Abstract: Compounds of formula (II) are provided for stabilizing protein transthyretin (TTR) and inhibiting amyloid fibril formation, for example, transthyretin-mediated amyloid fibril formation, and for treating, preventing, or ameliorating one or more symptoms of amyloid diseases, for example, transthyretin-related amyloidosis (ATTR).

Abstract: Disclosed are compounds that promote spinogenesis, are capable of reducing the neural toxicity of beta-amyloid peptides, and/or reduce the symptoms of traumatic brain injury in a patient.

Abstract: This invention provides preparations, compositions, products, and applications of photo-crosslinked hydrogels. Component A—a photosensitive polymer derivative, component B—the photoinitiator, and auxiliary component C—other biocompatible polymer derivative each are respectively dissolved in a biocompatible medium to obtain solution A, solution B, and solution C. The solution A, the solution B, and the optional solution C are mixed homogenously to obtain a hydrogel precursor solution. The hydrogel precursor solution is subject to irradiation of the UV light for photocoupled crosslinking to form a photo-crosslinked hydrogel. The photo-crosslinked hydrogel exhibit rapid speed of photo-curing, strong tissue adhesion, excellent mechanical properties, good biocompatibility, and excellent clinical operability.

Abstract: This disclosure relates generally to the facile and selective mono-perfluoro and poly-fluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics.

Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including autoimmune diseases, inflammatory diseases, chronic inflammatory diseases, diabetes, and infectious diseases, such as lupus, Sjögren's syndrome, rheumatoid arthritis, type 1 diabetes, inflammatory bowel disease, viral diseases, and nonalcoholic steatohepatitis. The compounds can also be used to generate cells, such as immune cells, for treating the conditions.

Abstract: This disclosure relates to pyrazoline dihydroquinolone derivatives, pharmaceutical compositions, and uses. In certain embodiments, the compounds are selective NMDA receptor inhibitors and are useful in therapeutic methods related thereto. In certain embodiments, this disclosure relates to pharmaceutical compositions comprising a compound of the following formula: or salts, esters, or prodrugs thereof, as provided herein.

Abstract: The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: (I) where A, L, R1, R2, R3, and n are described herein.

Abstract: Provided herein are compounds and methods for treating a disorder associated with aberrant A? peptide levels, including Alzheimer's disease.

Abstract: The present disclosure relates to novel compounds having estrogen receptor alpha degradation activity, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.

Abstract: The present disclosure relates to methods and intermediates useful for preparing a compound of formula I: or a co-crystal, solvate, salt or combination thereof.

Abstract: The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.

Abstract: The invention provides a novel class of propiolylamide-based irreversible inhibitors of PKM2 compounds of the general formula I, pharmaceutical compositions, and methods of inducing an anti-tumor effect in a subject suffering from tumor comprising administering to the subject a pharmaceutical composition comprising an effective amount of compound of formula I.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: The present invention provides substituted isoindole compounds which are selective allosteric EGFR inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances, generally of Formula: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of Formula II wherein X is selected from the group consisting of CH and N; Q is selected from the group consisting of CH3 and H; R is selected from the group consisting of and; or a pharmaceutically acceptable salt thereof, compositions, methods to treat liver disease and NASH.

Abstract: The present invention relates to a pyrrolo-pyridine derivative compound, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for the prevention or treatment of protein kinase-related diseases. A compound represented by chemical formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, according to the present invention, has excellent inhibitory activity against various protein kinases including DYRK1A, and therefore, the pharmaceutical composition containing the same as an active ingredient can be favorably used in the treatment or prevention of protein kinase-related diseases. Particularly, the pharmaceutical composition can be effectively used in the prevention, treatment, or alleviation of Alzheimer's disease, dementia, or Alzheimer's dementia.

Abstract: The present invention relates to novel methods of preparation of substituted pyridines and the compounds produced therefrom. In particular, the present invention provides efficient methods for the construction of diversely substituted pyridines, with varying substitution patterns under simple and metal-free conditions with high atom- and pot-economy and excellent functional group tolerance, and which are useful for the synthesis of natural products.

