Abstract: The invention relates to polycyclic diiminooxadiazinones of the formula I and/or of the formula II, in which in each case R1 to R12 are each independently hydrogen, a saturated or unsaturated, linear or branched, aliphatic or cycloaliphatic organic radical having 1 to 20 carbon atoms, which is unsubstituted or is substituted by radicals inert to isocyanate groups, and/or comprises heteroatoms inert to isocyanate groups in the chain, or are an aromatic organic radical having 6 to 20 carbon atoms, which is unsubstituted or is substituted by radicals inert to isocyanate groups, wherein two or more of the aforementioned radicals R1 to R6 may form further rings, in each case with one another and incorporating one, two or three carbon atoms of the fused ring segment X, and/or two or more of the aforementioned radicals R7 to R12 may form further rings, in each case with one another and incorporating one, two or three carbon atoms of the fused ring segment Y.

Abstract: The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.

Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

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

Abstract: The present invention relates to a compound (3S)-3-(4-((3-(6-Oxa-3-azabicyclo [3.1.1]heptan-3-ylmethyl)benzyl)oxy)phenyl)hex-4-ynoic acid methods for use of this and other compounds.

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I) and (II). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Abstract: The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.

Abstract: The present invention relates to novel full-color tunable light emitter based on N,C-chelate four-coordinate organoborons having excellent Quantum yield, stokes shift and solvate chromism of Formula (I);

Abstract: The present invention includes novel compounds and compositions including heteroaromatic Silicon-Fluoride-Acceptors, which are useful for PET scanning. The present invention further includes a novel method of 18F imaging for PET scanning, the method comprising the preparation of conjugates and bioconjugates of biological ligands of interest with heteroaromatic SiFAs. In one embodiment the invention is practiced in the form of a kit.

Abstract: Methods of synthesizing fluorosilanes containing cyano-substituted alkyl groups are provided. For example, 3-cyanopropyldimethylfluorosilane may be produced by reacting tetramethyldisiloxane and boron trifluoride to obtain fluorodimethylsilane and then reacting the fluorodimethylsilane with allyl cyanide, in the presence of a hydrosilylation catalyst.

Abstract: There is provided herein a method of preparing an isocyanatosilane including reacting an olefinic isocyanate with a hydridosilane in the presence of a dinuclear rhodium complex under hydrosilylation conditions.

Abstract: A novel compound chlorosilylarylgermane, a method for preparing the compound, and the use of the compound are described. A method for preparing trichlorosilyltrichlorogermane and the use of trichlorosilyltrichlorogermane are also described.

Abstract: A trichlorogermanide of formula (I): [R4N]/[R4P]Cl[GeCl3] (I), where R is Me, Et, iPr, nBu, or Ph, tris(trichlorosilyl)germanide of formula (II): [R4N]/[R4P][Ge(SiCl3)3] (II), where R is Me, Et, iPr, nBu, or Ph, a tris(trichlorosilyl)germanide adduct of GaCl3 of formula (III): [Ph4P][Ge(SiCl3)3*GaCl3], and a tris(trichlorosilyl)germanide adduct of BBr3 of formula (IV): [Ph4P][Ge(SiCl3)3*BBr3]. Also, methods for preparing the trichlorogermanides of formula (I), the tris(trichlorosilyl)germanide of formula (II), the tris(trichlorosilyl)germanide adduct of BBr3 of formula (IV).

Abstract: A multi-branched cationic phosphonium salt is provided. The multi-branched cationic phosphonium salt has a structure represented by formula (I): {Z[P+(R1)(R2)(R3)]n}(X?)n??(I) wherein each of R1, R2, and R3 is independently a linear or branched C1˜C10 alkyl group, X? is an organic or inorganic anion, and Z has a structure represented by Formula (IIb) or Formula (IIc): wherein a is an integer of 1˜15. In Formulas (IIb) and (IIc), Z is connected to [P+(R1)(R2)(R3)] at the position marked by an asterisk (*), and n is an integer of 3˜4.

Abstract: The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.

Abstract: The present invention relates to the field of pharmaceutical chemistry, and relates to a deuterium-modified Brigatinib derivative, preparation method thereof, pharmaceutical composition containing the same and the uses of the deuterium-modified Brigatinib derivative and the pharmaceutical composition thereof in preparing a medicament for treating the disease mediated by anaplastic lymphoma kinase. The deuterium-modified Brigatinib derivative of the present invention has an excellent inhibitory activity on anaplastic lymphoma kinase and has better pharmacodynamic or pharmacokinetic properties relative to Brigatinib.

Abstract: Disclosed herein, inter alia, are platinum-based compounds useful for treating cancer.

