Abstract: The invention relates to a compound of formula I: (I) or a pharmaceutically acceptable salt thereof, wherein each R3 is independently selected from H, halo, fluorinated C1-C10 alkyl, —I—C1-C10 alkyl, —NH—C1-C10 alkyl, —S—C1-C10 alkyl, —O-fluorinated C1-C10 alkyl, —NH-acyl, —NH—C(O)—NH-alkyl, —C—(O)—NH-alkyl, with the proviso that at least one of R3 is not H.

Abstract: An AB monomer, useful for the production of condensation polymers, wherein the AB monomer has the structure: A-X-C-Y-B; wherein A is reactive carbonyl derivative of carboxylic acids; Y is a bisanhydrohexitol unit derived from the group consisting of isosorbide, isoidide and isomannide; X is selected from the group consisting of: aromatic rings, including 1,4-phenylene, 1,3-phenylene, 2,6-naphthalene 2,7-naphthalene, and substituted derivatives thereof; heterocycles including, 2,5-furan, 2,5-thiophene, substituted 2,5-furan and substituted 2,5-thiophene; and saturated or unsaturated aliphatic chains; B is OH; and C is selected from the group consisting of ether oxygen, a sulfide, and an amine, wherein the amine is NH or NR wherein R is C1 to C6, attaching X to Y.

Abstract: The invention relates to heterocyclic compounds with benzo[c]coumarin structures and to electronic devices, in particular organic electroluminescent devices, containing said compounds.

Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R5, R5?, X1, X2, n, and m are described herein.

Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.

Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.

Abstract: The present invention provides compounds of Formula (A): (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent, and methods of using the compositions and combinations to treat conditions including cancers.

Abstract: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.

Abstract: The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, X1, X2, X3, n, and m are described herein.

Abstract: The present invention provides a new kind of vinca alkaloid derivatives, new applications thereof and preparation methods therefor. The vinca alkaloid derivatives comprise hydrazinolyzed vinca alkaloids and vinca alkaloid dipeptide derivative. The hydrazinolyzed vinca alkaloids are the compounds obtained from the reaction of vinca alkaloids or salts thereof with hydrazinolyzed hydrate; and the vinca alkaloid dipeptide derivatives are the compounds obtained from the condensation of hydrazinolyzed vinca alkaloids with N-benzyloxycarbonylglycyl proline. The present invention provides the uses of the vinca alkaloids derivatives or the pharmaceutical compositions thereof in anti-tumor, preventing or treating diabetic retinopathy, rheumatoid arthritis and serving as angiogenesis inhibitors or vascular disrupting agents.

Abstract: A method simply produces a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end without using a heavy metal catalyst.

Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate. The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.

Abstract: A transformed metal oxide sol, according to the present invention, has as main components: a hydrolysis product of a surface-active silane coupling agent, a transformed metal oxide sol which has been transformed by means of a hydrolysis product of a surface-active silane coupling agent, or a mixture and/or a condensate of the hydrolysis product of the surface-active silane coupling agent and the transformed metal oxide sol which has been transformed by means of the hydrolysis product of the surface-active silane coupling agent; and a mixture of transformed metal oxide sols which have been transformed by means of sulfur-containing functional groups, wherein a raw metal oxide sol of the transformed metal oxide sol is preferably an organosilica sol.

Abstract: The present invention relates complexes comprising a PSMA targeting compound linked to a radionuclide, such as 212Pb or 227Th. These compounds, and pharmaceutical compositions comprising them, can be used for medical applications. These applications include the treatment of prostate cancer, and the complexes allow for dual targeting of cancers.

Abstract: The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof.

Abstract: The present invention relates to the alkylidene phosphonate esters of formula I wherein, R1 is selected from a group consisting of hydrogen or alkyl group; R2 is selected from a group consisting of hydrogen, hydroxy, alkyl, alkoxy, nitro, halogen, amino, N-substituted alkylamino; alkyl group is selected from a group consisting of methyl, ethyl and isopropyl; Ar is selected from a group consisting of aryl, substituted aryl, fused aryl, heteroaryl, and substituted heteroaryl. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the alkylidene phosphonate esters. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.

Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.

Abstract: The present application relates to methods and compounds for enhancing contrast in magnetic resonance imaging. The methods comprise administering compounds of Formula I(a) or I(b) to a subject and obtaining a magnetic resonance image of the subject. The present application also relates to methods of preparing compounds of the Formula I(a) as well as intermediate compounds used in such a method of preparation.

Abstract: The present invention relates to the compounds of formula (I), pharmaceutically acceptable salts, and solvates thereof, wherein the various substituents are as defined herein. The compounds, solvates and salts thereof of Formula (I) are effective as anti-cancer compounds.

