Abstract: The invention provides novel phosphorus imidazoquinoline amine derivatives, having agonistic activities to Toll-like receptors (TLRs), in particular TLR7 and/or TLR8, pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by or associated with TLR7 and/or TLRS, e.g., cancer, graft rejection, autoimmunity, inflammation allergy, asthma, infection, sepsis, and immunodeficiency.

Abstract: The present invention relates to an arylphosphine oxide having inhibitory effect on protein tyrosine kinases, a pharmaceutical composition containing the same, a preparation and a use thereof. Specifically, the present invention discloses a compound represented by formula (I), a pharmaceutically acceptable salt, crystal form, prodrug, metabolite, hydrate, solvate, stereoisomer or isotope derivative thereof, wherein X, Y, R1, RP1, RP2, R2, W and m are as defined in the description. The compound of the invention can be used in the treatment of ALK-mediated cancer-associated disorders, such as non-small cell lung cancer, breast cancer, neurological tumors, esophageal cancer, soft tissue cancer, lymphoma or leukemia.

Abstract: The invention relates to crystalline forms of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbony]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms and their use as a medicament, especially as a P2Y12 receptor antagonist.

Abstract: A compound having the formula Ir(LA)n(LB)3?n, having the structure Formula I, is disclosed. In Formula I, each of Z1, Z2, Z3, and Z4 is CR2; X is O, S, or Se; n is an integer from 1 to 3; R1, R2, R3, R4, and R5 each independently represent mono- to a maximum possible number of substitutions, or no substitution; R1, R2, R3, R4, and R5 are each independently selected from a variety of substituents; any two substitutions in R1, R2, R3, R4, and R5 are optionally joined to form a ring; at least one pair of substitutions in R1, R2, R3, R4, and R5 are joined together to form a bridge structure comprising a backbone structure that forms a fused first ring, which can be further substituted; and the backbone structure is saturated. Organic light emitting devices and consumer products containing the compounds are also disclosed.

Abstract: A composition including a platinum-containing organometallic compound, a first compound, a second compound, and a third compound, and an organic light-emitting device including the same wherein the composition does not comprise iridium, the Pt-containing organometallic compound, the first compound, the second compound, and the third compound are different from each other, the first compound comprises at least one electron transport moiety, the second compound and the third compound do not include a metal, each of an absolute value of a HOMO energy level of the second compound and an absolute value of a HOMO energy level of the third compound is 5.30 eV to 5.85 eV, the difference between the absolute value of the HOMO energy level of the second compound and the absolute value of the HOMO energy level of the third compound is 0.01 eV to 0.30 eV.

Abstract: Compositions and methods comprising metal organic frameworks (MOFs) and related uses are generally provided. In some embodiments, a MOF comprises a plurality of metal ions, each coordinated with at least one ligand comprising at least two sets of ortho-diimine groups arranged about an organic core.

Abstract: The present invention relates to a method for preparing an activated lignin composition. In addition, the present invention also relates to a method for further processing the thus activated lignin composition in a method for preparing a lignin-phenol formaldehyde resin. Such a lignin-phenol formaldehyde resin can be used in the manufacturing of laminates by replacing the traditional synthetic phenol formaldehyde resin.

Abstract: Allulose crystals are efficiently produced from an allulose syrup using seed crystals.

Abstract: Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.

Abstract: Disclosed are aminocoumarin compounds, pharmaceutical compositions containing aminocoumarin compounds, and methods of their use, e.g., in the treatment of a Gram-negative bacterial infection.

Abstract: The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl), T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

Abstract: The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl), T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

Abstract: Provided herein are methods and labeling kits for synthesizing 2?-deoxy-2?-[18F]fluoro-5-methyl-1-beta-D-arabino-furanosyl-uracil in a one-pot reaction in compliance with CGMP. Also disclosed are labeling kits that can be assembled in an automated synthesis system to enable such a reaction.

Abstract: The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.

Abstract: The invention relates to a crystalline methanol or dimethyl sulfoxide solvated form of regadenoson and an anhydrous polymorph of regadenoson. The invention is also directed to the preparation of the methanol or dimethyl sulfoxide solvated and anhydrous solid-state forms of regadenoson. In particular, the invention relates to the preparation of the anhydrous polymorph of regadenoson in a stable form from the dimethyl sulfoxide solvated form of regadenoson, which preparation is purifiable and scalable.

Abstract: Compounds of formula I, wherein Base, R1 and R2 are defined as in claim 1, are modulators of STING.

Abstract: A compound of the structure: or a pharmaceutically acceptable salt or composition thereof for the treatment of a host infected with or exposed to an HCV virus or other disorders more fully described herein.

