Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Disclosed is a preparation method for a Palbociclib free base crystal form A as shown in Formula I, comprising the following steps: treating a Palbociclib free base and/or a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 35 to 100?C. to obtain a Palbociclib free base crystal form A, the water solvent being water or mixed solvent obtained by water and an organic solvent capable of being mixed and disclosed in the water. Also disclosed is a preparation method for a Palbociclib free base crystal form B, comprising the following steps: treating a Palbociclib salt compound by using an inorganic base in a water solvent at the temperature of 0 to 20° C. to obtain a Palbociclib free crystal form B, the water solvent being water or a mixed solvent obtained by water and an organic solvent capable of being mixed and dissolved in the water. The method is safe and convenient in operation and low in pollution, and facilitates industrial production.

Abstract: Imidazo[4,5-c] ring compounds of formula I, (particularly imidazo4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a guanidine substituted benzamide that is attached at the N?1 position by a linking group, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.

Abstract: The compounds of formula (I) are inhibitors of SSAO activity wherein V, W, X, Y, Z, R1 and R2 are as defined in the claims.

Abstract: The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives 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: Provided are methods of preparing compounds of Formula 201:

Abstract: The present disclosure provides a Baricitinib intermediate, a method for preparing the Baricitinib intermediate, and a method for preparing Baricitinib or a pharmaceutically acceptable salt thereof using the Baricitinib intermediate. The method for preparing the Baricitinib intermediate involves the use of a divalent palladium catalyst or a nickel catalyst and provides the Baricitinib intermediate in high yield.

Abstract: Provided are a preparation method for a chiral pyrrolopyrimidine compound and a related intermediate. In the method, a compound of formula A and a compound of formula 6 or a salt thereof are reacted to obtain a compound of formula 7 or a compound of formula 14, and a compound of formula I is prepared from the compound of formula 7 or the compound of formula 14. Also provided are the intermediate used, a preparation method for the intermediate and a use of the intermediate in the preparation of the compound of formula I. The preparation method has characteristics such as brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and a convenient post-treatment. The method avoids using an expensive asymmetric reaction catalyst, and is suitable for industrial production.

Abstract: The present invention relates to pyrazolopyrimidinone derivatives, such as those of Formula (I), that are useful as inhibitors of the activity of Wee-1 kinase.

Abstract: The present invention concerns the identification of inhibitors of ubiquitin specific protease 7 (USP7), and methods of use thereof.

Abstract: The present invention relates to 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.

Abstract: Disclosed are substituted fused hexacyclic benzimidazole derivatives of Formula (I) wherein the variables A, B, D, X, M, Q, n, p, q, Z, E, R5, and R12 are defined herein. These compounds are potent modulators of human TNF? activity and of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: Porous calcium lactate metal-organic frameworks (MOFs) comprise non-toxic metal ions—Ca(II) and non-toxic, renewable and cheap linkers—lactate and acetate. The MOFs are nontoxic and environmentally-benign, and can be used as degradable carriers.

Abstract: The present invention relates to a process for preparing halogenated pyridine derivatives of the formula (II) proceeding from compounds of the formula (I) via intermediates of the formula (IIIa) or (IIIb) where the radicals Q and W are each independently halogen, R2 is halogen or —O-pivaloyl, and Y is halogen, CO2R1 or NO2, where R1 is (C1-C6)-alkyl or (C1-C6)-haloalkyl.

Abstract: The present specification relates to a compound containing nitrogen, and a color conversion film, a backlight unit, and a display device, including the same.

Abstract: Coordinative alignment uses x-ray diffraction to precisely and unambiguously determine the structure of molecules bound or crystallized within chiral metal organic frameworks.

Abstract: The present invention provides a silicon-containing compound for resistance to hepatitis c virus infection, and in particular provides a compound represented by formula I, or a pharmaceutically acceptable salt, or a tautomer, or a stereoisomer, or a deuterated compound thereof and mixture among them, a preparation process therefor, and a pharmaceutical composition comprising the same. The present application also provides a use of the compound, or a pharmaceutically acceptable salt, or a tautomer, or a stereoisomer, or a deuterated compound thereof and mixture among them, and a pharmaceutical composition comprising the same in treatment of hepatitis c virus infection.

Abstract: Mixtures of cyclic branched siloxanes having exclusively D and T units, with the proviso that the cumulative proportion of the D and T units having Si-alkoxy and/or SiOH groups that are present in the siloxane matrix, determinable by 29Si NMR spectroscopy, is less than 2.0 and preferably less than 1.0 mole percent, are described, as are branched organomodified siloxanes obtainable therefrom.

