The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. These compounds are represented by the following formula (I):

##STR00001##

wherein R.sup.1, R.sup.2, etc. are defined as in claim 1.

The present invention relates to a 3′-ketoglycoside compound defined by formula (I) and its use for controlled release of alcohols, in particular alcohols showing an insect repellent effect. It relates also to a process for preparing the 3′-ketoglycoside compound of formula (I). It further relates to a composition comprising a 3′-ketoglycoside compound of formula (I). It relates also to the use of a 3′-ketoglycoside compound of formula (I) for the controlled release of alcohols. It related also to a method of use of such composition.

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

The present invention provides metabolites of the antiviral drug bictegravir, including compositions and salts thereof, which are useful in the prevention and/or treatment of HIV as well as analytical methods related to the administration of bictegravir.

The present invention provides metabolites of the antiviral drug bictegravir, including compositions and salts thereof, which are useful in the prevention and/or treatment of HIV as well as analytical methods related to the administration of bictegravir.

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 the pharmaceutical formulations comprising said compounds.

The present invention aims to provide a novel glycosyl hesperetin, which is significantly reduced in miscellaneous tastes characteristic of conventional products containing glycosyl hesperetin, and a method for producing the same and uses thereof; and the objects are solved by providing a glycosyl hesperetin which comprises glycosyl hesperetin in an amount of 90% or more by mass but less than 100% by mass, on a dry solid basis, but it does not substantially contain furfural, and a method for producing the same and uses thereof.

The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.

The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.

The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.