C07H15/14

MANNOSE 6-PHOSPHATE OR ASGPR RECEPTOR BINDING COMPOUNDS FOR THE DEGRADATION OF EXTRACELLULAR PROTEINS

Compounds and compositions that have a mannose 6-phosphate receptor or ASGPR binding ligand bound to an extracellular protein binding ligand are provided for the selective degradation of a target extracellular protein in vivo to treat disorders mediated by the extracellular protein.

RM2 antigens and use thereof

Described herein are synthetic glycan conjugates, immunogenic compositions thereof, vaccines thereof, and kits thereof. The present invention further provides methods of using the synthetic glycan conjugates, immunogenic compositions, or vaccines thereof to treat and/or prevent and/or diagnose proliferative diseases such as cancer. The provided glycan conjugate comprises a carrier and a glycan moiety of Formula (I-i) or Formula (I-ii): (structurally represented). ##STR00001##

RM2 antigens and use thereof

Described herein are synthetic glycan conjugates, immunogenic compositions thereof, vaccines thereof, and kits thereof. The present invention further provides methods of using the synthetic glycan conjugates, immunogenic compositions, or vaccines thereof to treat and/or prevent and/or diagnose proliferative diseases such as cancer. The provided glycan conjugate comprises a carrier and a glycan moiety of Formula (I-i) or Formula (I-ii): (structurally represented). ##STR00001##

LINCOMYCIN BIOSYNTHETIC INTERMEDIATES, METHOD FOR PREPARATION, AND USE THEREOF
20180251486 · 2018-09-06 ·

Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.

LINCOMYCIN BIOSYNTHETIC INTERMEDIATES, METHOD FOR PREPARATION, AND USE THEREOF
20180251486 · 2018-09-06 ·

Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.

INHIBITORS OF SODIUM GLUCOSE COTRANSPORTER 1

Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula:

##STR00001##

the various substituents of which are defined herein.

INHIBITORS OF SODIUM GLUCOSE COTRANSPORTER 1

Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula:

##STR00001##

the various substituents of which are defined herein.

Process for synthesizing highly optically active 1,3-disubstituted allenes
09873713 · 2018-01-23 · ·

The present invention relates to a process for efficiently synthesizing highly optically active 1,3-disubstituted allenes, i.e., a one-step process for preparing highly optically active 1,3-disubstituted allenes by using a functionalized terminal alkyne, an aldehyde and a chiral ,-diphenyl prolinol as reactants under the catalysis of a divalent copper salt. The operation of the process is simple, and the raw materials and reagents are readily available. The process has a broad-spectrum of substrates and a good compatibility for a wide variety of functional groups such as glycosidic units, primary alcohols, secondary alcohols, tertiary alcohols, amides, malonates, etc., and does not require the protection for the functional groups. The obtained axially chiral allene has a moderate to high yield and a good diastereoselectivity or enantioselectivity.

Process for synthesizing highly optically active 1,3-disubstituted allenes
09873713 · 2018-01-23 · ·

The present invention relates to a process for efficiently synthesizing highly optically active 1,3-disubstituted allenes, i.e., a one-step process for preparing highly optically active 1,3-disubstituted allenes by using a functionalized terminal alkyne, an aldehyde and a chiral ,-diphenyl prolinol as reactants under the catalysis of a divalent copper salt. The operation of the process is simple, and the raw materials and reagents are readily available. The process has a broad-spectrum of substrates and a good compatibility for a wide variety of functional groups such as glycosidic units, primary alcohols, secondary alcohols, tertiary alcohols, amides, malonates, etc., and does not require the protection for the functional groups. The obtained axially chiral allene has a moderate to high yield and a good diastereoselectivity or enantioselectivity.

Reagent-controlled stereoselective glycosylation

Provided are methods for the efficient stereoselective formation of glycosidic bonds, without recourse to prosthetic or directing groups.