Abstract: Provided herein are compounds of formula I: wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

Abstract: Compositions of the invention include metal-based coordination complexes, which are preferably tunable photodynamic compounds. The compositions and complexes are useful as therapeutic agents and as in vivo diagnostic agents for treating or preventing diseases including those that involve hyperproliferating cells in their etiology, such as cancer. Compositions and complexes of the invention are further capable of destroying microbial cells, such as bacteria, fungi, and protozoa, and destroying viruses. The compositions and complexes are also capable of modulating cell function in other ways.

Abstract: Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.

Abstract: The present invention relates to novel nucleoside derivatives, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer.

Abstract: The present invention is directed to modified oligonucleotides having the following Formula (I) wherein one or more of phosphate groups are substituted at phosphorus, and methods for their synthesis. The modified oligonucleotides are useful for diagnostic applications involving sequence specific recognition of a nucleic acid and for use in a method of medical treatment.

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I?), or of general formula (I?), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

Abstract: A compound and pharmaceutically acceptable salts thereof for treating cancer, having a structure represented by the following formula (I) or formula (II): in which X and Y each individually represent: R1, R2, R3, R4, and R5 individually represents hydrogen atom, acyl having 20 or less carbon atoms, alkyl having 20 or less carbon atoms, alkanoyl having 20 or less carbon atoms, aroyl having 20 or less carbon atoms, aryl having 20 or less carbon atoms, aralkyl having 20 or less carbon atoms, sulfonyl having 20 or less carbon atoms, phosphonyl having 20 or less carbon atoms, or haloacyl having 20 or less carbon atoms.

Abstract: In various embodiments methods and compositions to increase the rate and/or activity of ligation reactions catalyzed by a sortase. In certain embodiments reagents are provided that comprises, inter alia, a polypeptide comprising an amino terminal polyglycine sequence comprising at least three contiguous Gly residues (e.g., a triglycine sequence, a tetraglycine sequence, a pentaglycine sequence, etc.) followed by a peptide that is to be ligated to a moiety followed by a sequence comprising the catalytic domain of a Sortase A enzyme.

Abstract: To provide an affinity support in which a binding property of a ligand to a target substance is improved. The affinity support contains a solid phase support and a protein ligand, wherein the protein ligand is represented by formula (1): R—R1 (1) wherein R represents a linker binding to the solid phase support, which contains a polyproline, and R1 represents a protein showing an affinity to immunoglobulin, and the R is bound to a C terminal or an N terminal of an amino acid sequence in R1.

Abstract: The present invention provides compounds that can modulate opioid receptors. Some compounds of the invention are modulators of ?- and/or ?-opioid receptors. Still other compounds of the invention are opioid receptor antagonists. Some compounds of the invention can modulate opioid receptors with a significantly less likelihood of developing addiction or abuse compared to conventional opioid ligands, such as morphine. In particular, compounds of the invention are of the formula: wherein Ar1 is H, optionally substituted aryl or optionally substituted heteroaryl; R1 is a heteroalkyl; R2 is alkyl; R3 is an oligopeptide or a moiety of the formula —R4—Y; R4 is alkylene; Y is optionally substituted heteroaryl, optionally substituted aryl or a moiety of the formula —C(?X2)—X3—R5; each of X1, X2 and X3 is independently O, NR6 or S; and each of R5 and R6 is independently H or alkyl.

Abstract: Provided are a polypeptide having the activity of inhibiting autophagy in a cell, a composition for inhibiting autophagy in a cell, and particularly in a tumor cell, containing the polypeptide as an active ingredient, and a pharmaceutical composition containing the polypeptide, and more specifically, a composition for inhibiting autophagy in a cell containing a polypeptide inhibiting the control mechanism of autophagy as an active ingredient, and a pharmaceutical composition for preventing or treating a neoplastic disease or for inhibiting resistance to anticancer agents, containing the polypeptide.

Abstract: Peptides of 5 to 14 amino acids in length that stimulate subcutaneous adipogenesis and uses thereof are provided.

Abstract: A peptide can have a sequence of one of SEQ ID NOs: 78-91. A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion having a peptide sequence of one of SEQ NOs: 78-97. A cell-targeting compound can include a conformationally-constrained kinked peptide having a peptide sequence of one of SEQ ID NOs: 78-97. The peptide sequence can be one of SEQ ID NOs: 78-97, or 78-91, or 92-97. A cell-targeting compound can include a conformationally-constrained kinked peptide linked to a branched linker with one branch arm linked to a specific targeting moiety and one branch arm linked to a general targeting moiety. The specific targeting moiety can be an antibody. The general targeting moiety can be a lipid or cholesterol derivative.

