C07H19/09

SYNTHESIS OF [18F]-LABELED THYMIDINE ANALOGUES
20230416293 · 2023-12-28 · ·

Thymidine analogues, 5-substituted 2-deoxy-2-[.sup.18F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasively imaging cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2-deoxy-2-[.sup.18F]fluoro-5-methyl-1--d-arabinofuranosyluracil ([.sup.18F]FMAU) and other 2-deoxy-2-[.sup.18F]fluoro-5-substituted-1--d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiosynthetic yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for .sup.18F-labeling of other nucleoside analogues.

SYNTHESIS OF [18F]-LABELED THYMIDINE ANALOGUES
20230416293 · 2023-12-28 · ·

Thymidine analogues, 5-substituted 2-deoxy-2-[.sup.18F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasively imaging cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2-deoxy-2-[.sup.18F]fluoro-5-methyl-1--d-arabinofuranosyluracil ([.sup.18F]FMAU) and other 2-deoxy-2-[.sup.18F]fluoro-5-substituted-1--d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiosynthetic yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for .sup.18F-labeling of other nucleoside analogues.

[18F] FMAU LABELING FOR PET IMAGING OF CANCER PATIENTS
20210009624 · 2021-01-14 ·

Provided herein are methods and labeling kits for synthesizing 2-deoxy-2-[.sup.18F]fluoro-5-methyl-1-beta-D-arabino-furanosyl-uracil in a one-pot reaction in compliance with CGMP. Also disclosed are labeling kits that can be assembled in an automated synthesis system to enable such a reaction.

PHOSPHORAMIDATES FOR THE TREATMENT OF HEPATITIS B VIRUS
20200299320 · 2020-09-24 ·

Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine.

PHOSPHORAMIDATES FOR THE TREATMENT OF HEPATITIS B VIRUS
20200299320 · 2020-09-24 ·

Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine.

Phosphoramidates for the treatment of hepatitis B virus
10683319 · 2020-06-16 · ·

Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine.

Phosphoramidates for the treatment of hepatitis B virus
10683319 · 2020-06-16 · ·

Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine.

COMBINATION CANCER THERAPY

The present invention relates to combination therapies of a cytarabine conjugate and one or more anti-neoplastic agents for inhibiting cancer cell growth. In particular, the present invention relates to a conjugate of cytarabine and aspartic acid (BST-236) in combination with one or more additional anti-neoplastic agents for use in the treatment of hematological cancers.

THERAPEUTIC OLIGONUCLEOTIDES
20240140978 · 2024-05-02 ·

Methods and compositions are provided for oligonucleotides that bind targets of interest. The targets include cells and microvesicles, such as those derived from various diseases. The oligonucleotides can be used for diagnostic and therapeutic purposes. The target of the oligonucleotides can be a target such as PARP1, HIST1H1B, HIST1H1D, NCL, FBL, SFPQ, RPL12, ACTB, HIST1H4A, SSBP1, NONO, H2AFJ, and DDX21, or a complex, subunit or fragment thereof.

THERAPEUTIC OLIGONUCLEOTIDES
20240140978 · 2024-05-02 ·

Methods and compositions are provided for oligonucleotides that bind targets of interest. The targets include cells and microvesicles, such as those derived from various diseases. The oligonucleotides can be used for diagnostic and therapeutic purposes. The target of the oligonucleotides can be a target such as PARP1, HIST1H1B, HIST1H1D, NCL, FBL, SFPQ, RPL12, ACTB, HIST1H4A, SSBP1, NONO, H2AFJ, and DDX21, or a complex, subunit or fragment thereof.