Abstract: The present invention discloses novel and improved nucleosidic and nucleotidic compounds that are useful in the light-directed synthesis of oligonucleotides, as well as, methods and reagents for their preparation. These compounds are characterized by novel photolabile protective groups that are attached to either the 5?- or the 3?-hydroxyl group of a nucleoside moiety. The photolabile protective group is comprised of a 2-(2-nitrophenyl)-ethyoxycarbonyl skeleton with at least one substituent on the aromatic ring that is either an aryl, an aroyl, a heteroaryl or an alkoxycarbonyl group. The present invention includes the use of the aforementioned compounds in light-directed oligonucleotide synthesis, the respective assembly of nucleic acid microarrays and their application.

Abstract: Oligonucleotide probes containing two labels are provided and are useful in hybridization assays. The probes can also contain a minor groove binding group.

Abstract: A compound of formula (I) and pharmaceutically acceptable salts thereof; compositions containing it and its use in medicine, particularly for the treatment or inhibition of HCV infections, and processes for making it are disclosed.

Abstract: The present invention relates to the use of N-phosphonylmethoxyethyl nucleoside analogs for manufacturing a medicament for the treatment or prevention of Koi Herpes virus infections in fish, especially in carps.

Abstract: The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5?-methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.

Abstract: The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically accepatble salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).

Abstract: The invention relates to non-natural bases and base pairs that expand the normal DNA-based encoding system. Compositions herein may comprise at least one non-natural base that may interact with another base via a Watson Crick-type hydrogen bonding geometry and/or a Hoogsteen-type hydrogen bonding geometry. The bases may be used in a molecular entity, such as an oligomer or any other entity wherein the bases are attached to a backbone. For example, they may be comprised in DNA, RNA, or PNA, or a variety of other nucleic acid-type systems.

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: Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modification comprising a polycyclic sugar surrogate. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleoside of the oligomer has a polycyclic sugar surrogate modification.

Abstract: Fluorous-tagged oligonucleotide reagents and an oligonucleotide purification methodology making use thereof, the method comprising: Synthesizing oligonucleotides using oligonucleotide reagents each bearing at least one fluorous group to yield a mixture of synthesis products and reagents, the mixture including at least one target synthesized oligonucleotide bearing at least one fluorous group; passing the mixture through a separation medium having an affinity for the at least one fluorous group so that the target synthesized oligonucleotide bearing at least one fluorous group is adsorbed by the separation medium; washing the separation medium with at least a first solvent to selectively dissociate therefrom substantially all synthesis products and reagents of the heterogenous mixture other than the at least one target synthesized oligonucleotide bearing at least one fluorous group; and subsequently dissociating the at least one synthesized oligonucleotide from the separation medium, with or without the fluorou

Abstract: Disclosed are polymeric compounds which are useful as prodrugs, comprising a chain of monomeric nucleosides, nucleoside analogs or abasic nucleosides, wherein at least one of the nucleosides or nucleoside analogs or a heterocyclic derivative thereof is pharmaceutically active and the nucleosides, nucleoside analogs or abasic nucleosides are linked by a phosphodiester group, a phosphorothioate group or an H—, alkyl or alkenyl phosphonate group.

Abstract: The present invention relates to the field of improving the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. More particularly, the present invention provides flavour modulating substances selected from the group represented by formula (1): and edible salts thereof and edible esters thereof, which can advantageously be used for modulating the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. These flavour modulating substances can be used to impart desirable taste attributes in a wide variety of applications and products. In addition, the present flavour modulating substances are capable of modulating the taste and/or aroma impact of other, flavour imparting, substances contained within these same products, thereby improving the overall flavour quality of these products.

Abstract: A phosphorylated A2A receptor agonist providing agonist properties on the A2A receptor after dephosphorylation the phosphorylated A2A receptor agonist comprises a ribosyl moiety and a purine moiety and being phosphorylated at the 5?-position of the ribose moiety except adenosine monophosphate (AMP), adenosine diphosphate (ADP) or adenosine triphosphate (ATP), a medicament containing the compound of the invention including ADP and the use of the compound of the invention including ATP and ADP for several medical indications e. g. inflammatory events. In particular, compounds of formula (I) are also disclosed.

Abstract: The present invention relates generally to labeled and unlabled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.

Abstract: The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer.

Abstract: The present invention aims to provide a composition which has an extremely broad range of applications, has an excellent safety, and can be used for preventing, ameliorating, or therapeutically-treating diabetes. The present invention provides an agent for preventing, ameliorating, or therapeutically-treating diabetes or a diabetic complication, a glycemic control agent, and an insulin secretion-promoting agent, each of which contains reduced coenzyme A as an active ingredient. The present invention also provides a method for preventing, ameliorating, or therapeutically-treating diabetes or a diabetic complication, which includes administration of the aforementioned agent.

Abstract: The present invention concerns methods of polymerase independent template directed elongation of polynucleotides, nucleotide building blocks used in these methods as well as the use of the methods and building blocks for the determination of nucleotide sequences, in particular for the determination of SNPs, base modifications, mutations, rearrangements and methylation patterns.

Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The invention provides compounds of Formula (I), as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.

Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.

Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.

Abstract: The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs. In particular, the invention provides isoguanosine nucleosides and derivatives thereof as well a method of increasing the mutation rate of a virus such as bovine viral diarrhea virus (BVDV) and hepatitis C virus (HCV).

Abstract: The present invention provides a novel method for solid-phase phosphoramidite based synthesis of borane phosphonate DNA. Also provided are novel phosphoramidite molecules, novel extended length borane phosphonate nucleic acid compounds, and methods of use thereof.

Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Abstract: Provided are imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

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: The invention provides a 5?-amino-2?-fluoro-2?,5?-dideoxynucleoside compound represented by the formula [1]: wherein R1 represents a nucleic acid base which may have a protecting group; R2 represents a hydrogen atom or an amino protecting group; and R3 represents a hydrogen atom or a hydroxyl protecting group. The invention also provides a dideoxynucleoside-insoluble carrier bound substance and an oligonucleotide analogue involving the dideoxynucleoside compound.

Abstract: Disclosed are methods for treating hepatitis C viral infections using deaza-purine compounds of Formula I: wherein W, W1, W2, Y, R1, Z, Y? and R are as defined herein.

Abstract: Disclosed are ?-D-ribofuranosyl-pyrazolo[3,4-d]pyrimidine compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Representative compounds include those having the general formula.

Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue. The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. The derivative is useful as a medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

Abstract: One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3?-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a non-phosphate linkage occurs in only one strand. In certain embodiments, a non-phosphate linkage occurs in both strands. In certain embodiments, a ligand is bound to one of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, a ligand is bound to both of the oligonucleotide strands comprising the double-stranded oligonucleotide.

Abstract: A nucleotide analogue compound represented by formula (1) and salts thereof. In formula (1), A represents a direct bond, C1-4 alkylene, etc.; B represents an optionally substituted aromatic heterocyclic groups; and R1, R2, R3 and R4 each represents hydrogen, an amino-protecting group, a hydroxyl-protecting group, a phosphate group, or —P(R7)R8, wherein R7 and R8 each represents hydroxyl, protected hydroxyl, mercapto, protected mercapto, etc. The compounds are useful as nucleotide analogues for producing oligonucleotide analogues useful in an antisense method and for producing intermediates thereof.

Abstract: The present invention discloses compounds of formula (I) or (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).

Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.

Abstract: The insecticides of the invention target the downstream portions of the signaling sequence of B. thuringiensis toxin, specifically protein kinase A (PKA) or adenylate cyclase (AC).

Abstract: Disclosed herein are compounds that activate RNaseL, methods of synthesizing compounds that activate RNaseL and the use of compounds that activate RNaseL for treating and/or ameliorating a disease or a condition, such as a viral infection, cancer and/or parasitic disease.

Abstract: The present invention relates to the use of at least one Epac (Exchange Protein directly Activated by cAMP) antagonist for the manufacture of a medicament intended for the prevention or the treatment of pathologies selected from the list comprising cardiac hypertrophy, cardiac arrhythmias, valvulopathies, diastolic dysfunction, chronic heart failure, ischemic heart failure, and myocarditis.

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Abstract: It is intended to provide a novel monomer unit by which Z type DNA can be more effectively stabilized, a reagent for integrating this monomer unit into an oligonucleotide, and a method of stabilizing Z type DNA by using the reagent. Namely, a guanosine derivative represented by the following general formula [1]: wherein R1 represents acyl; R2 represents lower alkyl; R3 represents tri-substituted silyloxy or tetrahedropyranyloxy; and R4 represents cyanoethyl or allyl; a reagent for stabilizing Z type DNA which contains the guanosine derivative; and a method of stabilizing Z type DNA by using the guanosine derivative. It is also intended to provide a method of transferring guanosine having lower alkyl at the 8-position into an oligonucleotide by using the guanosine derivative; and an oligonucleotide carrying guanosine having lower alkyl at the 8-position transferred thereinto.

Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are obtained by attaching the phosphonate nucleoside of interest to alkyloxyalkyl-phosphate or alkyl-phosphate in a phosphate-phosphono anhydride linkage to provide a modified nucleoside phosphonate drug.

Abstract: The present invention generally relates to a fludarabine-phosphate with a purity of at least 99.5%.

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

Abstract: The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

Abstract: This invention relates to a medicament for protecting human mucosal cells from chemotherapy or radiotherapy induced cell death using formulations comprising adenosine or adenosine analogues as a reversible inhibitor of epithelial cell proliferation. The invention also relates to formulations containing adenosine for the prevention of or reduction in mucositis symptoms.

Abstract: In one aspect of the invention, a method is provided for end-labeling RNA (total RNA, mRNA, cRNA or fragmented RNA). In one aspect of the present invention, T4 RNA ligase is used to attach a 3?-labeled AMP or CMP donor to an RNA acceptor molecule. In another embodiment, a pyrophosphate molecule 3?-AppN-3?-linker-detectable moiety is used as donor molecule.

Abstract: Compositions and methods for detecting 5-methylcytosine in a nucleic acid are disclosed. A 5-methylcytosine discriminator, which is a deoxyribonucleosidetriphosphate comprising a cytosine-pairing moiety such as a guanosine and a moiety which hinders hydrogen bonding between the cytosine-pairing moiety and a 5-methylcytosine is described. The discriminator is able to base pair with a cytosine but not a 5-methylcytosine. A 5-methylcytosine comprised by a target nucleotide can be detected in a reaction using a DNA polymerase and a primer hybridized immediately adjacent to the target nucleotide. In the reaction, pyrophosphate released upon incorporation of a dNTP complementary to a target nucleotide is detected. Lack of incorporation of the discriminator, but incorporation of a dGTP, can indicate that the target nucleotide is a 5-methylcytosine.

Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Herein described are prodrugs activated by RNA-dependent DNA-polymerases, such as telomerase and retroviral reverse transcriptases, their use for the treatment of haematological tumours and of blood and blood derivatives from patients affected by retroviral infections, and their use for the preparation of pharmaceutical compositions, to be used for the treatment of solid tumours, of precancerous states and of diseases caused by infection with retroviruses.