Abstract: Polypeptides that bind to viral hemagglotinin are disclosed and methods for their use in treating or limiting influenza infection, and diagnosing influenza infection.

Abstract: An immunogenic fusion protein includes at least the following two peptides a) —on the C-terminal side, a first peptide constituted of: —the amino acid sequence of the protein S or the protein M of a human hepatitis B virus (HBV) isolate, which protein S or protein M is optionally deleted at the N-terminal end thereof, and b) —on the N-terminal side, a second peptide constituted of: —the sequence of amino acids of at least one transmembrane domain and the ectodomain of at least one protein of a Zika virus isolate selected from the envelope protein E or a fusion peptide including the envelope protein E and the protein prM.

Abstract: The present invention relates to compositions and methods for the prevention and treatment of Borrelia infection. Particularly, the present invention relates to a polypeptide comprising a hybrid C-terminal fragment of an outer surface protein A (OspA), a nucleic acid coding the same, an antibody specifically binding the same, a pharmaceutical composition (particularly for use as a medicament or in a method of treating or preventing a Borrelia infection) comprising the polypeptide and/or the nucleic acid and/or the antibody, a method of treating or preventing a Borrelia infection and a method of immunizing a subject.

Abstract: The present embodiments provide for an immunogenic multiple antigen presenting system comprising a polymer to which antigens are associated by complementary affinity molecules. For example, the polymer can be a polysaccharide, or antigenic polysaccharide, to which protein or peptide antigens from the same or different pathogens are indirectly linked. The present immunogenic compositions can elicit both humoral and cellular immune responses to one or multiple antigens at the same time.

Abstract: The present invention relates to a mutated immunoglobulin-binding protein having increased alkaline tolerance and, more specifically, to an immunoglobulin-binding protein in which, with respect to the A-domain of Staphylococcal protein A, or a functional variant thereof, an amino acid at a specific site is mutated and thereby exhibits an increased chemical stability at an alkaline pH value in comparison to a parental molecule. The present invention can provide an antibody-purifying immunoglobulin-binding protein ligand and matrix which have enhanced alkaline tolerance and accordingly enhanced stability in multiple times of alkaline cleaning.

Abstract: The present disclosure provides genetically modified Chlorella sorokiniana. DAD1 gene is overexpressed in wild type Chlorella sorokiniana to obtain the genetically modified Chlorella sorokiniana. The genetically modified Chlorella sorokiniana is characterized by increased biomass, increased carrying capacity, reduced clumping, and increased stress tolerance to ultraviolet light and high light intensity, as compared to the wild type Chlorella sorokiniana. The genetically modified Chlorella sorokiniana can be used for the production of industrially important products.

Abstract: Provided are isolated polypeptides, isolated polynucleotides encoding same, nucleic acid constructs comprising same, transgenic cells expressing same, transgenic plants expressing same and method of using same for increasing yield, abiotic stress tolerance, growth rate, biomass, vigor, oil content, photosynthetic capacity, seed yield, fiber yield, fiber quality, fiber length, early flowering, grain filling period, harvest index, plant height, and/or nitrogen use efficiency of a plant.

Abstract: A system, including methods and compositions, for treatment of ischemia.

Abstract: The present invention provides compositions and methods of treating various disorders associated with aberrant cell growth.

Abstract: This invention provides for a fusion protein between an IL2??? Selective Agonist protein (IL2 Selective Agonist) and a IgG Fc protein using a linker. The IL2 Selective Agonist moiety provides a therapeutic activity by selectively activating the IL2??? form of the receptor, thus selectively stimulating Tregs. The Fc moiety provides a prolonged circulating half-life compared to the circulating half-life of IL-2 or an IL2SA protein.

Abstract: The present invention relates to amylin analogs and to their use in the treatment or prevention of a variety of diseases, conditions or disorders, including obesity, excess food intake and associated metabolic diseases such as diabetes. The analogs have good physical and chemical stability, good solubility, and a long duration of action, and are well suited for use in the form of a liquid formulation.

Abstract: Amylin receptor antagonists capable of binding to the amylin receptor and inhibiting activity of amylin or amyloid-beta protein are provided. The amylin receptor antagonists can be administered in the form of pharmaceutical compositions or the like. Methods for preparing and using the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease are also provided.