Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, V, W, X, Y, n and q are defined herein, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.

Abstract: Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Research in humans suggests that glucosepane plays a critical role in the pathophysiology of both diabetes and human aging; yet comprehensive biological investigations of this ‘metabolite have been’ greatly hindered by a scarcity of chemically homogeneous material available for study. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole (hereafter termed an “iso-imidazole”), rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane, enabled by the development of a novel one-pot method for preparation of the iso-imidazole core. The synthesis of the present invention is concise (8-steps starting from commercial materials), convergent, high-yielding (12% overall), and enantioselective.

Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.

Abstract: Embodiments of the present invention are directed to methods and dosage forms for treating inflammation and rejection in transplantation injuries with Bryostatin-1, Bryostatin-1 analogs and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a novel chromone oxime derivative of formula (I), which is a modulator of nervous system receptors sensitive to glutamate and, furthermore, presents an advantageously high brain penetration upon oral administration. The invention also relates to a pharmaceutical composition containing this compound, and to its use for the treatment or prevention of conditions associated with altered glutamatergic signalling and/or functions, or conditions which can be affected by alteration of glutamate level or signalling, particularly acute and chronic neurological and/or psychiatric disorders.

Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.

Abstract: The invention relates to a novel process for preparing 5H-[1,2,5]thiadiazolo[3,4-f]isoindole-5,7(6H)-dione (“TID”) derivatives, especially for preparing 4,8-diaryl-TID derivatives, to novel intermediates obtained and/or used in this process, to novel TID derivatives prepared by this process, to the use of these TID derivatives as monomers or building blocks for preparing conjugated polymers, and to the use of these TID derivatives or conjugated polymers as organic semiconductors or in organic electronic (OE) devices.

Abstract: Described herein are novel compounds and methods for the treatment and/or prevention of cerebral amyloidoses such as Alzheimer's disease (AD) and/or cerebral amyloid angiopathy (CAA).

Abstract: A method for preparing an anionic polymerization initiator, a device for manufacturing the same, and an anionic polymerization initiator prepared therefrom is provided. And the method for preparing an anionic polymerization initiator according to the present invention is characterized in that in a continuous reactor an amine compound of Formula 1 and/or Formula 2; an organometallic compound; and/or a conjugated diene compound are introduced in the form of a solution and reacted.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions are disclosed.

Abstract: The present invention relates to novel aminosilane-functionalized diene compounds of the following Formula I: wherein each R? is independently selected from C1-C12 alkyl, C6-C18 aryl, C7-C18 alkylaryl, tri(C1-C6 alkyl, C6-C12 aryl or C7-C18 alkylaryl)silyl and allyl, wherein two R? groups may be connected to form a ring and the ring may contain, further to the Si-bonded nitrogen atom, one or more of an oxygen atom, a nitrogen atom, an >N(C1-C6 alkyl or C7-C18 alkylaryl) group and a sulfur atom; each R? is independently selected from C1-C6 hydrocarbyl; Ra, Rb, Rc, Rd and Re are independently selected from hydrogen, methyl and ethyl; x is an integer selected from 0, 1 and 2, y is an integer selected from 1, 2 and 3 and x+y=3. The diene compounds are useful as modifying monomers in the polymerization of conjugated diene monomers.

Abstract: Disclosed herein are methods for synthesizing low valence, titanium-aluminum complexes from half-metallocene titanium compounds and alkylaluminum compounds. The titanium-aluminum complexes can be used as components in catalyst systems for the polymerization of olefins.

Abstract: Benzocyclooctene (fused 6,8 ring system) analogues and corresponding indene (fused 6,5 ring system) analogues function as inhibitors of tubulin polymerization. The compounds are useful as anticancer agents in a new therapeutic approach for cancer treatment utilizing small-molecule inhibitors of tubulin polymerization that also act as vascular disrupting agents (VDAs).

Abstract: Methods, kits and devices for separating phospholipids and proteins from small molecules in biochemical samples can feature an apparatus having a wetting barrier, at least one frit and a separation media. For example, an apparatus can include at least one wall defining a chamber having an exit and an entrance; a wetting barrier disposed between the exit and entrance, so as to define a separation media space located between the wetting barrier and the exit and a sample receiving area located between the wetting barrier and the entrance; and a separation media disposed adjacent to the wetting barrier and having a specific affinity for phospholipids.

Abstract: Compounds having the following formula (E): or a pharmaceutically acceptable salt thereof, wherein R, R?, R?, X and n are as defined herein are provided. Methods comprising use of such compounds for the treatment of neurologic disorders, such as pantothenate kinase-associated neurodegeneration, and pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders are also provided.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: The invention relates to oligomerization of olefins, such as ethylene, to higher olefins, such as a mixture of 1-hexene and 1-octene, using a catalyst system that comprises a) a source of chromium b) one or more activators and c) a phosphacycle-containing ligating compound. Additionally, the invention relates to a phosphacycle-containing ligating compound and a process for making said compound.

