The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3-dipole compounds, in particular to halogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP), and to halogenated 1,3-dipole compounds comprising (peracylated) N-acetylglucosamine (GlcNAc), N-acetylgalactosamine (GalNAc), N-acetylmannosamine (ManNAc) and N-acetyl neuraminic acid (NeuNAc). ##STR00001##

The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3-dipole compounds, in particular to halogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP), and to halogenated 1,3-dipole compounds comprising (peracylated) N-acetylglucosamine (GlcNAc), N-acetylgalactosamine (GalNAc), N-acetylmannosamine (ManNAc) and N-acetyl neuraminic acid (NeuNAc). ##STR00001##

The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis.

The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis.

A functionalization is performed with a dissolved oligo- or polysaccharide derivative which contains at least one free functional group, especially an amino group, linked through a polar carbamate linkage and a spacer (X), according to the general formula I: ##STR00001##

A functionalization is performed with a dissolved oligo- or polysaccharide derivative which contains at least one free functional group, especially an amino group, linked through a polar carbamate linkage and a spacer (X), according to the general formula I: ##STR00001##

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.

The cell labeling agent includes a monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells. Among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives, at least one group that does not change, even when metabolized by the sialic acid biosynthetic pathway, includes a ring structure with a carbon-carbon double bond or triple bond.

The cell labeling agent includes a monosaccharide derivatives with a six-membered ring structure that are metabolized to sialic acid in the sialic acid biosynthetic pathway of cells. Among the groups bonded to carbon atoms constituting a six-membered ring in the monosaccharide derivatives, at least one group that does not change, even when metabolized by the sialic acid biosynthetic pathway, includes a ring structure with a carbon-carbon double bond or triple bond.

Provided herein are compounds for use as sialidase inhibitors, including alkynyl-3-fluorosialyl fluoride. The compounds, which include the compound DFSA, function by trapping a 3-fluorosialylenzyme intermediate (reporter-inhibitor-enzyme conjugate). These compounds can be conjugated with a detectable tagging moiety for isolation and identification of sialidases.