Abstract: A method of enhancing the growth of an animal, as well as treating or preventing antimicrobial infections is provided. The method includes causing the animal to ingest or absorb an effective amount of one or more Fe III complex compounds, including but not limited to Fe III complexes comprising ligands bound to the iron center such as amino acids or ?-hydroxy acids. The compounds are also useful for inhibiting, reducing, or preventing biofilm formation or buildup on a surface; the treatment of, inhibition of growth of, and inhibition of colonization by, bacteria, both in biological and non-biological environments; disinfecting surfaces, potentiating the effects of antibiotics and other anti-microbial agents, and increasing the sensitivity of bacteria and other microorganisms, to anti-microbial agents are also provided.

Abstract: A green route for preparing a metal organic framework include mixing metal precursor with a ligand precursor to form a solvent-free mixture; adding droplets of water to the mixture; heating the mixture at a first temperature after adding the water; and isolating the metal organic framework material including the metal and the ligand.

Abstract: The present application discloses a simple process for the purification of neutral human milk oligosaccharides (HMOs) produced by microbial fermentation. The process uses a combination of a cationic ion exchanger treatment, an anionic ion exchanger treatment, and a nanofiltration and/or electrodialysis step, which allows efficient purification of large quantities of neutral HMOs at high purity. Contrary to the purification currently used in fermentative production of neutral HMOs, the presented process allows the provision of HMOs without the need of a chromatographic separation. The so purified HMOs may be obtained in solid form by spray drying, as crystalline material or as sterile filtered concentrate. The provided HMOs are free of proteins and recombinant material originating from the used recombinant microbial strains and thus very well-suited for use in food, medical food and feed (e.g. pet food) applications.

Abstract: The invention provides a production method of a glycoside compound or a salt thereof, which includes subjecting a thioether compound and an alcohol compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid, and then distillation in the presence of at least one kind of additive selected from a sulfur-containing antioxidant and a maleimide group-containing compound to give a thioether compound and a step of subjecting a glycoside compound and a thioether compound to a coupling reaction in the presence of a halogenating agent, a desiccant and a Lewis acid to give a glycoside compound. By this method, a phosphoramidite preferable for the production (synthesis) of a nucleic acid can be produced more efficiently at a high purity.

Abstract: A compound represented by formula I or II below or a salt thereof: wherein B1 represents a purin-9-yl group or a 2-oxo-1,2-dihydropyrimidin-1-yl group that has any one or more substituents selected from the group consisting of a hydroxyl group, a hydroxyl group protected by a protecting group in nucleic acid synthesis, a C1 to C6 linear alkyl group, a C1 to C6 linear alkoxy group, a mercapto group, a mercapto group protected by a protecting group in nucleic acid synthesis, a C1 to C6 linear alkylthio group, an amino group, a C1 to C6 linear alkylamino group, an amino group protected by a protecting group in nucleic acid synthesis, and a halogen atom.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.

Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R6 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

Abstract: This invention is in the field of micro-organism and algal cell processing. The invention relates to a method of maximizing migration of micro-organism and/or algal cells to a solvent fraction while simultaneously displacing water in a separate fraction and subsequent extraction of hydrophobic products from the organisms. The invention further relates to a method of sequestration of protein from an aqueous phase to an organic solvent.

Abstract: Herein is reported a method for producing a polypeptide in monomeric form comprising the following step: recovering the polypeptide in monomeric form from an ion exchange chromatography material by applying a solution comprising a non-ionic polymer and an additive.

Abstract: Herein is reported a method for the purification of an antibody directly captured from clarified cell culture supernatants using Streamline CST and/or Capto MMC, wherein especially product related (aggregates and fragments) and process related impurities (host cell protein, media components) could efficiently be removed, resulting in a preparation with a purity comparable to classical protein A affinity chromatography.

Abstract: A binding agent is capable of binding to rare earth materials such as rare earths and inorganic compounds thereof. A rare earth material-binding agent includes a peptide capable of binding to a rare earth material including a rare earth and a rare earth inorganic compound.

Abstract: In fibrotic lung fibroblasts, basal levels of p53 protein (and miR-34a) are markedly suppressed, leading to reduced p53-mediated inhibition of uPA and uPAR, or concurrent induction of PAI-1. These changes contribute to excessive FL-fibroblast proliferation and production of extracellular matrix (ECM), and, therefore, pulmonary fibrosis. These processes are reversed by treating the cells, and treating subjects suffering from idiopathic pulmonary fibrosis (IPF) with the small organic molecule nutlin-3a (NTL) or with a peptide, CSP-4 (SEQ ID NO:1), or variants or derivatives or multimers of this peptide, which increase p53 levels by inhibiting MDM2-mediated degradation of p53 protein. Use of these compounds serves as a new approach to the treatment of IPF, as they restore p53 expression and p53-mediated changes in the uPA-fibrinolytic system in FL-fibroblasts and restrict production and deposition of ECM.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer, in particular myeloma. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: Compositions and methods useful for producing an immune response in a subject specific for the RSV G protein are described herein. The new methods and compositions described herein are made possible by the development of a new recombinant RSV G protein fragment, which has been engineered for in vitro production and is antigenically similar to the native RSV G protein. The recombinant RSV G protein fragment is capable of inducing the production of RSV G-specific antibodies when injected into a subject. These antibodies can recognize both RSV A and RSV B strains and inhibit infection of both viruses. Accordingly, the compositions and methods described herein may be useful in protecting subjects from RSV infection via immunization, raising antibodies specific for RSV, which can in turn be used to treat RSV infection.

