Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.

Abstract: The invention provides novel compounds and methods of using such compounds to treat or prevent cancer.

Abstract: The present invention is related to processes for preparing 4-chloro-7H-pyrollo[2,3,-d]pyrimidine, and related synthetic intermediate compounds. 4-Chloro-7H-pyrrolo[2,3,-d]pyrimidine is an intermediate for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines, which are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

Abstract: The present invention relates to a new class of substituted aza-triangulenium fluorescent dyes having a hydroxy group attached to an aryl as quenching group. The new substituted aza-triangulenium fluorescent dyes may be attached to a linker, conjugated to carrier molecule such as e.g. a protein, a nucleic acid, a lipid, or a saccharide, or deposited or immobilized on solid support materials. The substituted aza-triangulenium fluorescent dyes are useful for various purposes, including use in sensors for monitoring or determining the concentration of analytes, such as H+(pH), Na+, K+, Ca2+, O2, CO2, H2O2, ionic strength, redox potentials, metal ions, and metabolites.

Abstract: Congener of portimine of the structure: where: R1 is selected from H, acyl, alkyl, alkylene, aryl and aralkyl; R2 is selected from H, acyl, alkyl, alkylene, aryl and aralkyl; M is O, S, N—NH2, N(alkyl)2, N-alkoxy or N(aryl)2; W and X may form a bond, an epoxide, or are independently selected from H, halogen, OH and O-acyl. Y and Z form a bond, an epoxide, or are independently selected from H, halogen (X), OH and O-acyl; and R1 and R2 are not H, M is not O, or W and X or Y and Z do not form a bond.

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 a carboxylic acid or ester or reactive carbonyl derivative, Y is a bisanhydrohexitol unit derived from isosorbide, isoidide or isomannide; X is selected from the group consisting of aromatic rings, substituted or unsubstituted heterocycles, and saturated or unsaturated aliphatic chains; and B is OH and C is an ester carbonyl link with the carbon attached to X and the oxygen attached to Y, and wherein the AB monomer is at least about 98% pure endo-substituted bisanhydrohexitol derivative or an at least about 98% pure exo-substituted bisanhydrohexitol derivative.

Abstract: The present invention provides a compound having the structure:

Abstract: The invention relates to salinomycin derivatives such as compounds having the structure of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a therapeutically effective amount of compounds of formula (I), and the use of compounds of formula (I) for treating or inhibiting progression of cancer. The cancer is selected from the group consisting of breast cancer, pancreatic cancer, and prostate cancer.

Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A and B are defined herein, which are suitable for the treatment of diseases related to Vanin, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

Abstract: The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

Abstract: A process for a continuous production of a boronic acid derivative based on a Matteson boronic ester homologation and an apparatus of performing the process are disclosed.

Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: Group 4 transition metal-containing film forming compositions are disclosed. The Group 4 transition metal-containing film forming compositions comprise Group 4 transition metal precursors having the formula L2-M-C5R4-[(ER2)2—NR]—, wherein M is Ti, Zr, or Hf bonded in an ?5 bonding mode to the Cp group; each E is independently C, Si, B or P; each R is independently a hydrogen or a C1-C4 hydrocarbon group; and each L is independently a ?1 anionic ligand selected from the group consisting of NR?2, OR?, Cp, amidinate, ?-diketonate, or keto-iminate, wherein R? is a H or a C1-C4 hydrocarbon group and adjacent R?s may be joined to form a hydrocarbyl ring; provided that at least one R on the Cp is C1 to C4. Also disclosed are methods of synthesizing and using the disclosed precursors to deposit Group 4 transition metal-containing films on one or more substrates via vapor deposition processes.

Abstract: The present invention relates to a process for preparing a tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris-[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate by hydrosilylation, by in step A initially charging a mixture comprising at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short], at least one carboxylic acid and a Pt catalyst, heating the mixture to a temperature of 50 to 140° C., in step B adding a mixture of 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione and at least one alcohol to the mixture from step A while mixing, in step C leaving the mixture from step B to react while mixing and in step D working up the product mixture thus obtained.