Abstract: The present invention provides crystalline forms of the chloride monohydrochloride salt of fosnetupitant, methods of making the crystalline forms, and pharmaceutical dosage forms that make use of the crystalline forms.

Abstract: Provided herein are cyclic phosphorus-containing prodrug compounds, their preparation and their uses, such as treating diseases via modulating molecular targets in the liver.

Abstract: Metal coordination complexes comprising at least one diazabutadiene based ligand having a structure represented by: where A1, A2, A3, and A4 are atoms in a 6-membered ring and are independently selected from C, N, O, S, and P; and where R1, R2, R3, R4, R5, and R6 are independently selected from the group consisting of H, amino groups, C1-C6 alkyl groups, or C4-10 cycloalkyl groups; and further provided that alkyl groups may optionally contain silicon; and where the metal coordination complex is capable of participating in a Diels-Alder type reaction with a dienophile. Processing methods using the metal coordination complexes are also described.

Abstract: Metal coordination complexes comprising at least one diazabutadiene based ligand having a structure represented by: where R1 and R4 are selected from the group consisting of C4-C10 alkyl groups; and R2 and R3 are each independently selected from the group consisting of H, C1-C6 alkyl, cycloalkyl, or aryl groups and the difference in the number of carbons in R2 and R3 is greater than or equal to 2. Processing methods using the metal coordination complexes are also described.

Abstract: Compositions including derivatives of spinosyns and methods for the production of derivatives of spinosyns are provided. The spinosyn derivatives described herein include those functionalized on the C-5,6 double bond to provide an aziridine ring system. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and nematodes and are useful in the agricultural and animal health markets.

Abstract: The invention provides a process for the preparation of nicotinamide mononucleotide having formula (I): The method involves the protection of nicotinamide riboside by ketalization, followed by phosphorylation and then deprotection to provide nicotinamide mononucleotide.

Abstract: The present disclosure relates to cap analogs, which can result in high levels of capping efficiency and transcription and improved translation efficiencies. The present disclosure also relates to methods useful for preparing cap analogs and using mRNA species containing such analogs, as well as kits containing the novel cap analogs.

Abstract: The present invention aims to provide a more stable and efficient method for producing oligonucleotide, particularly, oligonucleotide having various functional groups linked to the 3?-terminal and the like.

Abstract: The present invention relates to oxysterols of formula (I): for use in the treatment of infections caused by a naked virus, in particular a virus selected from the group consisting of rotavirus, papillomavirus and rhinovirus.

Abstract: The present invention relates to processes for preparing compounds of Formula (I) and compounds of Formula (II): or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR or TGRS modulators. Specifically, the present invention relates to bile acid derivatives and methods for their preparation and use.

Abstract: Provided herein are novel methods and matrices for the purification an antibody from a starting material using a mimetope. The method comprises contacting an immunoaffinity chromatography matrix, comprising a solid support and a mimetope immobilized to the solid support, wherein the antibody in the starting material binds to the immobilized mimetope and altering the conditions of the immunoaffinity chromatography matrix to unbind the antibody from the mimetope. The matrix comprises a solid support and a mimetope immobilized to the solid support.

Abstract: The subject invention provides advantageous new salts of mu-opiate receptor peptides. These salts have been found to have excellent properties in terms of their crystal structure, stability, solubility, lack of impurities and/or the ability to be produced, with these advantageous properties, in amounts sufficient for the production of therapeutic compositions.

Abstract: The object of the present invention relates to a novel family of peptide conjugates of formula (I): A-X1-X2-Pro-Ala-X-B??(I) wherein: A represents a hydrogen atom, a C6 to C20 acyl group or a cholesterol residue; X1 represents a covalent bond, an alanine or a proline; X2 represents an arginine, a lysine, or an alanine; X represents a lysine, an alanine, or a phenylalanine; and B represents a hydroxyl or an amine; or one of its preferentially pharmaceutically, dermatologically or cosmetically acceptable salts, as well as their synthesis processes and their uses for reducing hair loss and stimulating hair growth.

Abstract: Provided herein are compositions including peptides, pharmaceutical preparations thereof, and methods of preventing photoreceptor death therewith and protecting of retinal cells, including, but not limited to, photoreceptors and retinal pigment epithelium, from Fas- or TRAIL-mediated apoptosis.