Abstract: Disclosed herein, inter alia, are pyridopyrazines and methods of using the same.

Abstract: A process for producing crystals of a compound represented by the following formula (I): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.

Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

Abstract: A compound containing indolocarbazole having a formula: Formula I is disclosed.

Abstract: Disclosed are a pyrazolo-heteroaryl derivative, a preparation method and medical use thereof. In particular, this invention relates to a new pyrazolo-heteroaryl derivative as shown in the general formula (I), a preparation method thereof and a pharmaceutical composition containing the derivative and the use thereof as a therapeutic agent, in particular as a TLR7 agonist, wherein each substituent in the general formula (I) is defined in the description.

Abstract: Provided are a compound represented by formula (I), an isomer or a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to A2A receptor. The R1, R2, R3, ring A, ring B, n, and m are as defined in the specification.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.

Abstract: The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention provides compositions and methods for the delivery of antivirals to a cell or subject.

Abstract: The present invention relates to bisaryl heterocycle compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators.

Abstract: Disclosed herein are improved methods for the synthesis of zinc-amino acid-halide complexes via reaction of zinc oxide and amino acid hydrochloride in a solvent comprising a polyol, as well as oral care compositions comprising said complexes made according to said method.

Abstract: Novel CUR— and CUR—BF2 compounds as well as novel bis and mono-NSAID/CUR—BF2 and NSAID/CUR hybrids exhibiting anti-tumor properties are presented. CUR compounds bearing fluorinated moieties with selective fluorine introduction into the ?-carbonyl moiety as well as CUR—BF2 adducts and CURs with diverse substitution patterns in the phenyl rings including fluorinated substituents (SCF3, OCF3, and F) and/or bulky activating groups (OMe, OAc, and OBz) are presented. Fluorinated aryl-pyrazoles and isoxazoles as well as novel CUR and CUR—BF2 compounds with monocyclic aromatic and bicyclic-heteroaromatic lateral rings, bearing fluorine(s), OCF3, CF3, and SCF3 groups, and their alpha-carbonyl-fluorinated analogs, as well as their pyrazole and isoxazole derivatives are presented. The CUR-pyrazoles embody analogs that are fluorinated at the phenyl-pyrazole moiety. The hybrids, compounds, and their derivatives exhibited exceptional cytotoxic and anti-proliferative activity against several cancer cell-lines.

Abstract: The present disclosure provides borate activators comprising cations having linear alkyl groups, catalyst systems comprising, and processes for polymerizing olefins using such activators. Specifically, the present disclosure provides polymerization activator compounds which may be prepared in, and which are soluble in aliphatic hydrocarbon and alicyclic hydrocarbon solvents.

Abstract: Provided are crystals of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, compositions comprising the same, and methods of making and using such crystals.

Abstract: Provided are an organometallic compound, an organic light-emitting device including the organometallic compound represented by Formula 1, and an organic light-emitting apparatus including the organic light-emitting device. The organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, the organic layer including an emission layer and at least one of the organometallic compound represented by Formula 1.

Abstract: High-potential photo-oxidants are provided with a supermolecule structure at least including a conjugated macrocycle linked to a metal complex. The conjugated macrocycle is electron-accepting relative to hydrogen or bears electron withdrawing substituents such as fluoroalkyl, fluoroaryl, fluoro, halo, cyano, or nitro. The metal complex is also electron-accepting relative to hydrogen or bears electron withdrawing substituents such as fluoroalkyl, fluoroaryl, fluoro, halo, cyano, or nitro. The linker can be thynyl, vinyl, thiophenyl, diethynylaryl, divinylaryl, diethynyl(unsaturated heterocycloalkenyl), divinyl(unsaturated heterocycloalkenyl), diethynyl(unsaturated heterocycloalkynyl), or divynyl(unsaturated heterocycloalkynyl). A specific implementation is an ethyne-bridged eDef-Rutpy-(porphinato)Zn(II) (eDef-RuPZn) supermolecule.

