Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: The present invention discloses a method for analysis of drug resistance of tumor cells. The method includes the steps of: (a) providing silicon dioxide nanoparticles, polystyrene-co-polyacrylic acid nanoparticles or metal-organic framework nanoparticles; (b) co-incubating the silicon dioxide nanoparticles, the polystyrene-co-polyacrylic acid nanoparticles or the metal-organic framework nanoparticles with the tumor cells; and (c) detecting endocytosis of the silicon dioxide nanoparticles, the polystyrene-co-polyacrylic acid nanoparticles or the metal-organic framework nanoparticles by the tumor cells. The analysis method of the present invention can analytically identify drug-resistant tumor cells in a clear, intuitive and efficient way. The provided nanoparticles feature simple synthesis processes that take short periods of time, and after they are co-incubated with the tumor cells, a flow cytometer is used for detection.

Abstract: The present disclosure relates to a novel heterocyclic amine derivative represented by the following Chemical Formula 1 and a pharmaceutical composition comprising the same, and the compound according to the present disclosure can be usefully used for the prevention or treatment of autoimmune diseases or cancers. wherein, in Chemical Formula 1, R1, R2, X1, X2, L, Y, A and B are the same as defined in the specification.

Abstract: A nicotinamide adenine dinucleotide phosphate-dependent steroid dehydrogenase-like (NSDHL) inhibitor provided according to an aspect of the present invention can be used not only as an anticancer agent capable of overcoming resistance to EGFR-targeting anticancer agents, but also advantageously in the treatment of hyperlipidemia.

Abstract: A RET inhibitor, a pharmaceutical composition thereof and uses thereof including a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Furthermore, a pharmaceutical composition including the compound, and uses of the compound and pharmaceutical composition thereof in the manufacture of a medicament for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

Abstract: The present invention relates to novel 5-azaindazole derivatives of formula (I), as described and defined herein, and pharmaceutically acceptable salts, solvates and prodrug thereof, as well as pharmaceutical compositions comprising such compounds. The 5-azaindazole derivatives according to the invention have been found to be highly effective dual A2A/A2B adenosine receptor antagonists, and can thus be used as therapeutic agents, particularly in the treatment or prevention of hyperproliferative or infectious diseases or disorders.

Abstract: The disclosure provides methods, treatments and materials for treating diseases or disorders associated with the dopamine D1 receptor intracellular pathway. In particular, the present disclosure provides for methods of treating such diseases and disorders in combination with a dopamine replacement therapy.

Abstract: The invention provides 7-phenoxy-N-(3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds of the general formula (I) wherein R1, Ar, n and m are as described herein, compositions including the compounds, processes of manufacturing the compounds and the compounds for use in methods of medical treatment. The present compounds are as gamma-secretase modulators for the treatment of diseases associated with the deposition of ?-amyloid in the brain, such as Alzheimer's disease, cerebral amyloid angiopathy, cochlear synaptopathy, hearing loss, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 54 to 74; examples 1 to 64; table). An exemplary compound is e.g. (R)-7-(3,5-difluorophenoxy)-N-((1R,5S,8s)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.

Abstract: The present invention encompasses compounds of formula (1) wherein the groups R1, A, G, LK and t have the meanings given in the claims and specification, their use as degraders of SMARCA2 and/or SMARCA4, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.

Abstract: A pyrimidopyrazolone derivative as a Wee1 inhibitor and use thereof in preparation of a medicament for treating Wee1-related diseases are described. In particular, the present invention relates to a compound of formula (I), an isomer or a pharmaceutically acceptable salt thereof.

Abstract: A pharmaceutical composition contains chlorogenic acid and coumaroyl quinic acid. The combined use of chlorogenic acid and coumaroyl quinic acid at a certain ratio can generate a synergistic enhancing effect to effectively inhibit the growth of human kidney cancer cell strain A479, rat kidney cell strain RuCa, and rat transplanted tumor RuCa, providing a novel choice for clinical treatment of kidney cancer and having good market application prospects.

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

Abstract: The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein A, LG, n and m are as defined in the Summary of the Invention.

Abstract: A method involves dissolving a curcuminoid in glycerol to make an administrable solution. An alkali salt is added to the glycerol to increase the solubility of the curcuminoid in the glycerol to more than 20 milligrams curcuminoid per millilitre of glycerol (and up to in excess of 200 milligrams curcuminoid per millilitre of glycerol with the addition of sufficient alkali salt in embodiments). The resulting administrable solution can be administered (such as by way of intramuscular injection) as is without the need of an aqueous emulsion and can be stored for more titan 24 hours without curcuminoid precipitation.

Abstract: Apurinic/apuyrimidinic endonuclease 1/Redox Factor-1 (APE/Ref-1) inhibitors are provided along with methods of using the same. The inhibitor has the structure of Formula I: or a pharmaceutically acceptable salt thereof. n is an integer from 4 to 14, X and X? are each independently H or OH, and Y and Y? are each independently H or OH.

Abstract: A compound, having a structure represented by a formula (I), and prepared by one-pot synthesis of benzophenone hydrazone, 7-chloroisatin, and copper(II) acetate monohydrate, and refluxing in 100 mL of anhydrous methanol solvent for 48 hrs. A method for preparing the compound includes: collecting and placing 0.0235 g of benzophenone hydrazone, 0.6914 g of 7-chloroisatin, and 0.6720 g of copper(II) acetate monohydrate complex in a 100.0 mL flask; adding 50 mL of anhydrous methanol as a solvent; stirring a resulting mixture at room temperature for 48 hrs; performing column chromatography separation, and elution with petroleum ether/dichloromethane in a volume ratio of 1:1, and collecting final component points and naturally volatilizing the final component points to obtain 7(E)-chloro-3-diphenylmethylindolin-2-one crystals. The compound is used as a catalyst for reaction between benzophenone imine and trimethylsilonitrile, and has a catalytic effect with a conversion rate reaching 99%.

Abstract: Disclosed are phenyltetrazole derivatives of formula (I), wherein A, R1, R2, X, R?, R?, and n are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the phenyltetrazole derivatives for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.

Abstract: Synergistic drug combinations with the small molecule PAC-1 against uveal or cutaneous melanoma. There are no current targeted drug treatments for the mutations associated with uveal melanoma. Despite primary radiation or surgical therapy, up to 50% of patients eventually develop metastatic disease, for which there is no standard therapy nor treatment shown to improve overall survival. Drug combinations with PAC-1 allow the use of lower dosages of this compound that result in cancer cell death in uveal melanoma. Drug combinations of PAC-1 with the kinase inhibitor entrectinib have shown a synergistic effect against uveal melanoma cell lines. Specifically, PAC-1 and entrectinib are synergistic against wild-type and mutant uveal melanoma cell lines (e.g., GNAQ and GNA11).

Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.