C07H19/11

Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides
09828409 · 2017-11-28 ·

Provided herein are bridged cyclic phosphates and phosphoramidates (bc-ProTides) of nucleosides, which is a compound, its stereoisomers, isotope-enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, with the following structure: ##STR00001##
These compounds can be used for the treatment of viral infections and/or neoplastic diseases in mammals. By optimizing combinations of Y.sub.2, Y.sub.3, R.sup.0, and M, the cleavability of these compounds as prodrugs can be attuned for different tissue targeting with various functional combinations. Also disclosed are processes and methods for preparation of these compounds.

Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides
09828409 · 2017-11-28 ·

Provided herein are bridged cyclic phosphates and phosphoramidates (bc-ProTides) of nucleosides, which is a compound, its stereoisomers, isotope-enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, with the following structure: ##STR00001##
These compounds can be used for the treatment of viral infections and/or neoplastic diseases in mammals. By optimizing combinations of Y.sub.2, Y.sub.3, R.sup.0, and M, the cleavability of these compounds as prodrugs can be attuned for different tissue targeting with various functional combinations. Also disclosed are processes and methods for preparation of these compounds.

Herbicidal composition comprising flazasulfuron and an inhibitor of protoporphyrinogen oxidase

Many herbicidal compositions have been developed and are presently used. However, weeds to be controlled are various in types and their emergence extends over a long period. Accordingly, it is desired to develop a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect. The present invention provides a herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one protoporphyrinogen oxidase inhibitor selected from the group consisting of a phenylpyrazole compound, a triazolinone compound, a N-phenylphthalimide compound, a pyrimidindione compound, an oxadiazole compound, an oxazolidinedione compound, a thiadiazole compound, pyraclonil, profluazol, flufenpyr-ethyl and their salts. According to the present invention, a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect can be provided.

Herbicidal composition comprising flazasulfuron and an inhibitor of protoporphyrinogen oxidase

Many herbicidal compositions have been developed and are presently used. However, weeds to be controlled are various in types and their emergence extends over a long period. Accordingly, it is desired to develop a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect. The present invention provides a herbicidal composition comprising (A) flazasulfuron or its salt and (B) at least one protoporphyrinogen oxidase inhibitor selected from the group consisting of a phenylpyrazole compound, a triazolinone compound, a N-phenylphthalimide compound, a pyrimidindione compound, an oxadiazole compound, an oxazolidinedione compound, a thiadiazole compound, pyraclonil, profluazol, flufenpyr-ethyl and their salts. According to the present invention, a herbicidal composition which has a broad herbicidal spectrum, a high activity and a long-lasting effect can be provided.

NUCLEOSIDE ANALOGS FOR TREATMENT OF THE FLAVIVIRIDAE FAMILY OF VIRUSES AND CANCER

The present invention is directed to compounds, compositions and methods for treating or preventing Flaviviridae family of viruses (including HCV, Yellow fever, Dengue, Chikungunya and West Nile virus), RSV, HEV, and influenza infection and cancer in human subjects or other animal hosts.

2′-alkynyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. ##STR00001##

2′-alkynyl substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. ##STR00001##

5-fluorouracil compounds
11427550 · 2022-08-30 · ·

The compounds are of the class of 5-fluorouracil derived acetal and hemiaminal ether compounds, useful in treating liver diseases and various types of cancer. The following formulas are representative of the class of compounds provided herein: ##STR00001##

Substituted nucleosides, nucleotides and analogs thereof

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, of the Formula (I). ##STR00001## Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.

Substituted nucleosides, nucleotides and analogs thereof

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, of the Formula (I). ##STR00001## Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.