Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.

Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.

Abstract: Compounds comprising piperazines, piperidines, spiro-furanopiperidines, and analogs thereof are provided that are modulators, such as positive allosteric modulators, of one or more subclasses of vasopressin receptors. The compounds can be selective modulators of one or more subclasses of vasopressin receptors. Compounds of the invention can be used in the treatment of a condition wherein modulating a vasopressin receptor is medically indicated for treatment of the condition.

Abstract: The invention belongs to the technical field of organic chemistry, in particular being a method for preparing (+)-tricyclic hydroxyl lactone. The preparation of the (+)-tricyclic hydroxyl lactone compound in the prior art has lengthy steps, low stereoselectivity and high costs. The (+)-tricyclic hydroxyl lactone of the invention is obtained by an asymmetric oxidation reaction of prochiral tricyclic lactones in an organic solvent with an optically active Davis oxidant in the presence of an organic base. The method of the invention uses easily available raw materials, has low costs, good selectivity, and is suitable for large-scale preparation.

Abstract: Disclosed are a method for preparing coumestrol and a method for preparing coumestrin preparation, wherein chitosan is treated for a predetermined amount of time during a bean growth period. Additionally, disclosed is the method for preparing coumestrol by performing an enzyme treatment or an acid treatment and the like on the coumestrin prepared by the preparation method.

Abstract: The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.

Abstract: The material for forming an underlayer film for lithography of the present invention contains a compound having a structure represented by the following general formula (1). (in formula (1), each X independently represents an oxygen atom or a sulfur atom, R1 represents a single bond or a 2n-valent hydrocarbon group having 1 to 30 carbon atoms, the hydrocarbon group may have a cyclic hydrocarbon group, a double bond, a hetero atom or an aromatic group having 6 to 30 carbon atoms, R2 represents a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, or a hydroxyl group, m is an integer of 0 to 3, n is an integer of 1 to 4, p is 0 or 1, and q is an integer of 1 to 100.

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.

Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present invention relates to compounds of formula (I) Wherein R1, R2, R3, R4, L and Z have the meaning given in claim 1, and their use in the prophylaxis and treatment of diseases.

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 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: This invention relates to new carbocyanine dye compositions, pharmaceutical compositions comprising such compositions, methods of detecting via near infrared fluorescent imaging incipient cancer cells and selective destruction of cancer cells identified by administration of such pharmaceutical compositions. A method of detecting and destroying cancer cells includes introducing a gold dye into an organism suspected of having a cancer cell. The gold dye is a carbocyanine dye covalently attached to a gold nanoparticle. A near infrared light is shined on a region suspected of having the cancer cell. Fluorescence from the gold dye is detected. A beam of radio frequency energy is directed at the region to induce hyperthermia in the cancer cell. The carbocyanine dye has the most basic structure of MHI-148 and structures 6 and 22 with a Aun—[CH2(CH2)9CH2—(OCH2CH2)4O]COCH2CH2-phenyl-O group on a cyclohexene ring that imparts activity to the cancer cell binding and destruction processes.

Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.

Abstract: Mono-substituted TSA precursor Si-containing film forming compositions are disclosed. The precursors have the formula: (SiH3)2N—SiH2—X, wherein X is selected from a halogen atom; an isocyanato group; an amino group; an N-containing C4-C10 saturated or unsaturated heterocycle; or an alkoxy group. Methods for forming the Si-containing film using the disclosed mono-substituted TSA precursor are also disclosed.

Abstract: The present invention relates to compounds of Formula (I), or a form thereof wherein ring A1, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

Abstract: The invention provides a phospholipid compound containing unsaturated fatty acid having a cyclopropane ring such as 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) and 8-(2-octylcyclopropyl)octanoic acid (DCP-OA) and the like, particularly 1,2-o-bis-[8-{2-(2-pentyl-cyclopropylmethyl)-cyclopropyl}-octanoyl]-sn-glycero-3-phosphatidylethanolamine (diDCP-LA-PE), which has a cognitive function improving effect and an anti-diabetes action, and which is useful as a medicine such as a therapeutic drug for dementia, a therapeutic drug for diabetes and the like.

Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;

Abstract: A method of producing a phospholene oxide is disclosed. A dihalohydrocarbylphosphine, 2-methyl-1,3-butadiene, and a halogenated hydrocarbon solvent are combined to form an adduct via an addition reaction in a homogenous system wherein the ratio of the 2-methyl-1,3-butadiene to the dihalohydrocarbylphosphine is from 1.0 to 2.0 and wherein the solvent is present in an amount of greater than 200 mL per mole of dihalohydrocarbylphosphine. The adduct is combined with alcohol and a carbonate or with a solution of metal hydroxide and water to form the phospholene oxide.

Abstract: The use of compounds of formula (1) as defined in the description, for reducing or preventing the onset of metastases in a patient suffering from cancer. Pharmaceutical compositions for using in human or veterinary medicine, including at least one compound of formula (1) are also described.

