Abstract: The present invention relates to substituted morpholine derivatives having pharmacological activity towards the sigma (?) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: The invention provides dihydro-2H-benzo[b] [1,4]oxazine sulfonamide and related compounds, pharmaceutical compositions, methods of promoting ROR? activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Abstract: The present invention includes novel RAD51 inhibitors. The compounds of the invention may be useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.

Abstract: Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I) or any one of Compounds 100-175) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.

Abstract: The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.

Abstract: Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.

Abstract: Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-? production in vivo. A compound represented by formula (I) [wherein X represents —CH?CH—, —NH—, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.

Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.

Abstract: The present invention relates to tetrahydropyrido[4,3-d]pyrimidine based compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.

Abstract: Bisaminoalkoxysilanes of Formula I, and methods using same, are described herein: R1Si(NR2R3)(NR4R5)OR6??I where R1 is selected from hydrogen, a C1 to C10 linear alkyl group, a C3 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C3 to C10 alkynyl group, a C4 to C10 aromatic hydrocarbon group; R2, R3, R4, and R5 are each independently selected from hydrogen, a C4 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C3 to C10 alkynyl group, and a C4 to C10 aromatic hydrocarbon group; R6 is selected from a C1 to C10 linear alkyl group, a C3 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C2 to C10 alkynyl group, and a C4 to C10 aromatic hydrocarbon group.

Abstract: The present invention relates to novel aminosilane-functionalized diene compounds of the following Formula I: wherein each R? is independently selected from C1-C12 alkyl, C6-C18 aryl, C7-C18 alkylaryl, tri(C1-C6 alkyl, C6-C12 aryl or C7-C18 alkylaryl)silyl and allyl, wherein two R? groups may be connected to form a ring and the ring may contain, further to the Si-bonded nitrogen atom, one or more of an oxygen atom, a nitrogen atom, an >N(C1-C6 alkyl or C7-C18 alkylaryl) group and a sulfur atom; each R? is independently selected from C1-C6 hydrocarbyl; Ra, Rb, Rc, Rd and Re are independently selected from hydrogen, methyl and ethyl; x is an integer selected from 0, 1 and 2, y is an integer selected from 1, 2 and 3 and x+y=3. The diene compounds are useful as modifying monomers in the polymerization of conjugated diene monomers.

Abstract: The present invention is related to a biotransformation process, effected by means of an isolated polypeptide possessing benzopyrone phosphate synthetase activity, and also a microorganism comprising a nucleic acid sequence that encodes the polypeptide, for the preparation of phosphate-conjugated derivatives of benzopyrone compounds. The hydrophilic property of the benzopyrone compounds is enhanced after catalyzed by the benzopyrone phosphate synthetase of the present invention.

Abstract: The present invention relates to the anticancer property studies of a series of chiral palladium N-heterocyclic carbene complexes of the general formula of (NHC)2PdX2 [NHC=chiral N-heterocyclic carbene ligand 1-(1S,2S,5R/1R,2R,5S)-menthyl-4-(R)-1,2,4-triazol-5-ylidene, wherein R=Et, allyl and CH2Ph; X?Br or OCOCF3], as designated by, (1S,2S,5R)-(1-3)b and (1R,2R,5S)-(1-3)b, (1S,2S,5R)-(1, 3)c and (1R,2R,5S)-(1, 3)c represented by formula (Ig, Ih) below. The present invention further investigates the influence of chirality on the anticancer activity, wherein the enantiomeric pairs of present chiral palladium N-heterocyclic carbene complexes of formula (Ig, Ih) shows no differential activity based on optical isomerism despite all of the palladium complexes exhibiting high anti-proliferative activity towards a variety of cancer cells.

Abstract: The current invention relates to series of co-crystals of carboplatin with cyclic amides as co-formers and their pharmaceutical use. The co-crystals of the current invention may be used in the treatment or prevention of cancers.

Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

Abstract: Oxysterol-bisphosphonate and oxysterol-alendronic acid compounds, compositions including them, and methods using them for the treatment of bone disorders.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.

Abstract: A precision volumetric liquid dispensing instrument is disclosed that includes two pressure sensors and a fluid passageway with a defined volume portion in communication with the two sensors for receiving and distributing liquid in relatively small volumes. One of the pressure sensors is positioned to measure pressure at one portion of the defined volume portion of the fluid passageway and the other of the gas pressure sensors is positioned to measure gas pressure at a different portion of the defined volume portion of the passageway. At least one valve is in communication with the passageway for moving fluids into or out of the defined volume portion of the fluid passageway, and a processor carries out a step selected from the group consisting of (i) calculating the volume of the liquid based upon the measured pressure and (ii) metering a liquid into the defined volume portion of the fluid passageway until the measured pressure indicates that a desired volume of fluid is in the fluid passageway.

