C07H15/26

O-GLCNACYLATED PROTEIN-LIKE SUBSTANCE AND FIBROSIS THERAPEUTIC DRUG CONTAINING SAME
20220389047 · 2022-12-08 ·

An O-GlcNAcylated protein-like substance having an N-acetylglucosamine unit, and at least one unit selected from the group consisting of a carboxy group-containing radically polymerizable unit, a styrene unit, a polyethylenimine unit, a poly-L-lysine unit, and a biotin unit; and a fibrosis therapeutic drug containing the O-GlcNAcylated protein-like substance.

O-GLCNACYLATED PROTEIN-LIKE SUBSTANCE AND FIBROSIS THERAPEUTIC DRUG CONTAINING SAME
20220389047 · 2022-12-08 ·

An O-GlcNAcylated protein-like substance having an N-acetylglucosamine unit, and at least one unit selected from the group consisting of a carboxy group-containing radically polymerizable unit, a styrene unit, a polyethylenimine unit, a poly-L-lysine unit, and a biotin unit; and a fibrosis therapeutic drug containing the O-GlcNAcylated protein-like substance.

CARBOHYDRATE CONJUGATE RNA AGENTS AND PROCESS FOR THEIR PREPARATION

This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.

CARBOHYDRATE CONJUGATE RNA AGENTS AND PROCESS FOR THEIR PREPARATION

This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.

NEUROKININ-1 ANTAGONIST
20220380393 · 2022-12-01 ·

A compound represented by formula II or a pharmaceutically acceptable salt thereof, and a preparation method therefor. The compound represented by formula II is an antagonist of a neurokinin-1 receptor, can be used for treating diseases related to the neurokinin-1 receptor, and can avoid hemolytic effects of drugs and reduce the side effects of drug administration.

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TOLL-LIKE RECEPTOR LIGANDS

Toll-like receptor (TLR) ligands having an allose-based core are stable in aqueous formulation and are useful in treating, preventing, or reducing susceptibility to diseases or conditions mediated by TLRs, such as cancer, infectious disease, allergy, autoimmune disease, sepsis, and ischemia reperfusion.

TOLL-LIKE RECEPTOR LIGANDS

Toll-like receptor (TLR) ligands having an allose-based core are stable in aqueous formulation and are useful in treating, preventing, or reducing susceptibility to diseases or conditions mediated by TLRs, such as cancer, infectious disease, allergy, autoimmune disease, sepsis, and ischemia reperfusion.

Lactuloside compounds and preparation and use thereof

The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and “custom character” indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an α-glycosidic bond or a β-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. ##STR00001##

E-SELECTIN ANTAGONIST COMPOUNDS, COMPOSITIONS, AND METHODS OF USE

Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.

E-SELECTIN ANTAGONIST COMPOUNDS, COMPOSITIONS, AND METHODS OF USE

Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.