Abstract: As a novel substance having a novel skeleton, an organometallic complex with high emission efficiency which achieves improved color purity by a reduction of half width of an emission spectrum is provided. One embodiment of the present invention is an organometallic complex in which a ?-diketone and a six-membered heteroaromatic ring including two or more nitrogen atoms inclusive of a nitrogen atom that is a coordinating atom are ligands. In General Formula (G1), X represents a substituted or unsubstituted six-membered heteroaromatic ring including two or more nitrogen atoms inclusive of a nitrogen atom that is a coordinating atom. Further, R1 to R4 each represent a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms.

Abstract: Provided is a method for manufacturing a nitrogen-containing carbon alloy having a sufficiently high oxygen reduction reaction activity, a nitrogen-containing carbon alloy, and a fuel cell catalyst. The method for manufacturing a nitrogen-containing carbon alloy comprises sintering a precursor which contains a nitrogen-containing compound and an inorganic metal salt, the nitrogen-containing compound having at least one heteroaromatic ring and a conjugated heterocycle, and the conjugated heterocycle having 12 or larger number of ring-forming atoms.

Abstract: A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.

Abstract: The present invention provides, among other things, methods of purifying messenger RNA (mRNA) including the steps of (a) precipitating mRNA from an impure preparation; (b) subjecting the impure preparation comprising precipitated mRNA to a purification process involving membrane filtration such that the precipitated mRNA is captured by a membrane; and (c) eluting the captured precipitated mRNA from the membrane by re-solubilizing the mRNA, thereby resulting in a purified mRNA solution. In some embodiments, a purification process involving membrane filtration suitable for the present invention is tangential flow filtration.

Abstract: Compounds of Formula (I) are useful as modulators of glycosylation. Compounds of Formula (I) have the following structure: (I) and the definitions of the other variables are provided herein.

Abstract: The present invention relates to a compound of the following formula (I) or to a salt, hydrate, or pharmaceutically acceptable solvate thereof, in which R is a monosaccharide or disaccharide residue. The hydroxyl functions of the monosaccharide or disaccharide residue are, independently, optionally substituted for a (C1-C6) alkyl or —C(O)NH—(C1-C6) alkyl group. The invention also relates to the method for preparing said compound, to a pharmaceutical composition containing same, and to the use thereof as a drug, particularly for cancer treatment.

Abstract: The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.

Abstract: The use of metal-accumulating plants for implementing chemical reactions especially catalytical reactions.

Abstract: The present invention provides novel compounds of 11?-hydroxy steroids and compositions and their application as pharmaceuticals for preventing or reversing injury to mitochondria, for treating or preventing diseases relating to mitochondrial dysfunction or depletion, and for inducing regeneration or restructuring of mitochondria as a means of treating diseases relating to abnormalities in mitochondrial structure and function in a human or animal subject. Also disclosed herein are methods for diagnosing injury to mitochondria and for diagnosing the success or failure of therapeutics designed to treat, prevent, or reverse injury to or depletion of mitochondria.

Abstract: Glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds of the glucocorticosteroid series.

Abstract: The present invention provides technology for making large (e.g., greater than 50 amino acids), semi-synthetic, stapled or stitched proteins. The method essentially involves ligating a synthetically produced stapled or stitched peptide to a larger protein. Modified version of IL-13 and MYC are provided as illustrative examples.

Abstract: A process of refolding a recombinant protein from inclusion bodies (IBs) formed inside a host cell, is provided. The process includes homogenising a wet cells slurry to obtain a cell lysate; incubating the cell lysate with a reducing agent to obtain a reduced cell lysate; isolating reduced IBs from the reduced cell lysate to obtain isolated IBs; solubilising the isolated IBs with a denaturing agent to obtain solubilised IBs; and subjecting the solubilised IBs to a unit process of refolding to obtain a refolded recombinant protein.

Abstract: Provided herein are methods for refolding proteins that are denatured. Exemplary methods comprise solubilizing the denatured protein with a denaturing agent, e.g., a chaotropic agent, and renaturing the protein using a buffer exchanging system, e.g., tangential flow filtration (TFF).

Abstract: A method of reducing the aggregate content in a protein preparation having a target protein includes contacting the protein preparation with a thio-heterocyclic cation to form a mixture, contacting the mixture with at least one functionalized solid to remove excess thio-heterocyclic cations; and optionally contacting the mixture, simultaneously or sequentially, with at least one further functionalized solid to further reduce aggregate content of the protein preparation.

