Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.

Abstract: Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.

Abstract: A method for the oxidation of ethylene to form ethylene oxide which comprises: providing an aqueous stream containing ethylene glycol and impurities; introducing the aqueous stream in a first ion exchange treatment bed to reduce the content of these impurities; determining whether an outlet of the first ion exchange treatment bed has a conductivity greater than about 5 ?S/cm; upon determining that the outlet of the first ion exchange treatment bed has a conductivity greater than about 5 ?S/cm, introducing the outlet of the first ion exchange treatment bed into a second ion exchange treatment bed; and upon determining that the outlet of the first ion exchange treatment bed has a conductivity greater than about 60 ?S/cm, redirecting the introduction of the aqueous stream to the second ion exchange treatment bed and regenerating the first ion exchange bed.

Abstract: A furfural derivative having the chemical formula (1) wherein R represents hydrogen, an alkyl group or an acyl group, is prepared in a process, which process includes reacting a fructose- and/or glucose-containing starting material with a liquid hydroxyl group-containing compound of formula R—OH in the presence of an acid catalyst at a reaction temperature in the range of 150 to 300° C. to produce an acid reaction mixture including the furfural derivative of chemical formula (1), which acid reaction mixture has a pH-value of smaller than 3; neutralizing the acid reaction mixture to a pH-value in the range of 3 to 6.5 to provide a partially neutralized reaction mixture; and purifying the partially neutralized reaction mixture to recover the furfural derivative of chemical formula (1).

Abstract: A purified acid composition including 2,5-furandicarboxylic acid is prepared by a process including a) providing an acid composition solution of a crude acid composition in a polar solvent, the crude acid composition including 2,5-furandicarboxylic acid (FDCA) and 2-formyl-furan-5-carboxylic acid (FFCA); b) contacting the acid composition solution with hydrogen in the presence of a hydrogenation catalyst to hydrogenate FFCA to hydrogenation products, such that the hydrogenation products contain a minor amount of 2-methyl-furan-5-carboxylic acid (MFA) or no MFA, yielding a hydrogenated solution; c) separating at least a portion of the FDCA from the hydrogenated solution by crystallization.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.

Abstract: Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV.

Abstract: Described herein are compounds that are somatostatin 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 somatostatin activity.

Abstract: The present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumors such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma.

Abstract: The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

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 or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E 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: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.

Abstract: The invention is directed to a compound of formula I, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula I, and a method of treatment of a disorder or condition in a mammal, including a human, selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis, toxoplasmosis and malaria.

Abstract: Provided herein are compounds of the formula: or pharmaceutically acceptable salts thereof, and compositions comprising such compounds for use in the treatment of diseases or conditions responsive to modulation of the small conductance calcium-activated potassium channel (SK channel).

Abstract: This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).

Abstract: The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Abstract: The present invention relates to novel processes for the preparation 1,3-Thiazol-5-ylmethyl[(2R,5R)-5-{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl} carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl] carbamate having the following structural formula-1 and it's intermediates thereof.

Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices, and to electronic devices containing one or more compounds of the formula (I). The invention furthermore relates to preparation processes for compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).

Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

Abstract: The invention relates to 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo [d] imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-5-yl) oxy)-3,4-dihydro-1, 8-naphthyridin-2 (1H)-one (Compound 1) maleate salts, in particular the sesqui-maleate salt and its crystalline forms, methods of preparation, pharmaceutical compositions, and therapeutic uses for treatment of diseases or disorders mediated by BRAF or other kinases.

Abstract: The invention relates to a crystalline form of (S)-2-(8-((5-chloropyrimidin-2-yl)(methyl)amino)-2-fluoro-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as CRTH2 receptor modulators.

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.

Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

Abstract: The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

Abstract: The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, X1, X2, m, and n are described herein.

Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

Abstract: Ether analogues of galiellalactone, methods of preparing the analogues, and use of the analogues in the treatment of cancer are disclosed.

Abstract: The present invention relates to a heterocyclic-substituted pyridinopyrimidinone derivative and the use thereof as a therapeutically effective cyclin-dependent kinase (CDK) inhibitor. In particular, the present invention relates to the use of a new heterocyclic-substitute pyridinopyrimidinone derivative as shown in formula (I) and a pharmaceutical composition thereof as a selective CDK4/6 inhibitor in preventing or treating diseases related to CDK4/6.

