Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

Abstract: The present invention relates to fused pyrimidine compounds, particularly pyrrolopyrimidine and thienopyrimidine compounds and derivatives thereof, pharmaceutical compositions thereof, and methods of inhibiting BRD4 and/or JAK2, as well as methods of treating various diseases and conditions, such as cancer and leukemia, with such compounds. Bromodomain binding and JAK activity are included.

Abstract: Provided herein are compounds useful for the treatment of various parasitic diseases. These compounds, as well as pharmaceutically acceptable salts thereof may be formulated in pharmaceutical compostions, veterinary compositions and may be used in methods of treatment and/or prophylaxis of diseases spread by parasites, including malaria and cryptosporidiosis.

Abstract: The present invention provides a compound of Formula I: wherein R is hydrogen or methyl; and Z is: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating neurodegenerative diseases, such as Alzheimer's disease.

Abstract: The present invention provides novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.

Abstract: The invention provides a chemical entity of Formula (I): wherein R1, R2, X, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods as disclosed herein, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.

Abstract: The present invention relates to compounds that are useful as radiopharmaceuticals and radioimaging agents which bear a radionuclide-chelating agent. These coordinated compounds are useful in radiotherapy and diagnostic imaging. The invention also relates to methods of diagnosis, prognosis and therapy utilising the non-coordinated and radiolabelled compounds of the invention.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of USP7 activity.

Abstract: The present invention is directed to 6,5-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: The present invention is directed to azabicyclo[4.1.0]heptane compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

Abstract: To provide novel pesticides, especially insecticides or acaricides. A condensed heterocyclic compound represented by the formula (1) or its salt, or N-oxide thereof: wherein Q is a structure represented by Q1, Q2 or the like, D substituted with —S(O)nR1 is a structure represented by D1 or D2, A1 is N(A1 a) or the like, A1 a is C1-C6 alkyl or the like, A4 is a nitrogen atom or C(R4), A5 is a nitrogen atom or C(R5), R1 is C1-C6 alkyl or the like, each of R2, R5 and R6 is independently a hydrogen atom or C1-C6 alkyl, each of R3, R4, Y1, Y2, Y3 and Y4 is independently a halogen atom, halo (C1-C6) alkyl or the like, and n is an integer of 0, 1 or 2.

Abstract: Porous calcium lactate metal-organic frameworks (MOFs) comprise non-toxic metal ions—Ca(II) and non-toxic, renewable and cheap linkers—lactate and acetate. The MOFs are nontoxic and environmentally-benign, and can be used as degradable carriers.

Abstract: The present specification relates to a compound containing nitrogen, and a color conversion film, a backlight unit, and a display device, including the same.

Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

Abstract: Silicone compounds, delivery compositions, compositions, packaged products and displays comprising such silicone compounds, and processes for making and using such benefit agent delivery compositions, compositions, packaged products and displays. Such compositions have improved deposition and retention properties that may impart improved benefit characteristics to a composition and/or situs.

Abstract: A method of producing a halosiloxane, the method comprising: combining water, a halosilane, and a first solvent, where the first solvent has a water solubility of >1.5 grams in 100 ml of solvent, to form a reaction mixture having a temperature above the melting point temperature of the solvent, partially hydrolyzing and condensing the halosilane to form a reaction product mixture comprising the halosiloxane, the solvent, a hydrogen halide and unreacted halosilane, and, optionally, adding a second solvent with a boiling point a the boiling point of the halosiloxane to the reaction mixture or the reaction product mixture.

Abstract: The present invention relates to a compound of formula 1 and an organic electronic device comprising an organic semiconductor layer, wherein at least one organic semiconductor layer comprises a compound of formula (1), wherein X is selected from O, S or Se; Ar1 is selected from unsubstituted or substituted C2 to C60 heteroarylene, and wherein the substituted C2 to C60 heteroarylene comprises at least about one to about six substituents, wherein the substituent of the substituted C2 to C60 heteroarylene are independently selected from C1 to C12 alkyl, C1 to C12 alkoxy, CN, OH, halogen, C6 to C36 arylene, or C2 to C25 heteroarylene; n is 1 or 2; L1 is selected from a single bond, C1 to C4 alkyl, substituted or unsubstituted C6 to C36 arylene, wherein the substituent of substituted C6 to C36 arylene is selected from C1 to C12 alkyl, C6 to C18 arylene; L2 is selected from a single bond or C1 to C6 alkyl; R1, R2 are independently selected from substituted or unsubstituted C1 to C16 alkyl, wherein the substituent o

Abstract: Materials and methods for preparing reactive lignin and for preparing a bio-based adhesive are described herein.

Abstract: The present invention relates to an indoleacetic acid derivative and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound shown in general formula (I), a preparation method thereof, a pharmaceutical composition comprising the same, and a use thereof as a cough suppressant in treating a disease such as a cough. The definition of each substituent in the general formula (I) is the same as the definition in the specification.

