Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.

Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.

Abstract: The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.

Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract: The present application discloses a luminescent lanthanide chelate of formula (I) with lanthanides such as europium, as well as the corresponding luminescence lanthanide chelating ligand. The application also discloses a detectable molecule comprising a biospecific binding reactant (such as an antibody) conjugated to the luminescent lanthanide chelate as well as a method of carrying out a biospecific binding assay, the use of such a detectable molecule in a specific bioaffinity based assay, the use of such a detectable molecule in a specific bioaffinity based binding assay utilizing time-resolved fluorometric determination of a specific luminescence, and a solid support material conjugated with the luminescent lanthanide chelate.

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: The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.

Abstract: The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia.

Abstract: A process comprising contacting a) an alkene, b) a hydrogen-boron bond containing compound, c) an ?-diimine metal salt complex comprising an ?-diimine iron salt complex or an ?-diimine cobalt salt complex, and d) a group 1 metal borohydride under conditions suitable to form an alkylboron compound. A process comprising contacting a) an alkene, b) a hydrogen-boron bond containing compound, and c) an ?-diimine metal salt complex comprising an ?-diimine iron methylenetrihydrocarbylsilyl complex or an ?-diimine cobalt methylenetrihydrocarbylsilyl complex, to form an alkyl-boron compound under conditions suitable to form an alkylboron compound. A process comprising contacting an alkene, a hydrogen-boron bond containing compound, and an ?-diimine metal salt complex to form an alkyl-boron compound under conditions suitable to form an alkylboron compound.

Abstract: The invention relates to a process of preparing substituted pentacenes, to novel pentacenes prepared by this process, to the use of the novel pentacenes as semiconductors or charge transport materials in optical, electrooptical or electronic devices including field effect transistors (FETs), electroluminescent, photovoltaic and sensor devices, and to FETs and other semiconducting components or materials comprising the novel pentacenes.

Abstract: The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Abstract: The invention relates to a novel group bridged metallocene transition metal complexes, wherein the complex includes at least one indenyl ligand substituted at the 4-position with a phenyl group, the 4-phenyl group being preferably substituted at the 3?, 4?, and 5? positions with particular combinations of substituents, particularly wherein the 4?-substituent is a group of the formula (XR?n)?, wherein X is a Group 14-17 heteroatom having an atomic weight of 13 to 79 and R? is one of a hydrogen atom, halogen atom, a C1-C10 alkyl group, or a C6-C10 aryl group and n is 0, 1, 2, or 3. Catalyst systems including the transition metal complex, polymerization processes using the transition metal complex, and polymers made using the transition metal complex are also described.

Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

Abstract: Generally, the present invention relates to improvements in metal utilization in supported, metal-containing catalysts. For example, the present invention relates to methods for directing and/or controlling metal deposition onto surfaces of porous substrates. The present invention also relates to methods for preparing catalysts in which a first metal is deposited onto a support (e.g., a porous carbon support) to provide one or more regions of a first metal at the surface of the support, and a second metal is deposited at the surface of the one or more regions of the first metal. Generally, the electropositivity of the first metal (e.g., copper or iron) is greater than the electropositivity of the second metal (e.g., a noble metal such as platinum) and the second metal is deposited at the surface of the one or more regions of the first metal by displacement of the first metal. The present invention further relates to treated substrates, catalyst precursor structures and catalysts prepared by these methods.

Abstract: Manganese coordination complexes with utility as magnetic resonance probes and as biological reductant sensors are disclosed. In one embodiment, ligands can stabilize both the Mn2+ and Mn3+ oxidation states. In the presence of a reductant such as glutathione, low relaxivity MnIII-HBET is rapidly converted to high relaxivity MnII-HBET with a 3-fold increase in relaxivity, and concomitant increase in magnetic resonance signal. In another embodiment, ligands were designed to chelate Mn(ll) in a thermodynamically stable and kinetically inert fashion while allowing for direct interaction of Mn(ll) with water. In yet another embodiment, high molecular weight multimers containing six Mn(ll) chelators were prepared. The high molecular weight results in slower tumbling of the molecules in solution and can strongly enhance the Mn(ll) relaxivity.