Abstract: Disclosed are messenger RNA molecules and related compositions incorporating a 4?-thio modification in the furanose ring of at least one nucleotide residue, and methods of using these mRNAs to produce an encoded therapeutic protein in vivo and to treat or prevent diseases or disorders. In certain embodiments, the 4?-thio modified mRNA provides for enhanced stability and/or reduced immunogenicity in in vivo therapies.

Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, or disorders that are affected by the modulation of STING. Such compounds are represented by Formula (I) as follows: wherein B2, X2, R2a, R2b, R2c, Z-M-Y, Y1-M1Z1, B1, X1, R1a, R1b, R1c are as defined herein.

Abstract: The present invention relates to methods and compounds for the solid phase synthesis of peptides carrying a substituent at an amino group of an amino acid side chain.

Abstract: In certain embodiments, the present invention provides a method of purifying a monomeric monoclonal antibody from a mixture which comprises the monomeric monoclonal antibody and one or more contaminants, comprising: a) subjecting the mixture to cation exchange chromatography (CEX) matrix, wherein the monomeric monoclonal antibody binds to the CEX matrix; b) contacting the CEX matrix with a wash solution at a pH which is between about 7 and about 7.8; c) eluting the monomeric monoclonal antibody from the CEX matrix into an elution solution, thereby purifying the monomeric monoclonal antibody.

Abstract: Provided herein are compositions and methods for protein purification.

Abstract: The present invention concerns a method for purifying a protein comprising in a continuous mode: one filtration step involving the use of at least one chelating agent, an exchanging step involving the use of at least one diafiltration membrane, and a polishing step involving the use of a combination of membrane adsorbers, wherein two membrane adsorbers of said combination are orthogonal in terms of mechanism of action.

Abstract: This invention relates to a hybrid ligand, a hybrid biomimetic chromedia and a preparing method and a use thereof, wherein the hybrid biomimetic chromedia takes hydrophilic porous microsphere as a substrate in chromatography, activated with allyl bromide and undergoing bromo-alcoholization with N-bromosuccinimide, then coupled with the hybrid ligands. The sequence of the hybrid ligand is phenylalanine-tyrosine-glutamine-5-aminobenzimidazole. The hybrid biomimetic chromedia has both of the two functional groups of phenylalanine-tyrosine-glutamine tripeptide and aminobenzimidazole, while maintaining the high antibody selectivity of polypeptide ligand, hydrophobic electric charge inductive ligand is introduced to achieve more moderate elution requirement, realizing effective antibody separation.

Abstract: AT-rich interactive domain-containing protein 5a (Arid5a) inhibitors can include mid-sized peptides (peptides having less than 15 amino acids) that inhibit the activity of Arid5a. The peptides include the sequence of SEQ ID NO: 1. In an embodiment, the Arid5a peptide inhibitors can include a peptide having a sequence selected from the group consisting of SEQ ID NO: 2, SEQ ID NO:3, and SEQ ID NO:4. The Arid5a peptide inhibitors can be useful for experimental investigation and treating a disease or disorder, such as, inflammation, diseases associated with inflammation, cancer, and autoimmune disease.

Abstract: The present disclosure provides peptides comprising a motif having four amino acids, wherein each of the amino acids at N-terminus and C-terminus of the sequence independently has a same or different positively charged side chain, and each of the amino acids between the N-terminal and C-terminal of the motif independently has a same or different uncharged side chain. The present disclosure surprisingly found that these peptides have advantageous effects in inhibiting or decreasing collagen breakdown, increasing production of collagen, elastin and/or hyaluronic acid, retarding aging, improving skin and inhibiting inflammation.

Abstract: The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases.

Abstract: Described herein are isolated peptides, compositions comprising the same, and methods of using such peptides or compositions in the treatment of depression, central nervous system disorders, and neurodevelopmental disorders.

Abstract: The invention is directed to modified HIV-1 envelopes, compositions comprising these modified envelopes and methods of using these modified HIV-1 envelopes to induce immune responses.

Abstract: The present invention relates to expression of Pneumococcal Surface Protein A (PspA). The invention represents an advancement in the field of genetic engineering and vaccine technology. The invention discloses expression vectors and recombinant host cells for expression of truncated PspA peptide. The invention also discloses vaccine compositions comprising the truncated peptides as carrier protein.