Abstract: The present invention provides prodrugs of clofarabine. The compounds of the invention have formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is H or —C(=0)-X—R3 and R2 is H or —C(=0)-Y—R4, wherein X and Y are each independently O, CH2 or CH(NH2), provided R1 and R2 are not both H; and R3 and R4 are each independently selected from the group of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl and substituted heteroalkyl. Compositions of formula (I) and methods for the treatment of cancer are also provided.

Abstract: The invention provides a a compound of formula I: wherein R1-R6 and X have any of the values described herein, as well as pharmaceutical compoustions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-?-hydroxysteroids from ?-9,11-ene, 11-keto or 11-hydroxy-?-steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.

Abstract: The present disclosure relates to site-selective labeling compounds, and methods of using such compounds.

Abstract: A chromatographic method for collecting blood coagulation factor VII (Factor VII) and/or activated blood coagulation factor VII (activated Factor VII) from plasma-derived fractions with high yield is provided. In accordance with the method of the present invention, Factor VII and/or activated Factor VII of interest can be collected with a recovery rate of as high as 90% or more by letting Factor VII and/or activated Factor VII which fails to be adsorbed to a first anion exchange resin and remains in a non-adsorption fraction be adsorbed in a second anion exchange resin.

Abstract: The present invention relates to a purification process of recombinant antibody fragments from inclusion bodies expressed in microbial cells. More particularly, the present invention relates to a process for purification of recombinant humanized (rHu) antibody fragment, Ranibizumab from inclusion bodies expressed in microbial cells.

Abstract: Compounds useful for the treatment of malaria, cancer, Parkinson's disease, diabetes, and bacterial infection.

Abstract: The present application discloses a crystal of oxidized glutathione dication salt and a method of producing the same.

Abstract: One aspect of this study was to provide a bioinformatic analysis to assess whether the MNTF-derived peptide known as GM6 alters the expression of genes associated with Alzheimer's disease. Gene expression analyses are performed using several gene expression profiling datasets generated by DNA microarray or RNA-seq technology. Our results show Alzheimer's disease-associated genes exhibit unique responses to GM6 treatment, impacting signaling pathways linked to core processes that underlie Alzheimer's disease onset and progression. The expression of one or more genes or gene variants of particular interest described herein. We show that ALS patients treated with GM6 exhibit significantly decreased abundance of plasma tau post-treatment (FIG. 1D). We also show that GM6 repressed MAPT mRNA in SH-5YSY cells (FIG. 2).

Abstract: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.

Abstract: The present invention relates to a nanocarrier peptide sequence (Sequence Id no. KXPXXXXA/V/GXGNXX; wherein X is selected from amino acid R, K, A or H. The present invention also relates to the method for cellular delivery, comprising the steps of: complexation of a peptide nanocarrier sequence: XPXXXXA/V/GXGNXX; where X is selected from amino acid R, K, A and H having SEQ ID NO 6 with a macromolecule to obtain a complex; and administering the complex to a targeted mammalian or plant cell or tissue.

Abstract: Described herein are compositions and methods for the modulation of T-cell tolerance, which can be upregulated or down regulated by concurrent enhancement or inhibition of CEACAM1/TIM3 interactions. As described herein, the discovery that CEACAM1 is a direct ligand of TIM3 and vice versa has been shown in cis and in trans. In addition, as demonstrated herein, CEACAM1 and TIM3 are co-regulated during the course of T-cell activation.

Abstract: There is described herein antagonists of ?4?7 integrin, and more particularly cyclic peptide antagonists, such as compounds of formula (I).

Abstract: The present invention provides an agent, or a composition containing an agent, for use in treating or preventing a bacterial infection in a subject, wherein said agent comprises: (i) an oligopeptidic compound comprising a PCNA interacting motif and a domain that facilitates the cellular uptake of said compound, wherein the PCNA interacting motif is X1X2X3X4X5 (SEQ ID NO: 1) and wherein: X1 is a basic amino acid; X2 is an aromatic amino acid; X3 is an uncharged amino acid other than an aromatic amino acid, Glycine (G) and Proline (P); X4 is any amino acid other than Proline (P), an acidic amino acid or an aromatic amino acid; and X5 is a basic amino acid or Proline (P); or (ii) a nucleic acid molecule comprising a sequence encoding the oligopeptidic compound of (i). In certain aspects the agent and compositions of the invention may be used as single agents.

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: Variant factor H binding proteins that can elicit antibodies that are bactericidal for at least one strain of Neisseria meningitidis, compositions comprising such proteins, and methods of use of such proteins, are provided.

Abstract: The present invention relates to novel hybrid peptides developed from the combination of membrane surface protein peptide fragments present in anaplasmosis microorganisms, and in particular, bacteria of the species Anaplasma marginale. The present invention further relates to hybrid peptide sets, compositions and kits comprising such novel hybrid peptides, their uses and methods of inducing immune response. Each hybrid peptide, according to the present invention, comprises two or more peptide fragments of amino acid sequences as defined in the present invention linked together by means of a spacer element. The combined peptide fragments are protein peptide fragments of MSP1, MSP1a, MSP1b, MSP2, MSP2-HRV, MSP3, OMP7, OMP8, VirB9 and VirB10.

Abstract: In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and/or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.

