C07H19/067

MODIFIED NUCLEOSIDE PHOSPHORAMIDITES

A method of making a compound represented by Formula (I):

##STR00001##

includes a reducing step, a protecting step, and a phosphitylating step, where X is NH; Y is OCF.sub.3, —O(CR.sup.4.sub.2).sub.aCR.sup.4.sub.3, —O(CR.sup.4.sub.2).sub.bOCR.sup.4.sub.3, or —O(CR.sup.4.sub.2).sub.b—CR.sup.4═CR.sup.4.sub.2; Z is H; B is adenine (A), guanine (G), thymine (T), cytosine (C), uracil (U), 5-methylcytosine (5-me-C), or a protected version of A, G, T, C, U, or 5-me-C; each R.sup.1 is independently C.sub.1-6 alkyl or cycloalkyl; R.sup.2 is CH.sub.2CH.sub.2CN or C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 together form an optionally substituted C.sub.1-6 cycloalkyl; R.sup.3 is H or PG; PG is a protecting group; R.sup.4 is independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.

Uridine diphosphate derivatives, prodrugs, compositions and uses thereof
11241450 · 2022-02-08 · ·

This disclosure relates to the use of uridine diphosphate (UDP) derivatives, salts and/or prodrugs thereof for the treatment of inflammatory conditions (e.g., psoriasis) and glaucoma, to prodrugs of UDP derivatives, compositions comprising therapeutically effective amounts of those prodrugs of the UDP derivatives and methods of using those prodrugs for treating various disorders including, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma, and inflammatory conditions, e.g., psoriasis and rheumatoid arthritis.

Uridine diphosphate derivatives, prodrugs, compositions and uses thereof
11241450 · 2022-02-08 · ·

This disclosure relates to the use of uridine diphosphate (UDP) derivatives, salts and/or prodrugs thereof for the treatment of inflammatory conditions (e.g., psoriasis) and glaucoma, to prodrugs of UDP derivatives, compositions comprising therapeutically effective amounts of those prodrugs of the UDP derivatives and methods of using those prodrugs for treating various disorders including, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma, and inflammatory conditions, e.g., psoriasis and rheumatoid arthritis.

Substituted gemcitabine aryl amide analogs
09744186 · 2017-08-29 · ·

In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to substituted gemcitabine aryl amide analogs, methods of making the same, pharmaceutical compositions comprising same, methods of treating viral disorders and disorders of uncontrolled cellular proliferation using same.

LIGAND-2'-MODIFIED NUCLEIC ACIDS, SYNTHESIS THEREOF AND INTERMEDIATE COMPOUNDS THEREOF
20220306679 · 2022-09-29 ·

The present invention relates to methods for synthesizing compounds useful as potent and stable RNA interference agents, derivatives thereof, and intermediates thereto.

LIGAND-2'-MODIFIED NUCLEIC ACIDS, SYNTHESIS THEREOF AND INTERMEDIATE COMPOUNDS THEREOF
20220306679 · 2022-09-29 ·

The present invention relates to methods for synthesizing compounds useful as potent and stable RNA interference agents, derivatives thereof, and intermediates thereto.

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′-end derivatives

The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. ##STR00001##

5′-end derivatives

The present invention provides compounds of formula (1). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene. ##STR00001##