Abstract: The present invention covers Pyrazolopyrimidine compounds of general formula (I): in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).

Abstract: The present invention relates to a method for preparing a pyrrolo[3,2-d]pyrimidine compound (the compound represented by formula I), and corresponding intermediates.

Abstract: A novel monothioglycoluril compound and a novel dithioglycoluril compound. A thioglycoluril compound of the following Formula (1): (wherein X is an oxygen atom or a sulfur atom, and four Rs are each a hydrogen atom, a linear, branched, or cyclic alkyl group having a carbon atom number of 1 to 4, a phenyl group, a naphthyl group, a benzyl group, or a C3-9 alkyl group having at least one ether bond on the main chain).

Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Abstract: The disclosure provides compounds of Formulae (I)-(IX). The disclosed compounds are capable of inhibiting a mammalian SHMT. Compounds of the disclosure have numerous uses, such as for treatment of cancer or autoimmue disorders.

Abstract: The present disclosure relates to solid forms of 3-(5-Fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo [4,5-f]indol-7-yl) pyrrole-2,5-dione, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof in treating disease.

Abstract: The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention relates to: a novel merocyanine-based compound which exhibits a fluorescence signal at a visible light region of at least 380 nm, and which may be used for detecting biomolecules; and a biomolecular labeling dye, kit and contrast agent composition comprising the same.

Abstract: The invention is directed to a process for the continuous preparation of a cycloadduct product from the reaction of a furanic with a dienophile, comprising heating a first liquid feed stream comprising the dienophile and a solvent in which the dienophile is dissolved; providing a second liquid feed stream comprising the furanic; leading the first liquid feed stream and the second liquid feed stream into a continuous reactor to produce a product solution stream comprising the cycloadduct product; and leading the product solution stream to an product isolation zone to produce an isolated cycloadduct product. A further aspect of the invention is an apparatus for carrying out this reaction.

Abstract: The present invention relates to novel substituted dihydrothienopyrimidines with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Abstract: The present disclosure provides for compounds of Formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).

Abstract: An object of the present invention is to provide a compound and a pharmaceutical composition which exhibit strong antibacterial activity against Gram-negative bacteria and drug-resistant Gram-negative bacteria. According to the present invention, a compound represented by General Formula [1] (the reference signs in the formula have the same definitions as those described in the present specification) or a salt thereof has strong antibacterial activity against Gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant Gram-negative bacteria including multidrug-resistant Pseudomonas aeruginosa, and the pharmaceutical composition containing the compound or a salt thereof is useful as an antibacterial agent.

Abstract: The invention relates to hydrocarbon-soluble halogen or thiolate/magnesium exchange reagents of the general formula R1MgR11?n(OR3)n·LiOR2·(1?n)LiOR3·aDonor in which: R1 is a C1-C8 alkyl and OR2 as well as OR3 are same or different and represent primary, secondary, or tertiary alkoxide residues having 3 to 18 carbon atoms, wherein R2 and/or R3 can for their part contain an alkoxy substituent OR4; a assumes a value of 0 to 2, n assumes a value between 0 and 1, and the donor is an organic molecule containing at least 2 nitrogen atoms.

Abstract: The present invention relates to solid forms of a substituted benzoxaborole compound, specifically crystalline forms of a compound of formula I, compositions comprising crystalline forms of the compound of formula (I), and methods of their use.

Abstract: The purification of monoalkyl tin trialkoxides and monoalkyl tin triamides are described using fractional distillation and/or ultrafiltration. The purified compositions are useful as radiation sensitive patterning compositions or precursors thereof. The fractional distillation process has been found to be effective for the removal of metal impurities down to very low levels. The ultrafiltration processes have been found to be effective at removal of fine particulates. Commercially practical processing techniques are described.

Abstract: The present disclosure relates to a method that includes treating a liquid that includes a first precursor at a concentration C1, a second precursor at a concentration C2, a third precursor at a concentration C3, and an additive at a concentration C4, where the treating results in a perovskite, each of C1, C2, and C3 are between 0.

Abstract: The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.

Abstract: A process is provided for preparing a salt of a hydroxy-substituted di-ester of phosphoric acid, comprising: (a) reacting a phosphating agent with a monohydric alcohol and with a propylene glycol, wherein the mole ratio of monohydric alcohol : propylene glycol is greater than about 4:1 and wherein an excess of the phosphating agent is employed such that the product mixture formed thereby contains phosphorus acid functionality; and (b) reacting the product mixture of step (a) with an amine. The product is useful as an antiwear agent.

Abstract: The invention provides compounds of the formula: R1 is OR11, or NR5R5?; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(?O)R6, O(C?O)R6 or O(C?O)OR6; R5? is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.

Abstract: Described herein is photocaging methodology using ruthenium (II) complexes with 7-deazahypoxanthine-based anticancer agents. Specifically, 7-deazahypoxanthines are converted into photoactivatable chemotherapeutic agents for the controlled release of these toxic agents selectively into tumor tissue upon irradiation with light.

