Abstract: A compound having anticancer activity, or a pharmaceutically acceptable salt thereof is provided. Used is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: (wherein, L1 and L2 are the same or different and each represents a group represented by one formula selected from the group consisting of formulas (A) to (F), and S represents a group represented by one formula selected from the group consisting of formulas (S1) to (S18)).

Abstract: An isoindolinone compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof can be used in the treatment of proliferative diseases. A pharmaceutical composition contains the compound or the salt thereof and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to a compound of formula (I) wherein n is 1 or 2, R1 is halogen, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, ethynyl, propargyl, or (C3-C6)cycloalkyl, or two R1 form a cyclopentane ring fused to the phenol; R2 and R3 represent H, cyano, ethynyl, propargyl, (C1-C4)alkyl, hydroxy(C1-C4)alkyl or a halo(C1-C4)alkyl, or R2 and R3 form together with the atoms connecting them a (C5-C6)carbocyclic ring fused to the pyridazine ring; R4 and R5 form together with N to which they are attached an optionally substituted 3-7 membered monocyclic heterocycloalkyl ring, 8-11 membered bicyclic heterocycloalkyl ring or 7-12 membered bicyclic heterocyclic spiro ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for treating for example Parkinson's disease or frontotemporal Dementia.

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Abstract: Compounds and pharmaceutical compositions for use in the treatment of a disorder or disease mediated by the mTOR pathway through more selective binding to FKBP12 of the group of FK506 binding proteins (FKBPs) are disclosed. With an unusual pharmacokinetic profile and an enhanced pharmacodynamic selectivity among target FKBPs, those compounds are useful for the treatment of age- or aging-related diseases, diabetes, cancers, as well as inflammation-associated disorders.

Abstract: Disclosed are an aroyl substituted tricyclic compound, a preparation method therefor and use thereof. Specifically, the aroyl substituted tricyclic compound of the present invention has a structure of formula (C), and has, as a BTK inhibitor, the advantages of high activity, good selectivity and low toxic and side effects.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.

Abstract: This disclosure relates to compounds of formula (I?), or pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the application. The compounds of the present disclosure are capable of inhibiting the activity of tyrosine kinase 2 (TYK2). The disclosure further provides methods of preparing the compounds of the disclosure, and methods for their therapeutic use.

Abstract: The present invention provides a novel polycyclic aromatic compound having a plurality of aromatic rings linked by a boron atom, a nitrogen atom, and the like, and thus increases the number of alternatives of a material for an organic electroluminescent (EL) device. Furthermore, the present invention provides an excellent organic EL device by using a novel polycyclic aromatic compound as a material for an organic EL device.

Abstract: Processes for producing an oxazaborolidines and their use in animal feeds. One process reacts an amino alcohol with a boronic acid with azeotropic removal of water to provide a mixture of the starting materials and an oxazaborolidine end product; and purifying the oxazaborolidine end product. One purification step dissolves a bicarboxylic acid in water and mixes this solution with the end product to precipitate out the starting material as a salt and produce an oxazaborolidine product filtrate. An alternative process reacts amino alcohol with trihydridoboron (BH3) in an organic solvent; and immediately alkylates the unalkylated intermediate compound produced using Alkyl Lithium to provide the oxazaborolidine end product.

Abstract: Alkylaluminoxane compositions are produced by a process that includes the steps of reacting trimethylaluminum, triethylaluminum, and water in a hydrocarbon solvent to form an alkylaluminoxane, and then removing insoluble aluminum-containing materials from the solvent to form the alkylaluminoxane composition containing from 0.1 to 20 wt. % of aluminum. Generally, the molar ratio of trimethylaluminum:triethylaluminum is from 5:95 to 80:20, and the molar ratio of water:aluminum is from 0.2:1 to 1:1. The alkylaluminoxane compositions can be utilized as an activator in transition metal-based catalyst systems and in ethylene oligomerization processes.

Abstract: Disclosed herein are compositions comprising amorphous psilocybin. The amorphous psilocybin may be a synthetic, a-polymorphic psilocybin. Also disclosed herein are methods of treatment using amorphous psilocybin and methods of manufacturing amorphous psilocybin.

Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.

