Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

Abstract: The present invention relates to a process for the preparation of pyridine derivatives of the formula (I) comprising two steps, namely, a selective chlorination followed by a selective fluorination.

Abstract: The present invention covers 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyri-dazine-4-carboxamide compounds of general formula (I): in which R1, R2, R4, R5, R6, X, Y and Z 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 cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

Abstract: An amide/iminium zwitterion catalyst has a catalyst pocket size that promotes transesterification and dehydrative esterification. The amide/iminium zwitterions are easily prepared by reacting aziridines with aminopyridines. The reaction can be applied a wide variety of esterification processes including the large-scale synthesis of biodiesel. The amide/iminium zwitterions allow the avoidance of strongly basic or acidic condition and avoidance of metal contamination in the products. Reactions are carried out at ambient or only modestly elevated temperatures. The amide/iminium zwitterion catalyst is easily recycled and reactions proceed in high to quantitative yields.

Abstract: There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of sarcomain a patient in need thereof.

Abstract: The present invention provides a dibutylfluorenyl derivative, an application of same as a photoinitiator, and a preparation method therefor. The present invention provides a photocuring composition including the compound and a photocuring method using the composition.

Abstract: Sustained-release abiraterone prodrug formulations, methods, and kits for parenteral administration to a subject having a sex hormone-dependent benign or malignant disorder such as prostate cancer, a syndrome due to androgen excess, and/or a syndrome due to glucocorticoid excess such as hypercortisolemia.

Abstract: The present disclosure provides compounds, pharmaceutical compositions, and methods for the treatment of cancer and fibrosis. The disclosed pharmaceutical compositions may include one or more pyrazolyl-containing compounds, or a derivative thereof.

Abstract: The present invention relates to a degenerative disease model Drosophila. More particularly, a technique is disclosed for alleviating the phenotypes of a degenerative disorder symptom of Drosophila. Using this technique, illumination with low dose radiation on a degenerative disease model Drosophila alleviates symptoms of the degenerative disease.

Abstract: The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent device having improved driving voltage and/or current efficiency characteristics can be provided by comprising the organic electroluminescent compound according to the present disclosure.

Abstract: Provided herein are modified amino acids comprising an azido group, polypeptides, antibodies and conjugates comprising the modified amino acids, and methods of producing the polypeptides, antibodies and conjugates comprising the modified amino acids. The polypeptides, antibodies and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.

Abstract: One embodiment of the disclosure is a compound represented by Formula I or a pharmaceutically acceptable salt thereof. The variables in Formula I are defined herein. Compounds of Formula I are selective MAP4K1 inhibitors, which can be used to treat a diseases or disorders in a subject that benefits from control of MAP4K1 activity.

Abstract: The disclosure provides cryptophycin intermediates, cryptophycin analogs, and cryptophycin chimeric molecules useful in treating cancer, as well as methods of producing these compounds and methods of treating cancer.

Abstract: A method for isolating cytisine from plant material includes dissolving the plant material in an alcohol to form a liquid mixture, acidifying the liquid mixture by addition of a mineral acid, and concentrating the liquid mixture to form a concentrated aqueous solution. The method also includes extracting the concentrated aqueous solution with a first extractant to form a purified aqueous concentrate, alkalizing the purified aqueous concentrate with an alkaloid to form an alkaline aqueous concentrate, and extracting the alkaline aqueous concentrate with a second extractant. The method further includes removing the second extractant to obtain cytisine.

Abstract: The present disclosure relates to compounds that bind to flavin-containing enzymes and inhibit mitochondrial function, referred to herein as mitoflavoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoflavoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoflavoscins to provide anti-aging benefits. Specific mitoflavoscin compounds are also disclosed.

Abstract: The present invention relates to herbicidally active pyridino-/pyrimidino-thiazole derivatives, as well as to processes and intermediates used for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, as well as to the use of such compounds and compositions in controlling undesirable plant growth: in particular the use in controlling weeds, in crops of useful plants.

Abstract: Compounds of formula (I), wherein A, R, W1, W2, W3, W4, W5, W6, L, Q, Rx and u have the meaning according to the claims, can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

Abstract: There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, ring A, m and n have meanings as provided in the description.

Abstract: Provided are a novel derivative of ?-apopicropodophyllin and a method of preparing the same, and more particularly, a compound represented by Formula 1 below, which is a novel derivative of ?-apopicropodophyllin derived from podophyllotoxin, which is an anticancer agent, a method of preparing the same, and a composition for treating cancer, which includes the compound. In Formula 1, R is a C2 to C10 alkyl group, a C2 to C10 alkyl group containing an allyl- or alkyne, a —[CH2]n—C3 to C8 cycloalkyl group, a substituted or unsubstituted —[CH2]n-phenyl group, a substituted or unsubstituted —[CH2]n—C5 to C6 heteroaromatic group, a —C(?O)—C1 to C8 alkyl group, a substituted or unsubstituted —C(?O)—[CH2]n-phenyl group, or a substituted or unsubstituted —C(?O)—[CH2]n—C5 to C6 heteroaromatic group, wherein n is an integer of 0 to 6.

Abstract: The present invention provides triazole carboxylic acids and related compounds, as well as pharmaceutically acceptable salts thereof, which are useful as glycolate oxidase inhibitors. Pharmaceutical compositions and methods for treating primary hyperoxaluria, type I (PH) and kidney stones are also described.