C07H5/04

BINDERS AND MATERIALS MADE THEREWITH
20210095156 · 2021-04-01 ·

A curable aqueous composition is disclosed comprising a carbohydrate, a crosslinking agent, and an amine base, wherein the curable aqueous composition has a pH adjusted by the amine base. Further disclosed is a method of forming a curable aqueous solution.

5-azido-5-deoxy-2 :3-isopropylidene-D-arabinose compounds; their method of manufacture and their use for the synthesis of ARA-N3, KDO-N3 and 4EKDO-N3

Disclosed are new compounds of formulae: ##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.

5-azido-5-deoxy-2 :3-isopropylidene-D-arabinose compounds; their method of manufacture and their use for the synthesis of ARA-N3, KDO-N3 and 4EKDO-N3

Disclosed are new compounds of formulae: ##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.

SIALIDASE INHIBITORS AND PREPARATION THEREOF
20200190130 · 2020-06-18 ·

New 2-deoxy-2,3-dehydro-sialic acids and 2,7-anhydro-sialic acids, which are useful as sialidase inhibitors, and enzymatic methods for preparing them are disclosed. The methods include forming a reaction mixture comprising a glycoside acceptor, a sialic acid donor, and a sialyltransferase; maintaining the reaction mixture under conditions sufficient to form a sialoside; and contacting the sialoside with a Streptococcus pneumoniae sialidase to form the sialic acid product. Methods for the inhibition and sialidases and the treatment of cancer and infectious diseases are also disclosed.

SIALIDASE INHIBITORS AND PREPARATION THEREOF
20200190130 · 2020-06-18 ·

New 2-deoxy-2,3-dehydro-sialic acids and 2,7-anhydro-sialic acids, which are useful as sialidase inhibitors, and enzymatic methods for preparing them are disclosed. The methods include forming a reaction mixture comprising a glycoside acceptor, a sialic acid donor, and a sialyltransferase; maintaining the reaction mixture under conditions sufficient to form a sialoside; and contacting the sialoside with a Streptococcus pneumoniae sialidase to form the sialic acid product. Methods for the inhibition and sialidases and the treatment of cancer and infectious diseases are also disclosed.

Method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose

Disclosed is a method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose. This method includes the chemical reaction of compound of formula X: ##STR00001##
Wherein: R.sup.1 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl; aryl including phenyl; each of these groups being substituted or not; and R.sup.2 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl, tert-butyl, isobutyl; each of these groups being substituted or not; with a deprotecting reagent including a Lewis or Brnsted acid in a polar aprotic solvent, thereby obtaining a free C-1 OH group. The method can also start with the preparation from commercially available D-galactose pentaacetate, D-galactose tetraacetate or tetraacetyl D-galactosyl trichloroacetimidate. The step of deprotecting the anomeric position avoids the use of cerium and allows the easy purification of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose.

Method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose

Disclosed is a method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose. This method includes the chemical reaction of compound of formula X: ##STR00001##
Wherein: R.sup.1 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl; aryl including phenyl; each of these groups being substituted or not; and R.sup.2 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl, tert-butyl, isobutyl; each of these groups being substituted or not; with a deprotecting reagent including a Lewis or Brnsted acid in a polar aprotic solvent, thereby obtaining a free C-1 OH group. The method can also start with the preparation from commercially available D-galactose pentaacetate, D-galactose tetraacetate or tetraacetyl D-galactosyl trichloroacetimidate. The step of deprotecting the anomeric position avoids the use of cerium and allows the easy purification of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose.

THIOSCCHARIDE MUCOLYTIC AGENTS

There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods.

THIOSCCHARIDE MUCOLYTIC AGENTS

There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods.

NOVEL GLYCAN CONJUGATES AND METHODS OF USE THEREOF
20200078452 · 2020-03-12 ·

The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.