Abstract: Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.

Abstract: The present invention generally relates to novel pharmaceutical formulations containing 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide, methods of preparation thereof and their use in medical therapy.

Abstract: Disclosed are compounds of Formula 1, N-oxides of the compounds and salts of the compounds and N-oxides: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, J, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of such a compound, N-oxide, salt or composition.

Abstract: Provided are a compound for the prevention and treatment of diseases associated with PD-L1, a preparation method therefor and use thereof. Specifically, provided are the compound of formula I, the stereoisomer and the racemate thereof, or pharmaceutically acceptable salts thereof, and also provided is an application thereof in the preparation of a drug for the prevention and treatment of diseases associated with PD-L1.

Abstract: This disclosure provides methods and pharmaceutical compositions for reducing or eliminating cardiotoxicity, particularly cardiotoxicity induced by a cancer treatment or other therapy. In some cases, the methods and compositions prevent or reduce cardiotoxicity caused by anthracycline treatment. The methods provided herein often comprise administering a protective agent such as myricetin, tricetin, robinetin, ficetin, vitexin, quercetin, dihydrorobinetin, kaempferol, 7,3?,4?,5?-tetrahydroxyflavone, and myricitrin in conjunction with the administration of a cancer drug or other treatment. They may comprise administering a protective agent in combination with dexrazoxane. The compositions provided herein include co-formulations of a protective agent with a different protective agent or with a cancer treatment (e.g., anthracycline drug).

Abstract: Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migration, and/or in treating cancer, are provided herein. The compounds are collectively represented by Formulae Ia or Ib: wherein A, B, D, E, G and R1-R5 are as defined in the specification, with one or more of D, E and G, preferably E, is hydroxy.

Abstract: The present invention provides a new production method for a chlorobenzene compound. Specifically, the present invention provides a production method in which the compound represented by formula (1) (in the formula, X1 represents a halogen atom) and chlorine are reacted in the presence of a Brønsted acid, thereby obtaining the chlorobenzene compound represented by formula (2) (in the formula, X1 represents the same as above).

Abstract: Compounds of formula (1): wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

Abstract: Described herein are crystalline forms of 4-[(3S)-3-aminopyrrolidin-1-yl]-6-cyano-5-(3,5-difluorophenyl)-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyridine-3-carboxamide, uses of such crystalline forms in the preparation of pharmaceutical compositions for the treatment of diseases or conditions that would benefit by administration with a somatostatin modulator compound.

Abstract: A method of treating severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), otherwise known as COVID-19, infection by administering nicotinic receptor antagonists and/or PPAR-? agonists is presented. A combination of mecamylamine, or an isomer thereof, and pioglitazone synergistically reduces replication of SARS-CoV-2 in virus-infected cells and also synergistically reduces inflammatory cytokines such as IL-6, IL-?, and TNF?, which have been associated with SARS-CoV-2 infection.

Abstract: Disclosed is a compound of formula (I) and a stereoisomer thereof: wherein R1, R2, R3 and R4 are as defined in the present disclosure.

Abstract: The present invention generally relates to novel pharmaceutical formulations containing 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide, methods of preparation thereof and their use in medical therapy.

Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.

Abstract: The present invention provides an effective production method for a pyridone compound. More specifically, the present invention provides a production method comprising: a step of reacting the compound represented by formula (1) (in the formula, X1 and X2 each independently represent a halogen atom, R1 represents a hydrogen atom, an amino group, or a group represented by NHCOR2, and R2 represents a C1-C5 alkyl group) with 4 to 10 times by mass, with respect to the compound represented by formula (1), of the compound represented by formula (2) (in the formula, R2 represents the same as described previously), in the presence of at least one of a tri(C1-C8 alkyl)amine and an alkali metal acetate, at a temperature of 100° C.

Abstract: Methods for reducing the oxidative effects of free radicals in an animal subject are described herein. Resveratrol, ellagic acid, and quercetin can be administered as a single composition to the animal subject, wherein the mass ratio of resveratrol, ellagic acid, and quercetin in the composition is 1:4:20.

Abstract: In one aspect, compounds and compositions that inhibit TXNIP expression and/or that lower hepatic glucose production and methods of identifying, making, and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with elevated TXNIP and/or elevated glucagon levels such as, for example, diabetes and associated disorders. Further provided are methods for treating hyperlipidemia or fatty liver disease, optionally associated with elevated TXNIP and/or elevated glucagon levels. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: A crystal form (such as formula I) of a 2-methyl-2-propanol and amino-substituted aryl compound and a preparation method therefor. Also provided is an application of the crystal form in the preparation of a medicine for treating related diseases.

Abstract: An efficient and commercial phosphorylation process of a complex alcohol, such as secondary and tertiary alcohols, with P4O10 at high temperatures, and a product obtained by the process.

Abstract: A thermal acid generator having a high acid generation temperature, and a resist composition using the same.

Abstract: The disclosure is directed to, in part, compounds, or pharmaceutically acceptable salts or solvates thereof, for modulating the activity of aldehyde dehydrogenase such as ALDH2 and/or methods for treating and/or preventing an alcohol related disorder such as alcohol use disorder, alcohol induced disorder, alcohol abuse, alcohol dependence, alcohol intoxication, alcohol withdrawal, and the like and/or methods for reducing the amount of alcohol consumed, reducing alcoholic cravings, or increasing the percentage of no heavy drinking days for a subject with alcohol use disorder.