C07H5/00

Stabilisation of radiopharmaceutical precursors

The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl--D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed.

CELL-PERMEABLE PROBES FOR IDENTIFICATION AND IMAGING OF SIALIDASES

Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

CELL-PERMEABLE PROBES FOR IDENTIFICATION AND IMAGING OF SIALIDASES

Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

Stabilisation of radiopharmaceutical precursors

The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl--D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed.

Cell-permeable probes for identification and imaging of sialidases

Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

Cell-permeable probes for identification and imaging of sialidases

Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

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.

One-pot synthesis of alpha/beta-O-glycolipids

The present invention provides a one-pot method of preparing an unprotected -O-glycolipid. The first step involves contacting a protected -iodo sugar with a catalyst and a lipid comprising a hydroxy group, under conditions sufficient to prepare a protected -O-glycolipid. The second step involves deprotecting the protected -O-glycolipid under conditions sufficient to prepare the unprotected -O-glycolipid, wherein the contacting and deprotecting steps are performed in a single vessel. The present invention also provides a one-pot method of preparing an unprotected -O-glycolipid following the steps for the preparation of the unprotected -O-glycolipid.

One-pot synthesis of alpha/beta-O-glycolipids

The present invention provides a one-pot method of preparing an unprotected -O-glycolipid. The first step involves contacting a protected -iodo sugar with a catalyst and a lipid comprising a hydroxy group, under conditions sufficient to prepare a protected -O-glycolipid. The second step involves deprotecting the protected -O-glycolipid under conditions sufficient to prepare the unprotected -O-glycolipid, wherein the contacting and deprotecting steps are performed in a single vessel. The present invention also provides a one-pot method of preparing an unprotected -O-glycolipid following the steps for the preparation of the unprotected -O-glycolipid.