Abstract: Provided herein are processes for the preparation of 5-azacytidine, useful for treating, preventing, and/or managing diseases or conditions including cancer, disorders related to abnormal cell proliferation, hematologic disorders, and myelodysplastic syndromes (MDS), wherein 5-azacytidine is represented by the structure:

Abstract: Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.

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: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

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 application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.

Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs, for example, 5-azacytidine or decitabine, for oral administration, wherein the compositions release the cytidine analog, for example, 5-azacytidine or decitabine, substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.

Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Abstract: Provided herein are pharmaceutical compositions or dosage forms comprising crystalline 5-azacytidine monohydrate. The pharmaceutical compositions or dosage forms provided herein may be used for oral administration in the treatment of diseases, including the treatment of myelodysplastic syndromes (MDS).

Abstract: Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form I and mixtures of azacitidine crystalline Forms I and II.

Abstract: A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnCl4 comprising the removal of SnCl4 by adding DMSO directly into the reaction mixture is described. Preferably said process is used for the preparation of antiviral and antitumor agents having a nucleoside or nucleoside-like structure, still more preferably for the preparation of azacytidine, decitabine, chlorfarabine, cladribine, mizoribine. A residual tin content lower than 300 ppm is obtained with said process.

Abstract: Provided herein are processes for the preparation of 5-azacytidine, useful for treating, preventing, and/or managing diseases or conditions including cancer, disorders related to abnormal cell proliferation, hematologic disorders, and myelodysplastic syndromes (MDS), wherein 5-azacytidine is represented by the structure:

Abstract: Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form I and mixtures of azacitidine crystalline Forms I and II.

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacyditine, 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: A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.

Abstract: A method of preparing purified decitabine comprises mixing crude decitabine with solvent, such as dimethylacetamide, to form a solution or suspension and forming the purified decitabine from the solution or suspension. The forming step comprises adding an anti-solvent, such as ethanol, to the solution or suspension. The forming step may further comprise after adding ethanol to provide a mixture of dimethylacetamide and ethanol: cooling the mixture; isolating the solid decitabine present in the cooled mixture; and evaporating residual dimethylacetamide and ethanol from the solid decitabine to provide the purified decitabine. The mixture of dimethylacetamide and ethanol may be heated. The purification method preferably results in decitabine having a ratio of the ?-anomer of decitabine to the ?-anomer of decitabine of at least about 99.9:0.1.

Abstract: Fluorinated pyrimidine analog compounds, compositions that include the fluorinated pyrimidine analog compounds, methods for making the fluorinated pyrimidine analog compounds, and methods for inhibiting DNA methyltransferase, treating solid tumors, and treating hematologic cancers by administering the fluorinated pyrimidine analog compounds.

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 includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

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 includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

Abstract: The present invention relates to 2?-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.

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 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 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 includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.

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 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 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

Abstract: The present application relates to processes for the preparation and purification of decitabine structurally represented by formula (I): and to processes for the preparation of a crystalline form of decitabine.

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 disclosure provides methods for treating subjects having non-small cell lung cancer, wherein the methods comprise administering to the subject a cytidine analog, such as 5-azacytidine. Also provided are methods relating to identification and treatment of particular non-small cell lung cancer types sensitive to particular cytidine analogs.

Abstract: Disclosed herein are methods of obtaining highly pure 5-azacytidine, which contains minimal amounts of degradation impurities and methods of assessing the impurity profile of the degradation of cytidine analogues, such as 5-azacytidine

Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.

Abstract: Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.

Abstract: Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form (I) and mixtures of azacitidine crystalline Forms (I) and (II).

Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of plasminogen or a protein that is a plasminogen analogue, an affinity adsorbent is used that is a compound of formula (II) wherein one X is N and the other is N, C—Cl or C—CN; A is a support matrix, optionally linked to the triazine ring by a spacer; Z is O, S or N—R and R is H, C1-6 alkyl, C1-6 hydroxyalkyl, benzyl or &bgr;-phenylethyl; B is an optionally substituted hydrocarbon linkage containing from 1 to 10 carbon atoms; D is H, OH or a primary amino, secondary amino, tertiary amino, quaternary ammonium, imidazole, guanidino or amidino group; or B-D is —CHCOOH—(CH2)3-4—NH2; and q is 2 to 6.

Abstract: Methods, uses, compositions and kits relating to the inhibition and/or prevention of undesirable cell proliferation, and prevention and/or treatment of diseases or disorders associated with such proliferation, such as cancer, using a cytosine nucleoside analog such as 5-aza-2?-deoxycytidine and an isoflavone such as genistein, are described.

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 includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.

Abstract: A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective flavivirus, pestivirus or hepacivirus treatment amount of a described base-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: New processes for producing decitabine are provided.

Abstract: Method of producing 2?-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I): wherein R is a removable substituent known per se; and R1 is a removable substituent; further providing a silylated base of formula (II): wherein R2 is a protecting group, preferably a trimethylsilyl TMS)-residue; reacting the compound of formula (I) and the compound of formula (II) together in a suitable anhydrous solvent and in the presence of a suitable catalyst; and removing the substituents R from the compound obtained in order to obtain the compound 2?-deoxy-5-azacytidine (Decitabine), characterized in that said catalyst is selected from the group comprising a salt of an aliphatic sulphonic acid or a salt of a strong inorganic acid.

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

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 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: A method for producing a ?-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula I; and b) quenching the reaction mixture of step a) with a base. The ?-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.

Abstract: The present invention relates to salts of 5-azacytidine as well as methods for synthesizing the salts described herein. Pharmaceutical compositions and methods of using the 5-azacytidine salts are also provided, including methods of administering the salts or pharmaceutical compositions thereof to treat conditions, such as cancer and hematological disorders.