Abstract: Aminocyclobutane compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R1, R2a, R2b, R3 and R4 are defined herein.

Abstract: Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as CMA modulators. The disclosure provides pharmaceutical compositions containing a compound of Formula I.

Abstract: Provided are a compound III serving as an LSD1 inhibitor and a crystal form thereof, as well as use of the compound and the crystal form thereof in preparation of a medicament for treating an LSD1 related disease.

Abstract: Compounds that inhibit p38? MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.

Abstract: The present invention provides: a method for producing an epoxyalkane capable of obtaining an epoxide in a high yield while attaining a high olefin conversion rate and a high selectivity for epoxides even when an olefin includes a long carbon chain, and a solid oxidation catalyst used in the method. The method for producing an epoxyalkane of the present invention comprises reacting an olefin with an oxidant in the presence of a solid oxidation catalyst, wherein the solid oxidation catalyst comprises a transition metal and a carrier that supports the transition metal, and the carrier is a metal oxide having a silyl group represented by the following general formula (1): R1R2R3Si—??(1) wherein R1, R2, and R3 are each independently a single bond, a hydrocarbon group, a halogenated hydrocarbon group, an alkoxy group, or a halogen, and at least one of R1, R2, and R3 is a hydrocarbon group having 3 or more carbon atoms or a halogenated hydrocarbon group having 3 or more carbon atoms.

Abstract: The present invention generally relates to compounds, composition matters, and methods for the treatment of a patient with an infection caused by microorganisms, including bacterial, viral, and fungal infections. In particular, this disclosure relates to safe, highly potent and fast acting antimicrobial agents ?-methylene and ?-aminomethyl lactones, lactams, iminolactones, and iminolactams, thiolactones, thionolactones, thiolactams, and thionolactams having a formula of I, II, III, or IV, for the treatment of viral and bacterial infections, especially for infections caused by methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: With the object of efficiently producing an oxidation product, the present invention provides a method for producing an oxidation product by oxidizing a raw material compound in the presence of oxygen, wherein the raw material compound is oxidized in the presence of manganese dioxide having a crystal structure of ?-type.

Abstract: A controlled decarboxylation of cannabinoids results in a high yield of decarboxylated forms of cannabinoids and also preserves the integrity of volatile components such as terpenoids and as well as fats and lipids that are present in the cannabis extract. The inventive apparatus allows the different components in the cannabis plant extract to be kept in the same reaction mixture during the decarboxylation process, while allowing the decarboxylation process to proceed without breakdown of the more volatile components of the mixture by use of a very low temperature condenser. The invention also relates to a method for controlled decarboxylation of cannabinoids using the novel apparatus.

Abstract: The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.

Abstract: Provided are compounds of Formula (I): Formula (I), including compounds of Formulas (II), (III), (IV), (V) and (VI), wherein X, R1, R2, R3, R4 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Abstract: A crystal form I of a morpholino quinazoline compound represented by the following formula A, a preparation method therefor and use thereof. The crystal form I has good stability and non-hygroscopicity, and the preparation method is simple and suitable for industrial production.

Abstract: The present invention provides novel compounds of Formulae (I?) and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.

Abstract: The present disclosure is concerned with 2-pyrimidone compounds that are capable of inhibiting a viral infection and methods of treating alphavirus viral infections such as, for example, chikungunya, Eastern equine encephalitis (EEEV), Western equine encephalitis (WEEV), and Venezuelan equine encephalitis using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).

Abstract: The invention relates to an organic molecule, in particular for use in optoelectronic devices. According to the invention, the organic molecule has one first chemical moiety with a structure of formula I, and three second chemical moieties, each independently from another with a structure of formula II, wherein the first chemical moiety is linked to each of the three second chemical moieties via a single bond; Y is the binding site of a single bond linking the first chemical moiety to one of the three second chemical moieties; and T, V, W are selected from the group consisting of the binding site of a single bond linking the first chemical moiety to one of the three second chemical moiety, and R1.

Abstract: Disclosed is a series of tricyclic substituted piperidine dione compounds, and applications thereof in the preparation of medicines for treating diseases related to CRBN protein; specifically disclosed are the derivative compound represented by formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present technology provides triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g. for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

Abstract: The present invention relates to a medicament for treating and/or preventing inflammatory bowel disease, comprising a quinolone compound of the formula shown below as an active ingredient.

Abstract: The present application relates to heterocyclic compounds, compositions containing such compounds, their use for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for the preparation of the heterocyclic compounds.

Abstract: Provided herein are 1,2,3-triazole derivatives and methods of use thereof.

Abstract: The technology described herein is directed to IL-4 and/or IL-13 inhibitors and uses thereof.

Abstract: The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

Abstract: Imidazo[4,5-c]quinoline compounds of Formula (I) having a substituent that is attached at the N?1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.

Abstract: The invention can provide compounds, analogs of blebbistatin, effective and selective inhibitors of nonmuscle myosin II relative to cardiac myosin II.

Abstract: The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).

Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Generally, the present invention provides novel quinolone and 5H-1,5,7,11b-tetraaza-benzo[c]fluoren-6-one compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.

