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8183216 |
Nucleoside derivatives as inhibitors of viral polymerases
A class of nucleoside derivatives of formula (I), as defined herein, that are useful as inhibitors of RNA-dependent RNA viral replication and in particular HCV replication, are provided. Also...
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8173620 |
BHQ-caged nucleotide probes photolysable by two-photon excitation
The disclosure encompasses caged compounds such as caged nucleoside phosphoesters (caged nucleotides). In an embodiment, the caged nucleotides include compounds corresponding to those described by...
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8163707 |
4′-allene-substituted nucleoside derivatives
The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: ...
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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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8101740 |
Positron emission tomography probes for imaging immune activation and selected cancers
Compounds for use as PET probes and methods for synthesizing and using these, comprising [18F]D-FAC and other cytosine and adenosine analogs.
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8093226 |
Cytostatic 7-deazapurine nucleosides
The invention provides compounds of formula I: wherein R1 and R2 have any of the values defined in the specification and salts thereof, as well as compositions comprising such compounds and...
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8034767 |
Method for producing purine nucleosides and nucleotides by fermentation using a bacterium belonging to the genus Escherichia or Bacillus
A method is provided for producing a purine nucleoside, such as inosine and guanosine, and a method for producing a 5′-purine nucleotide such as 5′-inosinic acid or 5′-guanylic acid, using a bacte...
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8034924 |
Process for production of crystal of purine nucleoside compound
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 ...
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8030478 |
Method for nucleic acid replication and novel artificial base pairs
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...
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7999098 |
Triphosphate oligonucleotide modification reagents and uses thereof
Hydrazino, oxyamino and carbonyl-based monomers and methods for incorporation into oligonucleotides during enzymatic synthesis are provided. Modified oligonucleotides are provided that incorporate...
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7989430 |
Antibacterial agents
The invention provides compounds of formula (I) and salts thereof: R1-L-R2—B wherein R1, L, R2, and B have any of the values defined herein, as well as compositions comprising such compounds, and t...
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7989422 |
Antibacterial agents
The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as...
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7960526 |
Colorimetric-oxycarbonyl protecting groups for use in organic syntheses
The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in...
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7947824 |
Process for preparing purine nucleosides
The present invention for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-α-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.
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7935674 |
Indole derivatives
Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is halogen, or alkyl, R2 is hydrogen, or halogen, Ar is phenyl, or thienyl, which may be...
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7928210 |
Nucleoside based proliferation imaging markers
Disclosed herein are novel radiolabeled nucleosides and methods for detecting cellular proliferation in a mammal, the method comprising administrating an effective amount of a radiolabeled...
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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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7863438 |
Stable salt of 3′-phosphoadenosine 5′-phosphosulfate
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 sal...
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7824851 |
2′-branched nucleosides and Flaviviridae mutation
The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2′-branched nucleoside, or a pharmaceutically acceptable prodrug and/or s...
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7816513 |
Inosine derivatives and production methods therefor
The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general...
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7781576 |
Process for preparing a synthetic intermediate for preparation of branched nucleosides
A process is provided for the preparation of a key intermediate in the preparation of 2′-branched nucleoside compounds. The process includes contacting a protected precursor 3...
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7745591 |
Phosphinoamidite carboxylates and analogs thereof in the synthesis of oligonucleotides having reduced internucleotide charge
Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy,...
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7723512 |
Oligonucleotides comprising a non-phosphate backbone linkage
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 p...
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7713941 |
Tricyclic nucleosides or nucleotides as therapeutic agents
Nucelosides and nucleotides containing a tricyclic base portion thereof are useful for treating infectious diseases and proliferative disorders, such as viral infections or cancer respectively.
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7709448 |
Prodrugs of 5-amino-3-(3′-deoxy-β-D-ribofuranosyl)-thiazolo[4,5-d]pyrimidin-2,7-dione
The invention is directed to 5-amino-3-(3′-deoxy-β-D-ribofuranosyl)-thiazolo[4,5-d]pyr
imidin-2,7-dione prodrugs, whose metabolized parent compound has immunomodulatory activity. The invention al...
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7632821 |
Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection
The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are...
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7615628 |
Imidazopyridine derivatives
The present invention relates to a novel imidazo[4,5-b]pyridine derivative compound represented by Formula (I) and a pharmaceutically acceptable salt thereof. The present invention also relates to...
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7615619 |
Nucleoside analogues and oligonucleotide derivative comprising nucleotide analogue thereof
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...
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7598361 |
Nucleic acid molecules and other molecules associated with the sucrose pathway
The present invention is in the field of plant biochemistry. More specifically the invention relates to nucleic acid sequences from plant cells, in particular, nucleic acid sequences from maize and...
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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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7563887 |
Universal nucleobase analogs
This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that can bind to nucleic acids, including compositions and processes that...
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7547776 |
Process for the production of fludarabine-phosphate lithium, sodium, potassium, calcium and magnesium salts and purification process for the production of fludarabine-phosphate and fludarabine-phosphate with a purity of at least 99.5%
The present invention generally relates to a fludarabine-phosphate with a purity of at least 99.5%.
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7534771 |
Tricyclic-nucleoside prodrugs for treating viral infections
Disclosed are compounds, compositions and methods for treating viral infections caused by a Flaviviridae family virus, such as hepatitis C virus.
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7528247 |
Process for preparing purine nucleosides
The present invention for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-α-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.
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7528115 |
Carbonate and carbamate prodrugs of thiazolo[4,5-d]pyrimidines
The invention is directed to carbonate and carbamate prodrugs of thiazolo[4,5-d]pyrimidine compounds, whose metabolized parent compound has immunomodulatory activity. The invention also relates to...
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7524825 |
Tricyclic-nucleoside compounds for treating viral infections
Disclosed are compounds represented by formulae I, II, and III, and the compositions and methods thereof for treating viral infections caused by a Flaviviridae family virus.
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7511133 |
Adenosine A3 receptor agonists
The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5′ p...
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7495095 |
Thionucleoside-S-nitrosyl derivative
The present invention provides a thionucleoside-S-nitrosyl derivative of the following Formula I or a salt thereof: [wherein R1 represents ribose, 2-deoxyribose or a derivative of either, and R2...
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7470784 |
Methods for synthesizing 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-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; ...
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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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7432272 |
Antiviral analogs
The application relates to 4′-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such c...
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7405204 |
Nucleoside compounds for treating viral infections
Disclosed are compounds, compositions and methods for treating viral infections caused by a Flaviviridae family virus, such as hepatitis C virus.
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7399754 |
N2-quinoline or isoquinoline substituted purine derivatives
Novel compound having the following formula: wherein W represents a hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-6 cycloalkyl, or an optionally substituted C1-6...
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7393954 |
Process for the production of pentostatin aglycone and pentostatin
A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available...
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7371737 |
2-substituted-6-trifluoromethyl purine derivatives with adenosine-A3 antagonistic activity
The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the...
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7321033 |
3-B-D-ribofuranosylthiazolo [4,5-d] pyrimidine 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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7294486 |
Enzymatic process for the synthesis of organo-fluorine compounds
There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be...
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7282581 |
Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid...
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7268119 |
Tricyclic nucleosides or nucleotides as therapeutic agents
Nucleosides and nucleotides containing a tricyclic base portion thereof are useful for treating infectious diseases and proliferative disorders, such as viral infections or cancer respectively.
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