Abstract: The present invention relates to hybrid fumarate-CO-releasing molecules capable of increasing heme oxygenase-1 (HO-1) activity and HO-1 protein expression and simultaneously releasing CO, their synthesis and their use in therapeutic applications, in particular their use in the treatment of inflammatory or cardiovascular diseases.

Abstract: The invention provides gemcitabine derivatives shown in the following formula (I) and preparation methods thereof. The invention further relates to a pharmaceutical composition which comprising the said gemcitabine derivatives in an effective amount and a pharmaceutically acceptable excipient or additive. The invention further provides use of the said derivatives for preparing anti-tumor drugs. The compound designed by the invention is novel in structure and has a remarkable anti-tumor activity. According to the compound designed by the invention, the preparation starting materials have extensive sources and are easily obtained, the preparation method is simple and easy to operate, and the yield of the product is high, so that industrial production on a large scale is facilitated.

Abstract: The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the COL1A1, TGF-?, and SMAD2/3 genes, and methods of using such dsRNA compositions to inhibit expression of COL1A1, TGF-?, and SMAD2/3.

Abstract: The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5?-androstane-3?,5,6?-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2? values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability.

Abstract: The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5?-androstane-3?,5,6?-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2? values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability.

Abstract: The present invention relates to compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more cysteine proteases. Also described are methods where the compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 are used in the prevention and/or treatment of various diseases and conditions in subjects, including cysteine protease-mediated diseases and/or caspase-mediated diseases such as sepsis, myocardial infarction, cancer, tissue atrophy, ischemia, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative diseases such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, and Huntington's disease.

Abstract: Provided herein are methods to generate and screen peptides that exhibit drug like stabilities in vitro and in vivo. By selecting for enzyme resistance, Applicants are able to derive peptides that are not only stable to a broad spectrum of proteases, but also stable to other drug processing enzymes such as cytochrome P450s. This approach provides a general method to the rapid development of highly stable peptides for therapeutic development and diagnosis. The peptides are further modified for oral bioavailability. The methods can be applied to similar peptides for the making of therapeutic compositions.

Abstract: The present invention discloses an integrin receptor targeting novel cationic CGKRK-lipopeptide. The present invention further discloses a liposomal formulation comprising the cationic CGKRK-lipopeptide, at least two co-lipids, at least one chemotherapeutic agent and a pharmaceutically acceptable carrier. The present invention also provides a method for regressing established tumors comprising administering therapeutically effective amount of the liposomal formulation comprising the chemotherapeutic agent.

Abstract: Peptides and peptide analogs that selectively inhibit angiotensin II are described. Additionally, a method for making and using the peptides and peptide analogs are also described.

Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Abstract: Provided herein are HIV vaccines that encompasses recombinant trimers that mimic native HIV-1 envelope trimers. Also provided are methods of administering to a subject in need thereof an HIV vaccine provided herein to elicit antibodies against a recombinant trimer in the subject. A recombinant trimer is formed by a recombinant protein comprising a recombinant HIV-1 gp140 fused to a tag through a linker at C-terminus of the recombinant HIV-1 gp140, wherein the linker is sufficiently long so that the tag is accessible for binding by a binding molecule bound on a solid matrix during purification of the recombinant trimer.

Abstract: This disclosure relates to a method of preventing or treating a recurrence of acute otitis media in a subject at risk comprising administering a therapeutically effective amount of a composition, at least once to the subject. The composition administered comprises at least one immunogenic polypeptide selected from the group consisting of Streptococcus pneumoniae PhtD, PhtE, PcpA, LytB and detoxified pneumolysin.

