Abstract: The present invention relates to a novel crystalline compound of Siponimod Hemifumarate, to processes and to intermediates for its preparation, to pharmaceutical compositions containing it and to the use in therapy.

Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject, either individually or in combination with other CNS active agents.

Abstract: Compounds of formula (1): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (1) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

Abstract: The present invention describes compounds modulating the function of mitochondrial complex I (NADH-quinone oxidoreductase) having formula (I)

Abstract: Compounds and methods for treating insulin resistance, obesity, Type 2 diabetes, Nonalcoholic fatty liver disease (NAFLD), and peroxisome proliferator-activated receptor gamma (PPARy) serine 273 phosphorylation in subjects in need of such therapy.

Abstract: The present invention belongs to the field of pharmaceutical chemistry, and relates to an N-(benzoyl)-phenylalanine compound used as an ?4?7 integrin antagonist, including the pharmaceutical composition and the use, and in particular to a compound represented by general formula (1). The compound exhibits good ?4?7 integrin binding inhibitory activity, can be used as a high-efficiency ?4?7 integrin antagonist, and used for preventing and/or treating ?4?7 integrin-related diseases such as autoimmune diseases and inflammatory diseases.

Abstract: Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.

Abstract: A crystalline carbazole derivative, pharmaceutical compositions thereof, and methods of treatment are provided herein.

Abstract: Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R1-R8, X, Y, Z, X?, Y?, Z?, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

Abstract: The present invention relates to intermediates and processes useful for preparing 1-ethyl-N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)piperidine-4-sulfonamide and salts thereof. The present invention further relates to 1-ethyl-N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)piperidine-4-sulfonamide and salts thereof when prepared by such processes and to associated pharmaceutical compositions and uses for the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

Abstract: The present invention aims to provide a method for producing a (2S,5R)-5-(protected oxyamino)-piperidine-2-carboxylic acid derivative at a low cost that can be performed under mild reaction conditions not requiring a facility at an extremely low temperature, is safer, can control the quality of the desired product with ease, and shows good workability in the site of production. A method for producing a compound represented by the formula (2) wherein PG1 is an amino-protecting group, PG2 is an amino-protecting group, PG3 is a hydroxyl-protecting group, LG is a leaving group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), including a step of reacting a compound represented by the formula (1): wherein each symbol is as defined above, with a hydroxylamine derivative represented by the formula PG2NHOPG3 wherein each symbol is as defined above, in the presence of a base in a solvent.

Abstract: Compounds of Formula (I): wherein R1, R3, R11, R12, X, Y1, Y2, Y3, Y4 and are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring anti-apoptotic inhibitors.

Abstract: Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R1, R2, R3, R4, R5, X1, X2, and n are described herein. Also provided is a method of treating an estrogen-mediated disease requiring inhibition of estrogen receptor alpha (ER-alpha), such as cancer, in a subject or inhibiting ER-alpha in a cell with the compound of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

Abstract: The present invention provides a compound having the structure: wherein X1 is N or CR5, wherein R5 is H, OH, halogen or alkyl; X2, X3 and X4 are each independently NH, N, S, O or CR6, wherein each R6 is independently H, OH, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, haloalkyl, —O—(alkyl), —S—(alkyl), —NH2, —NH—(alkyl), —N(alkyl)2 or —CO2H; R1, R2, R3 and R4 are each independently —H, —F, —Cl, —Br, —I, —NO2, —CN, —CF3, —CF2H, —OCF3, -(alkyl), -(haloalkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(cycloalkyl), -(cycloalkylalkyl), -(heteroalkyl), heterocycle, heterocycloalkyl, -(alkylheteroalkyl), -(alkylaryl), —OH, —OAc, —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), (heteroaryl), —SH, —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), —S-(heteroaryl), —NH2, —NH-(alkyl), —NH-(alkenyl), —NH-(alkynyl), —NH-(aryl), —NH-(heteroaryl), —C(O)R7, —S(O)R7, —SO2R7, —NHSO2R7, —OC(O)R7, —SC(O)R7, —NHC(O)R7 or —NHC(S)R7, wherein R7 is, H, —(alkyl), —OH, —O(alkyl), —NH2, —NH(alkyl)

Abstract: Provided herein are heterocyclic compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting the growth of gram-negative bacteria. The subject compounds and compositions are useful for the treatment of bacterial infections, such as pneumonia.

Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.

Abstract: The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

Abstract: Provided are modulators of androgen receptor (AR) condensates, methods of modulating or inhibiting AR condensates, and methods of treating diseases and conditions using such modulators or inhibitors of AR condensates.

Abstract: The present invention relates to compounds of the Formula (I), in which X represents Cl or Br. According to the present invention, the compounds have anticholinesterase activity. The present invention also relates to pharmaceutical compositions containing the compounds of the present invention, and the application of the compounds of the present invention for the treatment of Alzheimer's disease.

Abstract: The present invention relates to diaminotriazine compounds and to their use as herbicides. It also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation.

Abstract: Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms.

Abstract: Monomers which contain a 4-thiazolidinone unit linked to a benzene nucleus and which contain a (meth)acrylate function are provided. A process for the synthesis of the monomers and the use thereof in the synthesis of polymers by the radical route is also provided.

