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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...
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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 either...
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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, R...
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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...
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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...
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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 pre...
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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 e...
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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 containing...
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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 als...
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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...
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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
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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 of...
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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...
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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 i...
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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...
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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...
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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...
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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 ...
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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 b...
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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, cost-effec...
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6822089 |
Preparation of deoxynucleosides
Methods for preparing deoxynucleosides from their corresponding ribonucleosides by forming 3-tert-butylphenoxythiocarbonylderivatives of the ribonucleosides and subsequently effecting radical...
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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 R...
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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...
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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...
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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 ...
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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...
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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...
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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 an...
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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;wh...
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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...
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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...
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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...
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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"). Such...
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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...
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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 ...
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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...
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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...
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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##...
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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...
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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 ...
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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: ##STR1##...
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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.
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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...
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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 in...
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5830881 |
L-2'3',dideoxy nucleoside analogs as anti-hepatitus B (HBV) agents
The present invention relates to the surprising discovery that certain dideoxynucleoside analogs which contain a dideoxy ribofuranosyl moiety having an L-configuration (as opposed to the naturally...
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5831075 |
Amino acid ester of nucleoside analogues
A process for the preparation of an amino acid ester of a nucleoside analogue comprises reacting a nucleoside analogue having an esterifiable hydroxy group with a 2-oxa-4-aza-cycloalkane-1,3-dione....
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5783679 |
Purine nucleoside modifications by palladium catalyzed methods and oligonucleotides containing same
This invention discloses an improved method for the preparation modified purine nucleosides at the 2-, 6- or 8-position of the purine ring, using a palladium catalyst.
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5783688 |
Purification of 3'-FDDU and resultant compositions
2',3'-Dideoxy-3'-fluorouridine is purified by treating an aqueous or aqueous methanolic solution with charcoal.
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5770716 |
Substituted propargylethoxyamido nucleosides, oligonucleotides and methods for using same
Substituted propargylethoxyamido nucleosides are disclosed having the structure ##STR1## wherein X is selected from the group consisting of amino alkanoic acid, alkylamino benzoic acid, α-amino ...
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5736526 |
Mixtures of DDI and D4T with hydroxycarbamide for inhibiting retroviral replication
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...
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