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

Abstract: A method for synthesis of N-phosphonoalkyliminodiacetic acid or derivatives thereof by forming a reaction mixture having an acid catalyst, a compound of the following general formula R1—CH2—NX—CH2—R2 and a compound having one or more P—O—P anhydride moieties to form a compound having a formula R1—CH2—N(—CH2PO3R32)(—CH2—R2) wherein in R1—CH2—NX—CH2—R2: X is —CH2—OH or —CH2—COOH; R1 and R2 are independently selected from the group consisting of nitrile, C1-C4 alkyl carboxylate, and carboxylic acid for when X is —CH2—OH, or R1 and R2 are both carbonyl groups linked by a hydrogen substituted nitrogen atom or a C1-C4-alkyl substituted nitrogen atom; and R3 is H, an alkyl group, or an aryl group; the anhydride moieties in the P—O—P anhydride compound have one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V); and 2) hydrolyzing the mixture to form N-phosphonomethyliminodiacetic acid or one of its derivatives.

Abstract: Compounds having the following formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, D, E and R1 are as defined herein, are provided. Methods comprising the use of such compounds for the treatment of neurological disorders, such as pantothenate kinase-associated neurodegeneration, and pharmaceutical compositions containing such compounds, and their use in the treatment of neurological disorders, also are provided.

Abstract: Stable monomeric phosphaplatins, namely, (pyrophosphato)platinum(II) or platinum(IV) complexes containing a cis-cyclohexanediamine ligand or enantiomerically enriched or enantiopure trans-cyclohexanediamine ligands, and synthesis of these complexes, are provided. Efficacies and toxicities of the phosphaplatin compounds are determined toward a variety of cancers, including sensitive and resistant ovarian cancers, head and neck, and colon cancers. Compositions comprising the platinum complexes, and methods for treatment of proliferative diseases or disorders by means of the complexes or the compositions comprising them are disclosed.

Abstract: Improved methods of making anhydrosugars by pyrolysis of a substrate sugar to remove at least one water molecule thereby producing a desired anhydrosugar and side products, the improvement being either 1) protecting one hydroxyl group of the substrate sugar before pyrolysis; or (2) pretreating the substrate sugar with a metal salt and optional acid before pyrolysis, wherein lower amounts of said side products are produced by said improved method.

Abstract: A compound of Formula (I) wherein Y1, Y2, X1, X2, R1, R2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.

Abstract: The present invention provides compounds of Formula (I) or Formula (II): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Abstract: Methods of enhancing efficiency of downstream chromatography steps for purification of proteins comprising: (a) passing a composition comprising a polypeptide of interest and various contaminants through an ion exchange membrane, wherein the polypeptide and the membrane have opposite charge, at operating conditions comprised of a buffer having a pH sufficiently distinct from the pi of the polypeptide to enhance the charge of the polypeptide and a low ionic strength effective to prevent the shielding of charges by buffer ions, which cause the membrane to bind the polypeptide and at least one contaminant, (b) overloading the ion exchange membrane such that at least one contaminant remains bound to the membrane while the polypeptide of interest is primarily in the effluent; (c) collecting the effluent from the ion exchange membrane comprising the polypeptide of interest; (d) subjecting the membrane effluent comprising the polypeptide of interest to a purification step of similar charge as the previous membrane,

Abstract: The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.

Abstract: Disclosed is related to a synthetic peptide consisting of an amino acid sequence of ArgAsnProLeuGluGluThr (SEQ ID NO: 1). Also provided are a pharmaceutical composition benefic to eye care or eye health comprising the peptide, and a method for wound healing using the peptide.

Abstract: The present invention relates to peptides, 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 cytotoxic T cell (CTL) peptide epitopes, alone or in combination with other tumor-associated peptides that serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses. The present invention relates to several novel peptide sequences and their variants derived from HLA class I and HLA class II molecules of human tumor cells that can be used in vaccine compositions for eliciting anti-tumor immune responses.

Abstract: The present invention relates to ?-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.

Abstract: The invention generally relates to recombinant human cytomegalovirus (CMV) gB proteins and immunogenic fragments thereof, which do not comprise a transmembrane (TM) domain; and comprise one or more mutations that reduce the aggregation between the monomeric trimers of gB, and/or adhesion of the monomeric trimer of gB to the host cell.

