C07H13/12

CD206 TARGETED DRUG DELIVERY VEHICLES CARRYING NOVEL BISPHOSPHONATE DRUG PAYLOADS VIA A DEGRADABLE LINKER
20240294564 · 2024-09-05 ·

Provided are novel compounds containing a polymeric carbohydrate backbone, one or more mannose-binding C-type lectin receptor targeting moieties, and a nitrogenous bisphosphonate compound coupled to the backbone via a thiol-maleimide conjugation, in addition to pharmaceutical compositions, methods of synthesizing, and methods of use. The thiol-maleimide conjugation of a bisphosphonate to a polymeric carbohydrate backbone provides for methods of using the compounds and compositions thereof for releasing the therapeutic payload when internalized into a mannose-binding C-type lectin receptor-expressing cell, such as tumor associated macrophages (TAMs) for the treatment of various diseases, including, cancer, autoimmune diseases, and inflammatory disorders.

GLUCURONIDE PRODRUGS OF TOFACITINIB

The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I:

##STR00001##

where A.sup.1 and R.sup.1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

LIPOSOMES USEFUL FOR DRUG DELIVERY
20180235954 · 2018-08-23 ·

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

NUTRITIONAL COMPOSITIONS WITH 2FL AND LNNT FOR USE IN INDUCING A GUT MICROBIOTA CLOSE TO THE ONE OF BREAST FED INFANTS
20180220690 · 2018-08-09 ·

The present invention relates to a nutritional composition comprising at least one fucosylated oligosaccharide and at least one N-acetylated oligosaccharide for promoting or inducing a global gut microbiota that is closer to the one of infants fed exclusively with human breast milk, in comparison to infants fed with a conventional nutritional composition. The composition can be an infant formula and is in particular intended for infants between 0 and 12 months of age fed predominantly with infant formula. It promotes a healthy intestinal flora and has beneficial short and long terms effects.

PROTECTED MONOMER AND METHOD OF FINAL DEPROTECTION FOR RNA SYNTHESIS

A method of deprotecting a solid support bound polynucleotide comprising at least one 2-protected ribonucleotide in which a step of contacting the polynucleotide with a composition comprising a diamine is performed under conditions sufficient to deprotect and cleave the polynucleotide which remains retained on the solid support.

PROTECTED MONOMER AND METHOD OF FINAL DEPROTECTION FOR RNA SYNTHESIS

A method of deprotecting a solid support bound polynucleotide comprising at least one 2-protected ribonucleotide in which a step of contacting the polynucleotide with a composition comprising a diamine is performed under conditions sufficient to deprotect and cleave the polynucleotide which remains retained on the solid support.

LIPOSOMES USEFUL FOR DRUG DELIVERY
20180169014 · 2018-06-21 ·

The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

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.

5-ALA DERIVATIVES AND USE THEREOF
20180133320 · 2018-05-17 ·

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.