Abstract: Provided herein are crystalline and amorphous forms of a compound having structural formula (1). Also provided are pharmaceutical compositions comprising the crystalline and amorphous forms, methods for their manufacture, and uses thereof for treating a variety of diseases, disorders or conditions, associated with potassium channels.

Abstract: Substituted PYRAZOLO-PYRAZINES as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.

Abstract: Described herein is the MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, including crystalline forms and pharmaceutically acceptable salts and solvates thereof.

Abstract: Prodigiosin analogs which reactivate the p53 pathway are provided, as well as compositions of these compounds, and methods for reactivation of the p53 pathway using these compounds are provided. The prodigiosin analogs may be used to treat cancer in which p53 mutation plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.

Abstract: Pyranone compounds are disclosed herein, which were quite surprisingly found as having OMA1 and/or OPA1 modulatory properties. Compounds of present invention may provide useful for the treatment of certain conditions and diseases, which are amenable to OMA1 and/or OPA1-modulatory therapies. Such conditions may include conditions and diseases prevalent in the elderly, such as cancer and Alzheimer's disease. Pharmaceutical compositions comprising compounds of present invention may be combined with other treatments or further comprise other pharmaceutically active ingredients.

Abstract: The present invention provides novel compounds having the general formula (I) wherein R1 to R6, and m are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present disclosure provides compounds which are useful for a number of catalytic transformations of organic molecules, non-limiting examples including dehydrogenation of alkanes. The present disclosure further relates to methods of preparing the compounds of the present disclosure.

Abstract: The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3?: a C1-C6 alkyl group or the like].

Abstract: Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.

Abstract: Provided is a fused tri-cyclic compound as PDE3/PDE4 dual inhibitor, and a use thereof in the preparation of drugs for PDE3/PDE4 associated diseases, particularly in medicinal functions such as chronic obstructive pulmonary disease (COPD). Provided are specifically a compound of formula (I) and a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. The compounds can selectively inhibit the activity of epidermal growth factor receptor (EGFR) mutants, and shows good inhibitory effect towards mutant EGFR and anti-proliferative activity against cancer cells. Thus they can be used for treating tumors and related diseases.

Abstract: The present disclosure relates to compounds and salts thereof that are useful for modulating target polypeptides and proteins, in particular BRM. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various BRM-mediated and/or BRG1-mediated diseases or disorders.

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.

Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

Abstract: A medicament with excellent JAK kinase (Janus Kinase) inhibitory activity can be used to prevent, treat and/or improve an autoimmune disease (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus and the like). The present invention also provides a pharmaceutically acceptable composition containing the compound and a method for preparing these compounds.

Abstract: A 1H-pyrazolo[4,3-H]quinazoline compound represented by formula (I) can be used for treating cell proliferation dysfunction, and is an broad-spectrum and strongly-active inhibitor for a cell cyclin-dependent kinase (CDK).

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis, ankylosing spondylitis, and psoriatic arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.

Abstract: The present disclosure addresses this need by providing crystalline fine particle forms of PRX-3140 potassium salt, methods for preparation and the treatment for Alzheimer's disease (AD) and other dementias affecting the cholinergic and/or serotonergic systems including post-traumatic stress disorder (PTSD). In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or PRX-3140 potassium salts, crystalline fine particle forms of PRX-3140 potassium salt, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of PRX-3140 potassium salt which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of PRX-3140 potassium salt and excipients with improved stability.

Abstract: The disclosure includes compounds of Formula (A): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

Abstract: Equipotent indolocarbazole-derived analogs of staurosporine identified herein are prepared through C—H borylation chemistry. Functionality resides at C2 and C10 of the indolocarbazole aromatic region. Introducing functionality in this previously inaccessible region does not abrogate kinase activity and is shown to change the selectivity profile.

Abstract: The present invention is directed to compounds of formula I The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Parkinson's disease.

