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8912318 Nucleobase-functionalized conformationally restricted nucleotides and oligonucleotides for targeting nucleic acids  
Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these...
8722877 7-deazapurine modulators of histone methyltransferase, and methods of use thereof  
Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases...
8686130 Artificial fluorescent bases  
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...
8569478 Modified 4′-nucleosides as antiviral agents  
Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described...
8551966 Chemical compounds  
3-(2′,3′-dideoxy-ribo-β-L-furanosyl)[2,3-d]pyrimidin-2(3H)-o ne derivatives comprising 6-substitutents on the base moiety are shown to have anti-viral properties, particularly with respect to...
8394934 Method and process for synthesis of 2',3'-didehydro-2',3'-dideoxynucleosides  
A method is disclosed for synthesizing 2′,3′-didehydro-2′,3′-dideoxynucleosides (d4Ns) from a nucleophile-mediated elimination, such as a telluride-mediated elimination reaction. After...
8153781 Dendrimer conjugates of agonists and antagonists of the GPCR superfamily  
Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for...
8114986 Analogous compounds of 6-thioguanosine triphosphate, their use in medical fields and processes for their preparation  
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...
8039614 4' -C-substituted-2-haloadenosine derivative  
The present invention provides a method for producing a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom,...
7897759 Metabolically stable puromycin analogs  
Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure...
7777023 Method for the chemical synthesis of oligonucleotides  
The present invention features novel compositions, linkers, derivatized solid supports, and methods for the efficient solid phase synthesis of oligonucleotides, including RNA, DNA, RNA-DNA...
7750153 Process for the preparation of didanosine using novel intermediates  
The present invention relates to novel crystalline alkali metal and alkaline earth metal salts of 2′,3′-dideoxy-2′,3′-didehydroinosine. The present invention also provides a novel process for...
7625877 4′-c-substituted-2-haloadenosine derivative  
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...
7563886 Nucleoside releasing functional unit through oxidation and process for producing oligonucleotide containing thereof  
A method of easily releasing a useful substance bonded to oligonucleotide without impairing a target nucleic acid; and a novel base therefore. A nucleoside of nucleotide (oligonucleotide...
7439351 2′ or 3′ -deoxy and 2′, 3′-dideoxy-β-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti-viral agents  
Method for the sterospecific preparation of 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentafuranonucleoside compounds. 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentofuranonucleoside compounds are also...
7192932 Use of immunomodulating agents  
Pharmaceutical compositions useful for treating immunosuppressive disease and containing compounds capable of inhibiting cAMP-dependent protein kinase A (PKA) as well as use of the same, are...
7071173 Antiviral methods employing double esters of 2′, 3′-dideoxy-3′-fluoroguanosine  
A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig
7064112 Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist  
Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment...
6995259 Method for the chemical synthesis of oligonucleotides  
The present invention features novel compositions, linkers, derivatized solid supports, and methods for the efficient solid phase synthesis of oligonucleotides, including RNA, DNA, RNA-DNA...
6974802 Treatment of viral infections using prodrugs of 2′,3-dideoxy,3′-fluoroguanosine  
A method of treating HBV or HIV infections comprising administering to an individual an effective amount of the compound of formula IId′: wherein R2 is the residue of an aliphatic L-amino acid, p...
6962991 Process for the synthesis of pyrazolopyrimidines  
The present invention provides a nucleoside comprising a pyrazolopyrimidine base and a process for producing the same. In particular, the processes of the present invention comprises using a...
6960568 Nucleosides and related processes, pharmaceutical compositions and methods  
The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and...
6949521 Therapeutic azide compounds  
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and...
6924271 3-β-D-ribofuranosylthiazolo[4-5-d]pyridimine nucleosides and uses thereof  
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention...
6919320 Pharmaceutical compositions containing deoxyribonucleosides for wound healing  
The invention relates to compositions comprising 2′-deoxyribonucleosides. The invention also relates to methods of accelerating the healing of wounds, abrasions, cuts, incisions, and superficial...
6897302 Method for synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C)  
The invention provides a method of synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C). The method allows for large-scale production of β-L-FD4C in an efficient,...
6822089 Preparation of deoxynucleosides  
Methods for preparing deoxynucleosides from their corresponding ribonucleosides by forming 3-tert-butylphenoxythiocarbonylderivatives of the ribonucleosides and subsequently effecting radical...
6743910 Stereoselective synthesis of nucleoside analogues  
The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of β and α anomers represented by the following formula A or formula B: wherein...
6596858 Process for the production of 2-halo-6-aminopurine derivatives  
A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific...
6579976 Process for producing 2′,3′-diethyl substituted nucleoside derivatives  
There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing...