Abstract: Coccidioidomycosis is most often diagnosed serologically and the quantitative complement-fixing antibody test (CF) is considered prognostically useful. Because CF is complex, labor-intensive, and poorly standardized, an enzyme-linked immunoassay (ELISA) alternative would be attractive. The present invention features an antibody-binding domain that is restricted to a 200 amino acid recombinant peptide of the known antigen responsible for CF activity. Overlapping truncations of this peptide do not bind CF antibodies, suggesting that the responsible epitope(s) are conformational. Further, anchoring the antigenic peptide to the ELISA plate by means of a C-terminal tag instead of allowing the peptide to randomly adhere to the plastic plate improves sensitivity of antibody detection by one to two logs in different sera. The newly developed ELISA shows a significant quantitative correlation with CF. This ELISA shows potential as the basis for a new quantitative assay for coccidioidal antibodies.

Abstract: The present invention relates to novel chimeric molecules of ficolin-associated polypeptides, such as fusion polypeptides for the use in the treatment of conditions associated with inflammation, apoptosis, autoimmunity, coagulation, thrombotic or coagulopathic related diseases. The present invention further relates to nucleic acid molecules encoding such fusion polypeptides, vectors and host cells used in the production of the fusion polypeptides.

Abstract: The disclosure of the present application relates to a secretory deleted split hand/split foot 1 (sDSS1) protein, the amino acid sequence thereof, the nucleic acid sequence thereof, and the applications of the same. The sDSS1 protein is a secretory protein from higher primate, and can be detected in human serum and cerebral spinal fluid (CSF). The sDSS1 protein can form conjugate with oxidized protein under nonenzymatic condition or with amyloid-beta (A?) polypeptide to reduce formation of A? oligomer. The addition of sDSS1 protein to culture medium can shield the cytotoxicity induced by oxidized protein, A? oligomer, amylin oligomer and glycosylated protein, so as to protect the cells against these toxoproteins. The sDSS1 protein can prolong survival time of senescence-accelerated mice significantly.

Abstract: The present invention provides a C-terminal CDNF fragment sequence or a sequence which has at least 80% homology or sequence identity to said sequence. The C-terminal CDNF fragment protects ER stressed neurons, motoneurons and dopaminergic neurons and the fragment is capable of penetrating neuronal cell membrane as well as the blood-brain-barrier. The present invention further provides said fragment and pharmaceutical compositions comprising said fragment for use in treatments of degenerative diseases and disorders including central nervous system diseases, diabetes and retinal disorders. The present invention is also providing a C-terminal MANF fragment sequence or a sequence which has at least 80% homology or sequence identity to the said sequence and pharmaceutical compositions comprising said MANF fragment for use in the treatment of degenerative diseases and disorders including central nervous system diseases, diabetes and retinal disorders.

Abstract: Provided is a polynucleotide, including a cis-regulatory element and a nucleotide sequence encoding a vestigial like 4 protein, wherein the cis-regulatory element includes an uncoupling protein 1 enhancer and an uncoupling protein 1 promoter. Also provided is a viral vector including said polynucleotide. Also provided is a method of transfecting a cell or a subject with said polynucleotide or said viral vector.

Abstract: The present disclosure relates to a polypeptide exhibiting granulocyte-colony stimulating factor activity. The polypeptide comprises at least one non-native cysteine residue at a site selected from the group consisting of T1CP2 (SEQ ID NO: 25), P2CL3 (SEQ ID NO: 26), L3CG4 (SEQ ID NO: 27), G4CP5 (SEQ ID NO: 28), P5CA6 (SEQ ID NO: 29), A6CS7 (SEQ ID NO: 30), S96CP97 (SEQ ID NO: 31), P97CE98 (SEQ ID NO: 32), L99CG100 (SEQ ID NO: 33), P101CT102 (SEQ ID NO: 34), E122CE123 (SEQ ID NO: 35), L124CG125 (SEQ ID NO: 36), M126CA127 (SEQ ID NO: 37), P138CA139 (SEQ ID NO: 39), A143CF144 (SEQ ID NO: 40), R146CR147 (SEQ ID NO: 41), R169CH170 (SEQ ID NO: 42), H170CL171 (SEQ ID NO: 43), L171CA172 (SEQ ID NO: 44), A172CQ173 (SEQ ID NO: 45), and Q173CP174 (SEQ ID NO: 46) in an amino acid sequence having at least 90% sequence identity to sequence set forth in SEQ ID NO: 2.

Abstract: The present disclosure concerns agents and their use in the treatment of endocrine, nutritional and/or metabolic diseases in a mammal. The disclosure furthermore concerns novel peptides.

Abstract: A gene combination for expressing recombinant human nerve growth factor (rhNGF) includes an rhNGF precursor gene and an intron. The intron can have a nucleotide sequence shown in SEQ ID NO: 1 or SEQ ID NO: 2. A eukaryotic expression vector for rHNGF expression including the gene combination, a CHO cell including the eukaryotic expression vector, and methods for preparing rhNGF using the gene combination, the expression vector, and the CHO cell are also disclosed.