Abstract: Disclosed are acyclic nucleoside prodrugs with improved metabolic stability and oral bioavailability. In general, the prodrugs are derivatives of acyclic nucleoside phosphonates containing a lipid-like moiety that can increase oral absorption and subsequent stability in the liver and plasma. Preferably, the lipid-like moiety can resist enzyme-mediated ?-oxidation, such as ?-oxidation catalyzed by cytochrome P450 enzymes. Also disclosed are pharmaceutical formulations of the acyclic nucleoside prodrugs. The acyclic nucleoside prodrugs and pharmaceutical formulations thereof can be used to treat viral infections, such as HIV infections, and/or viral-associated cancer, such as HPV-associated cancers.

Abstract: The present patent application discloses the compounds according to Formula I shown below, or pharmaceutically acceptable salts thereof, wherein JB, n, R1, R2, R3, R4, R5, m and X as defined herein.

Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

Abstract: The present disclosure relates to salts and solid forms of a compound that are GLP-1 agonists, and its use as a therapeutic agent for treating diseases disorders, or conditions associated with GLP-1, such as type 2 diabetes mellitus (T2DM).

Abstract: The invention relates to carbon dioxide dioxaphosphetane compositions, including solid carbon dioxide dioxaphosphetane compositions. The invention includes compositions and methods for the capture, storage, and recycling of carbon, including methods of boric acid catalyzed reduction of carbonates in aqueous media and the use of phosphate solutions for capture and recycling of carbon.

Abstract: An organometallic compound represented by Chemical Formula 1, Ir(LA)m(LB)n, and an organic light-emitting diode including the same. The organometallic compound may act as a dopant of a light-emitting layer of the organic light-emitting diode. An operation voltage of the device may be lowered, and luminous efficiency and a lifespan thereof may be improved.

Abstract: The present invention includes tetradentate platinum (II) complexes for narrow band green and red phosphorescent emitters. The present invention also includes blue emitting metal complexes with six-membered chelate rings based on fused carbazole. The present invention also includes organic light emitting diodes (OLEDS) including these complexes, and devices including these OLEDS.

Abstract: The present invention relates to a method for preparing a crystalline functional sweetener, and more specifically, relates to a method for preparing a crystalline functional sweetener for raising the crystallization yield and increasing the particle size by controlling the content of impurities or production of impurities comprised in a solution for preparing the crystal.

Abstract: Disclosed are processes for the production of composition comprising one or more fructose amino acids, said process comprising the steps of: (a) providing plant material derived from a botanical source selected from plants of the families Solanaceae, Compositae, (Asteraceae), Guttiferae, Umbelliferae, Papaveraceae, Vitidaceae or Acanthaceae; (b) extracting one or more fructose amino acid(s) from said plant material; and optionally (c) detecting the presence and/or measuring the amount of said fructose amino acid(s) in the extract of step (b).

Abstract: A method of treating an infection of a lung in a patient in need thereof according to an embodiment includes administering to the patient an effective amount of a compound having the formula: or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein are deuterated compounds, pharmaceutical compositions thereof, and methods for treating ETBR-related cancers. Also disclosed herein is a delivery system for the controlled, systemic release of at least one deuterated ETBR antagonist, optionally in conjunction with an additional anti-oncologic agent.

Abstract: Disclosed are cell-penetrating cyclic peptides. The peptides can be used to deliver peptides and other biologically active moieties into cells. Formulations containing the cell-penetrating cyclic peptides are also described.

Abstract: The present disclosure relates to peptide having a sequence comprising: (SEQ?ID?NO:?1) Z1X1X2X3X4X5X6X7X8X9X10X11X12-NH2, and to their isomers, pharmaceutically acceptable salts, or prodrugs thereof, methods of use, and methods for their preparation. The peptides disclosed herein are useful for modulating orexin receptor activity and may be used in the treatment of disorders in which orexin receptor activity is implicated, such as narcolepsy, a hypersomnia disorder, a neurodegenerative disorder, a symptom of a rare genetic disorder, a mental health disorder, a metabolic syndrome, osteoporosis, cardiac failure, coma, or a complication in emergence from anaesthesia.

