Abstract: The present disclosure provides a compound and methods of preparing the compound. The compound has anti-microbial and anti-mite properties and can be bonded to materials such as fiber and synthetic polymer. The compound may also be used in a finishing agent for textiles, fibers, or yarns to protect these materials against microorganisms and mites. Additionally, when these materials are treated with a relatively low dosage of the compound, long-lasting and effective anti-mold and anti-mite effects may be achieved at a relatively low cost.

Abstract: The present technology relates to processes, mixtures and intermediates useful for making picolinamide fungicides. The picolinamide compounds are prepared by processes that include coupling together a 4-methoxy-3-acyloxypicolinic acid with key 2-amino-L-alaninate esters derived from substituted 2-phenylethanols.

Abstract: Provided are methods of preparing cannabinoids and cannabinoid derivatives and compositions containing the cannabinoids and derivatives.

Abstract: A process for chiral separation of ethyl 3-amino-1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]pyrazole-4-carboxylate (VI) from the racemic mixture of ethyl 3-amino-1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]pyrazole-4-carboxylate and ethyl 3-amino-1-[(3S,4R)-4-cyanotetrahydropyran-3-yl]pyrazole-4-carboxylate (V).

Abstract: The present invention relates to a composition of a CD47-SIRP? blocking agent and one or more anti-cancer agent(s), where the CD47-SIRP? blocking agents are represented by a compound of formula (I). The present invention also relates to a method of treating a cancer in a subject by administering a therapeutically effective amount of a CD47-SIRP? blocking agent represented by formula (I) in combination with one or more anti-cancer agent(s).

Abstract: Disclosed herein are small molecule inhibitors of platelet function, and methods of using the small molecules to treat diseases, such as platelet hemostasis and thrombosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Abstract: A method of producing refined oils and/or fats whereby the content of, e.g., glycidol, can be reduced and reductions in the content of tocopherols can be inhibited, and a method for producing low-impurity tocopherols. The method includes a first distillation step of subjecting raw material oils and/or fats to thin film distillation under a first condition; a second distillation step of subjecting a first distillate fraction obtained after the first distillation step to thin film distillation under a second condition; a third distillation step of subjecting a second residual fraction obtained after the second distillation step to thin film distillation under a third condition; and a mixing step of obtaining a mixed oil by mixing a first residual fraction obtained after the first distillation step, with a third distillate fraction obtained after the third distillation step. The first, second, and third conditions include specified temperature conditions and pressure conditions.

Abstract: The present invention relates to a process according to Scheme 1 for the preparation of microbiocidal 5-trifluoromethyl-1,2,4-oxadiazole derivatives of formula (I) suitable for use, e.g., as active ingredients, which have microbiocidal activity, in particular, fungicidal activity.

Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.

Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.

Abstract: The present invention relates to a process for preparation of palbociclib, compound of formula (1) or a salt thereof, wherein an intermediate, compound (2), is formed by reacting a compound of formula (3) and a compound of formula (4) in a solvent mixture comprising methanol and butanol: The intermediate (2) can be transformed into palbociclib or a salt thereof.

Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.

Abstract: Described are methods of providing contraception in a woman having a BMI?30.0 kg/m2, comprising: selecting a woman determined to have a BMI?30.0 kg/m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg. Also described are methods of contraception that achieves a Pearl Index of <5 in women having a BMI?30.0 kg/m2, comprising: selecting a woman determined to have a BMI?30.0 kg/m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg, wherein the method comprises daily administration of the estetrol component and drospirenone on 24 consecutive days followed by a hormone-free period of 4 consecutive days.

Abstract: Described herein are isotopically enriched analogs of methylone (e.g., deuterated analogs of methylone (e.g., (S)-methylone and (R)-methylone) with improved characteristics. Also described herein are salts (such as hydrochloride salt) and solid forms (e.g., crystalline forms) of methylone. Also described herein are stereoisomers (e.g., enantiomers) of methylone. The present disclosure also provides methods of making and methods of use of the methylone or methylone analogs and solid forms of 3,4-methylenedioxy-N-ethylcathinone hydrochloride described herein to treat brain and neurological disorders such as depression.

Abstract: Provided are a process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib, an intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate, an intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate, and a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof.

Abstract: This disclosure provides methods for treating a hepatocellular carcinoma (e.g., unresectable HCC) with lenvatinib or a pharmaceutically acceptable salt thereof. Also encompassed by the disclosure are dosage regimens described herein of lenvatinib or a pharmaceutically acceptable salt thereof for use in treating hepatocellular carcinoma (e.g., unresectable hepatocellular carcinoma) according to any of the methods described herein. Particularly useful dosages and dose modifications upon the occurrence of an adverse event or events are also disclosed.

Abstract: The present disclosure relates to compounds of formula (I), which are suitable as AhR modulators, in particular AhR inhibitors. The disclosure also relates to compositions comprising said compounds and use of said compounds or compositions in treatment, in particular in the treatment of cancer. The disclosure further relates to methods of preparing said compounds.

Abstract: The present invention features pharmaceutical compositions including sepiapterin, or a pharmaceutically acceptable salt and/or co-crystal thereof, and methods for the treatment of tetrahydrobiopterin-related disorders (e.g., tetrahydrobiopterin deficiency or phenylketonuria) with such compositions.

Abstract: Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.

Abstract: The present disclosure relates to use of a protein kinase C (PKC) inhibitor in the treatment or prevention of proliferative diseases. The disclosure also relates to corresponding pharmaceutical formulations, uses, methods, combinations, and related disclosure embodiments. The disclosure further relates to use of a pharmaceutical combination comprising a PKC inhibitor and another therapeutic agent, such as an MDM2 inhibitor, in the treatment or prevention of a proliferative disease.