Abstract: A one-bead-two-compound combinatorial synthesis technique provides libraries of macrocyclic peptidomimetic compounds and compositions with use as ligands for the Ephrin type-A receptor 2 (EphA2). The one-bead-two-compound technique and libraries of macrocyclic compounds are useful as research tools in drug discovery and/or to treat or prevent a range of diseases or disorders.

Abstract: The present disclosure relates to methods and compositions for treating disease related to disorders of bone remodeling. In particular, the present disclosure relates to compositions and methods for treating rheumatoid arthritis.

Abstract: Described are ?-PNA monomers, methodology for synthesizing them, and methodology for synthesizing PNA oligomers that incorporate them.

Abstract: Methods and compositions for producing, isolating and purifying virus-like particles (VLPs) containing long sense and antisense RNA molecules, including RNA molecules predicted to fold into double-stranded regions longer than the inner diameter of the VLP capsids are disclosed.

Abstract: The present invention relates to developing and providing a technique for saccharifying a plant biomass, particularly a lignocellulosic biomass efficiently in fewer steps and at low cost while suppressing environmental load, in order to efficiently and effectively use the energy of the plant biomass. Provided are a cellulase activator containing a lignocellulose degradation cofactor consisting of an amino acid sequence represented by SEQ ID NO: 1 as an active ingredient and a method for saccharifying a lignocellulosic biomass using the cellulase activator.

Abstract: Compositions having pesticidal activity and methods for their use are provided. Compositions include isolated and recombinant polypeptide sequences having pesticidal activity, recombinant and synthetic nucleic acid molecules encoding the pesticidal polypeptides, DNA constructs comprising the nucleic acid molecules, vectors comprising the nucleic acid molecules, host cells comprising the vectors, and antibodies to the pesticidal polypeptides. Nucleotide sequences encoding the polypeptides provided herein can be used in DNA constructs or expression cassettes for transformation and expression in organisms of interest, including microorganisms and plants. The compositions and methods provided herein are useful for the production of organisms with enhanced pest resistance or tolerance. Transgenic plants and seeds comprising a nucleotide sequence that encodes a pesticidal protein of the invention are also provided. Such plants are resistant to insects and other pests.

Abstract: Provided are non-naturally occurring cystine knot peptides (CKPs) that bind to VEGF-A. Additionally, provided are methods of using non-naturally occurring CKPs that bind to VEGF-A, including diagnostic and therapeutic compositions and methods. Non-naturally CKPs that bind low density lipoprotein receptor-related protein 6 (LRP6) are also provided.

Abstract: A composition comprising a plurality of bioactive peptides including SEQUENCE ID NO's 555 and 701 is described. The composition may be a powder that is enriched in peptides having a molecular weight less than 10 KD. The bioactive peptides included in the composition have been found to have anti-inflammatory, glucose-transport promoting, and cellular growth promoting activities.

Abstract: The specificity of CD4+ TH responses of German cockroach (Bla g) antigens, and whether differences exist in magnitude or functionality as a function of disease severity, is disclosed. Also disclosed are novel German cockroach allergens and epitopes.

Abstract: Disclosed are a human-derived ferritin monomer fragment and a fusion polypeptide using the same, and more particularly, to a human-derived ferritin of which a portion of a fourth loop and a fifth helix of the ferritin monomer fragment are removed, and a fusion polypeptide in which a polypeptide or a protein is fused to an N-terminus or a C-terminus of the ferritin monomer fragment.

Abstract: The present invention is related to development of the improved cell-permeable (CP)-?SOCS3 recombinant protein which disrupt the interaction of leptin receptor (ObR) and suppressor of cytokine signaling 3 (SOCS3), as protein-based anti-obesity or anti-diabetes agent by utilizing the platform technology for macromolecule intracellular transduction.

Abstract: Molecular determinants of cancer response to immunotherapy are described, as are systems and tools for identifying and/or characterizing cancers likely to respond to immunotherapy.

Abstract: The present invention provides method for promoting the maturation and export of T cells from thymic tissue by contacting the thymic tissue with supraphysiological levels of interleukin (IL)-15. The present invention also provides methods for preventing, alleviating, reducing, and/or inhibiting lymphopenia or peripheral depletion of lymphocytes in a patient in need thereof by administering to the patient IL-15.

Abstract: The present invention relates to novel insulins or insulins analogues that are extended with predominantly sequences of polar amino acid residues in order to improve the half-life and stability of the drug substance. The invention also provides pharmaceutical compositions comprising such drug substances, and relates to the use of such drug substances for the treatment or prevention of medical conditions relating to diabetes.

Abstract: The present invention relates to a method of preparing insulin from proinsulin comprising converting high-concentration proinsulin into insulin by enzymatic cleavage, a method of purifying insulin, and insulin prepared therefrom.

Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.