Patent classifications
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
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
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
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
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.