Abstract: The present disclosure relates to spiro-fused tetrahydroquinazoline compounds, to the compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP/TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to a method for the prevention or treatment of diseases comprising the use of the compounds. The present disclosure furthermore relates to pharmaceutical compositions or combination preparations of the compounds as well as to compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of YAP/TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to processes for the preparation of compounds.

Abstract: Provided herein are methods for treating cancer comprising administering to a subject in need thereof an adamantane derivative, or a pharmaceutically acceptable salt thereof, such as rimantadine or amantadine. In some embodiments, the adamantane derivative is PEGylated.

Abstract: Provided is a quinoline derivative having indoleamine-2,3-dioxygenase inhibitory activity, specifically, provided is a compound of general Formula (I) or pharmaceutically acceptable salt thereof, its pharmaceutical composition, preparation method and use in the manufacture of a medicament for immunomodulating and preventing and/or treating of a disease associated with IDO expression abnormality and/or tryptophan metabolism abnormality. Also provided is use of a combination medication of the quinoline derivative and HDAC inhibitor and its use in the manufacture of an anti-tumor drug.

Abstract: The present disclosure relates to chemical compounds that modulate pantothenate kinase (PanK) activity for the treatment of metabolic disorders (such as diabetes mellitus type II), neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment.

Abstract: The present disclosure relates to the field of medicinal chemistry, and specifically to brefeldin A derivatives represent by Formula (I) and its use in the inhibition of tumor proliferation activity. The new compounds provided herein are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, lung cancer, Bart's esophageal cancer, gastric cancer, cervical cancer, pancreatic cancer, kidney cancer, endometrial cancer, nasopharyngeal cancer, bone cancer, lymphoma, brain cancer, nerve cancer, oral cancer and colorectal cancer, and have the potential to be developed as novel antitumor agents.

Abstract: The invention involves a novel method of converting atrial fibrillation (AF) or atrial flutter (AFL) in a patient presenting with highly symptomatic AF or AFL by administering at least a loading dose of dofetilide intravenously, or if that fails cardioversion and a maintenance infusion followed by a switch to chronic oral dosing.

Abstract: The disclosure provides pharmaceutical formulations comprising d4-domperidone of the formula (I): (I) or a pharmaceutically acceptable salt thereof. The formulations also contain (i) a glyceryl stearate, and a medium chain triglyceride; or (ii) a stearoyl polyoxyl glyceride, a nonionic poly(ethylene oxide) polymer, and a medium chain triglyceride; or (iii) a nonionic poly(ethylene oxide) polymer, and a polyethylene glycol. The disclosure also provides methods for treating a disorder that is gastroparesis, nausea apart from gastroparesis, vomiting apart from gastroparesis, nausea associated with gastroparesis, vomiting associated with gastroparesis, gastroesophageal reflux disease, insufficient lactation, or a combination thereof in a patient, comprising administering to the patient a formulation described herein. In some aspects, the disorder is gastroparesis. In other aspects, the disorder is gastroesophageal reflux disease. In further aspects, the disorder is insufficient lactation.

Abstract: The present invention relates to a PD-L1 immunomodulator, and specifically discloses a compound of formula (I) as a PD-L1 immunomodulator, a pharmaceutically acceptable salt or an isomer thereof.

Abstract: The present invention relates to compounds of Table 1, which are encompassed by Formula I and/or Formula II, Ill, IV, V, or VI, and pharmaceutically acceptable salts, solvates or compositions thereof. Compounds of Table 1 are PCSK9 interacting small molecules that modulate PCSK9 activity and significantly increase low density lipoprotein receptor expression and activity, lower total circulating cholesterol and are useful for treating and delaying the onset of diseases that are associated with elevated cholesterol.

Abstract: The present invention relates to compounds binding to calreticulin which selectively inhibit growth of CALR mutant cells and/or exhibit selective cytotoxicity towards CALR mutant cells, to pharmaceutical compositions comprising such compounds as well as to their use in treating diseases or conditions caused by or associated with a mutation of CALR, in particular myeloid malignancies, such as myeloproliferative neoplasms or myelodysplasia syndrome. The present invention also relates to screening assays allowing the identification of such compounds.

Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of a Retroviridae infection, including an HIV infection.

Abstract: The present disclosure relates to solid state forms of Tafamidis and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof.

Abstract: The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular to modulate CFTR protein or ABC protein activities.

Abstract: Compounds of the invention, such as compounds of formula (I): where R, R1, R2, R3, R4, R5, R6, and R7 are defined herein, are useful for treating cancer, autoimmune disorders, and/or skin dermatitis, and/or methods for increasing peripheral blood counts and/or improving immune system function. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: Disclosed are assays for screening active compounds interfering with interaction between chitinase-like protein YKL-40 and chitin oligomers, as well as interfering with interaction between chitinase-like protein YKL-40 and heparan sulfate. Moreover, disclosed are active compounds identified by these assays as inhibitors of chitinase-like protein YKL-40, their therapeutic applications, and their use in biosensors measuring the level of chitinase-like protein YKL-40 in biological samples.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein one of X and Y is O and the other one is N; R1 is selected from halogen, CN, NH(CH3), N(CH3)2, C1-C4 alkoxy wherein the alkyl moiety of the C1-C4 alkoxy is optionally substituted by 1-3 halogens, and C1-C4 alkyl, wherein the C1-C4 alkyl is optionally substituted by 1-3 halogens, CN, NH(CH3), or N(CH3)2; and R2 is 3,4-dimethoxyphenyl or 1,3-dimethyl-1H-indazol-5-yl.

Abstract: Provided are a benzidine compound and an application thereof, the benzidine compound having the structure as shown in formula I below. Further provided are a pharmaceutically acceptable salt, isomer, racemate, prodrug co-crystal complex, hydrate, and solvate of the compound, as well as an application thereof in the preparation of a drug for the treatment or prevention of ROR?-regulated diseases; more importantly, such a compound can also be used in the preparation of a drug for the treatment of inflammation, immune diseases, cancer and neurological diseases.

Abstract: Disclosed herein is an imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as a TLR7 agonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as TLR7 agonist.

Abstract: The present disclosure provides a pharmaceutical composition of fused tricyclic gamma-amino acid derivatives and the use thereof. The pharmaceutical composition includes: (i) a compound having a structure represented by formula (I) or a pharmaceutically acceptable salt thereof, as an active material, in an amount of 1% to 45% by weight; (ii) optionally one or more fillers in an amount of 50% to 95% by weight; (iii) optionally one or more lubricating agents in an amount of 0.1% to 5.

Abstract: The present invention relates to a composition of disease-modifying antirheumatic drugs (DMARDs) for treatment of auto-immune diseases. More particularly, the invention relates to the microemulsion based emulgel composition of DMARD-leflunomide or its derivatives for treatment of auto-immune diseases such as rheumatoid arthritis, atopic dermatitis, psoriasis and skin cancer such as melanoma, squamous cell carcinoma. The invention also discloses a method for preparation of microemulsion based emulgel composition with improved physicochemical, pharmacokinetic properties of leflunomide to be used in pharmaceutical compositions. This invention discloses the delivery of leflunomide across human skin for the treatment of autoimmune and oncological conditions. The unique delivery of leflunomide in the form of microemulsion based emulgel composition is disclosed.