Abstract: The invention relates to nanoparticles made from organometallic hybrid materials made from iron carboxylates, used for example as contrast agents. The particles can also be used for the encapsulation and vectoring of molecules of interest such as active3 pharmaceutical agents, cosmetically interesting compounds and markers. Apart from the intrinsic properties thereof for imaging, said nanoparticles give good results in terms of capacity of loading with medicaments and in biocompatibility.

Abstract: The present invention is in the field of processes for the generation of thin inorganic films on substrates, in particular atomic layer deposition processes. The present invention relates to a process comprising bringing a compound of general formula (I) into the gaseous or aerosol state and depositing the compound of general formula (I) from the gaseous or aerosol state onto a solid substrate, wherein M is Mn, Ni or Co, X is a ligand which coordinates M, n is 0, 1, or 2, R 1, R2 are an alkyl group, an alkenyl group, an aryl group or a silyl group, m is 1, 2, or 3, R3, R4, and R5 are an alkyl group, an alkenyl group, an aryl group, an alkoxy group, or an aryloxy group, and p is 1, 2 or 3.

Abstract: The present invention relates to novel, improved processes for the preparation of sodium glucose co-transporter 2 (SGLT-2) inhibitors and novel intermediates thereof. More particularly, the present invention relates to a novel, improved process for the preparation of gliflozin compounds such as empagliflozin and dapagliflozin, intermediates thereof. The product obtained from the processes of present invention may be amorphous or crystalline, or in the form of amorphous/crystalline solid dispersions/solutions with pharmaceutically acceptable polymers and preparation process thereof. Also, the products obtained from the present invention may be used for the preparation of medicaments for the prevention and/or treatment of diseases and conditions associated with SGLT-2 inhibition.

Abstract: A baicalin magnesium compound and methods for preparing and extracting the same. The method for preparing the baicalin magnesium compound includes steps of preparation of a baicalin suspension, preparation of a magnesium ion-containing suspension, reaction and drying. The method for extracting the baicalin magnesium compound includes steps of pretreatment of macroporous resin, extraction, adsorption and elution, concentration and drying and purification. The methods restores the baicalin to the original form as found in radix scutellariae, and the baicalin magnesium compound may be used as a substitute for the baicalin in pharmaceutical applications. As compared to the baicalin, the baicalin magnesium has a greatly increased solubility, faster adsorption rate and higher oral bioavailability. The baicalin magnesium compound may also be easily formulated as a water-soluble injection or a powder injection.

Abstract: The present invention relates to novel salts and crystalline forms of (S)-2-ethylbutyl 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate for use in treating viral infections. In some embodiments, the viral infection is caused by a virus selected from the group consisting of Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, and Paramyxoviridae.

Abstract: The invention features a mononucleotide comprising a nucleobase bonded to a sugar having a 3?-carbon and a 5?-carbon, where the 5?-carbon is bonded to a phosphorus (V) atom of a phosphate group through an oxygen atom, the phosphorus (V) atom being bonded to (i) a disulfide bioreversible group through an oxygen atom; and (ii) (a) optionally substituted amino, optionally substituted alkoxy, optionally substituted aryloxy, or optionally substituted heteroaryloxy; or (b) the 3?-carbon through an oxygen atom. The invention also features methods of delivering the mononucleotide to a cell and methods of treating a subject having Hepatitis C.

Abstract: The present invention relates to a method for preparing Sofosbuvir crystal form-6. The method is simple in operation, stable in process condition, good in reproducibility, high in yield rate and high in purity, viscous gel-type products are not formed during the process, the problem of blocking of a discharge port is solved, and the method is suitable for mass industrial production and has high economic value.

Abstract: Protected fluorescent reagent compounds and their methods of synthesis are provided. The compounds are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The compounds contain fluorescent dye elements, that allow the compounds to be detected with high sensitivity at desirable wavelengths, binding elements, that allow the compounds to be recognized specifically by target biomolecules, and protective shield elements, that decrease undesirable contacts between the fluorescent dye elements and the bound target biomolecules and that therefore decrease photodamage of the bound target biomolecules by the fluorescent dye elements.

Abstract: The invention relates to nucleotide prodrugs and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel prodrugs of the invention.

Abstract: The sulfated oxysterol 5-cholesten-3?, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

Abstract: The present invention relates to a method for an improved preparative separation of proteins, particularly monoclonal antibodies (mAB) from its associated charge variants (e. g. acidic and basic monomers), glycosylation variants, and/or soluble size variants (e. g. aggregates, monomers, ? fragments, ¾ fragments, antigen binding fragments (Fab) and crystallisable fragments (Fc).

