Abstract: Described herein are methods for the continuous preparation of 1,2-di(furan-2-yl)ethane-1,2-diol from furan-2-carbaldehyde. The methods can proceed chemically or electrochemically. In certain examples, the methods further comprise the application of a static mixer. The present methods produce 1,2-di(furan-2-yl)ethane-1,2-diol in greater yield, purity, chemoselectivity, and stereoselectivity than traditional batch methods.

Abstract: The present disclosures are directed to processes for synthesizing (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide (“nirogacestat”).

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases comprising a diterpene, or a pharmaceutically acceptable salt thereof. Specifically, the diterpene of the present invention can prevent or treat neurodegenerative diseases caused by inhibition of Nurr1 activity by activating Nurr1 and inhibiting the inflammatory response.

Abstract: The invention discloses herein related to synergistic combination of exogenous bioactives for activating intracellular secondary messenger (cAMP) signalling pathway. Particularly, the invention relates to synergistic compositions comprising combination of therapeutically effective amount of (3R)-3-acetyloxy-4-(trimethylazaniumyl) butanoate and N-4-aminobutylguanidine and salts thereof present in a weight ratio of 1:0.01 to 1:2 along with pharmaceutically acceptable excipients. Furthermore, the composition is useful for treating disease conditions or disorders related to depletion of secondary messenger pathway. The present invention further provides method of treating disease conditions related mental illness or disorder.

Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated ?-ionyl derivatives. Photomediated disruption of the extended ?-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.

Abstract: Provided is a method for administering a corticosteroid to a patient in need thereof, comprising: determining a target threshold for the ratio of urinary (tetrahydrocortisol+allotetrahydrocortisol) to urinary tetrahydrocortisone for the patient; and administering an HSD1 inhibitor to the patient. Also provided is a method for reducing or preventing the side effects associated with corticosteroid administration to a patient in need thereof, comprising: determining a target threshold for the ratio of urinary (tetrahydrocortisol+allotetrahydrocortisol) to urinary tetrahydrocortisone for the patient; and administering an HSD1 inhibitor to the patient.

Abstract: The present invention relates to new compounds that are useful in the prevention or treatment of respiratory diseases, such as asthma, acute and chronic inflammatory conditions, and fibrotic diseases or conditions in which fibrosis contributes to the pathology of the condition. The invention also relates to the preparation of the compounds, and to compositions including the compounds. The present invention also relates to the use of the compounds, as well as compositions including the compounds, in treating or preventing respiratory diseases, acute and chronic inflammatory conditions, and fibrotic diseases or conditions in which fibrosis contributes to the pathology of the condition.

Abstract: A cholinesterase inhibitor polymorph, wherein specifically disclosed are a octahydroaminoacridine succinate polymorph, a corresponding crystal composition and pharmaceutical composition, and applications thereof. The compound octahydroaminoacridine succinate is used for screening and studying polymorphs, and the discovered polymorphs are appraised and evaluated; crystal forms having better physical and chemical properties are determined for subsequent development and study, and crystal forms having good stability and an excellent therapeutic effect are obtained.

Abstract: An object of the invention is to provide a crystal of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide which is excellent in stability and preferable from the viewpoint of manufacturing and formulation. The present invention provides a crystal having an X-ray powder diffraction spectrum having characteristic peaks at diffraction angles (2?±0.2°) of 6.0°, 7.7°, 8.9°, 10.6°, 12.1°, 13.1°, 14.0°, 14.7°, 15.5°, 15.8°, 16.8°, 17.7°, 18.1°, 18.4°, 19.4°, 23.4°, 24.1°, 24.7°, 25.1° and 25.7°.

Abstract: Solid forms comprising 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl] amino-1,3,5-triazin-2-yl)amino]propan-2-ol, compositions comprising the solid forms, methods of making the solid forms and methods of using the solid forms are disclosed.

Abstract: The invention relates to the field of medicine and to the chemical and pharmacological industry, and concerns medicaments for the treatment of breast cancer. In particular the invention relates to a use of 3-O-sulfamoyloxy-7?-methyl-D-homo-6-oxaestra-1,3,5 (10),8(9)-tetraen-17a-one as an anti-cancer agent in monotherapy and adjuvant therapy of breast cancer, including the triple negative breast cancer.

Abstract: Described is a stable buffered aqueous colchicine solution or suspension being free of benzyl alcohol, comprising colchicine, a water miscible solvent and a preservative, characterized in that the solution comprises 0.01-1.0 w/v % colchicine, 2.5-15.0 w/v % glycerol and 0.05-1 w/v % preservative, the pH of the solution or suspension being 4.5-7.0. A method for the preparation thereof is also disclosed.

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

Abstract: The present invention provides a compound represented by formula (I) wherein symbols in the formula are as defined in the specification.

Abstract: The present invention relates to a novel 4-carbonylamino-4-phenylpyrimidine compound or a pharmaceutically acceptable salt thereof. Specifically, the present invention relates to a novel 4-carbonylamino-4-phenylpyrimidine compound or a pharmaceutically acceptable salt thereof, which exhibits GDH activity and as such, is effective for prevention or treatment of obesity, diabetes, or fatty liver.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful in therapy, e.g. for the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase 4 or 2 (Nox4 or Nox2) activity. A pharmaceutical composition comprising the compound.

Abstract: This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedys disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

Abstract: Provided herein are compositions and methods for mechanochemical dynamic therapy.

Abstract: The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Abstract: Provided herein are pharmaceutical compositions comprising an MDM2 inhibitor and one or more anti-cancer agents for preventing and/or treating diseases, such as cancer. Methods for preventing and/or treating diseases, such as cancer, comprising administering to the patient in need thereof with the pharmaceutical compositions are also provided.