Abstract: The present invention relates to a method for preventing the unfolding of a (poly)peptide during drying and/or inducing the (re-)folding of a (poly)peptide after drying, comprising the step of embedding the (poly)peptide in an aqueous solution, wherein the solution comprises (i) at least three different amino acids; or (ii) at least one dipeptide or tripeptide; and wherein the solution is free or substantially free of (a) sugar; and (b-i) protein; and/or (b-ii) denaturing compounds; and (c) silanes.

Abstract: Polyelectrolyte based bioactive super-absorbent material ionotropically crosslinked/neutralized involving polyvalent carboxylic acids, citrate, Kojic Acid, Alpha Arbutin along with fish scale collagen cross linked with other polyelectrolyte biopolymers preferably selected from chitosan, alginate or their combinations is used in this invention. The advancement is also directed to process of extraction of collagen of high purity from fresh water fish scale by salt and alkaline washing, crushing followed by continuous dialysis thereby minimizing the chance of collagen degradation. Also disclosed are different forms of collagen-chitosan composite biomaterial using citrate as the neutralizing buffer in combination with antimicrobial agent, antioxidant, skin plumper and melanin reducer wherein the different forms of collagen chitosan particularly sheet, flakes, powder, gel, particles, fiber, film, spray etc. reveal efficient wound healing properties.

Abstract: Isoform-selective lysine deacetylase inhibitors are described. Inhibitors of the lysine deacetylase enzyme are useful as antitumor drugs and for treating addiction, asthma, cardio-vascular disease, immunosuppression, neurodegenerative diseases, sepsis, sickle-cell disease, uveal melanoma and termination of viral latency, particularly HIV-1 latency.

Abstract: The present invention relates to a carbazole compound having anti-virus activity, and more particularly, to a novel compound selected from the group of consisting of a carbazole compound which shows excellent anti-proliferative efficacy against hepatitis C virus (HCV), a pharmaceutically acceptable salt thereof, a hydrate thereof, and an isomer thereof; an anti-virus pharmaceutical composition including the novel compound as an active ingredient; a pharmaceutical composition for preventing or treating liver diseases caused by hepatitis C virus; and a method of preparing the novel compound.

Abstract: An autophagic cell targeted peptide and its use are described. More particularly, a polypeptide comprising an amino acid sequence represented by the general formula (I) and specifically binding to an autophagic cell and a composition for detecting autophagic cells comprising the same as an active ingredient are described. Also described are a drug delivery composition containing the same peptide as an active ingredient and a composition for imaging comprising the same peptide as an active ingredient. The peptide specifically binds to the cell membrane of autophagic cells and can be applied to various kinds of tissues and cells. The detection and imaging effect of autophagy is remarkable in vitro and in vivo.

Abstract: A novel peptide has both an antimicrobial effect and an immunocyte activity regulatory function. The peptide regulates immunocyte activity and also exhibits antimicrobial activity against various bacteria such as gram-negative bacteria and gram-positive bacteria, thereby being useful for treating various immune diseases such as atopic dermatitis and for treating diseases caused by the infection of pathogenic bacteria.

Abstract: A series of cationic cyclic peptides, useful for the treatment of infectious diseases in both human and veterinary clinical/surgical environment are described herein. The peptides of the invention have a length of 15 to 21 amino acids, and show a sequence A-B-C-D-C?-B?-A?, wherein units A and A? correspond to —NH2 terminal and —COOH terminal regions; units B and B? correspond to cyclizable amino acids containing sulfur; units C and C are sequences of 5 amino acids selected among hydrophobic amino acids, basic amino acids and amino acids forming hydrogen bonds; unit D is a dipeptide consisting of glycine and one basic amino acid. Said peptides show significant antibacterial activity, associated with high stability and resistance to the action of bacterial endopeptidases, and weak or null toxicity against eukaryotic cells.

Abstract: Described herein is the discovery of novel PSMA-specific peptides, which were identified through a novel combinatorial biopanning method. One of the novel PSMA-specific peptides discovered, GTIQPYPFSWGY (or GTI) (SEQ ID NO: 2), exhibits high binding affinity and selectivity to PSMA and PSMA-positive prostate cancer cells. It was found that GTI can mediate internalization of the apoptotic KLA peptide (SEQ ID NO: 10) to PSMA-positive LNCaP cells and induce cell death. Moreover, a FAM-labeled GTI peptide shows a high and specific tumor uptake in nude mice bearing human prostate cancer xenografts. It was demonstrated that the GTI peptide can be employed as a PSMA-specific ligand for prostate cancer diagnosis and/or for targeted drug delivery to prostate cancer cells.