Abstract: The present invention relates to novel peptides derived from melanoma-associated antigen C2 (MAGEC2), complexes comprising such peptides bound to recombinant MHC molecules, and cells presenting said peptide in complex with MHC molecules. Also provided by the present invention are binding moieties that bind to the peptides and/or complexes of the invention. Such moieties are useful for the development of immunotherapeutic reagents for the treatment of diseases such as cancer.

Abstract: The present invention provides FOXM1-derived epitope peptides having the ability to induce cytotoxic T cells. The present invention further provides polynucleotides encoding the peptides, antigen-presenting cells presenting the peptides, and cytotoxic T cells targeting the peptides, as well as methods of inducing the antigen-presenting cells or CTLs. The present invention also provides compositions and pharmaceutical compositions containing them as an active ingredient. Further, the present invention provides methods of treating and/or preventing cancer, and/or preventing postoperative recurrence thereof, using the peptides, polynucleotides, antigen-presenting cells, cytotoxic T cells or pharmaceutical compositions of the present invention. Methods of inducing an immune response against cancer are also provided.

Abstract: The present invention refers to a method for obtaining a cell culture supernatant or a fraction thereof having a specific tumor antigen peptide repertoire having the steps of: a) exposing in suitable conditions a tumor cell culture expressing the specific tumor antigen peptide repertoire to a Pattern Recognition Receptor (PRR) agonist and/or to one inflammatory cytokine to increase the opening of connexin-hemichannels (CxH); b) collecting the cell culture supernatant; and c) optionally obtaining a fraction of the supernatant, wherein the supernatant has MHC class I and MHC class II peptides and non-classical MHC molecules (HLA-E).

Abstract: The present invention relates to novel peptides derived from DDB1- and CUL4-associated factor 4-like protein 2 (DCAF4L2), complexes comprising such peptides bound to recombinant MHC molecules, and cells presenting said peptide in complex with MHC molecules. Also provided by the present invention are binding moieties that bind to the peptides and/or complexes of the invention. Such moieties are useful for the development of immunotherapeutic reagents for the treatment of diseases such as cancer.

Abstract: The present invention relates to novel peptides derived from piwi-like protein 1 (PIWIL1), complexes comprising such peptides bound to recombinant MHC molecules, and cells presenting said peptide in complex with MHC molecules. Also provided by the present invention are binding moieties that bind to the peptides and/or complexes of the invention. Such moieties are useful for the development of immunotherapeutic reagents for the treatment of diseases such as cancer.

Abstract: Peptides with anti-influenza properties are disclosed herein. The peptides include dextro (D) or a mixture of dextro/levo (L)-amino acids, possess anti-influenza properties against multiple types of human influenza viruses along with the types which infect animals and birds and are useful as pharmaceutical compositions for the treatment or prevention of influenza virus infections.

Abstract: The present invention relates to novel peptides derived from solute carrier family 45 member 2 (SLC45A2), complexes comprising such peptides bound to recombinant MHC molecules, and cells presenting said peptide in complex with MHC molecules. Also provided by the present invention are binding moieties that bind to the peptides and/or complexes of the invention. Such moieties are useful for the development of immunotherapeutic reagents for the treatment of diseases such as cancer.

Abstract: The present invention relates to lysobactin for use in the treatment of bovine mastitis.

Abstract: The invention relates to ?-amaninamide (1; x=0, 1 or 2), ?-amaninamidic acid (2; x=0, 1 or 2), and ?-amaninamidic hydroxamic acid (3; x=0, 1 or 2), novel derivatives of ?-amanitin (4), and methods and novel building blocks for the synthesis thereof.

Abstract: The invention provides methods and compositions for eliciting broad immune responses to HIV envelope proteins. The methods include use of nucleic acids constructs that encode conserved elements of HIV Env to induce immune responses.

Abstract: Stable pre-fusion class I fusion proteins in the pre-fusion conformation, including one or more mutations in the hinge-loop that is present between the base helix and the RR1, are described.

Abstract: Nucleic acid molecules and compositions comprising one or more nucleic acid sequences that encode an RSV immunogen are disclosed. Nucleic acids are disclosed that comprise the sequences that encodes consensus RSV F protein or immuno-genic fragment thereof, sequences that encodes an RSV G(A) protein or immunogenic fragment thereof and sequences that encodes an RSV G(B) protein or immunogenic fragment thereof. Compositions comprising one, combinations of two or all three sequences are disclosed. The coding sequences optionally include operable linked coding sequence that encode a signal peptide. Nucleic acid molecules and compositions comprising the chemokine CC20 and/or a consensus RSV M2-1 protein or immunogenic fragment thereof are also disclosed. Immunomodulatory methods and methods of inducing an immune response against RSV are disclosed. Methods of preventing RSV infection and methods of treating individuals infected with RSV are disclosed.

