Abstract: Chiral 3-sulfinylbenzoic acids of the respective absolute configuration given in formulae (I-R) and (I-S) are described as precursors for preparation of herbicidal compounds. In formulae (I-R) and (I-S). X. Z and R? represent radicals such as alkyl, cycloalkyl, haloalkyl and halogen.

Abstract: A method of making a pyrazole compound includes mixing a diazonium salt with a reactant in the presence of a solvent, thereby coupling a diazo group of the diazonium salt to an ?-carbon atom of the reactant to form a reaction intermediate having a formula of (I) or (II); mixing the reaction intermediate and hydrazine in the presence of a superparamagnetic iron oxide nanoparticles catalyst thereby cyclizing the hydrazine with an ester group of the reaction intermediate to form the pyrazole compound having a formula of (III) or (IV).

Abstract: A compound represented by formula (I) is effective in inhibiting the growth of Clostridium difficile. Compared with nitazoxanide and other antibiotics, the compound also has significantly less influence on intestinal probiotics and lower toxic side effects while significantly inhibiting the activity of Clostridium difficile, and the disease is not easy to relapse after the drug is stopped.

Abstract: The present invention provides a purification method for citalopram or S-citalopram or salts thereof, comprising the following steps: using a washing solution to treat a solution consisting of citalopram and a water-immiscible organic solvent and carrying out separation to obtain an organic layer containing citalopram, or using a washing solution to treat a solution consisting of S-citalopram and a water-immiscible organic solvent and carrying out separation to obtain an organic layer containing S-citalopram; and then, taking the organic layer and carrying out further separation to obtain citalopram or S-citalopram, or adding acid to form a salt and carrying out further separation to obtain an acid salt of citalopram or S-citalopram. The purification method provided by the present invention is simple in operation and high in impurity removal rate.

Abstract: A compound represented by the following formula (1): The R1 to R9, L1 to L3, and Ar1 to Ar2 in the formula (1) are as defined in the description. An organic electroluminescence device contains the compound, and an electronic instrument includes the organic electroluminescence device.

Abstract: Proposed are a novel flavone derivative and a composition for improving pulmonary fibrosis using the same. The flavone derivative inhibits the TGF-?1 signaling pathway without showing specific cytotoxicity to A549 cells, derived from lung cancer, Hulec-5a cells, derived from pulmonary vessels, and human lung fibroblasts (HLF), thereby inhibiting epithelial-mesenchymal transition (EMT). Additionally, the flavone derivative also shows the effect of regulating the expression of pulmonary fibrosis-related factors in the A549 cells and Hulec-5a cells treated with epidermal growth factor (EGF) or bleomycin, which causes pulmonary fibrosis.

Abstract: Provided is lipid and methods of making such lipid having the structure of Formula A: each R is an alkyl having a carbon backbone of C12 to C16 having 1 to 3 C?C double bonds, at least one having Z-geometry; R? is an optional alkyl of C2 to C24 having 0 to 3 C?C double bonds; each R, and the R? alkyl group if present, is optionally substituted at one or more positions with a C1 to C3 alkyl; W and X are O or S; Y is absent and C1 and C2 are bonded, or Y is present and is a metheno, etheno or ethyno bridge optionally substituted with an alkylamino chain [—(CH2)m—NG1G2G3], wherein m is 1-5 and G1, G2 are, independently, C1 to C3 alkyl, G3 is absent, hydrogen or C1 to C3 alkyl, or wherein NG1G2G3 is a heterocycle; and Z and Z? are H or alkylamino.

Abstract: A manufacturing method capable of improving the yield and properties of a cyclic sulfonic acid ester derivative compound includes (A) reacting a compound represented by Formula 1 and thioacetic acid to prepare a compound represented by Formula 2, and (B) subjecting the compound represented by Formula 2 to an oxidative cyclization reaction to prepare a compound represented by Formula 3: wherein m and R1 to R8 are described herein.

Abstract: The invention relates to a polymerizable photoinitiator, to a process for preparing a polymerizable photoinitiator, to a polymerizable composition comprising a polymerizable photoinitiator and an ethylenically unsaturated compound. The invention also relates to different uses of the polymerizable photoinitiator or polymerizable composition.

Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, especially as fungicides.

Abstract: This patent document reveals a class of pleiotropic pathway modifier (known as PPM) compounds that facilitate the degradation of multiple targeted proteins and regulate various signaling events involved in cancer cell survival and proliferation, as well as immune response. These compounds effectively recruit disease-causing proteins for swift destruction through the ubiquitin-proteasome pathway, exhibiting potent anti-cancer, immunomodulatory, and anti-inflammatory properties. Additionally, disclosed herein are methods for treating diseases encompassing cancers, autoimmune disorders, infections, inflammations, and other ailments.

Abstract: The present invention relates to a process for preparation of Batefenterol of Formula (I) or pharmaceutically acceptable salts thereof, and the process for the preparation of the chiral intermediate compounds including compound of Formula (VII) by chiral sulfide mediated epoxidation. The process involves preparation of the intermediate compounds of Formula (VII), followed by preparation of Batefenterol from the intermediate compounds of Formula (VII) via intermediate compounds of Formula (X) and Formula (XI); or via intermediate compounds of Formula (IX) and Formula (XI); or via intermediate compounds of Formula (VII) and Formula (XI); or via intermediate compounds of the Formula (XV) and Formula (XVI); or via intermediate compounds of the Formula (XIX) and Formula (XVI). The process is cost effective and gives higher yield and better purity.

Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.

Abstract: Indole-substituted quinolines (ISQs) are provided which may include a variety of substituted piperidines. Methods for treating cancers, including c-MYC-driven cancers, are described including administering the ISQs to a subject in need thereof. The compounds may be administered in combination with a polo-like kinase-1 (Plk1) inhibitor. The Plk1 and the compound may be administered in synergistically effective amounts.

Abstract: The present disclosure provides methods of producing a compound of structural formula (I): (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present application relates to chemical compounds of Formula (1), and pharmaceutically acceptable salts thereof, that inhibit IRAK4 and consequently have potential utility in medicine.

Abstract: a pyrazole derivative compound of Chemical Formula H, an adhesive composition including the same, and an adhesive film including the same are provided.

Abstract: A tetrahydropyrrolocyclic compound as represented by formula (I), a pharmaceutically acceptable salt thereof, and an application thereof in preparation of a drug for treating a disease related to a selective orexin-2 (OX-2) receptor antagonist, wherein the related disease is selected from insomnia and depression.

Abstract: A compound of Chemical Formula 1 and an organic light emitting device including the same: wherein: Ar1 is unsubstituted benzophenanthrenyl, chrysenyl, or fluoranthenyl; Ar2 is a substituted or unsubstituted C6-60 aryl, or a substituted or unsubstituted C6-60 heteroaryl containing any one or more of N, O and S; L1, L2, and L3 each independently is a direct bond or a substituted or unsubstituted C6-60 arylene; and R1 and R2 are each independently hydrogen, deuterium, a substituted or unsubstituted C1-12 alkyl, or a substituted or unsubstituted C6-14 aryl. The compound of Chemical Formula 1 can be used as a material for an organic material layer of an organic light emitting device for hole injection, hole transport, hole injection and transport, electron blocking, light emission, electron transport, or electron injection, and can improve the efficiency, achieve low driving voltage and/or improve lifetime characteristics of the device.

Abstract: Various amide compounds that bind Cbl-B, including those that are selective for C-Cbl, and methods of making and using the same.

Abstract: The present invention relates to: a novel compound having excellent GLP-1 agonist activity and an excellent DMPK profile, and thus useful as an agent for treating or preventing obesity or various metabolic diseases such as diabetes and hyperlipidemia; an isomer thereof or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the compound; and a method for preparing the compound.

Abstract: Anti-angiogenic treatments and compounds for use in anti-angiogenic treatments, particularly of conditions associated with abnormal angiogenesis or abnormal over-production of pro-angiogenic VEGFxxx isoforms in or on the eye are described.