Abstract: Described herein are modified fibroblast growth factors (FGFs), pharmaceutical compositions, formulations, and medicaments that include such modified FGFs, and methods of using such modified FGFs to treat mammalian diseases, disorders, or conditions.

Abstract: Methods are provided for protecting a subject from retinal degeneration, and/or treating uveitis, retinitis or chorioretinitis in a subject. The methods include selecting a subject with uveitis, retinitis, or chorioretinitis and/or in need of protection from retinal degeneration; and administering locally to the eye of the subject a therapeutically effective amount of: (a) a polypeptide comprising amino acids 1-182 of an interleukin (IL)-34, a variant of IL-34, or an Fc fusion protein of IL-34, wherein the polypeptide, variant, or Fc fusion protein is i) anti-inflammatory or ii) neuroprotective; or (b) a nucleic acid molecule encoding the polypeptide, variant, or Fc fusion protein. A pharmaceutical composition for use in any of the disclosed methods is also provided.

Abstract: The present invention provides compositions and methods for treating cancer in a human. The invention includes administering a genetically modified Th17 cell to express a CAR having an antigen binding domain, a transmembrane domain, and an ICOS intracellular signaling domain.

Abstract: The invention relates to the regulated expression of a chimeric antigen receptor (CAR) within a lentiviral vector. The CAR comprises a hook-binding domain that interacts with a hook, preferably encoded by the same lentiviral vector, which prevents proper processing and release of the CAR to the cell membrane. The invention encompasses vectors, methods of making the vectors, and methods of using them, including medicinal uses. The vectors can be used for administration to humans to induce immune responses and to treat cancers and tumors.

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: Provided are methods for activating an antigen-presenting cell and eliciting an immune response by inducing an inducible pattern recognition receptor adapter, or adapter fragment, and CD40 activity. Also provided are nucleic acid compositions comprising sequences coding for chimeric proteins that include an inducible CD40 peptide and an inducible pattern recognition receptor adapter or adapter fragment.

Abstract: The invention relates to novel TNF family ligand trimer-containing antigen binding molecules comprising (a) one Fab domain capable of specific binding to a target cell antigen, (b) a Fc domain composed of a first and a second subunit capable of stable association, and (c) a first polypeptide comprising two ectodomains of a TNF ligand family member or fragments thereof that are connected to each other by a peptide linker and a second polypeptide comprising one ectodomain of said TNF ligand family member or a fragment thereof, wherein the first polypeptide is fused at its N-terminus to the C-terminus of one of the subunits of the Fc domain and wherein the second polypeptide is fused at its N-terminus to the C-terminus of the other subunit of the Fc domain, wherein the TNF family ligand trimer-containing antigen binding molecule is monovalent for the binding to the target cell antigen.

Abstract: The invention features soluble FGF decoy polypeptides and fusion polypeptides comprising an FGF decoy polypeptide linked to a heterologous polypeptide, such as an aggrecan binding protein. Both soluble FGF decoy polypeptides and fusion polypeptides can be used to prevent or treat skeletal disorders, such as achondroplasia.

Abstract: The present invention relates to a method for preparing a composition comprising monomeric conjugates from a sample, said conjugate comprising (a) a polypeptide comprising the amino acid sequence of interleukin 15 or derivatives thereof, and (b) a polypeptide comprising the amino acid sequence of the sushi domain of IL-15R? or derivatives thereof; wherein said method comprises the use of anion-exchange chromatography followed by a hydrophobic interaction chromatography; and to a pharmaceutical composition which can be obtained by such a method.

Abstract: Provided herein are multifunctional heteromer proteins. In specific embodiments is a heteromultimer that comprises: at least two monomeric proteins, wherein each monomeric protein comprises at least one cargo polypeptide, attached to a transporter polypeptide, such that said monomeric proteins associate to form the heteromultimer. These therapeutically novel molecules comprise monomers that function as scaffolds for the conjugation or fusion of therapeutic molecular entities resulting in the creation of bispecific or multivalent molecular species.

Abstract: The disclosure describes a recombinant immunoglobulin heavy chain comprising a sortase conjugation loop, methods for conjugating and/or labeling such recombinant immunoglobulin heavy chains by use of the enzyme sortase and to the conjugates/labeled products obtained via the method.

Abstract: This disclosure relates to binding agents with specificity for HIV and to methods for using the same to treat, pre-vent and/or ameliorate HIV infection and/or AIDS.