Abstract: The present invention encompasses vaccines or compositions comprising the chimeric KSAC protein that possesses immunogenic and protective properties, and methods of use including administering to an animal the antigenic KSAC protein thereof to protect animals. The invention also encompasses methods for making and producing the soluble, disaggregated, refolded or active proteins from inclusion bodies produced from prokaryotes or eukaryotes.

Abstract: The invention provides pharmaceutical compounds and formulations comprising nucleic acids and polypeptides for regulating (including upregulating or inhibiting) the expression of ApoA-1 Binding Protein (APOAIBP, AIBP, or AI-BP) and methods for making and using them. In alternative embodiments, APOAIBP-inhibiting pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to stimulate tissue revascularizaton, e.g., supporting or stimulating revascularization of heart tissue, e.g., after a cardiac ischemia. In alternative embodiments, pharmaceutical compositions and formulations of the invention that comprise APOAIBP nucleic acids and polypeptides or result in an increase in expression or activity of APOAIBP nucleic acids and polypeptides are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate a dyslipidemia, e.g.

Abstract: (Objective) An objective of the present invention is to provide therapeutic agents that, in association with stimulation of PDGFR?-positive cells such as bone marrow mesenchymal stem cells, promote their mobilization into blood and accumulation in a damaged tissue, and induce tissue regeneration in a living body. (Means for solution) Multiple peptides were synthesized, and the migration-promoting activity of each peptide was evaluated. As a result, the present inventors successfully identified multiple peptides that have migration-promoting activity on a PDGFR?-positive bone marrow mesenchymal stem cell line (MSC-1). Further, the present inventors confirmed that the identified peptides also have migration-promoting activity on skin fibroblasts, which are PDGFR?-positive cells.

Abstract: The invention relates generally to the field of autoimmunity. More specifically, the invention relates to compositions and methods for the diagnosis, prevention, and treatment of human leukocyte antigen (HLA)-associated autoimmune diseases, and in particular HLA-B27-associated autoimmune diseases.

Abstract: The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF23 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from a disorder, and methods of screening for compounds with enhanced binding affinity for the ?Klotho-FGF receptor complex involving the use of chimeric proteins of the present invention.

Abstract: Provided are fusion proteins comprising a first domain and a second domain, wherein the first domain comprises a polypeptide that binds to and triggers PD-1 and the second domain comprises a polypeptide that binds to and triggers a TRAIL receptor or Fas. In some embodiments, the polypeptide that binds to and triggers PD-1 comprises at least a portion of the extracellular domain of PD-L1 or PD-L2 and the second domain comprises at least a portion of the extracellular domain of TRAIL or Fas ligand. Also provided are methods for treating autoimmune, alloimmune or inflammatory diseases, and methods for treating cancer, using the fusion proteins.

Abstract: The present disclosure relates to a class of engineered polypeptides having a binding affinity for programmed death-ligand 1 (PD-L1), and provides a PD-L1 binding polypeptide comprising the sequence ERTX4AX6WEIX10X11LPNLX16X17X18QX20GAFIX25X26LHD. The present disclosure also relates to the use of such a PD-L1 binding polypeptide a prognostic and/or diagnostic agent as well as a therapeutic agent.

Abstract: A method of treating a patient who has melanoma includes administering to said patient a composition containing a population of activated T cells that selectively recognize cells in the patient that aberrantly express a peptide. A pharmaceutical composition contains activated T cells that selectively recognize cells in a patient that aberrantly express a peptide, and a pharmaceutically acceptable carrier, in which the T cells bind to the peptide in a complex with an MHC class I molecule, and the composition is for treating the patient who has melanoma. A method of treating a patient who has melanoma includes administering to said patient a composition comprising a peptide in the form of a pharmaceutically acceptable salt, thereby inducing a T-cell response to the melanoma.

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 a collagen hydrolysate which is produced by enzymatic hydrolysis of type-B bone gelatin, wherein the collagen hydrolysate is formed from peptides of which at least 50% by weight, in particular at least 70% by weight have a molecular weight of 1,500 Da to 3,500 Da, and which have a mean molecular weight in the range from 4,000 Da to 8,000 Da, in particular in the range from 4,500 Da to 6,000 Da. The invention also relates to the use of this collagen hydrolysate as an active ingredient to maintain and/or improve the health of the bones, in particular to prevent and/or treat osteoporosis. The invention further relates to a nutritional supplement which comprises the collagen hydrolysate.