Abstract: A novel optogenetic system, including constructs and methods, is provided based on the interaction of Rhodopseudomonas palustris BphP1 and Rhodopseudomonas palustris PpsR2 or a non-dimerizing variant thereof.

Abstract: The present invention provides a multi-peptide composition with antibacterial activity comprising at least 3 peptides with the sequences as set forth in SEQ ID NO:1, 2 or 3 (or related sequences), respectively, in which the SEQ ID NO:1 sequence (or its related sequence) comprises at least two tryptophan residues. In particular the invention provides a new bacteriocin, Garvicin KS. The invention also provides compositions and host cells containing such antibacterial compositions. Uses of the antibacterial composition in treating bacterial infection and products treated with the antibacterial composition are also provided.

Abstract: According to present invention embodiments, a trackable moiety can be attached to a quorum sensing (QS) molecule to form a QS modulating conjugate. QS modulating conjugates retain their activity for QS manipulation and are able to be detected by imaging techniques. The QS portion of the QS modulating conjugate can play a role in affecting bacterial behaviors, such as, inhibition of biofilms or disruption of toxin production, while the trackable moiety of the QS modulating conjugate enables monitoring, visualization in real time of its binding to the receptor on the bacterial surface, and the location of the bacterium itself, for example, in a biofilm and/or at an infection site. Since binding of the QS modulating conjugate to its cognate receptor is specific, the QS modulating conjugate can be used for diagnostic applications by enabling pinpointing of specific bacteria at infection sites.

Abstract: The present invention relates to a new class of peptides having antibacterial activity and presenting D-amino acids and their uses. It also relates to a new enzyme presenting a peptide epimerase activity in vitro and in vivo, thereby being useful for modifying peptides in order to change the amino acid configuration from L to D.

Abstract: The invention concerns novel streptavidin muteins. In one embodiment such a mutein (a) contains two or more mutations in the region of the amino acid positions 117 to 121 with reference to the amino acid sequence of wild type streptavidin of which amino acid residues 14 to 139 are as set forth at SEQ ID NO:212 and (b) has a higher binding affinity than each of (i) a streptavidin mutein “1” (SEQ ID NO: 16) that comprises the amino acid sequence Val44-Thr45-Ala46-Arg47 (SEQ ID NO: 98), or (ii) wild type-streptavidin of which amino acid residues 14 to 139 are shown as SEQ ID NO: 212 for peptide ligands comprising the amino acid sequence Trp-Ser-His-Pro-Gln-Phe-Glu-Lys (SEQ ID NO: 100).

Abstract: This invention provides polypeptides that were identified as interacting with Vip3 toxin. This invention also provides a method of identifying agents that bind to Vip3 interacting polypeptides, which agents may act as insecticidal agent, cytotoxic agents and/or modulate the activity of Vip3 interacting polypeptides.

Abstract: The present invention provides an isolated nucleic acid molecule comprising, or consisting of, the nucleic acid sequence of SEQ ID NO:1 or a nucleic acid sequence of at least 300 bp having at least 80% identity to said sequence of SEQ ID NO:1, wherein said isolated nucleic acid molecule specifically leads to the expression in rod photoreceptors of a gene when operatively linked to a nucleic acid sequence coding for said gene.

Abstract: The present invention relates to isolated Nato3 mutant polypeptides. Methods for stimulating a brain cell to differentiate into a dopaminergic progenitor neuronal cell or a dopaminergic neuron comprises increasing phosphorylation of Nato3 in the brain cells and culturing the brain cells until a progenitor dopaminergic neuronal cell marker or a dopaminergic neuronal cell marker is expressed in the cultured brain cells. Methods for treating Parkinson's disease (PD) in a subject comprises administering to the subject in need thereof, a composition comprising progenitor dopaminergic neuronal cells and/or dopaminergic neuronal cells expressing a Nato3 mutant polypeptide to the brain of the subject.

Abstract: Provided herein are compositions and methods relating to cell-penetrating conjugates for the delivery of therapeutic polypeptides or polynucleotides to cells or tissues of the body. The delivery conjugate comprises a cell-penetrating peptide and a nuclear localization signal sequence plus an effector moiety (such as a polypeptide or polynucleotide) as the payload, optionally further including an epitope tag as well as a solubility peptide and a configurating peptide. The delivery conjugate can also include a component capable of specifically directing the conjugate to a target cell or tissue, making the conjugate effective for treating diseases in the target tissue.