Abstract: The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.

Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.

Abstract: The present invention is made to fulfill the foregoing need. Since most of antiHN nucleosides are 2?,3?-dideoxynucleosides that have been proved to be excellent substrates of kinases for the phosphorylations. 2?,3?-Dideoxy-2,-a-fluoro-2?-{3-C-methyl-nucleosides can be considered as one unique class of 2?,3?-dideoxynucleosides to be good substrate of kinases because fluorine mimics hydrogen. It also can be considered as ribo-nucleosides to incorporate into RNA of HCV because 2?-fluorine-a mimics 2?-a-OH group.

Abstract: A 2?-modified ribonucleoside having an alkoxymethyl protective group can be imparted with a high duplex-forming ability by introducing, as a substituent, a halogen atom into the protective group moiety. A modified form of RNA having a halogen-substituted alkoxymethyl protective group exhibits a high duplex-forming ability that is comparable to the duplex-forming ability of a 2?-O-methyl modified nucleic acid.

Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, R2, and R3 are as described herein.

Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:

Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.

Abstract: A method of modifying a nucleotide or a nucleotide analogue to increase its overall effectiveness in treating an antiviral disease is provided. In some cases, a compound comprising a base, sugar, phosphonate moiety, and amino acid residue is provided, where the base-sugar may be a nucleoside, and the amino acid residue may be a tyrosine residue. In certain cases, the tyrosine residue contains a long chain alkyl group on the carboxamide group of the residue. Methods of inhibiting viral replication and methods of treating a viral infection are also provided.

Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.

Abstract: Disclosed herein are double stranded RNA molecules which have been modified to exhibit one of the following, increased activity, enhanced nuclease stability, reduced off target activity and or reduced immunogenicity, to pharmaceutical compositions comprising such compounds and to methods of use. Further disclosed is a method for the synthesis of threose nucleic acid phosphoramidites and methods of use thereof.

Abstract: A method for preparing a phosphitylated compound comprising the step of:—reacting a hydroxyl containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R1, R2=either H or form a 5 to 6-membered ring together. X1, X2=independently either N or CH Y=H or Si(R4)3, with R4=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B=deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.

Abstract: This application discloses phosphoramidate and phosphonoamidate prodrugs of alcohol-based therapeutic agents, such as nucleosides, nucleotides, acyclonucleosides, C-nucleosides, and C-nucleotides, and use of these prodrugs for treatment of diseases or disorders, including infectious diseases and cancers. This application also discloses a general method for enhancing bioavailability and/or liver-targeting property of alcohol drugs through converting the alcohol drugs to phosphoramidate or phosphonoamidate prodrugs, and methods of preparation of these prodrugs.

Abstract: The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.

Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Abstract: Substitution derivatives of N6-benzyladenosine-5?-monophosphate of the general formula I, wherein (R)n represents 1 to 4 substituents (n is in the range 1-4), which can be the same or different, and R is selected from the group comprising C1 to C8 alkyl, C1 to C8 alkoxy, amino, halogen, hydroxy, mercapto and nitro groups, and the pharmaceutically acceptable salts thereof. A Method for their preparation, their use as medicaments and in other applications, and a therapeutic composition containing these derivatives is also disclosed.

Abstract: A method for preparing a phosphitylated compound comprising the step of:—reacting a hydroxyl containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R1, R2=either H or form a 5 to 6-membered ring together. X1, X2=independently either N or CH Y?H or Si(R4)3, with R4=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B=deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.

Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.

Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.

Abstract: The compounds are phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludarabine and clofarabine useful in the treatment of cancer.

Abstract: The present invention provides for compounds of Formula I: wherein X—N and R1-R4 have any of the values disclosed in the specification. The compounds of Formula I are useful as reagents to introduce N-alkyl nucleosides into DNA oligonucleotides. The present invention also provides for methods of synthesizing the compounds of Formula I.

Abstract: The compounds are phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludarabine and clofarabine useful in the treatment of cancer.

Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:

Abstract: Provided is a new production method for the synthesis of an NC type nucleoside efficiently and conveniently in a high yield without unnecessary protecting group conversion steps. It relates to a step of producing a compound represented by the formula (II): or a salt thereof, by inverting a compound represented by the formula (I): and a method of producing a compound represented by the formula (III): or a salt thereof (wherein each symbol is as defined in the specification), which includes the step.

Abstract: Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same.

Abstract: Phosphoramidate derivatives of nucleoside compounds of formula I derived from bases such as adenine and guanine have enhanced therapeutic potency, in particular, enhanced potency with respect to the prophylaxis or treatment of a viral infection such as hepatitis C virus. The glycoside moiety of the nucleoside compound is suitably substituted at the ?-2? position with methyl and the phosphoramidate group, suitably comprises 1-naphthyl linked by —O— to the P atom.

Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.

Abstract: The use of a sulfurizing agent of formula A: or a salt, hydrate, solvate, or a mixture thereof, in which all R groups, independently, represent H or an organic group, in sulfurization. The sulfurizing agent is preferably a formamidine disulfide. It is found a particularly suitable alternative to existing sulfurizing agents, since it is easy to synthesize from readily available, cheap starting materials.