Abstract: This invention relates generally to olefin metathesis catalysts comprising aniline type ligands, to the preparation of such catalysts, compositions comprising such catalysts, methods of using such catalysts, and the use of such catalysts in the metathesis of olefins. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and in industrial applications such as oil and gas, fine chemicals and pharmaceuticals.

Abstract: A series of functionalized imidazophenthridine analogue-based blue phosphorescent emitters have been designed, where bulky substituents (e.g., tetrabutyl, phenyl, mesityl, triisopropylbenzene, etc.) are introduced on an imidazophenthridine fragment of the emitters. Bulky substituents may suppress potential excimer formation, as well as improve the solubility of the complexes. This class of emitters may be utilized in luminescent labels, emitters for organic light emitting devices, and lighting applications.

Abstract: A method for preparing a biflavone-iron complex, includes using the amentoflavone as the ligand and the ferric ion as the central ion, the amentoflavone-iron complex is obtained by reaction, and the structure of the complex is characterized by infrared spectroscopy, UV-vis absorption spectroscopy and high resolution mass spectrometry. Meanwhile, the antitumor and antioxidant activities of the amentoflavone-iron complex are studied in the present invention. MTT method shows that the amentoflavone-iron complex has a relatively good antitumor activity, and the antitumor activity thereof is stronger than that of the amentoflavone. Pyrogallol auto-oxidation method and ABTS method show that the antioxidative activity of the amentoflavone-iron complex is stronger than that of the amentoflavone itself.

Abstract: A method for preparing a biflavone-cobalt complex includes using the amentoflavone as the ligand and the cobalt ion as the central ion, the amentoflavone-cobalt complex is obtained by reaction, and the structure of the complex is characterized by infrared spectroscopy, UV-vis absorption spectroscopy and high resolution mass spectrometry. Meanwhile, the antitumor and antioxidant activities of the amentoflavone-coablt complex are studied in the present invention. MTT method shows that the amentoflavone-cobalt complex has better antitumor activity, and the antitumor activity thereof is stronger than that of the amentoflavone. Pyrogallol auto-oxidation method, ABTS method and FRAP method show that the antioxidan activity of the amentoflavone-cobalt complex is stronger than that of the amentoflavone itself. The formation of the flavonoid-cobalt complex enhances the antitumor and anti-oxidation activities of the amentoflavone, and is expected to be used in the development of drugs.

Abstract: An exemplary embodiment presents a method of lignin extraction from lignocellulosic biomass. Lignin is a rich and economical source of various valuable products. It is a platform chemical for renewable biofuels, composite materials, biofilms etc. Delignification of lignocellulosic biomass affords cellulose-rich material as an additional product that is already known for many applications like bioethanol and other chemicals. The method includes grinding the lignocellulosic biomass, mixing the dried lignocellulosic biomass powder with ionic liquid, stirring and heating of the mixture followed by solvent extraction of lignin from the mixture.

Abstract: The present application relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, and intermediates thereto. The application also provides pharmaceutical compositions comprising compounds of the present invention and methods of using said compounds or compositions in the treatment of and immunization for infectious diseases.

Abstract: Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.

Abstract: Systems and methods of making lactobionic acid are described. The systems include two-compartment cation bipolar electrodialysis assemblies having at least one cell that includes a cation ion-exchange membrane and a bipolar membrane. The membranes define the borders of a pair of flow channels for a separate (i) caustic stream and (i) purified lactobionic acid stream. Lactobionate ions in the lactobionic acid stream do not cross a membrane in the electrodialysis assembly, which reduces membrane fouling. The methods include passing a lactobionate salt through a two-compartment cation bipolar electrodialysis assembly. The electrodialysis assembly includes at least one two-compartment cation bipolar membrane cell, and separates the lactobionate salt into a caustic compound and the lactobionic acid. The assembly is designed so the lactobionate ions do not cross an ion exchange membrane in the assembly to form the lactobionic acid, which reduces membrane fouling.

Abstract: The present invention provides a method of preventing or treating atherosclerosis or a symptom thereof comprising administering to a subject in need thereof a specific inhibitor of neuraminidase 1 (neu1); neuraminidase 3 (neu3); or a bispecific inhibitor of neu1 or neu3 of formula I; (I) and a compound of formula I.

Abstract: Provided are a long-acting prodrug of Entecavir, preparation method and use thereof, wherein the prodrug of Entecavir has a structure of formula I. The prodrug of Entecavir can be released slowly, sustainably and steady, and converted to active compound of Entecavir to achieve a long-acting effect.

Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to methods and novel intermediates useful in the preparation of a compound or a pharmaceutically acceptable salt thereof. An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.

Abstract: The invention relates to methods for preparing a compound comprising a peptide attached to a molecular scaffold whereby multiple peptide loops are formed, to compounds that can be obtained with such methods and uses thereof.

Abstract: The present invention concerns a method of storing a separation matrix comprising multimers of immunoglobulin-binding alkali-stabilized Protein A domains covalently coupled to a porous support. The method comprises the steps of: a) providing a storage liquid comprising at least 50% by volume of an aqueous alkali metal hydroxide solution; b) permeating the separation matrix with the storage liquid; and c) storing the storage liquid-permeated separation matrix for a storage time of at least days.

