Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.

Abstract: Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I): and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of CCR2 receptors.

Abstract: Solid forms of Compound I (and its S-enantiomer, Compound II), active on protein kinases, were prepared and characterized: Also provided are methods of using the solid forms.

Abstract: Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P1 and P2 are as defined in this disclosure.

Abstract: A process for preparation of a compound of Formula (I) is disclosed.

Abstract: The present invention provides compounds of Formula (V): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention is directed to a process for the preparation oxymorphone freebase, comprising hydrogenation of 14-hydroxymorphinone in DMF, to yield oxymorphone freebase, preferably oxymorphone freebase of improved appearance, purity and/or yield. The present invention is further directed to oxymorphone freebase with improved impurity profile. The present invention is further directed to an HPLC or UPLC system/method for analysis of opioid compounds.

Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.

Abstract: A method for preparing 9-allylcamptothecin derivatives using compound 14 as an essential intermediate. The total yield of the method is high.

Abstract: Provided are taxanes compounds having the structure of formula I, preparation method thereof, and uses of compositions having the compound, pharmaceutical salts and solvates thereof as active ingredients in the preparation of oral antitumor drugs. In the formula, R1 is —COR6, —COOR6, and —CONR7aR7b; R2 is C1-C6 alkyl, C1-C6 alkenyl group, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6, and —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b, H, and OH; R6 is C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl group, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; and R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group.

Abstract: The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein A, Y, Z, X1, X2, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Abstract: A coloring composition containing one or more species of compounds represented by Formula (I) or Formula (II) below, wherein each of R1 and R2 represents a hydrogen atom or substituent, each of Ar1 to Ar8 independently represents an optionally substituted aromatic hydrocarbon group or optionally substituted heterocyclic group, and each of L1 and L2 independently represents a divalent linking group which interrupts ? electron conjugated system:

Abstract: The present disclosure provides an energy storage molecular material, crystal dielectric layer and capacitor which may solve a problem of the further increase of volumetric and mass density of reserved energy associated with some energy storage devices, and at the same time reduce cost of materials.

Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.

Abstract: A description is given of a process for preparing 1-indanols and 1-indanamines by palladium-catalyzed arylation and of the use thereof as intermediates for the synthesis of fine chemicals and of active agrochemical ingredients.

Abstract: The invention relates to novel silane-modified formamides and/or pre-polymers for bonding and/or sealing diverse substrate materials, such as, for example metal, wood, glass and/or plastic, The invention also relates to a reactive single-component adhesive system comprising the claimed silane-modified formamide and/or pre-polymers.

Abstract: The invention relates to novel silane-modified formamide-polymers and/or pre-polymers for bonding and/or sealing diverse substrate materials, such as, for example metal, wood, glass and/or plastic. The invention also relates to a reactive single-component adhesive system comprising the claimed silane-modified formamide polymers.

Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.

Abstract: An object of the present invention is to provide a compound which is capable of attaining a composition having high storage stability without reacting with a base-reactive compound, even in the case of storage for a long period of time in a mixed state with the base-reactive compound, such as an epoxy-based compound, as well as capable of generating a strong base (guanidines, biguanides, phosphazenes or phosphoniums) by irradiation of light (active energy rays) or heating; a base generator comprising the compound; and a base-reactive composition comprising the base generator and the base-reactive compound. The present invention relates to the compound represented by the general formula (A); the base generator comprising the compound; and the base-reactive composition comprising the base generator and the base-reactive compound.

Abstract: There are provided compounds of formula I. wherein R1 to R5, X1, X2, Ar, L, A, A1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.

Abstract: The present invention discloses a method for purifying oxidized form of ?-nicotinamide adenine dinucleotide, comprising the steps of: sequentially microfiltrating and nanofiltrating a reaction solution obtained after an enzymatic reaction by using filteration membranes, to collect a concentrate for use; then adding an acid to the concentrated filtrate, to adjust the pH of the concentrate, and purifying by gradient elution using a reverse-phase chromatographic column as a stationary phase, a buffer solution as a phase A, and ethanol as a phase B; and concentrating the purified solution by nanofiltrating it with a filtration membrance, and then freeze drying it in a vacuum freeze drier. In the present invention, the oxidized form of ?-nicotinamide adenine dinucleotide is purified by reverse phase high performance liquid chromatography, such that the oxidized form of ?-nicotinamide adenine dinucleotide has a high purity and high yield, thus meeting the requirements in industry.

Abstract: The present invention discloses an oxidized form of ?-nicotinamide adenine dinucleotide phosphate and a method for purifying the same. The method comprises specifically the steps of: a. sequentially microfiltrating and nanofiltrating a pretreated coenzyme II solution with membrane concentration devices, to obtain a concentrated crude product solution; b. adjusting the obtained crude product solution to pH 2-4, loading it onto a preparative reverse phase high performance liquid chromatographic column, and purifying by gradient elution, to obtain a purified sample solution; and c. nanofiltrating the purified sample solution with a membrane concentration device, and freeze drying it in a vacuum freeze drier, to obtain a purified coenzyme II. The coenzyme II prepared in the present invention has a high purity, a high yield, and thus a promising prospect in the market.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.

Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.

Abstract: The present invention discloses a method for purifying reduced form of ?-nicotinamide adenine dinucleotide, comprising the steps of: sequentially microfiltrating and nanofiltrating a reaction solution obtained after an enzymatic reaction, to collect a concentrate for use; then adding an ion pair reagent to the concentrate, and purifying by gradient elution using a reverse-phase chromatographic column as a stationary phase, a buffer solution as a phase A, and ethanol as a phase B; changing the cations in the purified filtrate into sodium ions by using a cation exchange resin; and nanofiltrating the filtrate obtained in Step c, and finally freeze drying it in a vacuum freeze drier. In the present invention, the reduced form of ?-nicotinamide adenine dinucleotide is purified by reverse phase high performance liquid chromatography and cation exchange, such that the reduced form of ?-nicotinamide adenine dinucleotide has a high purity and high yield, thus meeting the requirements in industry.

Abstract: The present invention is directed to RNA monomers comprising O-acetal levulinyl protecting groups at the 2? and/or the 5?-hydroxy functionalities of the ribose moiety. Said monomers may be incorporated into oligoribonucleotides or RNA polynucleotides. Furthermore, the invention is directed to methods for the synthesis of said RNA monomers, oligoribonucleotides and RNA polynucleotides, as well as methods for their deprotection and methods for the use of said compounds and compositions comprising said compounds. In particular, such compounds and compositions comprising them are used in methods for light-directed synthesis of RNA microarrays.

Abstract: (3?,9?,10?,13?,14?,17?,20S,22E)-Ergosta-5,7,22-trien-3-ol. A method for preparing the same by drying a fruiting body of Cordyceps militaris, grinding the fruiting body to yield ultrafine powders; boiling and extracting the ultrafine powders, centrifuging and collecting a precipitate. A method for treating a tumor by administering to a patient in need of treating a tumor (3?,9?,10?,13?,14?,17?,20S,22E)-ergosta-5,7,22-trien-3-ol.

Abstract: Disclosed is a method for refolding recombinantly produced polypeptides comprising the steps of (a)providing inclusion bodies comprising recombinantly produced polypeptides comprising the recombinantly produced polypeptides, (b)dissolving the inclusion bodies under chaotropic conditions in so as to obtain denatured recombinantly produced polypeptides, and (c)refolding the denatured recombinantly produced polypeptides inclusion bodies by addition of a refolding buffer,so as to obtain refolded re-combinantly produced polypeptides, and (d) further processing the refolded recombinantly produced polypeptides by at least one processing step, wherein at least steps (c) and (d) are performed in a tubular reactor in a continuous manner.

Abstract: The invention provides a process for the separation of pea protein. The process begins with an aqueous extract or solution of pea protein, which is passed through at least one expanded bed absorption (EBA) process. The EBA process comprises contacting the aqueous extract or solution of pea protein with at least one adsorbent resin, said adsorbent resin comprising at least one ligand (L1 or L2), having particular chemical structures. Proteins of interest are isolated by eluting them from said adsorbent resin. The invention also provides various protein compositions obtainable via the method of the invention.

Abstract: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.

Abstract: The present invention relates to the field of molecular biochemistry and medicine, and in particular to ligands comprising modified amino acid residues, targeting the amyloid-? peptide associated with Alzheimer's disease for prevention of aggregation, neurotoxicity and use thereof as drugs for treatment of Alzheimer's disease.

Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.

Abstract: The present technology provides peptides, methods of generating the peptides, and pharmaceutically acceptable salts of the peptides. In some embodiments, the peptide is D-Arg-2?6?-Dmt-Lys-Phe-NH2.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Abstract: There is described a material comprising tapes, ribbons, fibrils or fibres characterized in that each of the ribbons, fibrils or fibres have an antiparallel arrangement of peptides in a ?-sheet tape-like substructure wherein the material comprises a pair of self assembling complementary polypeptides.

Abstract: The present invention provides mutant adeno-associated virus (AAV) that exhibit altered capsid properties, e.g., reduced binding to neutralizing antibodies in serum and/or altered heparin binding and/or altered infectivity of particular cell types. The present invention further provides libraries of mutant AAV comprising one or more mutations in a capsid gene. The present invention further provides methods of generating the mutant AAV and mutant AAV libraries, and compositions comprising the mutant AAV. The present invention further provides recombinant AAV (rAAV) virions that comprise a mutant capsid protein. The present invention further provides nucleic acids comprising nucleotide sequences that encode mutant capsid proteins, and host cells comprising the nucleic acids. The present invention further provides methods of delivering a gene product to an individual, the methods generally involving administering an effective amount of a subject rAAV virion to an individual in need thereof.