Abstract: The present disclosure provides for compounds of the general Formula (I) wherein R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and Ring A have any of the values defined in the specification, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to novel monocyclic and bicyclic ring system substituted carbanucleoside analogues of Formula (I), wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: Tunable thermochromic materials comprise a metal salt with a varying proportion of two different anions and an organic ligand. Partial substitution via doping during the initial synthesis with a macro-structurally similar (generating an isostructural material) yet chemically different anion creates a material with altered thermochromic properties. For example, in bromide-doped bis(N,N?-diethylethylenediamine)nickel(II)) tetrafluoroborate; both the tetrafluoroborate (BF4-) and bromide (Br—) derivatives are isostructural. Substitution of BF4- for Br— causes a decrease in the materials' thermochromic transition temperature by approximately 10° C.

Abstract: The present specification relates to a compound represented by Chemical Formula 1, a composition for forming an optical film and an optical film comprising the same, and a display device comprising the optical film.

Abstract: Provided is an organic light-emitting material having an ancillary ligand with partially fluorinated substituents. The organic light-emitting material is a metal complex having a diketone ancillary ligand with partially fluorinated substituents and may be used as a light-emitting material in an organic electroluminescent device. These new types of metal complex can fine-tune the emission wavelength more effectively, reduce voltage, improve efficiency, prolong lifetimes, and provide better device performance. Further provided are an organic electroluminescent device and a compound formulation.

Abstract: The invention relates to complexing agents of formula (I): wherein Chrom1, Chrom2 and Chrom3 are as defined in the description. The invention also relates to lanthanide complexes obtained from these complexing agents.

Abstract: Provided are a nitrogen-containing ring compound of the following Chemical Formula 1: and a color conversion film, a backlight unit and a display device including the same.

Abstract: The invention relates to aminosilyl-functionalized conjugated dienes, their preparation and their use in the production of rubbers. Further, the invention relates to rubbers and rubber compositions, and tires produced therefrom. The functionalized conjugated dienes are selected from the group of compounds of formula (Ilia), (Nib), (lllc).

Abstract: Methods, systems, and computer-readable media for providing a continuous flow synthesis process including two or more multiphase reactions for producing a diphenyl siloxane product. Reactants and supporting substances are continuously added in-line of the continuous flow path to eliminate downtime associated with batch processes and increase the overall yield of the synthesis over time.

Abstract: Flame retardant material comprising a compound of empirical formula (III) wherein R is H, an alkyl, aryl, alkylaryl, or arylalkyl group; M is a metal and y is 3, such that M(+)y is a metal cation where (+)y represents the charge formally assigned to the cation; a, b, and c represent the ratio of the components to which they correspond relative to one another in the compound, and satisfy a charge-balance equation 2(a)+c=b(y); and a and c are not zero. The presently disclosed flame retardants are useful, for example, in polymer compositions, particularly thermoplastics processed at high temperatures, over a wide range of applications.

Abstract: Preparation of phosphorus fine chemicals from phosphate sources is described.

Abstract: The present invention relates to fractions of high purity lignin which are thermally stable, and to methods of producing said fractions from lignocellulosic material.

Abstract: The present invention is directed to novel calicheamicin derivatives useful as payloads in antibody-drug-conjugates (ADC's), and to payload-linker compounds and ADC compounds comprising the same; to pharmaceutical compositions comprising the same and to methods for using the same to treat pathological conditions such as cancer.

Abstract: Embodiments of the present application relate to functionalized N-acetylgalactosamine-analogs, methods of making, and uses of the same. In particular, mono or trivalent N-acetylgalactosamine analogs may be prepared by utilizing a wide variety of linkers containing functional groups. These functionalized N-acetylgalactosamine-analogs may be used in the preparation of targeted delivery of oligonucleotide-based therapeutics.

Abstract: Methods of synthesizing chondroitin sulfate oligosaccharides are provided. Enzymatic schematic approaches to synthesizing structurally defined homogenous chondroitin sulfate oligosaccharides at high yields are provided. Synthetic chondroitin sulfate oligosaccharides ranging from 3-mers to 15-mers are provided.

