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: 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: 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: 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: 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.

Abstract: The disclosure provides polynucleotides encoding a polypeptide including a morpholino linker. In some embodiments, the polynucleotides of the invention have increased stability compared to wild-type polynucleotides.

Abstract: The compounds are nucleoside and nucleotide analogues that can be used as cardioprotective agents. The compounds include tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary stereogenic all-carbon centers at the 2? position and a phosphonate ester at C5? position.

Abstract: The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: A simplified method of obtaining purified nucleic acids uses a single buffer solution to both wash and elute nucleic acids bound to a binding phase. Use of a single buffer solution avoids the time-consuming aspect of using different wash and elution buffer solutions during multiple nucleic acid purification steps. The method for purifying nucleic acids using a single buffer solution includes steps of: exposing a sample comprising nucleic acids to a nucleic acid binding phase, where the nucleic acid binding phase may include magnetic particles, silica particles, or a mixture thereof; and allowing the nucleic acids to bind to the nucleic acid binding phase; washing the nucleic acids bound to the nucleic acid binding phase at least once with the single buffer solution at room temperature; and eluting the nucleic acids from the nucleic acid binding phase with ?50 ?l of the single buffer solution, at a temperature of ?40° Celsius.

Abstract: The compounds are of the class of 5-fluorouracil derived acetal and hemiaminal ether compounds, useful in treating liver diseases and various types of cancer.

Abstract: Disclosed herein are oligonucleotides, such as nucleic acid inhibitor molecules, having a 4?-phosphate analog and methods of using the same, for example, to modulate the expression of a target gene in a cell. The oligonucleotide of the disclosure comprises a 5?-terminal nucleotide represented by Formula III: wherein Ra, Rb, B, X2 and Y are as defined in the specification. The phosphate analogs are bound to the 4?-carbon of the sugar moiety (e.g., a ribose or deoxyribose or analog thereof) of the 5?-terminal nucleotide of an oligonucleotide. Typically, the phosphate analog is an oxymethylphosphonate, where the oxygen atom of the oxymethyl group is bound to the 4?-carbon of the sugar moiety or analog thereof.

Abstract: The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier.

Abstract: Disclosed are co-crystal forms of N-(2-(5-(((2R,3R,4S,5R)-3,4-dihydroxy-5-methoxy-6,6-dimethyltetra-hydro-2H-pyran-2-yl)oxy)-3?-fluoro-[1,1?-biphenyl]-2-yl)ethyl)-acetamide and L-proline or D-proline, their pharmaceutical compositions, processes of manufacture, and methods of use for treating neurodegenerative disorders such as diabetic peripheral neuropathy.