Abstract: The present invention relates to Shiga toxin effector polypeptides with reduced antigenic and/or immunogenic potential. Immunogenicity can be a limitation for the repeated administration to mammals of proteins and polypeptides derived from Shiga toxins. The Shiga toxin effector polypeptides of the present invention have uses as components of therapeutics, diagnostics, and immunization materials. The cytotoxic proteins of the present invention have uses for selective killing of specific cell types and as therapeutics for the treatment of a variety of diseases, including cancers, immune disorders, and microbial infections. The proteins of the present invention also have uses for detecting specific cell types, collecting diagnostic information, and monitoring the treatment of a variety of diseases, such as, e.g., cancers, immune disorders, and microbial infections.

Abstract: This disclosure describes fusion polypeptides and complexes, compositions, and methods involving the fusion polypeptides. Generally, the fusion polypeptides include at least a portion of a protein of interest and at least a functional portion of a HUH polypeptide. Generally, the functional portion of a HUH polypeptide includes at least a portion of a Rep/relaxase domain that includes at least one catalytic polar amino acid residue and at least one metal-coordinating amino acid residues.

Abstract: The present application discloses a method of growing or proliferating nerve cells by contacting the cells with phosphatase and tensin homolog (PTEN) lipid phosphatase inhibiting peptide.

Abstract: Provided herein are SIRP-gamma, SIRP-beta or SIRP-beta2 decoy polypeptides for immunotherapy and/or treatment of cancer, anemia, transplant, asthma, allergy, auto-immune disease, and viral infection.

Abstract: The present invention provides isolated peptides or the fragments derived from SEQ ID NO: 45, which bind to an HLA antigen and induce cytotoxic T lymphocytes (CTL). The peptides may include the above mentioned amino acid sequence with substitution deletion, or addition of one, two, or several amino acids sequences. The invention also provides pharmaceutical compositions including these peptides. The peptides of this invention can be used for diagnosing or treating cancer.

Abstract: The invention relates to novel TNF family ligand trimer-containing antigen binding molecules comprising (a) at least one moiety capable of specific binding to a target cell antigen, (b) a polypeptide comprising three ectodomains of a TNF ligand family member or fragments thereof that are connected to each other by peptide linkers and (c) a Fc domain composed of a first and a second subunit capable of stable association, and to methods of producing these molecules and to methods of using the same.

Abstract: Single chain insulin analogs are provided having high potency and specificity for the insulin receptor. As disclosed herein optimally sized linking moieties can be used to link human insulin A and B chains, or analogs or derivatives thereof, wherein the carboxy terminus of the B25 amino acid of the B chain is linked to the amino terminus of the A1 amino acid of the A chain via the intervening linking moiety. In on embodiment the linking moiety comprises a polyethylene glycol of 6-16 monomer units and in an alternative embodiment the linking moiety comprises a non-native amino acid sequence derived form the IGF-1 C-peptide and comprising at least 8 amino acids and no more than 12 amino acid in length. Also disclosed are prodrug and conjugate derivatives of the single chain insulin analogs.

Abstract: Disclosed are methods and compositions that employ FKBP-L polypeptides for modulating angiogenesis and/or tumor metastasis. The FKBP-L polypeptides may be used for the treatment of disorders mediated by angiogenesis such as cancer.

Abstract: Disclosed are methods and compositions that employ FKBP-L polypeptides for modulating angiogenesis and/or tumor metastasis. The FKBP-L polypeptides may be used for the treatment of disorders mediated by angiogenesis such as cancer.

Abstract: Provided is a method for determining a TCR polypeptide chain that can form a TCR specific for a peptide of interest. Also provided are methods and compositions for producing a cell expressing a T cell receptor (TCR) specific for a peptide of interest, methods and compositions for producing a TCR chain nucleic acid and/or pair of TCR chain polypeptides and/or nucleic acids encoding a TCR, a cell population comprising the cell harboring the nucleic acids encoding a TCR obtained by said method, and a method for treating a disorder comprising administering to the subject said cell population.

Abstract: A T cell receptor molecule (TCR) containing an alpha chain portion and a beta chain portion wherein the alpha chain portion contains three complementarity determining regions (CDRs): CDR1?: SSYSPS CDR2?: YTSAATL CDR3?: VVSPFSGGGADGLT or comprising or consisting of SPFSGGGADGLT and the beta chain portion contains three complementarity determining regions (CDRs): CDR1?: DFQATT CDR2?: SNEGSKA CDR3?: comprising SARDGGEG or comprising or consisting of RDGGEGSETQY, or wherein up to three amino acid residues in one or more CDRs are replaced by another amino acid.