Abstract: A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.

Abstract: The present invention provides compounds and methods for treatment of viral diseases and cancer.

Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for oral administration, wherein the compositions release the cytidine analog substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.

Abstract: The present invention is directed toward compounds of Formula (I) as follows: wherein, R is H, R5C(O), R5CH2OC(O), or R5CH2NHC(O); R1 is where the crossing dashed line illustrates the bond formed joining R1 to the molecule of Formula (I); R2 and R3 are independently OH or H, provided that R2 and R3 are not simultaneously OH; R4 is H, R5C(O), R5CH2OC(O), or R5CH2NHC(O), provided that R and R4 are not simultaneously H; and R5 has the general formula: CH3—(CH2)n—(CH?CH—CH2)m—CH?CH—(CH2)k—; k is an integer from 0 to 7; m is an integer from 0 to 2; and n is an integer from 0 to 10, or a pharmaceutical salt thereof. Methods of making and using these compounds are also disclosed.

Abstract: The present invention is directed toward compounds of Formula (I) as follows: wherein, R is H, R5C(O); R1 is where the crossing dashed line illustrates the bond formed joining R1 to the molecule of Formula (I); R2 and R3 are independently OH or H, provided that R2 and R3 are not simultaneously OH; R4 is H or R5C(O), provided that R and R4 are not simultaneously H; and R5 is a C3-C26 alkenyl, or a pharmaceutical salt thereof. Methods of making and using these compounds are also disclosed.

Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

Abstract: The present application describes deuterium-enriched decitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: 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 the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

Abstract: The present invention provides novel crystalline forms of 5-deazacytidine, and pharmaceutical compositions comprising these novel forms. The invention also provides methods for the preparation of the novel forms and compositions.

Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: The present invention provides visible light sensitive and ultraviolet (UV) light sensitive composition for DNA transfer comprising acid sensitive polyacetals developed as DNA/RNA delivery agents, a photoacid generator and optionally a photosensitizer.

Abstract: The present invention provides a method for preparation of 2?-deoxy-2?,2?-difluoro-?-cytidine or pharmaceutically acceptable salt thereof, comprising starting from 1,6-anhydro-?-D-glucose as raw material, oxidizing, and fluorinating to obtain 2-deoxy-2,2-difluoro-D-ribofuranose as intermediate. The 2?-deoxy-2?,2?-difluoro-?-cytidine was finally prepared from the intermediate of 2-deoxy-2,2-difluoro-D-ribofuranose. The method is simple in operation and has a high yield. The method can effectively be used in large-scale production.

Abstract: 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: The disclosure also includes pharmaceutical compositions comprising said forms.

Abstract: 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 the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.

Abstract: The invention provides compounds of the Formula 1 wherein the definitions of m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are in the specification. These compounds are useful as antibacterial agents.

Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: 1

Abstract: The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: 1

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: 1

Abstract: The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds and methods for treatment of viral diseases and cancer.

Abstract: Disclosed are oligonucleotides and oligonucleosides that include one or more modified nucleoside units. The oligonucleotides and oligonucleosides are particularly useful as antisense agents, ribozymes, aptamer, siRNA agents, probes and primers or, when hybridized to an RNA, as a substrate for RNA cleaving enzymes including RNase H and dsRNase.

Abstract: Propargylethoxyamino nucleosides are disclosed having the structure wherein R1 and R2 are —H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W1 is —H or —OH; W2 is —OH or a moiety which renders the nucleoside incapable of forming a phosphodiester bond at the 3′-position; and W3 is —PO4, —P2O7, —P3O10, phosphate analog, or —OH. Additionally, a primer extension method is provided employing the above propargylethoxyamino nucleosides.

Abstract: Nucleic acid ligands containing modified nucleotides are described as are methods for producing such oligonucleotides. Such ligands enrich the chemical diversity of the candidate mixture for the SELEX process. Specific examples are provided of nucleic acids containing nucleotides modified at the 2′- and 5-position. Specific 2-OH and 2′-NH2 modified RNA ligands to thrombin are described.