Abstract: Methods for treating non-alcoholic steatohepatitis and/or hepatocellular carcinoma include administering a polypeptide antagonist of a Na/K ATPase/Src receptor complex to a subject in need thereof. Methods and assays for diagnosis or prognosis of non-alcoholic steatohepatitis and/or hepatocellular carcinoma in a subject are also provided and include the steps of providing a biological sample from the subject, determining an expression level or activity in the sample of at least one biomarker selected from Caveolin-1, Survivin, and SMAC; and comparing the expression level or activity of the at least one biomarker in the sample, if present, to a control expression level or activity of the at least one biomarker. Prophylaxis or treatment of the non-alcoholic steatohepatitis and/or hepatocellular carcinoma in a subject can then be initiated based on the expression level or activity of Caveolin-1, Survivin, and SMAC in the sample.

Abstract: The disclosure includes peptides of Formula (I): S1-[block-1]m-x-[block-2]n-y-[block-3]o-z-[block-4]p-S2. Also included are pharmaceutical compositions containing the peptides and methods of treating microbial infections using the peptides.

Abstract: In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-1 and are capable of inhibiting the interaction of PD-1 with PD-L1. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.

Abstract: Among other things, the present disclosure provides various useful agents. In some embodiments, provided agents can bind to beta-catenin. In some embodiments, the present disclosure provides technologies for modulating beta-catenin functions. In some embodiments, the present disclosure provides technologies for preventing and/or treating conditions, disorders or diseases associated with beta-catenin. In some embodiments, the present disclosure provides designed amino acids and agents which can provide improved properties and/or activities.

Abstract: The present disclosure relates to an attenuation method of an influenza virus, an attenuated influenza virus strain, and the use thereof, and belongs to the technical field of biomedicine. The attenuation method of the present disclosure includes the following step: deleting a random number of bases at a random position for a transmembrane domain and a cytoplasmic domain of an M2 protein in a conserved region of the influenza virus to obtain an attenuated influenza virus with a corresponding base deletion. An attenuated influenza virus strain prepared by the attenuation method of the present disclosure exhibits prominent growth characteristics on an M2 protein-expressing MDCK cell line; and the virus strain at a high dose can grow in an MDCK cell or a chicken embryo and has a high agglutination titer of chicken red blood cells (CRBCs). Results of intranasal immunization of Balb/C mice show that the virus strain is non-pathogenic to mice compared with the parental virus IAV PR8.

Abstract: Disclosed herein are recombinant fusion proteins comprising transmembrane domains, a display polypeptides, and oligomerization domains wherein when the recombinant fusion protein is expressed on the surface of an enveloped particle, the recombinant fusion protein is displayed in an oligomeric format, and enveloped particles containing the same, and methods of usc.

Abstract: Provided herein is a nucleic acid comprising consensus amino acid sequence of foot-and-mouth disease FMDV VP1-4 coat proteins of FMDV subtypes A, Asia 1, C, O, SAT1, SAT2, and SAT3 as well as plasmids and vaccines expressing the sequences. Also provided herein is methods for generating an immune response against one or more FMDV subtypes using the vaccine as described above as well as methods for deciphering between vaccinated mammals with the vaccine and those that are infected with FMDV.

Abstract: The present disclosure provides a novel polypeptide. Also provided is an ophthalmic composition for treating or preventing dry eye (DE) or DE associated disorders. Also provided is a method for treating or preventing DE or DE associated disorders, stimulating tears, stabilizing tear film or any combination thereof in a subject in need thereof, comprising administering to the subject an effective amount of the novel peptides. Also provided is a contact lenses care product comprising the novel peptides and the preparation method 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: New insecticidal proteins, nucleotides, peptides, their expression in plants, methods of producing the peptides, new processes, production techniques, new peptides, new formulations, and new organisms, a process which increases the insecticidal peptide production yield from yeast expression systems. The present disclosure is also related and discloses toxins called AVPs, which are modified from the Av3 toxin derived from sea anemone; here we describe the genes encoding the new polypeptide, as well various formulations and combinations; of both genes and peptides, useful for the control of insects.

Abstract: The present disclosure provides, in part, structurally stabilized peptidomimetic compounds that can be used in treatment of integrin-related disorders, to methods of producing structurally stabilized peptidomimetic compounds, and to methods of treating integrin-related disorders by administering structurally stabilized peptidomimetic compounds to subjects in need thereof.

Abstract: The present invention relates to a nanosphere comprising an equal number of a human SEC14-like protein and a cognate ligand of said SEC14-like protein as well as to methods of producing the same and uses of said nanospheres.

Abstract: The invention provides Brachyury deletion mutant polypeptides, nucleic acids encoding the polypeptides, non-yeast vectors comprising the nucleic acids, non-yeast cells, and methods of use.