Abstract: Provided herein are compounds having one or more cleavable disulfide moieties and one or more hydrophobic tail moieties (HTM) for delivery of one or more therapeutic or diagnostic agents. In some embodiments, the one or more therapeutic or diagnostic agents are biologics. In some embodiments, the one or more therapeutic or diagnostic agents are delivered to cancer cells.

Abstract: A method for maximizing the selectivity (S) of an epoxidation catalyst in an ethylene oxide reactor system, comprising: receiving a measured reactor selectivity (Smeas), a measured reactor temperature (Tmeas), and one or more operational parameters from an ethylene oxide production system, the measured reactor selectivity (Smeas), the measured reactor temperature (Tmeas), and the one or more operational parameters comprise real-time and historical operating data points over time generated by the ethylene oxide production system, and using a processor to conduct various calculations and determination in order to output an actionable recommendation that includes a target change (Mchange) of a moderator level (M) of a chloride-containing catalyst moderator to its optimal value (Mopt). The method further includes using the processor to (f) display the actionable recommendation on a display.

Abstract: The invention relates to processes for preparing benzoprostacyclin analogues and intermediates prepared from the process, and the benzoprostacyclin analogues prepared therefrom. The invention also relates to cyclopentenone intermediates in racemic or optically active form.

Abstract: An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group; A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.

Abstract: The invention provides compositions comprising a source of protein and a urolithin. The invention also provides uses and methods associated with, or making use of the compositions, such as a medicament, dietary supplement, functional food or medical food and in the treatment and/or prophylaxis of a muscle-related pathological condition. The invention also provides kits comprising urolithin and protein.

Abstract: Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.

Abstract: Provided is a compound represented by formula (I): or an N-oxide compound thereof, wherein the variable groups are as defined in the specification. Also provided is an arthropod pest control agent containing a compound represented by formula (I) and an inert carrier. The compound represented by formula (I) and arthropod pest control agent exhibit an excellent controlling effect against arthropod pests.

Abstract: Provided herein are uses of the compounds for the treatment of various indications, including prostate cancer and Kennedy's disease.

Abstract: Described herein are HSD17B13 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of liver disease, metabolic disease, or cardiovascular disease, such as NAFLD or NASH, or drug induced liver injury (DILI).

Abstract: The disclosure relates to allosteric modulators of ?2-adrenoceptor, pharmaceutical compositions thereof, and use thereof for the treatment of disease.

Abstract: Compounds, compositions and methods are provided for modulating the activity of EP2 and EP4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP2 and EP4 receptors. In certain embodiments, the compounds are antagonists of both the EP2 and EP4 receptors.

Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.

Abstract: Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: wherein R1, R2, R3a, R3b, R4, R5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (Mpro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.

Abstract: The present disclosure provides compounds of Formula I or II. Compounds of Formula I or II may be used in pharmaceutical formulations, and may be used for modulating glucocorticoid receptors.

Abstract: The invention provides pyrazolylsulfonamide compounds, pharmaceutical compositions, their use for inhibiting mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), and their use in the treatment of a disease or condition, such as a proliferative disorder, inflammatory disorder, or autoimmune disorder.

Abstract: or a salt (e.g., pharmaceutically acceptable salt) or stereoisomer thereof, wherein X, Y, R1a, R1b, R2, R3, R4s, R5, p, and n are as defined herein. Use of the compounds as a component of a pharmaceutical compositions and methods for their use are also provided.

Abstract: Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

Abstract: The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

Abstract: The present invention relates to a novel compound as protein kinase inhibitors.

Abstract: Disclosed are compounds of Formula (I?) methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

Abstract: The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancers and viral infections.

Abstract: A fluorine-containing pyrimidine compound is represented by the following formula (1) or (2): wherein R represents a hydrocarbon group having 1 to 12 carbon atoms; and X and Y each independently represent a hydrogen atom, a halogen atom, a hydrocarbon group having 1 to 10 carbon atoms, —CnF2n+1 where n is an integer of 1 to 10, a nitro group, a boronic acid group, —OA1, —SOmA1 where m is an integer of 0 to 3, —NA1A2, —COOA1, or —CONA1A2, where A1 and A2 each independently represent a hydrogen atom or a hydrocarbon group having 1 to 10 carbon atoms.

Abstract: Provided herein are compounds, pharmaceutical compositions, and methods of use thereof, including methods of treating a neurological or psychiatric disease or disorder. For example, provided herein is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., Ring A, X1, R1, R2, R3, R4, and R5) are as disclosed herein. The compounds disclosed herein (e.g., compounds of Formula I, or pharmaceutically acceptable salts thereof) and pharmaceutical compositions can be used to treat a neurological or psychiatric disease or disorder.

Abstract: The present invention relates to a pidolate salt and malate salt of a compound represented by a formula 1 with an excellent liquid-phase stability, solid-phase stability, water solubility, precipitation stability and hygroscopicity all together as a compound for preventing and treating diseases mediated by an acid pump antagonistic activity, as well as a method for preparing the same.