Abstract: The present disclosure involves optimized methods for production of hiologically active proteins termed optimally manufactured stradomers. The present disclosure further provides compositions and methods useful in the treatment of diseases and conditions including autoimmune diseases, inflammatory diseases, or infectious diseases.

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

Abstract: The present invention provides a peptide of formula (I), or a pharmaceutically acceptable salt thereof, wherein the N-terminal group of the peptide is a monoradical of formula —NHR1; the C-terminal group of the peptide is a monoradical of formula —C(O)—R2; R1 is a monoradical selected from hydrogen and —C(O)—(C1-C20)alkyl; R2 is a monoradical selected from —OH and —NR3R4 radical; R3 and R4 are independently selected from hydrogen and (C1-C10)alkyl; “a” to “j” are integers from 0 to 1, provided that at least one of “a” to “j” is 1; and X1 represents any amino acid. The present invention also provides conjugates and compositions comprising the peptide of formula (I).

Abstract: Disclosed herein is a cell death-inducing peptide that rapidly acts. The peptide is derived from Noxa protein and comprises 16 amino acid residues including MTD. The peptide is designated extended MTD (eMTD) because it contains the 10-mer MTD. eMTD rapidly exhibits potent necrotic cell death in various cell lines and, as such, can be applied to the treatment of various diseases including cancer when used in conjugation with peptides or materials for targeting specific cells.

Abstract: The present invention provides methods for guiding preservation of human neurons or human nerves during surgery by administering a fluorescently-labeled peptide that specifically binds to the human neurons or human nerves. The invention further provides human neuron or nerve targeting molecules comprising fluorescently-labeled peptides that specifically bind to human neurons or human nerves and compositions thereof.

Abstract: The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of ?4?7 to the mucosal addressing cell adhesion molecule (MAdCAM) in vivo.

Abstract: Disclosed are protein switches that can sequester bioactive peptides and/or binding domains, holding them in an inactive (“off”) state, until combined with a second designed polypeptide called the key, which induces a conformational change that activates (“on”) the bioactive peptide or binding domain, components of such protein switches, and their use.

Abstract: The present invention relates to a polypeptide comprising a mutant fragment of an outer surface protein A (OspA), a nucleic acid coding the same, a pharmaceutical composition (particularly for use as a medicament of in a method of treating or preventing a Borrelia infection) comprising the polypeptide and/or the nucleic acid, a method of treating or preventing a Borrelia infection and a method of immunizing a subject.

Abstract: The present invention is directed to novel polynucleotides, polypeptides, and polyproteins of Mycoplasma surface proteins, all of which are useful in detecting infection and for the preparation of vaccines for treating and preventing diseases in swine and other animals. Vaccines provided according to the practice of the invention are effective against Mycoplasma infections. Detection and therapeutic polyclonal and monoclonal antibodies are also a feature of the present invention. Assays, kits, systems, and nanoparticle encapsulated compositions related to the polynucleotides, polypeptides, polyproteins, antibodies or fragments, derivatives, and variants thereof are also disclosed.

Abstract: The invention features engineered probiotic lacto acid bacteria (LAB) expressing a chimeric Clostridium difficile/Lactobacillus acidophilus SlpA, or fragment thereof, and its use for the treatment or prevention of Clostridium difficile infection and gut colonization.

Abstract: The present invention provides a modified botulinum neurotoxin A (BoNT/A) L-chain protease that demonstrates enhanced cleaveage of human SNAP-23 (hSNAP-23) relative to unmodified (wild-type) BoNT/A L-chain protease, together with the use thereof for cleaving hSNAP-23.

Abstract: The present invention relates to nanostructured proteins, more specifically to fusion proteins suitable for their selective delivery to specific cell and tissue types. It also relates to nanoparticles comprising such nanostructured proteins, as well as nucleic acids, vectors, cells that comprise said proteins, and the therapeutic uses thereof.

Abstract: Disclosed herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is part of the E3 ligase complex and the protein is modified to alter the substrate recognition of the E3 ligase complex. In some instances, also provided herein are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the protein is modified or tagged for degradation. In some instances, additionally provided herein are cysteine-containing protein binding domains that interact with a probe and/or a ligand described herein.

Abstract: Disclosed are knottin peptides containing non-natural amino acids so that they can be formed by chemical conjugation into two or more knottin monomers. The knottin monomers comprise a non-natural amino acid such as an aminooxy residue within the polypeptide sequence. The exemplified dimers were produced by oxime formation between two aldehyde groups present on a polyether linker and an aminooxy functional group that was site-specifically incorporated the knottin. Knottins variants based on EETI (Ecballium elaterium trypsin inhibitor) and AgRP (Agouti-related protein) were engineered to contain integrin-binding loops. These dimers were shown to have increased binding strength to integrins on U87MG tumor cells, achieving significant increases in inhibition of cell adhesion and proliferation. Also disclosed are knottin monomers comprising an aminooxy residue; these may be conjugated to molecules such as doxorubicin.