Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of compounds of Formula (I) and salts thereof to treat or prevent ATM mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising to substituted imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; and intermediates useful in such manufacture.

Abstract: Provided are a process for preparing a Parp1/2 inhibitor, i.e., (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one (hereinafter referred to as Compound A), crystalline forms (poly-morphs) of Compound A or hydrate or solvate thereof, methods for preparing the crystalline forms, and the use thereof.

Abstract: Compounds having a structure according to formula (I), (II), or (III) where R1, R2, R3, R5X1, X2, and X3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Abstract: Disclosed are small molecules and pharmaceutical compositions comprising them that can be used in treating diseases associated with the major histocompatibility complex (MHC) molecule MR1.

Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: Compounds of formula (I): wherein R1, R2, R5, R6, R7, R12, X, Y, A, E and n are as defined in the description. Medicinal products containing the same which are useful in treating a condition requiring a pro-apoptotic agent.

Abstract: The present invention provides a compound of Formula XXXI: or a salt or a hydrate of said compound, and further provides a pharmaceutical composition comprising the compound of Formula XXXI and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula XXXI, or a pharmaceutical composition comprising a compound of Formula XXXI and one or more acceptable pharmaceutical carriers to the patient is disclosed.

Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6 and Y are as defined in the description. Medicaments.

Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.

Abstract: The present disclosure provides macrocyclic compounds of Formula (I). The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.

Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: Embodiments of the present disclosure provide for methods of making an organoboron compound, organoboron compounds, and the like.

Abstract: A compound may be represented by Chemical Formula 1, an organic photoelectronic device may include a first electrode and a second electrode facing each other with an active layer that includes the compound represented by Chemical Formula 1 between the first electrode and the second electrode, and an image sensor may include the organic photoelectronic device.

Abstract: The present invention relates to process for preparation of tavaborole with high purity. The present invention relates to method of assessing the purity of tavaborole.

Abstract: The invention relates to a method for producing cationic silicon (II) compounds of general formula I (RaSi)+HA???(I) by reacting the silicon (II) compounds of general formula II (Rb?H)(RaSi)+??(II) with a hydride acceptor compound A, wherein Ra, (Rb?H) and A have the definitions described in claim 1; to the cationic silicon (II) compounds of general formula I and use thereof as catalysts.

Abstract: A method of stabilizing imino-functional silane involving adding thereto at least one Brønsted-Lowry base to inhibit, suppress or prevent the addition reactions of the imino-functional silane with itself to form a imino- and amino-functional silane and the subsequent deamination reactions to form conjugated carbon-carbon double bond-containing imino-functional silanes and stabilized imino-functional silanes containing the at least one Brønsted-Lowry base.

Abstract: A method of preparation of stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs) of one of the following general formulas is provided:

Abstract: A compound that has the structure according to Formula M(LA)x(LB)y(LC)z: wherein ligand LA is ligand LB is and ligand LC is and devices and formulations containing these compounds are disclosed. In Formula M(LA)x(LB)y(LC)z: M is a metal having an atomic number greater than 40; x is 1 or 2; x+y+z is the oxidation state of the metal M; X1-X4 and A1-A8 are C or N; at least one of A1-A8 is N; X is O, S, or Se; two adjacent RB form a six-member aromatic ring E fused to ring B; wherein ring E can be substituted by RE; each RA-RE and R1-R4 is independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof.

Abstract: Disclosed herein are prodrugs of platinum containing anticancer agents such as cisplatin that contain an alkylating moiety. Upon administration, the prodrugs release the platinum containing anticancer agent and the alkylating agent, which can form an adduct with DNA or can protect the platinum containing agent from removal. The disclosed prodrugs can be used to treat various cancers, including cisplatin resistant cancers.

Abstract: The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.

Abstract: The present invention relates to dicaffeoyl spermidine cyclized derivatives and a preparation method and use thereof. Biological activity experiments show that the dicaffeoyl spermidine cyclized derivatives of the present invention have anti-Senile dementia activity and antioxidant activity, and their activity are even better than that of a positive control drug, thus suitable for the prevention and treatment of neurodegenerative diseases such as Senile dementia.