Abstract: Nutritive proteins are provided. In some embodiments the nutritive proteins comprise a first polypeptide sequence comprising a fragment of a naturally-occurring nutritive protein. In some embodiments the fragment comprises at least one of a) an enhanced ratio of branch chain amino acid residues to total amino acid residues present in the nutritive protein; b) an enhanced ratio of leucine residues to total amino acid residues present in the nutritive protein; and c) an enhanced ratio of essential amino acid residues to total amino acid residues present in the nutritive protein.

Abstract: We describe the rational structure-based design of monomeric and dimeric forms of a nanobody-enhanced GFP (termed vsfGFP) that demonstrates ˜1.3-fold higher brightness than sfGFP in a monomeric form and ˜2.5-fold higher brightness in a dimeric form. These new vsfGFP variants demonstrate high stability and brightness in both bacterial and eukaryotic cells and are thus ideal for in vivo imaging applications. The combination of higher brightness, facile folding, stable expression, and tunable dimerization makes them ideal partners in essentially all in vitro applications already described for fluorescent proteins, including antibody fusion-based molecular probes, for which the higher brightness and tunable dimerization provide distinct advantages. Furthermore, the vsfGFP variants retain folding properties of sfGFP that enable bright fluorescence in oxidizing environments such as the bacterial periplasm.

Abstract: Chlorotoxin variants, chlorotoxin variant conjugates, compositions that include the chlorotoxin variants or conjugates, and methods for using the chlorotoxin variants, conjugates, and compositions.

Abstract: The disclosure provides an antigenic peptide targeting the extracellular, but not the intracellular, form of CETP to reduce the level of LDL (including oxLDL and other derivatives of LDL) and increase the level of HDL. Accordingly, the disclosure provides a CETP vaccine to overcome the low immunogenicity of CETP and for long-term inhibition of CETP activity to prevent or treat oxLDL or other LDL derivative-related diseases/symptoms.

Abstract: The present invention relates to a pharmaceutical composition comprising complement split product C4d for use in treating an inflammatory condition, such as graft rejection, graft versus host disease, an autoimmune disease or atopy. The C4d to be used may be a multimer. Accordingly, also C4d multimers and their use in medicine, like the treatment of inflammatory conditions, is provided. Furthermore, the present invention provides a protein complex comprising C4d interacting with its ILT4 receptor. This protein complex may be used in screening methods Also antibodies specifically binding to the C4d multimer or the C4d/ILT4-protein complex are subject of the present invention.

Abstract: This invention provides a method for treating tumors in a subject, comprising administering to the subject an effective amount of a recombinant interferon, wherein the interferon has the amino acid sequence of SEQ ID NO:2 and is encoded by the nucleotide sequence SEQ ID NO:1, wherein the tumors are selected from the group consisting of skin cancer, basal cell carcinoma, liver cancer, thyroid cancer, rhinopharyngeal cancer, solid carcinoma, prostate cancer, esophageal cancer, pancreatic cancer, superficial bladder cancer, hemangioma, epidermoid carcinoma, cervical cancer, glioma, leucocythemia, acute leucocythemia, chronic leucocythemia, lymphadenoma, and polycythemia vera.

Abstract: Peptide containing sequence from both the GLP-1 peptide and glucagon peptide, compositions comprising said peptides and methods of using said peptides for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as obesity or diabetes, are provided.

Abstract: The present invention relates to a non-peptidyl polymer-insulin multimer comprising two or more of a non-peptidyl polymer-insulin conjugate prepared by linking a non-peptidyl polymer and insulin via a covalent bond, in which the conjugates are complexed with cobalt ion to form a multimer, a method and kit for the preparation of the multimer, a pharmaceutical composition for the prevention or treatment of diabetes comprising the multimer as an active ingredient, and a method for preventing or treating diabetes by administering the composition to a subject.

Abstract: Mutant forms of human CTLA4, and their use, e.g., in xenotransplantation.

