C07H15/207

Highly potent multimeric e-selectin antagonists

Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are desorbed and pharmaceutical compositions comprising at least one of the same.

Electrocatalytic synthesis of dihydrochalcones

The disclosure relates to methods of forming a dihydrochalcone using electrocatalytic dehydrogenation. In particular, the disclosure relates to methods of forming a dihydrochalcone electrocatalytically hydrogenating (ECH) a reactant compound over a catalytic cathode in a reaction medium having a non-alkaline pH value, thereby forming a dihydrochalcone product; wherein the reactant compound has a structure according to Formula (I). The method can be used to prepare dihydrochalcone sweeteners, such as, for example, naringin dihydrochalcone and neohesperidin dihydrochalcone. ##STR00001##

Electrocatalytic synthesis of dihydrochalcones

The disclosure relates to methods of forming a dihydrochalcone using electrocatalytic dehydrogenation. In particular, the disclosure relates to methods of forming a dihydrochalcone electrocatalytically hydrogenating (ECH) a reactant compound over a catalytic cathode in a reaction medium having a non-alkaline pH value, thereby forming a dihydrochalcone product; wherein the reactant compound has a structure according to Formula (I). The method can be used to prepare dihydrochalcone sweeteners, such as, for example, naringin dihydrochalcone and neohesperidin dihydrochalcone. ##STR00001##

Compounds comprising cleavable linker and uses thereof

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO.sub.2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

Compounds comprising cleavable linker and uses thereof

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO.sub.2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

PROCESS FOR PRODUCTION OF ASCARYLOSE AND RELATED COMPOUNDS
20230279040 · 2023-09-07 · ·

This application relates to efficient methods for the synthesis of ascarylose and its derivatives. A method for the production of ascarylose includes: providing, as a feedstock, a 1-O-substituted rhamnose; forming a mono-sulfonate ester at the 3—OH group of the 1-O-substituted rhamnose; and treating the mono-sulfonate ester with a hydride source to form a 1-O-substituted ascarylose. Forming the mono-sulfonate ester can advantageously be conducted on a 1-O-substituted rhamnose without hydroxyl protecting groups at either the 2—OH or 4—OH—positions.

PROCESS FOR PRODUCTION OF ASCARYLOSE AND RELATED COMPOUNDS
20230279040 · 2023-09-07 · ·

This application relates to efficient methods for the synthesis of ascarylose and its derivatives. A method for the production of ascarylose includes: providing, as a feedstock, a 1-O-substituted rhamnose; forming a mono-sulfonate ester at the 3—OH group of the 1-O-substituted rhamnose; and treating the mono-sulfonate ester with a hydride source to form a 1-O-substituted ascarylose. Forming the mono-sulfonate ester can advantageously be conducted on a 1-O-substituted rhamnose without hydroxyl protecting groups at either the 2—OH or 4—OH—positions.

Coumarin Derivatives of Sugar Analogs and Uses Thereof
20230138729 · 2023-05-04 ·

Provided herein are coumarin derivatives of sugar analogs which are used to measure the rate of hydrolysis of these sugar analogs when contacted with a glycosidase. The reactivity of the coumarin derivatives serves as a convenient method for estimating for the rate of hydrolysis of sugar analogs when used a promoiety with cytotoxic drugs to generate senolytic agents with improved selectivity for killing senescent cells.

Coumarin Derivatives of Sugar Analogs and Uses Thereof
20230138729 · 2023-05-04 ·

Provided herein are coumarin derivatives of sugar analogs which are used to measure the rate of hydrolysis of these sugar analogs when contacted with a glycosidase. The reactivity of the coumarin derivatives serves as a convenient method for estimating for the rate of hydrolysis of sugar analogs when used a promoiety with cytotoxic drugs to generate senolytic agents with improved selectivity for killing senescent cells.

HIGHLY POTENT MULTIMERIC E-SELECTIN ANTAGONISTS

Compounds, compositions, and methods for treatment and/or prevention of at least one disease, disorder, and/or condition by inhibiting binding of an E-selectin to an E-selectin ligand are disclosed. For example, highly potent multimeric E-selectin antagonist are dessorbed and pharmaceutical compositions comprising at least one of the same.