Patent classifications
C07H19/056
AMYLOID TARGETING AGENTS AND METHODS OF USING THE SAME
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
Reagents based on a tertiary amine backbone to introduce chemical functionality in nucleic acids and sequence-controlled polymers
It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.
Mannose Derivatives for Treating Bacterial Infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I:
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The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Mannose Derivatives for Treating Bacterial Infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I:
##STR00001##
The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
ASGPR CELL SURFACE RECEPTOR BINDING COMPOUNDS AND CONJUGATES
The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface asialoglycoprotein receptor (ASGPR). The cell surface ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided herein methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.
Amyloid targeting agents and methods of using the same
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
Amyloid targeting agents and methods of using the same
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
Cyclodextrin-linked polyvalent ligands for complexation of metal ions
Compounds are described which include polyvalent ligands linked to a cyclodextrin scaffold which exhibit strong binding affinities for lanthanides and favorable characteristics with respect to altering the relaxation time of coordinated water molecules. The compounds are useful as contrast agents in applications such as magnetic resonance imaging. The polyvalent ligands are also useful in applications requiring chelation of metal ions in other applications such as water treatment, sequestration of metal ions and treatment of diseases or conditions caused by exposure to toxic or radioactive metal ions.
NOVEL GALACTOSIDE INHIBITOR OF GALECTINS
A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.
NOVEL GALACTOSIDE INHIBITOR OF GALECTINS
A compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.