Abstract: It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Described herein are catalytic hydrogenation and the use of ruthenium complexes having a bidentate diphosphine ligand or two monodentate phosphine ligands, two carboxylate ligands, and optionally a diamine ligand in hydrogenation processes for the reduction of imines into the corresponding amines.

Abstract: A method of producing a cannabinoid nanoparticle carrier composition for administration to a human, including the steps of incorporating non-ionic surfactants with cannabinoid oils and lipids; inducing sonication for a predetermined period of time at a predetermined amplification with a ultrasonic liquid processor until completely integrated; dissolving ascorbic acid into a carrier fluid; combining in sequence the non-ionic surfactants, lipids, and cannabinoids with a carrier fluid consisting of distilled water and ascorbic acid; sonicating using an ultrasonic liquid processor at predetermined amplitude for a predetermined period of time at a controlled temperature.

Abstract: A method for producing a nitroso compound of the following formula (3), comprising reacting a compound of the following formula (1) with a compound of the following formula (2) by using a tertiary alcohol and a base. wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently a hydrogen atom, a halogen atom, a (C1-C4) alkyl, or a (C1-C4) alkoxy.

Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard.

Abstract: The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, R1, R2, R3, R4, R5, R6 and Q 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, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

Abstract: This disclosure generally relates to therapeutic conjugates that covalently bind to a biological target. Methods of administering the compositions to a subject in need thereof are also provided herein.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: The present invention relates to a derivative compound in which a biphenyl group is introduced into an aminoalkanoic acid, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits excellent antifungal and fungicidal effects. Furthermore, the compound of the present invention exhibits a synergistic effect when used in combination with a conventional antifungal agent. Furthermore, the compound of the present invention provides broad-spectrum antifungal activity against a wide range of fungal pathogens. Therefore, the compound of the present invention may be widely used in fields requiring treatment with antifungal or fungicidal agents against human pathogenic fungi and animal pathogenic fungi, and phytopathogenic fungi.

Abstract: Subject-matter of the present invention are novel 3-ketocoumarins, a process for their preparation and their use as photoinitiators in photopolymerization reactions, advantageously in photopolymerization reactions for inkjet printing inks. The invention also concerns a process for the photopolymerization of compositions also comprising said 3-ketocoumarins.

Abstract: Compounds, compositions, methods, and uses are described for therapeutic deuterated N,N-dimethyltryptamine compounds (e.g., a single compound or a plurality of deuterated N,N-dimethyltryptamine compounds) such as N,N-dimethyltryptamine compounds, ?-protio, ?-deutero-N,N-dimethyltryptamine compounds, ?,?-dideutero-N,N-dimethyltryptamine compounds, and pharmaceutically acceptable salts of these compounds. The deuterated N,N-dimethyltryptamine compound may have an increased half-life compared with the half-life of undeuterated N,N-dimethyltryptamine. For example, a deuterated N,N-dimethyltryptamine compound may be used in therapy and have a Formula (I): wherein: the ratio of deuterium:protium in the compound is greater than that found naturally in hydrogen; each R1 is independently selected from H and D; R2 is selected from CH3 and CD3; R3 is selected from CH3 and CD3; each yH is independently selected from H and D, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel organic dinitroxide biradical compounds and their use as polarizing agents, in particular, in the techniques of Nuclear Magnetic Resonance (NMR) of solids or liquid samples and medical imaging.

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity such as cancer.

Abstract: Described herein are crystalline forms of pharmaceutically acceptable salts of the lysyl oxidase-like 2 (LOXL2) inhibitor (3-(4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone. Also described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 inhibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.

Abstract: Psoralen compounds of compounds having formulae 1A-10A, 1B-10B, 1C-10C, 1D-10D, 1E-10E, 1F-10F, 1G-10G, and 1H-5H as shown in FIG. 1, and pharmaceutically acceptable salts thereof; and their use in methods for the treatment of a cell proliferation disorder in a subject, pharmaceutical compositions containing the psoralen derivatives, a kit for performing the method, and a method for causing an autovaccine effect in a subject using the method.

Abstract: A process for producing a compound of the formula (I) involves at least reacting a compound of the formula (II) with hydrogen and water in the presence of at least one homogeneous transition metal catalyst TMC 1.

Abstract: The present invention relates to pharmaceutical compositions comprising Lenalidomide. More particularly, the present invention relates to a stable composition comprising anhydrous Lenalidomide Form I and one or more pharmaceutically acceptable excipients and process for preparing such compositions.