Abstract: Compositions and methods for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or 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 PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.

Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.

Abstract: This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

Abstract: The invention provides indazolyl thiadiazolamines and related compounds, pharmaceutical compositions, methods of inhibiting Rho-associated protein kinase, and methods of treating inflammatory disorders, immune disorders, fibrotic disorders, and other medical disorders using such compounds. An exemplary indazolyl thiadiazolamine compound is an N-(5-[5-[(1H4ndazol-5-yl)amino]-1,3,4-thiadiazol-2-yl]pyridin-3-yl)acetamide compound.

Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

Abstract: The present invention is directed to compounds of Formulas (I, Ia, IIa and IIb). The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, Ia, IIa and IIb). Methods of making and using the compounds of Formulas (I, Ia, IIa and IIb) are also within the scope of the invention.

Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disorders

Abstract: The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

Abstract: The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CR6 or N; W is: (i) —(CR3R3)1-4— or (ii) —(CR3R3)x-Y—(CR3R3)y-; and Y, R1, R2, R3, R5, R6, R7, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The present invention relates to the compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with cancers associated with protein kinases, to their use as medicaments for use in the production of inhibition of mTor, pi3k reducing effects in warm-blooded animals such as humans.

Abstract: Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.

Abstract: Described herein are 6-aminopurine compounds comprising formula (III) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (III) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample.

Abstract: The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: The present invention is directed to imidazo[1,2-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: The present invention provides a compound of Formula I: useful for treating chronic kidney disease and diabetic kidney disease.

Abstract: Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R1, X1 and X3 are as described herein.

Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.

Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2, A3, A4, A5, W1, Y, R1, R2, R3, R4, R5, R6a, R6b, R7, R8, R8a, R8b, R9, R9a, R9b, and R10 and subscript “n” are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

Abstract: An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present disclosure provides thiazolyl-containing compounds of Formula (I), (II), or (III). The compounds described herein may be able to inhibit protein kinases (e.g., Src family kinases (e.g., hemopoietic cell kinase (HCK)), Bruton's tyrosine kinase (BTK)) and may be useful in treating and/or preventing proliferative diseases (e.g., myelodysplasia, leukemia, lymphoma (e.g., Waldenström's macroglobulinemia)) and in inducing apoptosis in a cell (e.g., malignant blood cell). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The present disclosure relates to a novel compound, a color conversion film, a backlight unit and a display device comprising the same.

Abstract: Methods for the selective borylation of arenes, including arenes substituted with an electron-withdrawing group (e.g., 1-chloro-3-fluoro-2-substituted benzenes) are provided. The methods can be used, in some embodiments, to efficiently and regioselectively prepare borylated arenes without the need for expensive cryogenic reaction conditions.

Abstract: In one aspect, cobalt complexes are described herein. In some embodiments, such cobalt complexes are operable as catalysts for hydroboration and borylation applications.

Abstract: Boron-based prodrugs of phenol- or aromatic hydroxyl group-containing therapeutic molecules (“original drugs”), uses thereof, and methods of making the same, are provided for achieving, for example, improved bioavailability, prolonged retention (e.g., in a circulatory system) and, in particular, significantly lowered therapeutically effective dosage in order to reduce adverse effects while maintaining the desired therapeutic effects of the original drugs.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

Abstract: The invention relates to the use of compounds of formulae (I) and/or (II) as colorless 1R absorbers wherein M is Ni, Pd, Pt, Au, Ir, Fe, Zn, W, Cu, Mo, In, Mn, Co, Mg, V, Cr or Ti, X1, X2 and X3 are each independently of the others sulfur or oxygen, R1, R2, R3, R4, R5 and R6 are each independently of the others hydrogen, NR7R8, unsubstituted or substituted C1-C18alkyl, C1-C18 alkyl wherein the alkylene chain is interrupted with oxygen, unsubstituted or substituted C1-C18alkenyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, R7 and R8, each independently of the other, being unsubstituted or substituted C1-C18alkyl, unsubstituted or substituted aryl, unsubstituted or substituted arylalkyl or unsubstituted or substituted heteroarylalkyl, a further IR absorber optionally being added to the compounds of formulae (I) and (II).

Abstract: Disclosed herein are catalyst compositions containing bicyclic bridged metallocene compounds. These catalyst compositions can be used for the polymerization of olefins. For example, ethylene polymers produced using these catalyst compositions can be characterized by low molecular weights and high melt flow rates, and can be produced without the addition of hydrogen.

Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Abstract: A process for the synthesis of Sofosbuvir is provided comprising the steps of selectively mono-deacetylating a compound of formula (V) enzymatically using a resin supported lipase B derived from Candida Antarctica to obtain a compound formula (IV), then converting the compound of formula (IV) to a compound of formula (II) by reacting the compound of formula (IV) with a compound of formula (III), and then converting the compound of formula (II) to Sofosbuvir of formula (I) by deacetylation reaction.

Abstract: The present invention relates to DOT1L inhibitors and methods of identifying, designing, or optimizing them. The present invention also relates to crystals of DOT1L-inhibitor complexes, the crystal structures thereof, and the use of the crystal structures. Also disclosed are pharmaceutical compositions containing these DOT1L inhibitors and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: Embodiments relate to methods of sequencing nucleic acids. Embodiments encompass the use of nucleotide analogs and a nucleic acid polymerase enzyme or enzyme complex comprising proofreading activity. The nucleotide analogs may become incorporated into a replicating strand and induce the proofreading activity of the polymerizing enzyme, thereby prolonging the duration of a signal associated with nucleotide incorporation, resulting in more observable sequencing events and increasing the accuracy of nucleic acid sequencing.

Abstract: The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

Abstract: A method of purifying a desired protein from a preparation includes (a) providing the preparation in a form having less than about 5% of chromatin residing in an original production medium, (b) contacting the preparation with a nonionic organic polymer and a salt, a concentration of nonionic organic polymer being sufficient to precipitate the desired protein or cause its accretion on a hydrophilic surface, or maintain it in a precipitated state or accreted on the hydrophilic surface, the salt concentration being sufficient to produce greater than physiological conductivity, and (c) contacting the preparation with at least one electropositive surface, optionally in the presence of a salt concentration sufficient to produce greater than physiological conductivity, the desired protein does not substantially adsorb to the at least one electropositive surface while not preventing adsorption of acidic contaminants to the at least one electropositive surface.

Abstract: A process for purifying fibrinogen from a fibrinogen containing source by precipitation of fibrinogen by a precipitating agent from a fibrinogen containing solution in the presence of one or more chelating agent(s) and removal of the supernatant from the fibrinogen paste, characterized in that fibrinogen is extracted from the paste forming a liquid fraction containing fibrinogen, and an undissolved residue, which is separated from the liquid.

Abstract: An enantioselective process for the production of (2S,3aS,6aS)-cyclopenta[b]pyrrole-2-carboxylic acid and its conversion into Ramipril is provided.

Abstract: Novel efficient, time-saving and reliable radiofluorination procedures for the production of 18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with 18F? are described. The active ester including [18F]F-Py-TFP and [18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.

Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Abstract: The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.

Abstract: Provided are a synthetic peptide having a multinucleation-inducing activity that can cause multinucleation in a target cell, a multinucleation-inducing agent containing this peptide, and a multinucleation induction method that uses this peptide. The synthetic peptide provided by the present invention is an artificially synthesized peptide that contains (A) a membrane-permeable peptide sequence and (B) a multinucleation-inducing peptide sequence, and that can cause multinucleation in at least one type of eukaryotic cell of human origin or non-human mammal origin. The multinucleation-inducing peptide sequence is constituted of an amino acid sequence given by SEQ ID NO: 1 or SEQ ID NO: 2 or a modified amino acid sequence therefrom.

Abstract: An object of the present invention is to provide a novel peptide and a novel immunostimulant or hair grower containing the peptide as an active ingredient. The present invention provides a peptide of 23 or less amino acids comprising the amino acid sequence LHRLKRLRKRL (SEQ ID NO: 1), preferably the amino acid sequence LHRLKRLRKRLK (SEQ ID NO: 9), and also provides an immunostimulant containing the peptide, a vaccine adjuvant containing the peptide, a vaccine composition containing the peptide, and a hair grower containing the peptide.

Abstract: Influenza viruses have traditionally been administered by intramuscular injection. The invention is based on the idea of using alternative routes of delivery for influenza vaccines, more specifically routes that do not require as large a dose of antigen. Delivery of influenza antigen to the Langerhans cells is the route of choice according to the invention. This route has been found to be particularly useful for vaccinating patients who are naïve to influenza virus (i.e. have not previously mounted an immune response to an influenza virus), which means that it is advantageous for immunising young children.