Abstract: A family of platinum(II) complex with mixed ligands as anticancer agents. The platinum(II) ion is coordinated to dicyclopentadiene and dithiocarbamate ligands. Also described are a pharmaceutical composition incorporating the platinum(II) complex, a methods of synthesizing the platinum(II) complex, and a method of treating cancer. The platinum(II) complexes exhibit potent cytotoxicity against lung and cervical cancer cell lines as well as low nephrotoxicity.

Abstract: The present invention relates to the preparation of novel nickel complexes containing iminopyrrolyl-type ligands, having the general molecular structure (I), and to their use as active catalysts in the polymerisation reaction of ethylene to hyperbranched polyethylene. The structure of the ligand precursor is such that it allows the occurrence of a cyclometallation reaction by the activation of a C—H bond, in the coordination reaction to the metal centre, generating a C,N,N?-tridentate complex.

Abstract: The present invention provides carbohydrate-based surfactants and methods for producing the same. Methods for producing carbohydrate-based surfactants include using a glycosylation promoter to link a carbohydrate or its derivative to a hydrophobic compound.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention relates a process for the recovery of one or more steviol glycosides from a steviol glycoside-containing fermentation broth, which method comprises (a) providing a fermentation broth comprising one or more steviol glycosides and one or more non-steviol glycoside components; (b) separating the liquid phase of the broth from the solid phase of the broth; (c) providing an adsorbent resin; (d) contacting the liquid phase of the broth with the adsorbent resin in order to separate at least a portion of the one or more steviol glycosides from the non-steviol glycoside components, thereby to recover one or more steviol glycosides from the fermentation broth containing one or more steviol glycosides. The invention also relates to a purified steviol glycoside composition prepared using such a process.

Abstract: Disclosed herein is a modular composition comprising 1) an oligonucleotide; 2) one or more tetraGalNAc ligands of Formula (I), which may be the same or different; optionally, 3) one or more linkers, which may be the same or different; 4) one or more peptides independently selected from Table 3, which may be the same or different; and optionally, 5) one or more targeting ligands, solubilizing agents, pharmacokinetics enhancing agents, lipids, and/or masking agents.

Abstract: The disclosed invention relates to the novel composition of matter that allows for the controlled release of highly active compounds to be delivered to a desired site. This novel composition utilizes the immune system to allow for the controlled release of desired compounds. The present invention can utilize a plurality of highly active compounds, with one embodiment being the use of chemotherapeutics for the treatment of cancer.

Abstract: An icariside compound as shown in Formula I wherein the compound is a natural chemical component in the traditional Chinese herbal epimedium or a chemically modified or a totally synthetic product based on the natural component. The compound can be used for preparing pharmaceuticals, health care products, cosmetic and skin care products and the like for improvement of immunity in a human body.

Abstract: Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3? or C4? modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

Abstract: The present invention provides methods, compositions, mixtures and kits utilizing deoxynucleoside triphosphates comprising a 3?-O position capped by a group comprising methylenedisulfide as a cleavable protecting group and a detectable label reversibly connected to the nucleobase of said deoxynucleoside. Such compounds provide new possibilities for future sequencing technologies, including but not limited to Sequencing by Synthesis.

Abstract: This invention claims processes that append a single nucleotide having a 3?-ONH2 moiety to the 3?-ends of an oligonucleotide primer using 3?-deoxynucleoside triphosphates that have, instead of a 3?-OH moiety, a 3?-ONH2 moiety, where the nucleotides contain both standard and non-standard nucleobases, and where as a key claim limitation, substantially no hydroxylamine is present in the solutions used in the claimed processes.

Abstract: A class of phosphorus containing polycyclic compounds of general formula I, of general formula I? or of general formula I?, wherein B1, B2, R1, R2, R1?, X1, X2, Y1, Y2, BL1, BL2, Z1, and Z2 are defined herein, that may be useful as modulators of type I interferon production, specifically as STING modulating agents, are provided. Also, provided are use of such compounds.

Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to novel intermediates useful for the preparation of DCA and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBARI mediated diseases.