Abstract: The present application belongs to the technical field of proteolysis-targeting chimeras (PROTACs), and discloses a PROTAC molecule and a preparation method and use thereof. A ligand for a target protein in the PROTAC molecule of the present application is a pyridine carboxylic acid-1-oxide derivative. In cell and zebrafish experiments, the PROTAC molecule exhibits no toxic and side effects at a drug concentration allowing a desired effect. At a cellular level, an inhibition level of the PROTAC molecule for human tyrosinase (TYR) reaches less than or equal to 1 ?mol/L. The PROTAC molecule in the present application can significantly reduce the generation of melanin by degrading TYR, and has excellent solubility, safety, and efficacy and a low effective concentration.

Abstract: The present invention provides a method for safe and efficacious administration of esketamine.

Abstract: The compound of formula (1a) wherein p is 1 or 2, R1-R4 are hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

Abstract: The present invention relates to methods of treating schizophrenia using a combination of aripiprazole, aripiprazole lauroxil, and a nanoparticle dispersion of aripiprazole lauroxil.

Abstract: Provided herein are methods of treating cancer in a subject, wherein the cancer is extrachromosomal DNA-positive (ecDNA-positive) or therapeutically resistant, the method comprising administering to the subject a therapeutically effective amount of a replication stress (RS) pathway agent alone or in combination with a targeted therapeutic.

Abstract: Provided are crystalline forms of acid addition salts of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)furo[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide, and a pharmaceutical composition including the same. The crystalline forms may be easily used in preparing the pharmaceutical composition including the same as an active ingredient.

Abstract: A quaternary ammonium salt compound of formula I is fast-acting and has a long-term local anaesthetic effect after a single administration, the sensory nerve block time being longer than the motor nerve block time, has both a long-acting local anaesthetic effect and a selective local anaesthetic effect, and also significantly reduces the side effects of quaternary ammonium salt compounds with the structural features of surfactants and is highly safe; thus, the compound of formula I and the pharmaceutically acceptable salt thereof can be used for the preparation of saft drugs having a long-term local anaesthetic effect and a selective local anaesthetic effect

Abstract: The present invention relates to stable pharmaceutical compositions comprising apixaban or its pharmaceutically acceptable salts thereof. The present invention further relates to a capsule composition comprising a therapeutically effective amount of apixaban solubilized or dispersed in a pharmaceutically acceptable carrier, wherein the therapeutically effective amount of apixaban ranges from about 0.5 mg/unit dosage form to about 50 mg/unit dosage form. The present invention also provides manufacturing processes thereof and use of the said compositions for prevention, treatment or prophylaxis of disorders in human patients in need thereof.

Abstract: The present invention relates to compounds of formula (I) that have the ability to inhibit CD151.

Abstract: The current methods and compositions provide for a novel therapeutic method for treating patients diagnosed with melanoma, especially those that have become resistant to certain other therapies. Accordingly, certain aspects of the disclosure relate to a method for treating melanoma in a subject, the method comprising administering a composition comprising a ferroptosis-inducing agent or other dedifferentiated melanoma-targeting agent to the subject.

Abstract: The present application relates to treating and/or preventing breast cancer, including locally advanced or metastatic, ER+, HER2? breast cancer, in a subject in need of treatment, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, isotopic derivative, or prodrug thereof, wherein R1, R2, R3, R4, m, and n are defined herein.

Abstract: The present disclosure provides compounds and pharmaceutically acceptable salt thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

Abstract: The present invention relates to chemical compounds which can be used in particular as structural mimetics of proline-rich peptides. The compounds of the present invention are capable of selectively inhibiting Ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of these compounds as pharmaceutical agents and the use of the pharmaceutical agents for the treatment of tumor diseases.

Abstract: The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (ROR?) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of ROR?-mediated diseases or disorders.

Abstract: The present invention provides novel pharmaceutical formulations comprising derivatives of NDGA, including M4N (tetra-0-methyl nordihydroguaiaretic acid) and temozolomide and their use in the inhibition and treatment of neoplastic diseases, including glioblastoma multiforme, lung and other cancers.

Abstract: The present invention relates to a process for producing a sterile liquid pharmaceutical composition suitable for administration by inhalation comprising ensifentrine particles, wherein the process comprises: (a) heating ensifentrine particles at a temperature of from 100° C. to 220° C. to obtain sterile ensifentrine particles; and (b) combining the sterile ensifentrine particles with a sterile liquid vehicle to produce the sterile liquid pharmaceutical composition suitable for administration by inhalation. A process for producing an ampule comprising the sterile liquid pharmaceutical composition is also described.

Abstract: The discovery of mutant or fusion kinases that drive oncogenesis, and the subsequent approval of specific inhibitors for these enzymes, has been instrumental in the management of some cancers. However, acquired resistance remains a significant problem in the clinic, limiting the long-term effectiveness of most of these drugs. Herein is demonstrated a strategy to overcome this resistance through drug-induced MEK cleavage (via direct procaspase-3 activation) combined with targeted kinase inhibition. This combination effect is shown to be general across diverse tumor histologies (melanoma, lung cancer, and leukemia) and driver mutations (mutant BRAF or EGFR, fusion kinases EML4-ALK and BCR-ABL). Caspase-3-mediated degradation of MEK kinases results in sustained pathway inhibition and substantially delayed or eliminated resistance in cancer cells in a manner superior to combinations with MEK inhibitors.

Abstract: The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

Abstract: Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis.

Abstract: Compositions and methods for treating multiple myeloma (MM), acute myeloid lymphoma (AML) or a myeloproliferative disease (MPD) in a human patient in need thereof. The methods entail administering to the patient an effective amount of cerdulatinib.