Abstract: A method for the purification of a desired protein from a protein preparation includes conditioning the protein preparation by treatment with soluble organic multivalent ions, immobilized organic multivalent ions, or both, optionally in the presence of supersaturated allantoin, thereby removing at least 90% of chromatin, then (1) precipitating the desired protein with a nonionic organic polymer in the presence of non-protein-precipitating salts at greater than physiological concentration to provide a precipitate of the desired protein; or (2) precipitating the desired protein with a nonionic organic polymer in the absence of non-precipitating salts at greater than physiological concentration to provide a precipitate and subsequently washing the precipitate with a nonionic organic polymer in the presence of non-protein-precipitating salts at greater than physiological concentration.

Abstract: The present invention provides novel and improved protein purification processes which incorporate certain types of carbonaceous materials and result in effective and selective removal of certain undesirable impurities without adversely effecting the yield of the desired protein product.

Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: A short chain polypeptide having antioxidant activity is provided. The short chain polypeptide has 2 to 4 amino acids bonded to form a polypeptide chain having an amine-terminal end and a carboxyl terminal end; wherein a net charge of the short chain polypeptide is positive, the amino terminal amino acid is an amino acid selected from the group consisting of arginine, lysine and histidine, the polypeptide chain following from the amino terminus comprises a hydrophobic or neutral amino acid, and the polypeptide chain is free of an amino acid having a negatively charged side-chain group. A method to prepare a composition having antioxidant activity and a composition having antioxidant activity are also provided.

Abstract: A method of treatment of Immune Reconstitution Inflammatory Syndrome (IRIS) in a patient is disclosed. The method comprises preparing a composition comprising a D peptide and a pharmaceutically acceptable carrier.,said D peptide further comprises the general structure: A-B-C-D-E-F-G-H in which: A is Ala, or absent, B is Ser, Thr or absent, C is Ser, Thr or absent, D is Ser, Thr, Asn, Glu, Arg, Ile, Leu, E is Ser, Thr, Asp, Asn, F is Thr, Ser, Asn, Arg, Gln, Lys, Trp, G is Tyr, and H is Thr, Ser, Arg, Gly, and All amino acids are the D stereoisomeric configuration. The composition is administered to the patient in a therapeutically effective dose and the composition acts to treat IRIS in the patient.

Abstract: The present invention relates to pharmaceutically and/or diagnostically active compounds, in particular peptide analogues (peptidomimetics), which can be reversibly controlled between an active and an inactive state by irradiation with light of different wavelengths. The present invention further relates to an intermediate compound usable in the manufacture of such pharmaceutically and/or diagnostically active compounds, as well as a manufacturing method thereof.

Abstract: The present invention provides polypeptides that cross the blood brain barrier (BBB). These polypeptides are therefore BBB transport agents. The polypeptides are typically able to cross the BBB at a level effective to be therapeutically or diagnostically useful or physiologically significant, either alone or when coupled to a therapeutic or diagnostic agent.

Abstract: Disclosed herein are polypeptides that bind to the hemagglutinin protein of influenza virus, and which can be used for treating and diagnosing influenza infection.

Abstract: The invention relates to agents and to pharmaceutical compositions for reducing the formation of amyloid and/or for promoting the disaggregation of amyloid proteins. The compositions may also be used to detect amyloid.

Abstract: Described herein are capsid proteins and adeno-associated viruses capable of targeting various types of ocular cells including bipolar and horizontal cells. Also described herein are methods of treating various ocular disorders in a subject in need thereof by administering to the subject an effective concentration of a composition comprising the recombinant adeno-associated virus (AAV) of the invention.

Abstract: The use of flagellin and flagellin related polypeptides for the protection of mammals from the effects of apoptosis is described.

Abstract: This disclosure relates to immunogenic compositions comprising mutant Streptococcus pneumonia pneumolysin (PLY) proteins. Nucleic acids, polypeptides encoded thereby, compositions containing the same, methods for using such nucleic acids, polypeptides and compositions are also provided.

Abstract: Compositions and methods for conferring pesticidal activity to bacteria, plants, plant cells, tissues and seeds are provided. In particular, methods for killing or controlling a coleopteran pest population, particularly a corn rootworm pest population, are provided. The methods include contacting the coleopteran pest with a pesticidally-effective amount of a polypeptide comprising a coleopteran toxin, particularly a corn rootworm toxin. Further included are methods for increasing yield in plants by expressing the toxin of the invention.

Abstract: Compositions and methods for conferring pesticidal activity to bacteria, plants, plant cells, tissues and seeds are provided. The toxin coding sequences can be used in DNA constructs or expression cassettes for expression in plants and bacteria. Compositions include transformed bacteria, plants, plant cells, tissues, and seeds. In particular, polynucleotide sequences and the toxin proteins encoded thereby are provided. Also provided are antibodies specifically binding to those amino acid sequences. In particular, the invention encompasses nucleotide sequences encoding fusion proteins, as well as biologically active variants and fragments thereof, wherein the fusion protein contains the C-terminal portion of SEQ ID NO:43. The fusion protein may also contain the N-terminal portion of SEQ ID NO:45.