Abstract: Disclosed is a simplified, readily scalable series of individual methods that collectively constitute a method for the synthesis of C2?epiAmB, an efficacious and reduced-toxicity derivative of amphotericin B (AmB), beginning from AmB. Also provided are various compounds corresponding to intermediates in accordance with the series of methods.

Abstract: The present disclosure provides a taxane compound and a preparation method and application thereof. The preparation method includes: protecting two hydroxyl groups in gemcitabine, conducting a condensation reaction between the protected gemcitabine and alkyl chloroformate, and removing of hydroxyl protecting groups to obtain an intermediate G1; protecting a first hydroxyl group of the intermediate G1, and then protecting the other one of the hydroxyl groups, and removing a protecting group of the first hydroxyl group to obtain an intermediate G2; reacting 7,10-di-troc-docetaxel with dianhydride to obtain an intermediate D1; conducting a condensation reaction between the intermediate D1 and the intermediate G2 to obtain an intermediate D2; and subjecting the intermediate D2 to hydroxyl deprotection to obtain a target product comprising the disclosed taxane compound.

Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.

Abstract: The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substitutents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone.

Abstract: This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.

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 method for preparing 3,6-anhydro-L-galactose, and use thereof. More specifically, 3,6-anhydro-L-galactose, which is a monosaccharide constituting agar, is produced in a high yield through chemical and enzymatic methods, and the physiological activities thereof such as whitening, moisturizing, antioxidant, antiinflammatory activities and the like are displayed, thereby enabling industrial use thereof.

Abstract: The present invention relates to a mesitylene-cored amphiphile, a method of preparing the same and a method of extraction, solubilization, stabilization, crystallization or analysis of a membrane protein using the same. When a mesitylene-cored compound according to the present invention is used, membrane proteins can be stored in a stable conformation for a long time in an aqueous solution in comparison with conventional compounds, by which the membrane proteins are usable in both functional and structural analyses thereof. The functional and structural analyses of membrane proteins are one of the fields that are most spotlighted in current biology and chemistry. The present invention can be used to research on a protein structure closely related to new drug development.

Abstract: Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L1. L2, L3, L4, L5, L6, L7, L8, L9, L10, Y1, Y2, Y3, Y4, R1, R2, R3, R4, R5, R6, are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Abstract: Modified Tryptamine, Tryptamine-2?-deoxy-uridine (TrpdU) and TrpdU-phosphoramidites for oligonucleotide synthesis are provided, as well as improved methods of their synthesis and oligonucleotides comprising at least one modified TrpdU nucleotide.

Abstract: Truncated triterpene saponin analogues containing a trisaccharide or tetrasaccharide ester are disclosed. Also disclosed are pharmaceutical compositions comprising truncated saponin analogues and synthetic methods of producing the truncated saponin analogues. Another aspect of the present application relates to a method for immunizing a subject, comprising administering to the subject the pharmaceutical composition comprising a minimal saponin analogue and an antigen.

Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

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 provides methods for inhibition of human herpes virus replication in a subject comprising administering to the subject a therapeutically effective amount of a pharmaceutically acceptable composition comprising a cardiac glycoside analog, including for example, a digitoxin analog and pharmaceutically acceptable carrier. Other methods of the present invention include administering a digitoxin analog along with at least one other biologically active compound and pharmaceutically acceptable carrier. Methods for inhibition of the ?3 subtype of the Na/K ATPase in a subject comprising administering to the subject a therapeutically effective amount of a pharmaceutically acceptable composition comprising a digitoxin analog are also provided.

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: This disclosure features dinucleotide compounds that modulate Stimulator of Interferon Genes (STING) activity, for use for example in the treatment of cancer. This disclosure also features compositions as well as other methods of using and making the same (Formula (A)). A and B are each independently selected from the group consisting of Formulae (i), (ii), (iii), and (iv).

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: Disclosed is a method for mitigating or ameliorating osteoarthritis in vertebrate subjects including administering to a subject a therapeutically effective amount of an exogenous hyaluronan formulation. Also disclosed is an oral or parenteral hyaluronan composition comprising a polydisperse hyaluronan and a pharmaceutically acceptable carrier, and a method of manufacturing the composition.

Abstract: The present invention provides (i) processes for preparing a 2?-deoxy-2?-fluoro-2?-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2?-deoxy-2?-fluoro-2?-C-methyl-ß-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.

Abstract: Compounds, methods and uses of pseudo-trisaccharide aminoglycosides represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification, in the treatment of Rett syndrome are disclosed.