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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...
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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 R 1 represents a nucleic acid base which may have a protecting...
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7601702 |
Dutpase Inhibitors
Deoxyuridine derivatives of Formula (I′); where A is O, S or CH 2 ; B is O, S or CHR 3 ; R 1 is H, or various substituents; R 2 is H, F; R 3 is H, F, OH, NH 2 ; or R 2 and R 3 together form...
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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...
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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...
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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...
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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...
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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,...
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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:R 1 =R 2 =R 3 =R 4 =H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors....
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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...
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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 2 1 -deoxy-2 1 ,2 1 -D-ribofuranosyl difluoronucleosides...
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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 R 1 —SO 3 , where R 1 is an unsubstituted or substituted C 1 –C 5 -alkyl group, or an unsubstituted or substituted phenyl...
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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...
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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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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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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,...
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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...
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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...
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6936596 |
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...
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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...
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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...
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6908906 |
Crystalline forms of pyrimidine nucleoside derivative
The present invention provides crystalline forms and compositions thereof, of a pyrimidine nucleoside derivative of formula (I) having anti-tumour activity, wherein formula (I) is:
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6905669 |
Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA...
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6894159 |
Process for the preparation of 2′-fluoro-5-methyl-beta-L-arabino-furanosyluridine
The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-β-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially...
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6891033 |
Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof
The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[ 18 F]fluoro-3′-deoxythymidine and that have formula (1),
in which
R denotes...
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6884880 |
Process for the preparation of 9-β-anomeric nucleoside analogs
A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base...
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6875751 |
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...
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6864244 |
Anhydrous crystalline 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine hemisulfate as useful as an antiviral agent
The present invention relates to the hemisulfate salt of 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyc
lopentyl]cytosine (Ia) with improved stability and physical properties which...
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6846810 |
Antiviral nucleoside derivatives
The present invention relates to nucleoside derivatives for the treatment of Hepatitis C viral infections including compounds of formula I, pharmaceutical compositions comprising these compounds...
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6822090 |
Process for the preparation of cytidine derivatives
An efficient method for producing cytidine derivatives that took away the previous drawbacks by efficiently synthesizing cytidine derivatives by utilizing a tertiary amine can be provided.
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6777387 |
Terminally-branched polymeric linkers containing extension moieties and polymeric conjugates containing the same
The present invention is directed to polymeric prodrug transport forms and methods of making and using the same. In one preferred aspect, the prodrugs are of the formula: wherein G is a...
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6727231 |
Uridine therapy for patients with elevated purine levels
The invention is based on the discovery that patients having elevated purine levels, e.g., individuals diagnosed with pervasive developmental disorders, such as autistic disorder, and/or...
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6720306 |
Tetrapartate prodrugs
A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L 1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be...
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RE38416 |
Cross-linking oligonucleotides
This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a...
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6673544 |
Method for the light-controlled synthesis of biochips
The present invention relates to a method for the photolithographic synthesis of biochips in which photolabile protective groups of the 2-(2-nitrophenyl)ethyl type are used, whereby the irradiation...
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6646118 |
Solid phase synthesis
The present invention relates to a support system for solid phase synthesis of oligomers, such as oligonucleotides, wherein the starting compound is bound to the support via a disiloxyl linkage....
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