Abstract: Provided herein are antibodies that specifically bind and neutralize Staphylococcus enterotoxin B. In addition, nucleic acids encoding such antibodies, and cells that express such antibodies are provided. Also provided are methods for treating diseases mediated by, and for neutralizing Staphylococcus enterotoxin B.

Abstract: The invention relates to novel monoclonal anti-alpha-synuclein antibodies. The antibodies can be used for treating a synucleinopathy such as Parkinson's disease (including idiopathic and inherited forms of Parkinson's disease), Diffuse Lewy Body Disease (DLBD), Lewy body variant of Alzheimer's disease (LBV), Combined Alzheimer's and Parkinson disease, pure autonomic failure and multiple system atrophy.

Abstract: The invention relates to a novel use of monoclonal anti-alpha-synuclein antibodies. The antibodies can be used to prevent tau aggregation and thereby treating tauopathies such as Alzheimer's disease.

Abstract: The invention relates to humanized antibodies directed against the human lymphocyte receptor CD28. When used in a monovalent form these antibodies are antagonists, i.e. capable of blocking of the CD28/B7 interaction, without activating CD28. These antibodies can be used in particular as therapeutic agents for blocking T cell activation through the CD28 receptor.

Abstract: The present invention provides antibodies and antigen-binding molecules thereof which specifically bind the ? and/or ? subunits of the non-active form of the GPIIb/IIIIa receptor. The antibodies and antigen-binding molecules can be genetically fused and/or conjugated to heterologous moieties and used, for example, as targeting moieties. The invention also includes methods for screening for these antibodies, as well as methods of making and methods of using chimeric molecules derived from the antibodies.

Abstract: The present disclosure relates to an antibody binding to Neuropilin 1 (NRP1) or an antigen-binding fragment thereof, a nucleic acid encoding the same, a vector comprising the nucleic acid, a cell transformed with the vector, a method for preparing the antibody or the antigen-binding fragment thereof, an antibody-drug conjugate comprising the antibody or the antigen-binding fragment thereof, and a composition thereof for preventing or treating a cancer.

Abstract: The invention relates to anti-HER3/HER4 antigen binding proteins, e.g. anti-HER3/HER4 antibodies, that bind to the beta-hairpin of HER3 and the beta-hairpin of HER4, methods for selecting these antigen binding proteins, their preparation and use as medicament.

Abstract: The invention relates to antibodies that bind to VEGFR-2. The antibodies are used for treating neoplastic diseases, hyperproliferative disorders, and angiogenic disorders and can be used alone or in combination with other agents.

Abstract: Herein is reported a blood brain barrier shuttle module comprising a brain effector entity, a linker and one monovalent binding entity which binds to a blood brain barrier receptor, wherein the linker couples the effector entity to the monovalent binding entity which binds to the blood brain barrier receptor wherein the monovalent binding entity does not comprise the variable domains of the anti-transferrin receptor antibody 8D3 (SEQ ID NO: 01 and SEQ ID NO: 02) or of the variant anti-transferrin receptor antibody 8D3v (SEQ ID NO: 01 and SEQ ID NO: 03).

Abstract: The present invention relates to a polypeptide capable of binding specifically to the extracellular domain of epidermal growth factor receptor, a polynucleotide that encodes the polypeptide, an expression vector comprising the polynucleotide, a recombinant microorganism having the expression vector introduced therein, and a method of producing the polypeptide using the recombinant microorganism. The polypeptide according to the present invention can bind to the extracellular domain of epidermal growth factor receptor with a high binding affinity comparable to those of existing monoclonal antibodies that are widely used as targeted therapeutic agents, thereby inhibiting the activity of the epidermal growth factor receptor. The polypeptide is useful for the development of agents for the prevention or diseases associated with overexpression of epidermal growth factor receptor.

Abstract: The present invention is directed to methods of preparing a conjugate of a cell-binding agent and a drug (such as a cytotoxic compound). The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents.

Abstract: Purified or highly pure recombinant monoclonal antibodies that bind to human colorectal and pancreatic carcinoma-associated antigens (CPAA), along with nucleic acid sequences encoding the antibody chains, and the amino acid sequences corresponding to said nucleic acids and uses for said sequences are provided.