Abstract: Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3?-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2?epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

Abstract: The present invention relates to chiral phosphoramidites represented by formula (Ia) or formula (Ib) as novel monomers for the synthesis of stereodefined phosphorothioate MOE oligonucleotides. Furthermore, the present invention relates to a method for synthesizing stereodefined phosphorothioate MOE oligonucleotides using said novel chiral phosphoramidites.

Abstract: CD73 (also known as ecto-5?-nucleotidase) inhibitor compounds are provided, as well as compositions and uses thereof for treating or preventing CD73-associated or related diseases, disorders and conditions, including cancer- and immune-related disorders. CD73 inhibitor compounds include compounds having the structure set forth in Formula I and pharmaceutically acceptable esters or salts thereof.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: Provided are methods for treating ocular inflammatory disorders, including macular edema, using an AMP kinase activator, e.g., 5-aminoimidazole-4-carboxamide-1-?-d-ribofuranoside (AICAR). The method reduces inflammation, thereby minimizing the loss of vision or visual function associated with these ocular disorders.

Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.

Abstract: The present application relates to novel nucleoside derivatives of formula (I) as claimed in claim 1, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: Compounds for treatment of a patient having a tumour that is metastatic and/or that reduces an organ function, wherein the compounds are of the general formula: wherein X is O, NH and S, wherein n is 0, 1 or 2, wherein R1 and R2 are H, methyl or ethyl, or together form a group CR3R4, and wherein R3 and R4 are H, methyl or ethyl.

Abstract: Provided are a newly developed tandem malonate-based amphipathic molecule, a method of preparing the same, and a method of extracting, solubilizing, stabilizing, crystallizing or analyzing a membrane protein using the same. In addition, the compound may be used to efficiently extract membrane proteins having various structures and characteristics from a cell membrane, compared to a conventional compound, to stably store the proteins in an aqueous solution for a long time, and may be used in functional and structural analysis thereof. The analysis of the structures and functions of the membrane proteins is one of the most attractive fields in current biology and chemistry, which are closely related to new drug development.

Abstract: The present invention relates to a quinoline derivative of formula (I) or anyone of its pharmaceutically acceptable salt, or anyone of its metabolites, for use for treating or preventing a viral infection, in particular a HIV infection or a HIV-related condition in a patient; and then terminating said treatment when: the viral load is low or undetectable; and/or the level of CD4+ cell count is maintained or restored.

Abstract: What claimed is a method of sweetening or enhancing sweetening effect of a composition that is administered orally to an individual by adding a specific triterpene glycoside obtained from Momordica grosvenorii (Siraitia grosvenori).

Abstract: Provided is a compound of the general formula (1), which 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, as well as 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.

Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Abstract: The present invention relates to a newly developed resorcinarene-based amphipathic compound, a method for producing the same, and a method for extracting, solubilizing, stabilizing, crystallizing, or analyzing a membrane protein by using the same. In addition, compared to a conventional compound, the compound can efficiently extract, from a cell membrane, membrane proteins having a greater variety of structures and characteristics, and can stably store such membrane proteins for a long time in an aqueous solution. Therefore, the compound can be used to analyze the functions and structures of such membrane proteins. Analysis of the structures and functions of membrane proteins, being closely related to the development of new drugs, is one of the fields of greatest interest in biology and chemistry today.

Abstract: This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations which comprise a polar aprotic solvent, preferably dimethyl acetamide (DMA). Formulations comprising this solvent provide therapeutically effective treatments of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate. The invention also relates to methods of using said formulations and kits comprising said formulations.

Abstract: The present invention provides a novel nucleoside derivative or a salt thereof, a polynucleotide synthesis reagent, a method for producing a polynucleotide, a polynucleotide, and a method for producing a binding nucleic acid molecule. The nucleoside derivative or a salt thereof of the present invention is represented by the following chemical formula (1): where in the chemical formula (1), Su is an atomic group having a sugar skeleton at a nucleoside residue or an atomic group having a sugar phosphate skeleton at a nucleotide residue, and may or may not have a protecting group, L1 and L2 are each independently a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms, X1 and X2 are each independently an imino group (—NR1—), an ether group (—O—), or a thioether group (—S—), and the R1 is a hydrogen atom or a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms.

Abstract: The present invention relates to a TRIS- or neopentyl glycol-based amphipathic compound, a method of preparing the same, and a method of extracting, solubilizing, stabilizing, or crystallizing a membrane protein using the same. By using the TRIS- or neopentyl glycol-based compound according to the present invention, a superior membrane protein solubilization effect is exhibited, a membrane protein can be stably stored for a long time in an aqueous solution, and the structural fluidity of the membrane protein can be excellently maintained. Accordingly, the TRIS- or neopentyl glycol-based compound can be utilized in analyzing functions and structures of membrane proteins. Membrane protein structure and function analysis is currently one of the most attractive fields of research in biology and chemistry. Since more than half of the new drugs under development target membrane proteins, the compound can be applied to membrane protein structure research closely related to drug discovery.