Aspects of the invention relate to novel synthetic compounds having binding affinity with galectin proteins.

Aspects of the invention relate to novel synthetic compounds having binding affinity with galectin proteins.

This invention relates to compounds that are useful as cancer therapies. The compounds comprise azithromycin derivatives having a phosphonium cation tethered to the azithromycin macrocycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.

The present invention relates to modified, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and intermediates thereof. More particularly, the present invention relates to improved processes for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds and the compounds used in such preparations.

It is an object of the present invention to provide a fluorescence imaging probe capable of selectively visualizing target cells such as cells expressing β-galactosidase (lacZ expressing cells) at a single-cell level in a red fluorescence region, and of performing co-staining together with GFP. An intracellularly-retainable red fluorescent probe comprising a compound represented by the following formula (I) or a salt thereof: ##STR00001## wherein: A represents a monovalent group cleaved by an enzyme; R.sup.1 represents a hydrogen atom, or one to four of the same or different substituents bonded to a benzene ring; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each independently represent —CFR.sup.10R.sup.11, —CF.sub.2R.sup.12, a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom, wherein at least one of R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is —CFR.sup.10R.sup.11 or —CF.sub.2R.sup.12; R.sup.2 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group; R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom, an alkyl group, or an alkenyl group; X represents Si(R.sup.a) (R.sup.b), wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group; and Y is —C(═O)— or —R.sup.cC(═O)—, wherein R.sup.c is an alkylene group having 1-3 carbon atoms.

It is an object of the present invention to provide a fluorescence imaging probe capable of selectively visualizing target cells such as cells expressing β-galactosidase (lacZ expressing cells) at a single-cell level in a red fluorescence region, and of performing co-staining together with GFP. An intracellularly-retainable red fluorescent probe comprising a compound represented by the following formula (I) or a salt thereof: ##STR00001## wherein: A represents a monovalent group cleaved by an enzyme; R.sup.1 represents a hydrogen atom, or one to four of the same or different substituents bonded to a benzene ring; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each independently represent —CFR.sup.10R.sup.11, —CF.sub.2R.sup.12, a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom, wherein at least one of R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is —CFR.sup.10R.sup.11 or —CF.sub.2R.sup.12; R.sup.2 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group; R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom, an alkyl group, or an alkenyl group; X represents Si(R.sup.a) (R.sup.b), wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group; and Y is —C(═O)— or —R.sup.cC(═O)—, wherein R.sup.c is an alkylene group having 1-3 carbon atoms.

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)

##STR00001##