Abstract: There is provided novel anticancer and antibacterial compounds, pharmaceutically acceptable salts thereof, and processes for their preparation. The compounds have anticancer activity, which results in the reduction of tumour cell proliferation, enhances cancers cells apoptosis and regulation of iron signalling. The compounds are also particularly active against various Gram-negative and Gram-positive multidrug-resistant bacteria, such as extended-spectrum beta-lactamase (ESBL) producing and colistin-resistant Escherichia coli, carbapenem-resistant E. coli, carbapenem-resistant Acinetobacter baumannii, and methicillin-resistant Staphylococcus aureus (MRSA) including those with reduced susceptibility to many control antibiotics.

Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

Abstract: Provided are compounds of formula (Ia), (Ib) and (IIa), and pharmaceutically acceptable salts thereof. Additionally provided are compositions and pharmaceutical compositions comprising the compounds, therapeutic methods using same for modulating (e.g., inhibiting) CREB binding protein (CBP)/?-catenin mediated signaling in treating a condition, disease or disorder (e.g., fibrosis, cancer, neurological conditions, metabolic disorders (e.g., diabetes, etc.), and skin conditions (dermatitis, psoriasis, scarring, alopecia, etc.) mediated by aberrant CBP/?-catenin signaling, and cosmetic methods for treating skin conditions (e.g., aging, etc.). Additionally, provided are methods for enhancing vaccine efficacy using the compounds and compositions. Further provided are methods for efficiently synthesizing a clinical grade drug, comprising use, in a penultimate, or last reaction step under GMP conditions, of an intermediate 2-propynyl-compound to form a clinical grade isoxazole derivative (e.g.

Abstract: Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.

Abstract: Provided are a novel compound having an antagonistic activity for the P2X7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X7 receptor.

Abstract: Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein Q1, Q2, Q3, R2a, R2b, R3 and X are as defined herein.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1, L1, L2, L3, A1, A2, A3, A4, G1, G2, E, W, X, Y, Z, m, and n are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.

Abstract: Provided is a photochromic indolenapthtopyran having the core skeletal structure of Formula (I): wherein R1 and R2 are each independently substituted or unsubstituted alkyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted alkylthio, substituted or unsubstituted arylthio, substituted or unsubstituted ether, substituted or unsubstituted thioether, amino, a nitrogen-containing heterocycle, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —NHC(O)Ra, or —OC(O)Ra, wherein Ra is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted alkylthio, or substituted or unsubstituted arylthio; R4 is selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heterocycloalkyl, allyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and B and B? are each independently

Abstract: A method of producing levoglucosenone from particulate cellulosic material. The method comprises forming a premix of particulate cellulosic material, water, acid and a polar organic solvent. The solvent has a higher boiling point than levoglucosenone. The pre-mix is fed into a pyrolysis reactor, such as a fluidised bed reactor, in which the pre-mix is fluidised by a fluidising gas. The reactor is maintained at a temperature within the range 250° C. to 450° C., and gaseous products and char are withdrawn from the pyrolysis reactor. Levoglucosenone and the polar organic solvent are condensed from the gaseous products, produced by the reactor.

Abstract: The present invention provides compounds of Formula (Ia) or (Ib) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein.

Abstract: A thienopyridine derivative compound represented by Formula 1 or pharmaceutically acceptable salts thereof have an excellent inhibitory effect on protein kinase activity, and accordingly, pharmaceutical compositions containing the thienopyridine compound can be usefully used for the prevention or treatment of a disease associated with the activity of a protein kinase.

Abstract: Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of USP7 activity.

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

Abstract: The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: where A, B, R1, X1, X2, and W are described herein.

Abstract: Provided are far red to near-infrared nerve-sparing fluorescent compounds, compositions comprising them, and methods of their use in medical procedures.

Abstract: Disclosed are a series of tricyclic furan-substituted piperidinedione compounds and an application thereof in preparing a drug for treating a disease related to CRBN protein. In particular, disclosed is a derivative compound represented by formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: The present application discloses compounds that are inhibitors of Btk, compounds that are inhibitors of PI3K?, and compounds that are dual inhibitors of both Btk and PI3K?. Also described are methods for synthesizing such inhibitors and methods for using such inhibitors for the treatment of diseases wherein inhibition of Btk and PI3K? provides a therapeutic benefit to a patient having the disease.

Abstract: The present invention relates to novel compounds of formula (I), wherein R1 to R7 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: The present invention provides a novel method for preparing high-purity gadobutrol or hydrates thereof. The preparation method of the present invention can have an advantage of simplifying a process by forming a gadolinium complex in-situ without purification of a butrol intermediate and omitting a resin purification process unlike a conventional method for synthesizing gadobutrol. In addition, the preparation method of the present invention can be used to produce high-purity gadobutrol or hydrates thereof at a high yield only through the simple process as above, and thus can be useful in mass production.

Abstract: Disclosed herein are compounds of Formula (I) or (II). The compounds include an agent (e.g., pharmaceutical agent, cosmetic agent, or nutraceutical agent) through a linker that includes a boronic ester moiety in the backbone of the linker. The compounds may be monomers. Also provided are polymers prepared by polymerizing the monomers. The polymers may be useful for delivering the agent to a subject, tissue, biological sample, or a cell. Also provided are methods of preparing the polymers, compositions and kits comprising the polymers, and methods of use (e.g., use in delivering the agent, treating a disease, preventing a disease, diagnosing a disease) involving the polymers or compositions. The structure of the boronic ester moiety may be fine tuned so that the properties related to delivery to a subject, biological sample, tissue, or cell may be fine tuned.