Abstract: A monoallophanate can be used in paint or adhesive compositions. The monoallophanate has the formula 1: where R, R1-R6 are each independently identical or different hydrocarbyl radicals having 1-8 carbon atoms, which may be branched or cyclic, or else may be integrated together to form a cyclic system, and m and n are each independently 0-2.

Abstract: Provided herein are transmitter ligands that improve photon upconversion of near infrared light (NIR) to visible light. The presently provided ligands are complexed to semiconductor nanocrystals and improve triplet energy transfer from semiconductor nanocrystal to annihilator in triplet-triplet annihilation. Suitable applications include bio-imaging.

Abstract: Provided are phosphonopyrazole-based phosphohistidine analogs that are useful as haptens for the preparation of immunogens, immunogens that include these haptens linked to carrier molecules, antibodies thereto and uses of these antibodies, haptens, immunogens and phosphohistidine analogs. The invention is based in part on new pHis analogs that are chemically stable and which have been used as haptens and immunogens to generate specific anti-pHis antibodies that bind with high affinity and specificity.

Abstract: The present invention provides novel phospholipidated imidazoquinolines of formula (I) as TLR7 and TLR8 agonists, pharmaceutical compositions, therapeutic uses and processes for preparing the same.

Abstract: Ligands for use with catalyst compositions used in hydroformylation reactions are described herein. The ligands are used with various octofluorotoluene or hydrocarbon solvents and achieve an increase in isoselectivity with an increase in temperature, an increase in TON with an increase in temperature, and/or will show isoselectivity that is surprisingly high in comparison to the hydroformylation reactions using common solvents.

Abstract: An alkoxide compound is represented by General Formula (I) below: wherein R1 to R3 each independently represent hydrogen, a C1-12 hydrocarbon group, etc.; R4 represents a C1-12 hydrocarbon group, etc.; L represents hydrogen, halogen, a hydroxyl group, an amino group, an azi group, a phosphido group, a nitrile group, a carbonyl group, a C1-12 hydrocarbon group, etc.; and M represents a metal atom or a silicon atom, n represents an integer of 1 or more, m represents an integer of 0 or more, and n+m represents the valence of the metal atom or silicon atom.

Abstract: The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers. The disclosed compounds are useful for treating a neoplasm in mammalian subjects. The cytidine derivative dimer has the following general formula (I). where R1 is C1-C10 alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R2 is C1-C10alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R3 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; R4 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; and R5 is —(CH2)n—, substituted —(CH2)n—, or —(CH2)n1—O—(CH2)n2-Ph-, where n, n1, and n2 are an integer from 0 to 3. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.

Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate (I) and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate (II) for various hormonal therapies, dosage forms comprising 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.

Abstract: Method of recovering sterols from tall oil pitch which contains steryl esters. In the method the tall oil pitch is subjected to a transefterification reaction with a lower alcohol in a reaction zone to provide a reaction product mixture containing lower alkyl fatty acid esters, free sterols, and at least some unreacted steryl esters. The invention comprises separating the transesterified esters from the reaction product mixture to form a sterol rich fraction which contains free sterols and unreacted steryl esters, liberating sterols from the unreacted steryl esters to form further free sterols, and recovering and optionally purifying the free sterols. The recovery of free sterols can be increased to up to 80 wt % or more while avoiding the formation of undesired side streams containing troublesome impurities.

Abstract: The invention relates to 3?-ethynyl, 3?-hydroxy, 5?-pregnan-20-oxime, represented by the following structural formula: or a pharmaceutically acceptable salt thereof, which compounds and/or salts are useful as modulators of the mammal brain excitability via the gamma-aminobutyric acid receptor-chloride ionophore (GABAA-R) complex and in the treatment of disorders such as hepatic encephalopathy, Down's syndrome and Alzheimer's disease.

Abstract: Provided herein are synthetic analogs of withanolide natural products of formula (I), wherein R1-R4 are as defined herein, and their pharmaceutical uses in treating neurodegenerative diseases.