C07H15/18

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##

Selective glycosidase inhibitors and uses thereof

The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##

Compositions and methods for functional gylcomics

The disclosure relates to labeling glycans and glycosphingolipids from undefined mixtures with chemical moieties that emit light when exposed to electromagnetic radiation and uses of these labeled glycans and glycosphingolipids in microarrays for research and diagnostic purposes. In certain embodiments, the disclosure relates to derivatizing glycosphingolipids with a marker.

Compositions and methods for functional gylcomics

The disclosure relates to labeling glycans and glycosphingolipids from undefined mixtures with chemical moieties that emit light when exposed to electromagnetic radiation and uses of these labeled glycans and glycosphingolipids in microarrays for research and diagnostic purposes. In certain embodiments, the disclosure relates to derivatizing glycosphingolipids with a marker.

Tailored glycopolymers as anticoagulant heparin mimetics

The present disclosure provides for methods and compositions comprising a series of synthetic glycopolymers. The disclosure also relates to a kit which is suitable for carrying out the inventive methods.

Trityl-mono-GalNAc compounds and their use
11248019 · 2022-02-15 · ·

This invention generally relates to the field of phosphoramidite derivatives. In particular, the invention relates to N-Acetylgalactosamine (GalNAc) compounds, in particular phosphoramidite or phosphonoamidite molecules of formula (I) with only one GalNAc moiety (formula II) and to conjugates of nucleic acid molecules with such N-Acetylgalactosamine containing molecules. Also provided are methods for preparation of these molecules and possible uses thereof, in particular in medicine. Wherein R.sup.1 is H or C.sub.1-6alkyl; R.sup.2 is a triphenylmethyl-based hydroxyl protecting group R.sup.3 is a phosphorus-containing group, particularly a phosphoramidite or a phosphonoamidite group, and K is represented by the general formula (II). ##STR00001##

Trityl-mono-GalNAc compounds and their use
11248019 · 2022-02-15 · ·

This invention generally relates to the field of phosphoramidite derivatives. In particular, the invention relates to N-Acetylgalactosamine (GalNAc) compounds, in particular phosphoramidite or phosphonoamidite molecules of formula (I) with only one GalNAc moiety (formula II) and to conjugates of nucleic acid molecules with such N-Acetylgalactosamine containing molecules. Also provided are methods for preparation of these molecules and possible uses thereof, in particular in medicine. Wherein R.sup.1 is H or C.sub.1-6alkyl; R.sup.2 is a triphenylmethyl-based hydroxyl protecting group R.sup.3 is a phosphorus-containing group, particularly a phosphoramidite or a phosphonoamidite group, and K is represented by the general formula (II). ##STR00001##

Thiopyranose compound and method for producing same

There is provided a production method of a thiopyranose compound represented by the following Formula (2) by reacting a compound represented by the following Formula (1) with a sulfur compound. ##STR00001##
X represents a leaving group. A represents an oxygen atom or a sulfur atom. Further, each of R.sup.1A to R.sup.4B, R.sup.1B to R.sup.4B, and R.sup.5 represents a hydrogen atom or a specific substituent.

Thiopyranose compound and method for producing same

There is provided a production method of a thiopyranose compound represented by the following Formula (2) by reacting a compound represented by the following Formula (1) with a sulfur compound. ##STR00001##
X represents a leaving group. A represents an oxygen atom or a sulfur atom. Further, each of R.sup.1A to R.sup.4B, R.sup.1B to R.sup.4B, and R.sup.5 represents a hydrogen atom or a specific substituent.

QUATERNARY AMMONIUM SALTS AS INHIBITORS OF TRIMETHYLAMINE PRODUCTION

Provided are compounds that can inhibit pathogenic, bacterial metabolite production and conjugates of the same. Also provided are pharmaceutical compositions comprising the same and methods of using the same.