Abstract: The present invention relates to a novel process for the preparation of 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine-1-oxide of formula (I) The present invention also relates to the novel intermediate compounds of formula (V), formula (VII), and their processes for the preparation thereof. The present invention also relates to the use of compounds of formula (V), formula (VII) intermediate in the preparation of 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1, 2, 4-oxadiazol-3-yl)-4, 6-dimethylpyridine-1-oxide of formula (I).

Abstract: The present invention relates to ampakines, including low impact ampakines, and pharmaceutical compositions and methods employing ampakines for treating central nervous system (CNS) disorders, including attention deficit disorders. Novel compositions and methods are provided employing anti-ADHD ampakines to treat attention deficit hyperactivity disorder (ADHD) and related cognitive, behavioral and psychiatric conditions.

Abstract: Provided are an N-phenylimine derivative and a preparation method and use thereof. Provided is an N-phenylimine derivative, being selected from the group consisting of: a 1,2,4-oxadiazole-N-phenylimine derivative represented by formula 1, a 1,3,4-oxadiazole-N-phenylimine derivative represented by formula 2, an N-phenylimine amide (ester) derivative represented by formula 3, and an N-phenylimine benzoate derivative represented by formula 4.

Abstract: Disclosed is the 1:1 phosphate salt of Compound (I) as well as a novel crystal form thereof. Also disclosed is a novel crystal form of Compound (I). The present invention also provides methods of increasing the activity of HMOX-1 in a subject, of activating transcription factor Nrf2 in a subject or of reducing the amount of ROS in a subject by administering an effective amount of the 1:1 phosphate salt of Compound (I), the crystal form thereof or the crystal form of Compound (I) to the subject.

Abstract: Disclosed herein are compounds and methods of using the same for treating a subject in need of a treatment for infection by a microbe and inhibiting growth or proliferation of a microbe. The method may comprise administering an effective amount of a compound or a pharmaceutical composition comprising the effective amount of a compound to the subject. Suitably the microbe is Mycobacterium tuberculosis.

Abstract: The present invention discloses a series of new compounds containing beraprost and nitric oxide donors, as shown in formula I below, relating to the series of compounds and their pharmaceutical compositions and uses. The invention provides a class of beraprost sodium and NO donor combination drugs, solves the short half-life of clearance problem of beraprost sodium , more daily administration, efficacy of saturation capping effect, and rapid catabolism half-life of NO. The new compound could reduce the dose and frequency, at the same time in-situ generated of NO could induce relaxation smooth muscle effect, through dual action, showcasing the synergistic effect, improving the effectiveness and safety of the drug.

Abstract: This invention relates to compounds which are microtubule associated serine/threonine-like kinase (MASTL) inhibitors and the use of the compounds in the treatment of diseases and medical conditions mediated by MASTL, for example in the treatment of cancer and other target related diseases.

Abstract: This disclosure provides compounds containing 6-(pyrimidin-4-yl)quinoline structure, the use thereof for selectively inhibiting the activity of CDK4, and pharmaceutical compositions comprising the compounds as treatment of various diseases including cancer.

Abstract: The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

Abstract: This disclosure provides compounds of Formula (I), Formula (II), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Ka). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3Ka activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

Abstract: Disclosed are novel heterocyclic compounds such as novel phenothiazinyl compounds and pharmaceutical compositions thereof which may be used to treat or prevent bacterial infections including gram positive bacterial infections, skin infection, endocarditis, osteomyelitis, pneumonia, HIV infection, cancer, Alzheimer's disease, pox, rabies and coronavirus infection. Also disclosed are the general use of known phenothiazinyl compounds and pharmaceutical compositions thereof to treat r prevent bacterial infections including gram positive bacterial infections, skin infection, endocarditis, osteomyelitis, pneumonia, HIV infection, cancer, Alzheimer's disease and coronavirus infection.

Abstract: Provided herein are HPK-1 inhibitors, such as a compound of Formula X. Also provided are pharmaceutical compositions comprising the HPK-1 inhibitors, methods of using HPK-1 inhibitors, for example, for treating cancer. Method of preparing such HPK-1 inhibitors and novel synthetic intermediates are also provided.