Abstract: Embodiments of the invention are generally directed to lignin-modifying enzymes and systems and methods of their manufacture. In many embodiments, the lignin-modifying enzymes are lignin-degrading enzymes capable of breaking down lignin into component parts that are usable for other purposes. Several embodiments are directed to systems for producing lignin-modifying enzymes in vivo, including in yeast and/or plant species, and certain embodiments are directed to methods of creating these systems, including transfecting the species to produce lignin-modifying enzymes.

Abstract: The invention relates to a method for preparing a protein isolate of the biomass of microalgae of the genus Chlorella, characterised in that it comprises the following steps: supplying a microalgal biomass produced by fermentation, washing the biomass so as to eliminate the soluble interstitial compounds and concentrating the biomass, mechanically grinding the washed and concentrated biomass in a horizontal ball grinder-type system in order to produce an emulsion, destructuring the emulsion thus produced, triple-phase separation so as to separate the soluble fraction from the fractions containing the lipids and the cell debris, recovery of the soluble fraction thus produced in order to produce the soluble protein isolate, then evaporation, pasteurisation and atomisation of said protein isolate.

Abstract: Compositions comprising an isolated peptide, which may for example optionally comprise a sequence consisting of SVHSFDYDWYNV, or any cyclized version thereof, and methods of using same, including for treatment of or prevention of formation of microbial biofilms and against adhesion of a cell to a surface.

Abstract: An object of the present invention is to provide a soluble RNA-binding protein having high binding ability. The present invention provides an RNA-binding protein having an amino acid sequence represented by R1?-R1X-R2X-(R5X or R6Y)L-(R5X-R6Y)M-(R5X or R6Y)N-R7X-R8X-R8? wherein each symbole means an amino acid sequence recited in the specification.

Abstract: Methods and compositions for rapidly replacing cMyBP-C in sarcomeres featuring the creation of Spy-C mice, which are mice genetically engineered to express cMyBP-C with a protease recognition site and SpyTag peptide introduced into the cMyBP-C gene. In permeabilized myocytes from the Spy-C mice, the cMyBP-C protein can be cleaved at the protease recognition site, and the N-Terminus of cMyBP-C can be removed while the C-terminus remains anchored to the thick filament. A new peptide featuring the SpyCatcher sequence can be covalently bonded to the remaining portion of cMyBP-C, thereby creating a modified cMyBP-C protein. The methods and compositions of the present invention allow for the reconstitution of full-length cMyBP-C at the precise position of native cMyBP-C in the sarcomere and allow for a variety of modifications to be introduced to cMyBP-C in situ.

Abstract: The present invention provides methods for assessing whether a subject is at risk of developing a neurological disorder, diagnosing or confirming whether a subject is afflicted with a neurological disorder, assessing a neurological disorder is developing in a subject who has been identified as being at risk of developing the neurological disorder, assessing whether a subject afflicted with a neurological disorder is likely to benefit iron a therapy, assessing whether a subject afflicted with a neurological disorder has benefited from a therapy, treating a subject afflicted with a neurological disorder, and prophylactically treating a subject who has been identified as being at risk, of developing a neurological disorder. The present invention also provides epitopes, compounds and compositions relating to these methods.

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: Nucleotide sequences including a micro-dystrophin gene are provided. The micro-dystrophin genes may be operatively linked to a regulatory cassette. Methods of treating a subject having, or at risk of developing, muscular dystrophy, sarcopenia, heart disease, or cachexia are also provided. The methods may include administering a pharmaceutical composition including the micro-dystrophin gene and a delivery vehicle to a subject. Further, the methods may include administering the pharmaceutical composition a subject having Duchenne muscular dystrophy or Becker muscular dystrophy.

Abstract: Provided is an isolated cell including a modified amyloid beta precursor protein (APP) gene. The modified APP gene encodes a secretory peptide, and the secretory peptide is Amyloid Beta1-40 (A?1-40) or Amyloid Beta1-42 (A?1-42). The isolated cell can additionally have a modified Apolipoprotein E (APOE) gene, and/or at least one marker. Also provided is an in vitro model including at least one population of cells having a modified APP gene encoding a secretory peptide such as A?1-40 or A?1-42. The population of cells is subjected to at least one differentiation protocol. Further provided is a method of screening treatments including contacting at least one population of cells disclosed herein with at least one agent and determining if the agent has an effect on phenotype. The agent is a drug, a salt, a mineral, an antibody, a humanized antibody, an enzyme, a protein, a peptide, a cell, a modified cell, a stem cell, a plant-based substance, a plant derivative, an antioxidant, or an antioxidant derivative.

Abstract: The present invention provides for engineered molecular opsonins that may be used to bind biological pathogens or identify subclasses or specific pathogen species for use in devices and systems for treatment and diagnosis of patients with infectious diseases, blood-borne infections or sepsis. An aspect of the invention provides for mannose-binding lectin (MBL), which is an abundant natural serum protein that is part of the innate immune system. The ability of this protein lectin to bind to surface molecules on virtually all classes of biopathogens (viruses, bacteria, fungi, protozoans) make engineered forms of MBL extremely useful in diagnosing and treating infectious diseases and sepsis.