Abstract: Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R2, R3, R4, R5, R6, R7, R11a, R11b, R12, R16, R17, R19, and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

Abstract: The invention provides a method for producing a peptide which comprises the following steps (1) and (2): (1) a step of condensing a C-protected amino acid or a C-protected peptide to a C-terminal of an N-protected amino acid or an N-protected peptide represented by the formula (I): wherein Y represents an amino acid in which a C-terminal is unprotected or a peptide in which a C-terminal is unprotected, R1, R2 and R3 each independently represent an aliphatic hydrocarbon group which may have a substituent(s), a total number of the carbon atoms in the R1R2R3Si group is 10 or more, and the R1R2R3SiOC(O) group is bonded to the N-terminal in Y, and (2) a step of removing the protective group at the C-terminal of the peptide obtained in step (1).

Abstract: Herein is reported a method for the purification of a protein comprising erythropoietin and a single poly (ethylene glycol) residue from reaction by-products or not reacted starting material by a cation exchange chromatography method. It has been found that by employing a cation exchange Toyopearl® SP-650 chromatography material and employing a second wash step with an increased pH value compared to the first wash step a fusion protein of erythropoietin and a single poly (ethylene glycol) residue can be obtained in a single step with high purity and yield and suitability for large scale applications.

Abstract: A large-scale process is described herein for preparing a cyclic peptide as described, comprising solid phase peptide synthesis of a linear peptide and cleaving it from the resin; oxidizing cysteine residues to form an intramolecular disulfide bond; and isolating the cyclic peptide, wherein: (i) coupling uses diisopropylcarbodiimide and ethyl cyanohydroxyiminoacetate and/or N-hydroxybenzotriazole; (ii) cleaving comprises contacting the peptide with a solution comprising TFA and dithioerythritol and/or dithiothreitol; (iii) the peptide is precipitated after cleaving without prior concentration of the peptide by evaporation; (iv) oxidizing comprises contacting an aqueous solution comprising at least 5 mg/mL peptide with hydrogen peroxide; (v) isolating comprises loading the peptide on a reverse phase chromatography at up to 40 grams/kg column, and elution from the column; (vi) isolating comprises lyophilization, followed by grinding the peptide; and/or (vii) substitution of the resin is at least 0.

Abstract: The present disclosure provides compositions and methods related to the modulation of the inflammation response activated by a host's immune system. In particular, the present disclosure provides novel inhibitors of proteins that exhibit pro-inflammatory activity (e.g., RIPK1, RIPK3, ZBP1, TRIF, CUL1, SKP1, and NF-?B, among others), as well as corresponding therapeutic compositions and methods of treatment using these inhibitors.

Abstract: In some embodiments, the present invention provides respiratory syncytial virus (RSV) F proteins, polypeptides and protein complexes that comprise one or more cross-links to stabilize the protein, polypeptide or protein complex in its pre-fusion conformation. In some embodiments the present invention provides RSV F proteins, polypeptides and protein complexes comprising one or more mutations to facilitate such cross-linking. In some embodiments the present invention provides compositions comprising such proteins, polypeptides or protein complexes, including vaccine compositions, and methods of making and using the same.

Abstract: The present disclosure discloses a recombinant varicella-zoster virus (VZV) vaccine, including a fusion protein formed by an amino acid sequence of an extracellular domain of a recombinant glycoprotein gE of a live attenuated VZV strain (OKA strain) gene and an Fc fragment of human immunoglobulin. The present disclosure further provides preparation and use of the fusion protein, a corresponding recombinant gene, a eukaryotic expression vector, etc. The fusion protein of the present disclosure has prominent immunogenicity and can induce the high-level expression of neutralizing antibodies in serum.

Abstract: This invention relates to the field of genetic engineering. Specifically, the invention relates to the construction of operons to produce biologically active agents. For example, operons may be constructed to produce agents that control the function of biochemical pathway proteins (e.g., protein phosphatases, kinases and/or proteases). Such agents may include inhibitors and modulators that may be used in studying or controlling phosphatase function associated with abnormalities in a phosphatase pathway or expression level. Fusion proteins, such as light activated protein phosphatases, may be genetically encoded and expressed as photoswitchable phosphatases. Systems are provided for use in controlling phosphatase function within living cells or in identifying small molecule inhibitors/activator/modulator molecules of protein phosphatases associated with cell signaling.

Abstract: This disclosure relates to antigenic OspA polypeptides and their use in eliciting antibodies against OspA. Also disclosed are antigenic polypeptides comprising an OspA polypeptide and a ferritin protein.