Abstract: Among commonly known 3?,3?-cGAMP is a lyophilized product. The lyophilized product needs a lyophilizer during the manufacture. This, itself, causes a limitation in scale-up for mass production. Thus, it has been desired to develop and obtain a large amount of their crystals in a simple manner without using a special apparatus such as a lyophilizer. In addition, conventionally known lyophilized products or ethanol precipitates are highly hygroscopic. Hence, the present invention addresses the problem of providing an easy-to-handle crystal with excellent shelf life. A hydrate crystal of 3?,3?-cGAMP according to the invention may be either a crystal of alkali metal salt or a crystal of free acid. Either is less hygroscopic than existing powder. Thus, each is easy to handle in various purposes and is thus useful as a pharmaceutical raw material or the like.

Abstract: Hsp90 C-terminal inhibitors and pharmaceutical compositions containing such compounds are provided. The compounds of the disclosure are useful for the treatment and/or prevention of neurodegenerative disorders such as diabetic peripheral neuropathy.

Abstract: The invention relates to a compound of formula (I) wherein R2 and R4 are joined and together form a group, such a —CH2O—. The compound of formula (I) can be used in the manufacture of 5?S-LNA oligonucleotides as antisense drugs.

Abstract: An object of the present invention is to provide a liquid medicinal preparation which does not generate precipitates and is suitable for mass production. According to the present invention, provided is a liquid medicinal preparation that contains 1-(2-deoxy-2-fluoro-4-thio-?-D-arabinofuranosyl)cytosine or a salt thereof, a polyhydric alcohol having a molecular weight of 100 or less, and water. The polyhydric alcohol is preferably glycerin, propylene glycol, or butanediol.

Abstract: Provided is an artificial nucleoside or artificial nucleotide capable of composing an artificial oligonucleotide having superior nuclease resistance. The artificial nucleoside or artificial nucleotide is a compound represented by formula (I) or a salt thereof (wherein, Bx represents a pyrimidine base or purine base, R1, R2, R3 and R4 represent hydrogen atoms, C1-6 alkyl groups or the like, Y represents NR5R6 (wherein, R5 and R6, independently of each other, represent a hydrogen atom, C1-6 alkyl group or the like, or R5 and R6, together with a nitrogen atom bound thereto, form a 3- to 11-membered nitrogen-containing non-aromatic heterocyclic group) or an optionally substituted C2-9 aromatic heterocyclic group, Z1 and Z2 represent hydrogen atoms, hydroxyl group-protecting groups, phosphorous-containing groups or the like, and n represents an integer of 1 to 3).

Abstract: This invention relates to a crystalline form of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate.

Abstract: The invention relates to a pharmaceutical or nutraceutical composition comprising an alkalized organic substance selected from the group comprising proteins, carbohydrates, lipids, amino acids, vitamins, therapeutic agents and mixtures thereof. Such compositions are useful for treating a range of diseases and conditions. They also give rise to beneficial physiological effects such as, for example, increasing physical strength, muscle mass and endurance.

Abstract: A heparin structure with increased anticoagulant activity and method of making the same are disclosed. A heparin sample is provided and treated with a heparan sulfate sulfotransferase in an enzymatic reaction to add sulfuryl groups from a sulfuryl group source to the heparin sample, resulting in a heparin structure having above about 8% more 3-O-sulfo groups relative to wild-type bovine intestinal heparin. The added sulfuryl groups modify the heparin structure and increase the sample's binding to antithrombin III and its anticoagulant activity to be more similar and a viable alternative to porcine intestinal heparin. The modified heparin exhibits an anti-FXa activity and an anti-FIIa activity greater than about 180 U/mg, and a ratio of the anti-FXa activity to the anti-FIIa activity of about 0.9 to about 1.1, consistent with U.S. Pharmacopeia (USP) heparin activity specifications.

Abstract: A pharmaceutical composition containing any one or more of 4?-O-isolvalerylspiramycin I, II and III counters tumorigenesis and reduces or prevents metastasis by inhibiting selenoprotein H to trigger genomic instability and cell-cycle arrest in cancer cells.

Abstract: Cytidine nucleoside analogues of Formula I, wherein the variables are as described herein, in combination with uridine nucleoside analogues of Formula II, wherein the variables are as described herein, produce a synergistic effect on the inhibition of HCV polymerase.

Abstract: Gellan gum-based hydrogels are disclosed herein for in vitro cell culture and tissue engineering and regenerative medicine applications. Such gellan gum-based hydrogels may be used alone or combined with live cells and/or biomolecules for application in humans and/or animals. Chemical modification of gellan gum with selected ion-chelating substituents affords novel gellan gum hydrogels endowed with tunable physicochemical and biological properties. The modified gellan gum hydrogels described herein present advantages over existing hydrogel systems, including solubility, ionic crosslinking versatility, ease of formulation and injectability and greater adhesiveness within biological tissues and surfaces, whilst maintaining encapsulated cells viable during long culture periods and up-regulating the expression of healthy extracellular matrix markers.