Abstract: The invention provides a novel method of 2?,3?-cyclic phosphate and phosphorothioate of mono and oligonucleotide synthesis. The invention also provides a novel method of the synthesis of 3?,5?-cyclic phosphate and phosphorothioate mononucleotide. The invention also envisions providing kits comprising at least one composition disclosed in the present invention.

Abstract: The present invention relates to novel phosphoramidites, A-n-bz, C-n-bz, C-n-ac, G-n-ac and U are produced with an HPLC purity of greater than 98% and 31P NMR purity greater than 99%. A novel process of reverse 5??3? directed synthesis of RNA oligomers has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.

Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.

Abstract: Provided are methods of designing a putative inhibitor of a human 5?-methylthioadenosine phosphorylase (MTAP). Also provided are methods of inhibiting a human MTAP.

Abstract: This invention relates to an improved process for the industrial manufacture of S-adenosyl-L-methionine (SAMe) of formula (I), which consists of stereo-selective methylation of S-adenosyl-L-homocysteine (SAH) with the enrichment of active (S,S)-isomer.

Abstract: The present invention relates to a method for nucleic acid replication and novel artificial base pairs. The method of the present invention for nucleic acid replication is characterized in that a deoxyribonucleoside 5?-triphosphate, in which the hydroxyl group of phosphoric acid at the ?-position is substituted with a group selected from the group consisting of an amino group, a methylamino group, a dimethylamino group, a mercapto group and a fluoro group, is used as a substrate during replication reaction. The novel artificial base pairs of the present invention are characterized in that 7-(2-thienyl)-imidazo[4,5-b]pyridine (Ds) or an analog thereof forms a base pair with pyrrole-2-carbaldehyde (Pa) or an analog thereof.

Abstract: Crystals of a purine nucleoside compound, particularly crystals of 2?,3?-dideoxyinosine, which have excellent storage stability and have a concentration of phosphate attached to the crystal of 25 ppm or more, may be produce by: (1) preparing an aqueous solution containing phosphate ion (PO43?) and a purine nucleoside compound; and (2) crystallizing the purine nucleoside compound from the aqueous solution.

Abstract: The present invention provides a stable salt of 3?-phosphoadenosine 5?-phosphosulfate (PAPS) and a production method therefor. The present invention is directed to a stable salt of PAPS (amine salt), which is formed between PAPS and an amine compound, and to a method for producing a stable salt of PAPS, which includes adding an amine compound to an aqueous PAPS solution in an amount by mole equal to or greater than that of PAPS, and lyophilizing the resultant solution. The present invention has first realized production of a solid-form PAPS salt having considerably improved stability through a very simple technique. Since the thus-produced amine salt of PAPS is very stable, the salt can be stored or employed without taking much care about decomposition thereof at ambient temperature.

Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.

Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

Abstract: This invention provides novel 8-carbyl substituted Camps (adenosine 3?,5?-cyclic monophosphorothioate) and a novel procedures for the preparation of 8-Br-cAMP, a key starting material.

Abstract: Disclosed are compounds, compositions and methods for treating hepatitis C virus infections.

Abstract: Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or pharmacology as, for example, active compounds for crop protection or pharmaceuticals for humans or animals.

Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.

Abstract: Purine nucleotide derivative disodium crystals having a minimized amount of remaining alcohol such as methanol, ethanol or a mixture thereof are produced by overdrying purine nucleotide derivative disodium crystals containing the alcohol; and bringing the overdried purine nucleotide derivative disodium crystals into contact with an aqueous solution containing a hydrophilic organic solvent to control the humidity of the purine nucleotide derivative disodium crystals under a high humidity condition.

Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.

Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.

Abstract: The present method describes the use of thio-phosphate as a feed source for micro-organisms and multi-cellular organisms. This compound enters into nucleotide pools and ultimately into polymers of both RNA and DNA forming stable phosphorothioate internucleotide linkages. The method enables the microbial synthesis of both plasmid and phage DNA substituted with phosphorothioate. Furthermore, methods are described for the preparation of phosphorothioate oligo mixtures from recombinant phage DNA grown in modified media for use in antisense studies.

Abstract: Propargylethoxyamino nucleosides are disclosed having the structure wherein R1 and R2 are —H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W1 is —H or —OH; W2 is —OH or a moiety which renders the nucleoside incapable of forming a phosphodiester bond at the 3?-position; and W3 is —PO4, —P2O7, —P3O10, phosphate analog, or —OH. Additionaly, a primer extension method is provided employing the above propargylethoxyamino nucleosides.

Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds as adenosine A2a receptor agonists.

Abstract: A process for substantially enhancing the regio and stereoselective synthesis of 9-?-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-?-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2?-deoxy, 3?-deoxy, 2?-deoxy-2?-?-fluoro and 2?,3?-dideoxy-2?-?-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.