Abstract: The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof, The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: The invention provides a process for the separation of pea protein. The process begins with an aqueous extract or solution of pea protein, which is passed through at least one expanded bed absorption (EBA) process. The EBA process comprises contacting the aqueous extract or solution of pea protein with at least one adsorbent resin, said adsorbent resin comprising at least one ligand (L1 or L2), having particular chemical structures. Proteins of interest are isolated by eluting them from said adsorbent resin. The invention also provides various protein compositions obtainable via the method of the invention.

Abstract: A carrier for ligand immobilization obtained by shrinking polysaccharide porous beads not less than 10% by a shrinkage rate defined by the following formula, and crosslinking the polysaccharide porous beads: Shrinkage rate (%)=(1?V2/V1)×100 (wherein, V1 indicates the gel volume of polysaccharide porous beads before shrinkage, and V2 indicates the gel volume of polysaccharide porous beads after shrinkage).

Abstract: Water dispersible, multivalent ligand-lipid constructs that spontaneously and stably incorporate into membranes are disclosed.

Abstract: In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Stable pre-fusion respiratory syncitial virus (RSV) F polypeptides, immunogenic compositions including the polypeptides, and uses thereof for the prevention and/or treatment of RSV infection are described.

Abstract: The present invention relates to novel antimicrobial peptide and variants thereof. The invention further relates to method of killing or inhibiting growth of microbes and use of the peptide here disclosed as a medicament, feed additive, preservative or surfactant.

Abstract: The present invention relates to novel antimicrobial peptide and variants thereof. The invention further relates to method of killing or inhibiting growth of microbes and use of the peptide here disclosed as a medicament, feed additive, preservative or surfactant.

Abstract: Provided are a novel Dermatophagoides farinae protein, and a diagnostic drug, a prophylactic drug and a therapeutic drug for an allergic disease caused by Dermatophagoides farinae. A Dermatophagoides farinae protein selected from the group consisting of the following (a) to (c), or a fragment peptide thereof: (a) a protein including an amino acid sequence set forth in SEQ ID NO:2; (b) a protein including an amino acid sequence in which one or several amino acids have been substituted, deleted, or added relative to the amino acid sequence set forth in SEQ ID NO:2, and having allergenicity of Dermatophagoides farinae; and (c) a protein including an amino acid sequence having 90% or higher identity with the amino acid sequence set forth in SEQ ID NO:2, and having allergenicity of Dermatophagoides farinae.

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: This invention provides long-acting, superactive analogs of glycoprotein hormones demonstrating enhanced bioactivity both in vitro and in vivo as compared to wild type counterparts. The analogs are particularly useful for treating subjects showing low receptor expression or poor receptor responsiveness, and for the treatment of any condition associated with glycoprotein hormone activity.

Abstract: The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

Abstract: Provided herein are variants of an archaerhodopsin useful for application such as optical measurement of membrane potential. The present invention also relates to polynucleotides encoding the variants; nucleic acid constructs, vectors, cells comprising the polynucleotides, and cells comprising the polypeptides; and methods of using the variants.

Abstract: The instant disclosure provides a microscale method for providing correctly folded, and assembled biologically active proteins in an efficient and shorted time frame, compared to conventional protein production techniques. Proteins produced from inclusion bodies and other aggregated protein sources are provided. Microscale production of correctly folded and assembled class I MHC protein and complexes thereof are also provided for, as well as for high throughput production for use in epitope discovery protocols. Microscale production of complex proteins from protein aggregates and preparations containing protein aggregates is provided that requires less than 24 hours of processing time.

Abstract: Provided herein are polypeptides that bind to a blood-brain barrier (BBB) receptor, methods of generating such polypeptides, and methods of using the polypeptides to target a composition to a BBB receptor-expressing cell, e.g., for transport across the BBB. Also provided herein are transferrin receptor (TfR) constructs that comprise a monomeric TfR apical domain or one or more portions of the TfR apical domain which have been circularly permuted relative to the full-length TfR sequence.

Abstract: The technology provided herein relates to novel isolated polypeptides and peptides having a growth inhibitory effect on human cancer cells. Nucleic acid molecules encoding said polypeptides/peptides, vectors, host cells containing the nucleic acids and methods for preparation and producing said polypeptides/peptides. Compositions and methods for using such polypeptides/peptides for the prevention and treatment of cancer are also encompassed by the present disclosure.

