be identical or different. X represents O, S, NH, or NRN. n represents an integer of 1-4. RN represents a C1-6 alkyl group which may be substituted or unsubstituted.).