Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.

Abstract: The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.

Abstract: Minimally invasive treatment methods for benign prostatic hyperplasia (BPH) tissue. A system includes a sustained release formulation comprising a cytostatic or cytotoxic drug, and an applicator or delivery system for local delivery of a composition comprising or consisting essentially of the sustained release formulation to the prostate. The applicator containing the composition is characterized by a KIR value of between 40 and 400 Centipoise per unit area.

Abstract: This disclosure provides electrochemically-cleavable linkers with cleavage potentials that are less than the redox potential of the solvent in which the linkers are used. In some applications, the solvent may be water or an aqueous buffer solution. The linkers may be used to link a nucleotide to a bound group. The linkers include a cleavable group which may be one of a methoxybenzyl alcohol, an ester, a propargyl thioether, or a trichloroethyl ether. The linkers may be cleaved in solvent by generating an electrode potential that is less than the redox potential of the solvent. In some implementations, an electrode array may be used to generate localized electrode potentials which selectively cleave linkers bound to the activated electrode. Uses for the linkers include attachment of blocking groups to nucleotides in enzymatic oligonucleotide synthesis.

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

Abstract: Methods of preparing nicotinamide riboside and derivatives thereof.

Abstract: A chemotherapy drug-sensitizing method includes: transfecting antisense oligonucleotide (e.g., siRNA-1976 or antagomir-1976) to a cancer cell to form a transfected cancer cell for blocking miR-1976 of the cancer cell; providing a treatment of cancer drug (or anticancer drug combination) to the transfected cancer cell whose miR-1976 is blocked by the antisense oligonucleotide; the transfected cancer cell providing a degree of sensitivity for the cancer drug due to its miR-1976 being blocked.

Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

Abstract: The present invention relates to the field of oligonucleotide conjugates and to methods of synthesis thereof. In the present method a low-water content solvent environment allows a more efficient conjugation, reducing the amount of conjugate moiety needed and increasing the conjugation reaction speed.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The present invention relates to modified, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and intermediates thereof. More particularly, the present invention relates to improved processes for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

Abstract: Certain anti-viral compounds, pharmaceutical compositions, and methods related thereto are disclosed.

Abstract: Provided is a degrader for injured mitochondria based on an autophagy mechanism, the degrader including a compound or a salt thereof, the compound containing a ligand capable of binding to or accumulating in mitochondria and a substituent represented by the following general formula (1): where R1, R2, and R3 are identical to or different from each other, and each represent a hydrogen atom or the like.

Abstract: The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

Abstract: The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

Abstract: An example composition includes a therapeutically effective amount of a histidine kinase inhibitor. The histidine kinase inhibitor includes at least one of a 6-benzo[d]thiazol-2-amine derivative, a purine derivative, an adenine derivative, an adenine-sulfonyl fluoride derivative, a riluzole analog, a riluzole-sulfonyl fluoride derivative, a 6-benzo[d]thiazol-2-amine-sulfonyl fluoride derivative, a 6,6?-oxybis(benzo[d]thiazol-2-amine) derivative, or a 6,6?-oxybis(benzo[d]thiazol-2-amine)-sulfonyl fluoride derivative. An example technique for treating a bacterial infection includes administering a composition comprising a histidine kinase inhibitor to a patient.

Abstract: The present invention aims to provide a novel glycosyl hesperetin, which is significantly reduced in miscellaneous tastes characteristic of conventional products containing glycosyl hesperetin, and a method for producing the same and uses thereof; and the objects are solved by providing a glycosyl hesperetin which comprises glycosyl hesperetin in an amount of 90% or more by mass but less than 100% by mass, on a dry solid basis, but it does not substantially contain furfural, and a method for producing the same and uses thereof.

Abstract: The invention relates to a combination comprising an antineoplastic agent, e.g. an antimetabolite antineoplastic agent and a type 1 serotonin receptor (HTR1) modulator, e.g. a HTR1 antagonist. In addition the invention relates to a pharmaceutical composition comprising a combination of the invention and a pharmaceutically acceptable excipient. The invention also relates to the combination and pharmaceutical composition according to the invention for use in medicine, particularly for use in the prevention and/or treatment of a hematological malignancy.

Abstract: Described herein are small molecule cap-dependent inhibitors, including the compound of the formula: which compounds that can induce the accumulation of the p53 tumor suppressor protein in cancer cells that still express wild-type p53, as well as methods of using those compounds to, among other things, treat neuroblastoma, pediatric glioblastoma multiforme or breast cancer.