Abstract: In certain embodiments, this present invention provides antibodies and Fc fusion proteins with enhanced pharmacokinetics, such as biotinylated antibodies or biotinylated Fc fusion polypeptides.

Abstract: The present invention refers to a method for the separation of host cell proteins (HCPs), antibody fragments and low molecular weight substances from solutions containing antibodies.

Abstract: The invention provides anti-OspA antibodies and methods of using the same.

Abstract: Compositions and methods for the therapy and diagnosis of Inflammatory Bowel Disease (IBD), including Crohn's Disease and Ulcerative Colitis, are disclosed. Illustrative compositions comprise one or more bacterial polypeptides, immunogenic portions thereof, polynucleotides that encode such polypeptides, antigen presenting cell that expresses such polypeptides, and T cells that are specific for cells expressing such polypeptides. The disclosed compositions are useful, for example, in the diagnosis, prevention and/or treatment of IBD.

Abstract: Anti-SpA murine, chimeric and humanized monoclonal antibodies, and variant antibodies having a heavy chain with at least one amino acid substitution are provided. Such antibodies may be used to prevent or treat microbial infections.

Abstract: The present invention provides for methods of preventing and/or treating S. aureus-associated bacteremia and sepsis, and methods for preventing and/or treating S. aureus-associated pneumonia in immunocompromised patients using anti-S. aureus alpha-toxin (anti-AT) antibodies. Also provided are methods of reducing S. aureus bacterial load in the bloodstream or heart of a mammalian subject comprising administering to the subject an effective amount of an isolated anti-S. aureus alpha toxin (anti-AT) antibody or antigen-binding fragment thereof. Methods of reducing S. aureus bacterial agglutination and/or thromboembolic lesion formation in a mammalian subject comprising administering to the subject an effective amount of an isolated anti-S. aureus alpha toxin (anti-AT) antibody or antigen-binding fragment thereof, are also provided. Also provided are methods of preventing or reducing the severity of S. aureus associated pneumonia in an immunocompromised mammalian subject.

Abstract: The present invention provides methods for treating, reducing the severity, or inhibiting the growth of cancer (e.g., skin cancer). The methods of the present invention comprise administering to a subject in need thereof a therapeutically effective amount of a programmed death 1 (PD-1) antagonist (e.g., an anti-PD-1 antibody). In certain embodiments, the skin cancer is cutaneous squamous cell carcinoma or basal cell carcinoma.

Abstract: Described herein is an isolated antibody or antigen-binding fragment including a heavy chain variable region including three heavy chain complementary determining regions (HCDRs), wherein the sequence of HCDR1 is GYRLSELS (SEQ ID NO: 1), the sequence of HCDR2 is ISGWDGNT (SEQ ID NO: 2), and the sequence of HCDR3 is ARASGYNY(SEQ ID NO: 3), wherein the isolated antibody or antigen-binding fragment specifically binds human HSP90, specifically HSP90 beta. Also included are detection and therapeutic methods using the isolated antibodies or antigen-binding fragments.

Abstract: This invention pertains to monovalent agents, including Fab fragments and monovalent monoclonal antibodies analogous to MetMab, having binding specificity to human Nerve Growth Factor (“NGF”), and methods of treating pain in an individual wherein there is no substantial increase in the inflammatory response of the individual following administration of the monovalent agents.

Abstract: This disclosure provides compositions and methods for controlling pain. In particular the disclosure provides a method for controlling pain comprising co-administration of an NGF antagonist and a TNF? antagonist. The NGF antagonist and the TNF? antagonist can be separate molecules or part of a multifunctional polypeptide, e.g., a multispecific binding molecule that comprises an NGF antagonist domain and a TNF? antagonist domain. This disclosure also provides multifunctional polypeptides, e.g., multispecific binding molecules, comprising an NGF antagonist domain, and a TNF? antagonist domain. The method provides improved pain control. Administration of an NGF antagonist and a TNF? antagonist as provided herein can control pain in the subject more effectively than an equivalent amount of the NGF antagonist or the TNF? antagonist administered alone.