Abstract: The technology relates generally to the field of immunology and relates in part to compositions and methods for controlling the proliferation of T cells, for example, therapeutic T cells. The methods further relate to compositions and methods for inducing an immune response in a subject.

Abstract: The present invention relates to variants of a parent albumin, the variants having altered plasma half-life compared with the parent albumin. The present invention also relates to polynucleotides encoding the variants; nucleic acid constructs, vectors, and host cells comprising the polynucleotides; and methods of using the variants.

Abstract: The present invention a method for producing a human immunoglobulin G (IgG) antibody using a prime-boost regime in a Bone Marrow Liver Thymic (BLT) mouse.

Abstract: The present specification discloses HIV antigens, immunogenic compositions and medicaments comprising such HIV antigens, methods and uses for such HIV antigens and immunogenic compositions and medicaments for making a ?-HIV antibody, as well as ?-HIV antibodies, therapeutic compositions an medicaments comprising such ?-HIV antibodies, and methods and uses for such ?-HIV antibodies and therapeutic compositions and medicaments for treating an HIV-based disease.

Abstract: The invention relates to the field of immunology and vaccine development. In particular, it relates to antibodies and fragments thereof against Staphylococcus aureus and to therapeutic and diagnostic uses thereof. Provided is an isolated antibody or a functional fragment thereof, which binds to an epitope of the Immunodominant Staphylococcal antigen A (IsaA), wherein said antibody comprises at least four Isa A epitope-binding CDR sequences selected from the group consisting of SEQ ID NO: 1; SEQ ID NO: 2; SEQ ID NO: 3; SEQ ID NO: 4; SEQ ID NO: 5; SEQ ID NO: 6, and functional equivalents thereof having an amino acid sequence that is at least 85% identical to an amino acid sequence of SEQ ID NO: 1-6.

Abstract: Described are transgenic, non-human animals comprising a nucleic acid encoding an immunoglobulin light chain, whereby the immunoglobulin light chain is human, human-like, or humanized. The nucleic acid is provided with a means that renders it resistant to DNA rearrangements and/or somatic hypermutations. In one embodiment, the nucleic acid comprises an expression cassette for the expression of a desired molecule in cells during a certain stage of development in cells developing into mature B cells. Further provided is methods for producing an immunoglobulin from the transgenic, non-human animal.

Abstract: Antibodies to human N3pGlu A?, compositions comprising such N3pGlu A? antibodies, and methods of using such N3pGlu A? antibodies for the treatment of a disease characterized by deposition of A? including clinical or pre-clinical Alzheimer's disease, Down's syndrome, and clinical or pre-clinical cerebral amyloid angiopathy.

Abstract: The present invention relates to antibodies specifically binding CCL17, polynucleotides encoding the antibodies or fragments, and methods of making and using the foregoing.

Abstract: Antibodies that modulate insulin receptor signaling are provided.

Abstract: The use of a modulator of the Nav 1.9 sodium channel is described for treating an inflammatory skin disease. Also described, is a pharmaceutical composition including a modulator of the Nav 1.9 sodium channel, and in vitro diagnostic methods based on the detection or quantification of Nav 1.9.

Abstract: The balance and distribution of epithelial cell types is required to maintain tissue homeostasis. In the lung, perturbations of this balance are hallmarks of human respiratory diseases, including goblet cell metaplasia and enhanced mucus secretion in asthma and chronic obstructive pulmonary disease. We found that inflammatory cytokine treatment resulted in a skewing of basal cell differentiation towards a goblet cell fate, culminating in enhanced mucus production. We identified Notch2 as a key node required for cytokine-induced goblet cell metaplasia in vitro and in vivo Inhibition of Notch2 prevents goblet cell metaplasia induced by a broad range of stimuli, which is a hallmark of many respiratory diseases.

Abstract: The invention relates to purinergic (P2X) receptors, to generation of antibodies and to use of antibodies and immunogens for detection and treatment of a disease or condition, especially cancer.