Abstract: The present invention is situated in the field of multimers used for targeted therapies. More particularly, the present invention provides a dimeric protein complex comprising a first polypeptide comprising a first functional component and the C-terminal fragment of the C4bp beta-chain, wherein said first functional component is coupled to the C-terminus of the C-terminal fragment of the C4bp beta-chain; and a second polypeptide comprising a second functional component and the C-terminal C4bp beta-chain, wherein said second functional component is coupled to the C-terminus of the C-terminal fragment of the C4bp beta-chain; wherein said first and second polypeptides are identical or different and wherein said first and second functional components are proteins or polypeptides. Further provided are nucleic acids encoding said first or second polypeptide of the dimeric protein complex and pharmaceutical compositions comprising the dimeric protein complex.

Abstract: The present invention broadly relates to the field of biotechnology. More particularly, the present invention relates to recombinant vector systems for the production of animal free milk proteins and a process for the production of the animal protein in recombinant host cells.

Abstract: Compositions and methods for NK cell based treatments, and particularly NK cells that express and intracellularly retain IL-2, are presented in which the NK cells are stimulated with a chimeric protein that has a cancer cell targeting portion and an IL-12 portion. Beneficially, such chimeric protein has substantially reduced systemic toxicity and induces IFN-? secretion in a targeted manner. Moreover, chimeric proteins contemplated herein also significantly enhanced IFN-? secretion in NK cells that express and intracellularly retain IL-2 as compared to native NK cells. Preferred chimeric proteins comprise SEQ ID NO:1 or SEQ ID NO:2, and SEQ ID NO:3.

Abstract: Provided are a fusion protein of interleukin 2 and application thereof in the treatment or prevention of amyotrophic lateral sclerosis (ALS).

Abstract: The present invention discloses a polypeptide derivative with dual GLP-1R and GIPR targeting agonism, and a preparation method and use thereof. The polypeptide derivative is set forth in the formula (I). The formula (II) is a branched-chain modification structure of a peptide chain. The groups are defined in this specification. The polypeptide derivative and a pharmaceutically acceptable salt thereof that are provided in the present invention can be used in the fields of treatment of diabetes, weight loss, metabolism-related diseases such as NASH, and neurodegenerative disorders.

Abstract: The present invention relates to peptidic selective GIP receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, hyperglycemia, as well as the treatment of disorders associated with nausea and vomiting.

Abstract: The present invention relates to a novel dimer composed of a first Fab monomer and a second Fab monomer, each Fab monomer comprising a VH and a VL region, wherein two of such VH or VL regions are covalently linked by a disulfide bond between an additional non-naturally occurring cysteine residue at their respective N-termini.

Abstract: The invention relates to an inhibitory chimeric antigen receptor (N-CAR) comprising an extracellular domain comprising an antigen binding domain, a transmembrane domain and, an intracellular domain wherein the intracellular domain comprises an Immunoreceptor Tyrosine-based Switch Motif ITSM, wherein said ITSM is a sequence of amino acid TX1YX2X3X4, wherein X1 is an amino acid X2 is an amino acid X3 is an amino acid and X4 is V or I.

Abstract: Provided herein are immunomodulatory proteins comprising variant PD-1 polypeptides, nucleic acids encoding such proteins and engineered cells expressing such proteins. The immunomodulatory proteins provide therapeutic utility for a variety of immunological and oncological conditions. Compositions and methods for making and using such proteins are provided.

Abstract: Provided is a polynucleotide comprising at least one sequence encoding a fusion protein comprising (a) an antigen-presenting MHC molecule, which can be presented outside the membrane of a cell or an extracellular vesicle; (b) at least one T-cell stimulatory cytokine or subunit thereof, which can be presented outside the membrane of a cell or an extracellular vesicle; (c) a T-cell costimulatory molecule, which can be presented outside the membrane of a cell or an extracellular vesicle; (d) an antigen-presenting MHC molecule and at least one T-cell stimulatory cytokine or subunit thereof, which can be presented outside the membrane of a cell or an extracellular vesicle; or (e) an antigen-presenting MHC molecule, at least one T-cell stimulatory cytokine p or subunit thereof, and a T-cell costimulatory molecule, which can be presented outside the membrane of a cell or an extracellular vesicle.