6555676 Biologically active phosphotriester-type compounds  
Compounds of formula RS—P(═O)(QR)—Nu where: R is a radical —(CH2)n—W—X; X is a radical —C(═Z)(Y) or —S—U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or saccharide radical...
6500946 Methods for producing nucleoside derivatives and intermediates therefor  
Novel intermediates of nucleoside derivatives, of which the 6-position of the nucleic acid base moiety is substituted with a halogen atom, are produced. Using those novel intermediates, even...
6458772 Prodrugs  
Compounds of the formula I or corresponding monohydroxynucleoside derivatives wherein:R1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon;a C4-C22 saturated or...
6407077 β-L nucleosides for the treatment of HIV infection  
Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering...
6392032 Heavily fluorinated sugar analogs  
Heavily fluorinated sugar analogs of formula whereinR1 is selected from alkyl, alkenyl, aryl, —CH2—O-alkyl, —CH2—O-aryl, —CH2OPO3H, —CH2—O-carbohydrate, —CH2—NH-peptide, or —CH2—O-peptide;wherein...
6271212 Prodrug azide compositions and compounds  
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and...
6252060 Antiviral liponucleosides: treatment of hepatitis B  
Compounds for treating hepatitis B infections. The compounds consist of nucleoside analogues having anti-hepatitis B activity which are linked, commonly through a 5' phosphate of the pentose...
6232300 Treatment of HIV by administration of β-D-2', 3'-didehydro-2',3'-dideoxy-5-fluorocytidine (D4FC)  
A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or...
6207650 Antiviral, highly water soluble, stable, crystalline salts of 2', 3'-dideoxyinosine, 2', 3'-dideoxy-2', 3'-didehydrothymidine and 2', 3'-dideoxy-2'-fluoroinosine  
Provided are very highly water soluble, stable, crystalline salts of 2',3'-dideoxy-2',3'-didehydrothymidine ("d4T"), 2',3'-dideoxyinosine ("ddI"), and 2',3'-dideoxy-2'-fluoroinosine ("F-ddI")....
6194390 Procedure to block the replication of reverse transcriptase dependent viruses by the use of inhibitors of deoxynucleotides synthesis  
A method for inhibiting replication of reverse transcriptase dependent virus in plant or animal cells, comprising the step of administering to said cells a compound that depletes the intracellular...
6156737 Use of dideoxy nucleoside analogues in the treatment of viral infections  
The present invention is directed to a method of treating hepatitis B viral infections in mammals comprising the administration of β-L-5-fluoro-2',3'-dideoxycytidine and pharmaceutically...
6117849 S-(+)-adenosylmethionine and 3'-azido-2', 3'-dideoxy-nucleoside complexes as potent inhibitors of HIV-replication  
Molecular Complexes, comprising of S-(+)-adenosylmethionine and 3'-azido-2',3'-dideoxy nucleosides are prepared, and shown to have synergistic inhibitory effects on the replication of...
6093702 Mixtures of dideoxy-nucleosides and hydroxycarbamide for inhibiting retroviral spread  
A method and composition for inhibiting the spread of a retrovirus such as HIV in a human cell population in which a retrovirus such as HIV is present has been found. The spread of the retrovirus...
6069132 Phosphazole compounds  
A class of substituted and unsubstituted nucleo-base analogs and related azoles, designated as "phosphazoles," is disclosed, certain preferred embodiments having the basic structure of ##STR1##...
6025482 Backbone modified oligonucleotide analogs and preparation thereof through reductive coupling  
Methods for preparing oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. In preferred embodiments, the methods involve reductive coupling of...
6005097 Processes for high-yield diastereoselective synthesis of dideoxynucleosides  
The present invention relates to methods for substantially enhancing the stereoselective synthesis of β-anomeric nucleoside analogs. In methods according to the present invention, the introduction...
5994321 Antiviral guanine analogs  
A series of guanine analogs and physiological salts thereof, which are useful as virus inhibitors and as antiviral agents in the treatment of viral disease, having the basic structures of:...
5990093 Treating HBV with phospholipid prodrugs of β-L-2',3'-dideoxyadenosine 5'-monophosphate  
A method for treating HBV infections comprising administering a 5'-phospholipid prodrug of β-L-2',3'-dideoxyadenosine 5'-monophosphate.
5922890 Organic compounds  
New trityl linkers for use in solid phase synthesis comprise compounds of formula II ##STR1## wherein R4 is alkyl (e.g. C1-4 alkyl), halogen, NO2, or hydrogen; Z is a coupling group chosen from...
5880106 Oral dosing formulations of dideoxy purine nucleosides  
Improved oral dosage formulations for acid-labile dideoxy purine nucleoside derivatives such as ddA, ddI, and ddG, have been developed by incorporating selected water-insoluble buffering systems...

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