C07H19/24

Photoresponsive nucleotide analog capable of photocrosslinking in visible light region

Provided are a compound represented by formula I that can be used in nucleic acid photoreaction techniques, and a photoreactive crosslinking agent comprising the compound. ##STR00001##

Compounds for fluorescence sensing of duplex formation

Herein reported are new tricyclic cytidine compounds, such as 8-diethylamino-tC (8-DEA-tC), that respond to DNA and/or RNA duplex formation with up to a 20-fold increase in fluorescent quantum yield as compared with the free nucleoside, depending on neighboring bases. This turn-on response to duplex formation is by far the greatest of any reported nucleoside analogue that can participate in Watson-Crick base pairing. Measurements of the quantum yield of 8-DEA-tC mispaired with adenosine and, separately, opposite an abasic site show that there is almost no fluorescence increase without the formation of correct Watson-Crick hydrogen bonds. Kinetic isotope effects from the use of deuterated buffer show that the duplex protects 8-DEA-tC against quenching by excited state proton transfer. DFT calculations provide a rationale for the observed photophysical properties that is dependent on duplex integrity and the electronic structure of the analogue.

Compounds for fluorescence sensing of duplex formation

Herein reported are new tricyclic cytidine compounds, such as 8-diethylamino-tC (8-DEA-tC), that respond to DNA and/or RNA duplex formation with up to a 20-fold increase in fluorescent quantum yield as compared with the free nucleoside, depending on neighboring bases. This turn-on response to duplex formation is by far the greatest of any reported nucleoside analogue that can participate in Watson-Crick base pairing. Measurements of the quantum yield of 8-DEA-tC mispaired with adenosine and, separately, opposite an abasic site show that there is almost no fluorescence increase without the formation of correct Watson-Crick hydrogen bonds. Kinetic isotope effects from the use of deuterated buffer show that the duplex protects 8-DEA-tC against quenching by excited state proton transfer. DFT calculations provide a rationale for the observed photophysical properties that is dependent on duplex integrity and the electronic structure of the analogue.

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS
20220281909 · 2022-09-08 · ·

A D-galactopyranose compound of formula (1)

##STR00001## wherein the pyranose ring is α-D-galactopyranose, and these compounds are high affinity galectin-3 inhibitors. Also, pharmaceutical compositions including these compounds. Further, a method for treatment of a disorder relating to the binding of a galectin-3 to a ligand, such as inflammation, in a mammal, such as a human, wherein a therapeutically effective amount of at least one of these compounds is administered to a mammal in need of the treatment.

NOVEL GALACTOSIDE INHIBITOR OF GALECTINS
20220281909 · 2022-09-08 · ·

A D-galactopyranose compound of formula (1)

##STR00001## wherein the pyranose ring is α-D-galactopyranose, and these compounds are high affinity galectin-3 inhibitors. Also, pharmaceutical compositions including these compounds. Further, a method for treatment of a disorder relating to the binding of a galectin-3 to a ligand, such as inflammation, in a mammal, such as a human, wherein a therapeutically effective amount of at least one of these compounds is administered to a mammal in need of the treatment.

Galactoside inhibitor of galectins

A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

Galactoside inhibitor of galectins

A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

GALECTIN-3 INHIBITING C-GLYCOSIDES

Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.

GALECTIN-3 INHIBITING C-GLYCOSIDES

Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of galectin-3 to ligands are disclosed. For example, inhibitors of galectin-3 are described and pharmaceutical compositions comprising at least one such agent is described.

Small molecule inhibitors of Galectin-3

The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions. ##STR00001##