Abstract: A process of forming a gluten-derived flame retardant material includes forming an amine-functionalized flame retardant molecule that includes an aryl halide group and a phosphorus moiety. The process also includes chemically reacting the amine-functionalized flame retardant molecule with a gluten protein under transamidation conditions to bind the phosphorus moiety to a first portion of the gluten protein. The process further includes initiating a cross-coupling reaction between the aryl halide group and amine group of a second portion of the gluten protein to form a gluten-derived flame retardant material.

Abstract: There is provided a peptide which is capable of binding to an MHC molecule in vitro and being presented to a T cell without antigen processing (i.e. an apitope) which peptide comprises a portion of the region 40-60 of myelin oligodendrocyte glycoprotein (MOG). In particular there is provided an apitope which is selected from the following myelin oligodendrocyte glycoprotein peptides: MOG 41-55, 43-57, 44-58 and 45-59. There is also provided the use of such a peptide in a pharmaceutical composition and a method to treat and/or prevent a disease using such a peptide.

Abstract: Provided herein are compositions and methods for the treatment of Chronic Kidney Disease (CKD) and/or the amelioration or prevention of symptoms, conditions and diseases associated therewith.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention relates to anti-BAFF antibody molecules, including novel humanized anti-BAFF antibodies, therapeutic and diagnostic methods and compositions for using the same.

Abstract: Modified FGF-21 polypeptides and uses thereof are provided.

Abstract: Modified FGF-21 polypeptides and uses thereof are provided, for example, for the treatment of diseases associated with fibrosis. Modified FGF-21 polypeptides are disclosed that contain an internal deletion and optionally replacement peptide, optionally modified with at least one non-naturally-encoded amino acid, and/or optionally fused to a fusion partner.

Abstract: A region of the TRPV1 protein that functions as a temperature switch (FIG. 1) has been identified, and can be expressed, purified and applied in combination with other proteins. The function of the switch is maintained even when the region or domain is isolated from the entire protein. As the protein domain is a temperature switch, it can be used to control other proteins and signaling pathways in vitro and in vivo; and TRPV1 is a therapeutic target that is being pursued primarily for intervention in pain (neuropathic and inflammatory) and cancer.

Abstract: The present invention pertains to novel high avidity antigen recognizing constructs, such as antibodies or T cell receptors, which specifically bind to the melanoma associated antigen (MAGE) A1. The constructs of the invention are particularly useful for the diagnosis, prevention or therapy of tumorous diseases which are characterized by the specific expression of the MAGE-A1 antigen. Furthermore provided are nucleic acids, vectors and host cells—such as CD4 or CD8 positive T cells—which encode, comprise or present the antigen recognizing constructs of the invention. The invention thus provides new means for immune therapy, specifically adoptive T cell therapy, for treating cancer.

Abstract: Sulfated glycoproteins, and methods of making and using such sulfated glycoproteins, are described.

Abstract: The present invention provides for a therapeutic cancer treatment using a soluble CD80 fusion protein that binds to PDL1 and inhibits PDL1-PD1 interactions thereby overcoming PDL1-induced immune suppression and restoring T cell activation.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention describes a simple purification process for recombinant human serum albumin. The process results in highly purified protein with limited number of purification steps. The broth containing human albumin is clarified by centrifugation and microfiltration, diafiltered and captured by cation exchange chromatography by a process that allows 140-230 mg of albumin to be captured per ml of resin. Product related impurities are removed by hydrophobic interaction chromatography, optimized to allow 87-97% recovery in flow through mode. The final series of processes are so combined that there is easy transition from one step to the next with minimal interventions and adjustments. The entire process of purification is completed within two days from harvest to final product. Thus a cost-effective process with improved recovery of protein at each step is developed. The purified human serum albumin is analyzed for purity and shows physicochemical characteristics that are similar to standard albumin.

Abstract: The peptides described herein can function as carrier peptides. These peptides can associate with (e.g., non-covalently bind) biologically active molecules or imaging agents to transport the biologically active molecules or imaging across the blood-brain barrier. In some cases, such transport may increase the effectiveness of the biological molecules or imaging agents.