Abstract: A preparation method for an esterified selenium polysaccharide includes the steps of: adding O?SeCl2 dropwise to a triethylamine-containing D-galactose allyl glucoside solution and reacting at room temperature to obtain 3,4-oxo-cyclo selenite galactose allyl glucoside; mixing NaHCO3 into a polysaccharide solution, adding acryloyl chloride dropwise to the polysaccharide solution and maintaining a temperature of a reaction solution to not exceed 40° C. during a dropwise addition to obtain acrylated polysaccharide; and performing a displacement reaction of the acrylated polysaccharide with the 3,4-oxo-cyclo selenite galactose allyl glucoside under an action of a Ru catalyst to obtain the esterified selenium polysaccharide. The esterified selenium polysaccharide prepared by the preparation method improves an immunity of a tested organism by increasing a selenium content in blood.

Abstract: Covalently modified alginate polymers, possessing enhanced biocompatibility and tailored physiochemical properties, as well as methods of making and use thereof, are disclosed herein. The covalently modified alginates are useful as a matrix for the encapsulation and transplantation of cells. Also disclosed are high throughput methods for the characterizing the biocompatibility and physiochemical properties of modified alginate polymers.

Abstract: Isolated heparin or heparan sulphate oligosaccharide fragments having a chain length of at least 10 saccharides and no more than 50 saccharides, which are capable of binding BMP2, are disclosed. Also disclosed is the use of the same heparin or heparan sulphate oligosaccharide fragments in kits and pharmaceutical compositions, and the use of the same heparan sulphate oligosaccharide fragments in the repair and/or regeneration of connective tissue and bones, and the treatment of wounds.

Abstract: Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Abstract: In some variations, the invention provides a process for producing a microcrystalline cellulose material, comprising: fractionating lignocellulosic biomass feedstock in the presence of an acid, a solvent for lignin, and water, to generate cellulose-rich solids and a liquid containing hemicellulose and lignin; chemically and/or mechanically treating the cellulose-rich solids to form microcrystalline cellulose having an average crystallinity of at least 60%; and recovering the microcrystalline cellulose as a pharmaceutical excipient. The pharmaceutical excipient may function as an antiadherent, a binder, a coating, or a disintegrant. In some embodiments, the pharmaceutical excipient further comprises a lignin-derived lubricant, glidant, sorbent, preservative, or other component. The pharmaceutical excipient may be present in a pill, tablet, capsule, powder, slurry, or other pharmaceutically effective and acceptable form.

Abstract: The present invention relates to a process for the preparation of Molnupiravir. The present invention also relates to an improved and commercially viable process for preparation of Molnupiravir with high yield and purity.

Abstract: The present invention provides a method for producing pentosan polysulfate, the method including a first step of obtaining an acidic xylooligosaccharide from a plant-derived raw material, and a second step of obtaining pentosan polysulfate from the acidic xylooligosaccharide. The first step includes a step of depolymerizing the plant-derived raw material. The second step includes a step of sulfating the acidic xylooligosaccharide. The method further includes a deacetylation step of adding a base to achieve a pH of 11 or higher. The deacetylation step is a step performed after the depolymerization step. The production method of the present invention can provide pentosan polysulfate having a low acetyl group content, and also produce pentosan polysulfate with a high yield inexpensively and efficiently.

Abstract: The invention relates to a process for preparing a 3?-O-amino-ribonucleotide. It also relates to a compound of formula (III), and its use as a precursor for the synthesis of a 3?-O-amino-ribonucleotide. In formula (III), B is a nitrogenous base or a protected derivative thereof, G and G? are identical or different, and are a protecting group, and RN— is a phthalimido or an imino group.

Abstract: A method for preparing high-purity sugammadex sodium, which realizes the preparation by using inositol phosphate and derivatives thereof, includes: adding a specific type of protective agent to crude sugammadex sodium, and performing recrystallization under the protection of inert gas to obtain pure sugammadex sodium. The protective agent is selected from inositol phosphate and derivatives thereof, such as inositol hexaphosphate and salts or esters thereof; one or a mixture of two or more of partial degradation products of inositol hexaphosphate, such as inositol pentaphosphate, inositol tetraphosphate, inositol triphosphate, inositol diphosphate, inositol monophosphate, and salts or esters thereof, in any ratio. The method has the advantages of simple operation, high product purity, good safety and less allergic reaction, and the method is cost-effective and more suitable for industrial production.