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8168766 |
Process of making 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides and intermediates therefor
A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective...
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8114854 |
Crystalline forms of gemcitabine amide prodrug, compositions and use thereof
The present invention relates to novel crystal forms of an amide prodrug of gemcitabine, compositions thereof and methods for using.
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8058260 |
2′-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions and uses thereof
The present disclosure provides 2′-C-methyl-ribofuranosyl cytidine prodrugs, methods of making 2′-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions of 2′-...
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8026348 |
Nucleoside derivative, modified oligonucleotide, method for their synthesis and applications thereof
Compositions and methods of preparing carboranes and metallacarboranes, which can be used as a new type of electrochemically active label for biological compounds, are disclosed. Nucleic acid...
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7994310 |
Process for preparing 2′-deoxy-2′, 2′-difluorocytidine
Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compo...
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7935681 |
Antiviral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3
-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed...
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7851599 |
Combination of an anti-ED—B fibronectin domain antibody—IL-2 fusion protein and gemcitabine
The invention refers to the use of L19IL2 for treatment of pancreatic cancer. In another embodiment, the invention relates to a combination (i) of a fusion protein, comprising an Interleukin 2 part...
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7825103 |
Pyrimidine nucleoside compound or its salt
Provided is a pyrimidine nucleoside compound represented by the following formula (1): or a pharmaceutically acceptable salt thereof, wherein one of X and Y represents a cyano group, and the other...
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7799907 |
Method for the preparation of 2′-deoxy-2′,2′-difluorocytidine
Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formu...
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7776838 |
Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents. Disclosed are acylated derivatives...
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7772208 |
2′,3′-dideoxynucleoside analogues for the treatment or prevention of Flaviviridae infections
A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an...
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7772207 |
Combination of a CDK inhibitor and CS-682 or a metabolite thereof
A first aspect of the invention relates to a combination comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-β-D-arabino-pentofuranosyl)-N4-palmito
yl cytosine, or a metabolite thereof. A second ...
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7759513 |
Photolabile protective groups for improved processes to prepare oligonucleotide arrays
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...
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7754699 |
Antiviral nucleosides
Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication,...
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7741473 |
Process for the preparation of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles
The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process...
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7691826 |
Polysialic acid derivatives
A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of...
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7666856 |
Antiviral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3
-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed...
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7645745 |
Antiviral nucleosides
Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication,...
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7632940 |
Process for the preparation of 4′-azido cytidine derivatives
The invention relates to a novel process for the preparation of 4′-azido-cytidine (I) or a pharmaceutically accepted salt thereof. The compound of formula I is useful for treating virus mediated d...
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7629447 |
Dideoxynucleoside derivatives
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 represe...
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7601702 |
Dutpase Inhibitors
Deoxyuridine derivatives of Formula (I′); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D...
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7595390 |
Industrially scalable nucleoside synthesis
An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional thir...
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7589078 |
Anti-viral nucleoside analogs and methods for treating viral infections, especially HIV infections
The present invention relates to compounds according to the general formula: wherein B is or and the remaining variables are defined in the specification, and compositions comprising the compounds....
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7589077 |
Antiviral nucleosides
Disclosed are nucleosides which are useful in diagnosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.
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7585851 |
3′-prodrugs of 2′-deoxy-β-L-nucleosides
The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3′-esters of 2...
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7544794 |
Method for sequencing DNA and RNA by synthesis
This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates...
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7485717 |
Synthesis of protected 3′-amino nucleoside monomers
Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unp...
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7456155 |
2′-C-methyl-3′-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
The 3′-L-valine ester of β-D-2′-C-methyl-ribofuranosyl cytidine provides superior results against flaviviruses and pestiviruses, including hepatitis C virus. Based on this discovery, comp...
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7427679 |
Precursors for two-step polynucleotide synthesis
Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl...
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7385050 |
Cleavable linker for polynucleotide synthesis
Functionalized supports for polynucleotide synthesis are disclosed. The supports have linker moieties that are stable to conditions used in polynucleotide synthesis, but may be cleaved to release...
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7378402 |
Anti-viral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-hydroxymeth
yl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also...
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7276228 |
Methods for treating hematological disorders through inhibition of DNA methylation and histone deacetylase
Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute...
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7271258 |
Methods of synthesizing oligonucleotides using carbonate protecting groups and alpha-effect nucleophile deprotection
The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect n...
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7247621 |
Antiviral phosphonate compounds and methods therefor
Pharmaceutical compositions comprise a nucleotide analog with a phosphonate group at a concentration effective to act as a substrate and/or inhibitor of a viral polymerase, and especially of the...
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7235647 |
Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides
The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of ...
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7148207 |
Oral fludara of high-purity formulation with quick release of active ingredient
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.
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7145000 |
Markable compounds for easy synthesis of 3'-[18F] fluoro-3'-deoxynucleotides, and method for their production
What is described are compounds wherein R represents Br, I or R1—SO3, where R1 is an unsubstituted or substituted C1–C5-alkyl group, or an unsubstituted or substituted phenyl group;X is O or NR″...
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7132409 |
Adenosine derivatives and use thereof
2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5′-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent e...
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7105498 |
Acylated uridine and cytidine and uses thereof
The invention relates to compositions comprising acyl derivatives of cytidine and uridine. The invention also relates to methods of treating hepatopathies, diabetes, heart disease, cerebrovascular...
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7105499 |
Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are...
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7078518 |
Forms of 5-Azacytidine
The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula:...
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7038038 |
Synthesis of 5-azacytidine
The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by...
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6992072 |
Combating side-effects
The invention relates to the use of active ingredients, which increase the concentration of pyrimidine-based elements for nucleic acid biosynthesis in the body, in particular to the use of...
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6972330 |
Chemical synthesis of methoxy nucleosides
Process for chemical synthesis of methoxy nucleosides.
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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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6936597 |
Prodrugs of anticancer agents employing substituted aromatic acids
Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties;Y1 is...
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6936709 |
Method for purifying protected 2′-deoxycytidines and hydrated crystals thereof
A protected 2′-deoxycytidine is purified by precipitating the protected 2′-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the pro...
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6933288 |
Pyranosyl cytosines: pharmaceutical formulations and methods
This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using...
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6930097 |
Matrix metalloproteinase and tumor necrosis factor inhibitors
A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryi
midine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of...
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6924272 |
Medicinal composition for diabetic neuropathy
The present invention relates to an agent for the prophylaxis or treatment of diabetic neuropathy, which contains cytidine 5′-diphosphocholine (CDP-choline) as an active ingredient. The agent for t...
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