Abstract: The present application relates to novel compounds described herein, the method of preparing the same, its pharmaceutical composition and method for use thereof. In particular the invention relates to compounds of formula (A) or their pharmaceutically acceptable salts thereof as inhibitors of KRAS protein and useful in treatment, prevention and/or amelioration of diseases or disorders associated with KRAS especially the Cancer.

Abstract: The present invention relates to novel salts of a heterocyclic compound as a protein kinase inhibitor and uses thereof. The novel salts are superb in terms of water solubility and physical and chemical stability and thus can be usefully employed in formulating medicinal products. In addition, the heterocyclic compound or the salts thereof can effectively treat and prevent atopic dermatitis and inflammatory bowel disease.

Abstract: The present invention relates to a novel compound as a protein kinase inhibitor, a RON inhibitor in particular.

Abstract: Disclosed a CLY series compound, a preparation method therefor and the use thereof in the preparation of drugs. The CLY series compound can significantly prolong the survival time of acute GVHD mice, and can reduce clinical symptoms, exhibiting a therapeutic effect on acute GVHD; in a pulmonary fibrosis mouse model, same can obviously reduce the levels of MMP-2 and MMP-9 in the lung tissue, increase the levels of TIMP-1 and VEGF, and simultaneously increase the levels of SOD and CAT enzymes in peripheral blood; and same can also improve the arthritis symptoms of rheumatoid arthritis mice by means of reducing the level of IL-17 in peripheral blood and increasing inflammatory indexes such as IL-10. The compound can be used alone or in combination with other drugs, and provides a new drug choice for the treatment of the above diseases.

Abstract: The present disclosure provides a compound represented by structural formula (I): (I) or a pharmaceutically acceptable salt thereof useful for treating a cancer.

Abstract: Imidazo[4,5-c]quinoline compounds 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 present application provides heterocyclic compounds that modulate the activity of JAK2, which are useful in the treatment of various diseases, including cancer.

Abstract: A novel crystalline form of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-N-methylazetidin-3-amine hemisuccinate is provided along with pharmaceutical compositions comprising the same. Also disclosed is the use of the novel polymorph for the treatment of diseases, such as atopic dermatitis (AD), itch, pruritus and various forms of urticaria for example chronic idiopathic urticaria subtypes.

Abstract: Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide (Compound A) (Formula I), including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions or pharmaceutical formulations that include the compound, as well as methods of using the compound, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, diabetes, and inflammatory diseases or conditions.

Abstract: Disclosed herein is a compound of Formula (I) for activating T cells, promoting T cell proliferation, and/or exhibiting antitumor activity, a method of using the compounds disclosed herein for treating cancer, and a pharmaceutical composition comprising the same.

Abstract: The present invention provides a compound having a PDHK inhibitory activity and useful for the treatment or prophylaxis of diabetes (type 1 diabetes, type 2 diabetes etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract etc.), cardiac failure (acute cardiac failure, chronic cardiac failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral arterial disease, intermittent claudication, chronic obstructive pulmonary disease, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension or Alzheimer disease. The present invention relates to a compound of the formula [I-a] or the formula [II], or a pharmaceutically acceptable salt thereof: wherein each symbol means the same as that described in the specification.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.

Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.

Abstract: The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 represents a hydrogen atom, a halogen atom, or a (C1 C4)hydroxyalkyl group, R2 represents a (C1-C6)alkyl group, and R3 represents a hydrogen atom, a (C1-C4)alkyl group or a halogen atom, and Ar represents a divalent aromatic ring or a (C5-C11) heteroarylene group. It further relates to the therapeutic uses thereof, in particular as anticancer agents.

Abstract: The present invention relates to tetrazole substituted ethylsulfone/sulfoximine-pyridine derivatives of formula (I), (Ia) or (Ib) wherein the variables are as defined in the description and/or in the claims, which can be used as antiparasitic agents for the treatment, prevention and/or control of parasitic infections and/or infestations in/on animals as well as as crop protection agents.