Abstract: A cell-penetrating peptide characterized in that it comprises an amino acid sequence: X1X2X3WWX4X5WAX6X3X7X8X9X10X11X12WX13R (SEQ ID No: 10), wherein X1, is beta-A or S, X2 is L or none, X3 is R or none, X4 is L, R or G, X5 is R, W or S, X6 is S, P or T, X7 is W or P, X8 is F, A or R, X9 is S, L, P or R, X10 is R or S, X11 n is W or none, X12 is A, R or none and X13 is W or F, and wherein if X3 is none, then X3, X11 and X12 are none as well.

Abstract: Peptides effective as delta opioid receptor agonists and compositions comprising same are provided. Further provided are methods for targeting medical conditions amenable to treatment with an opioid receptor agonist, including but not limited to, conditions involving pain as well as reducing cocaine craving.

Abstract: This disclosure relates to peptides useful for targeting inflamed or distressed tissue and uses related thereto. In certain embodiment, the peptides comprise SEQ ID NO: 1-14, or variants or derivatives thereof. In certain embodiments, peptides disclosed herein are conjugated to a label to detect, measure, or image cardiac tissue useful in the diagnosis of myocarditis. In certain embodiments, the peptides are conjugated to a particle coating for use in ultrasound imaging, MRI, or targeted therapy. In certain embodiments, peptides disclosed herein are conjugated to a drug or a particle containing a drug useful for targeted therapy.

Abstract: The invention provides processes of preparing a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-249 described herein.

Abstract: Systems and methods have been developed to design and engineer glycan dynamics to improve immunogen antigenicity. These include systems for identify glycosylation sites that that impact binding of antibodies to the immunogen, and modifying the glycan profiles on these glycosylation sites to synthesize novel immunogens, antibodies and vaccines. Then, the machine learning algorithm may output data relating to the glycosylation sites that are determinant or likely impact the binding affinity of the variants to the one or more antibodies.

Abstract: The invention relates to an engineered outer domain (eOD) of HIV gp120 and mutants thereof and methods of making and using the same. The mutant eODs may be advantageous for the elicitation of CD4-binding site (CD4bs)-directed broadly-neutralizing antibodies (bnAbs) and/or improve binding to mature VRC01 and/or improve binding to germline VRC01 and the germlines of other VH1-2 derived broadly-neutralizing antibodies. The mutant eODs may also include glycan-masking mutations on eOD. The present invention also includes fusions of eOD to various protein multimers to enhance immunogenicity as well as the design of cocktails of different eODs that represent the full diversity of HIV sequences within the VRC01 epitope and surroundings.

Abstract: The present invention relates to a new feline capsid protein, to live attenuated feline calicivirus comprising that capsid protein, to live recombinant carrier viruses and live attenuated hybrid feline calicivirus comprising that capsid protein, to vaccines comprising such live attenuated feline caliciviruses, live recombinant carrier viruses and live attenuated hybrid feline calicivirus, and to methods for the preparation of such viruses.

Abstract: The present invention is directed to vegetative insecticidal proteins (Vips) modified to comprise heterologous carbohydrate binding modules and methods of use thereof.

Abstract: The inventors provide a composition comprising an antimicrobial polypeptide comprising Blad or an active variant thereof for use in a method of treatment of the human or animal body by therapy or prophylaxis, such as for use in a method of treating or preventing an infection in or on a subject by a microorganism. Also provided is the use of a composition comprising an antimicrobial polypeptide comprising Blad or an active variant thereof to kill, or inhibit the growth of, a microorganism that is pathogenic to a human or an animal at a site that is not on or in the human or animal body.

Abstract: The present invention relates to a proton-transport vesicle and a method for preparing the same, the proton-transfer vesicle comprising: (a) a single phospholipid bilayer liposome; (b) a rhodopsin protein; and (c) a photosystem II protein, wherein the rhodopsin protein and the photosystem II protein are inserted and located in a bilayer of the liposome. Since the heterologous photosensitive proteins are inserted and located in the bilayer of the liposome, the vesicle has an absorption wavelength band of the whole region of visible light by utilizing absorption bands of different lights of the respective photosensitive proteins. Thus, the restricted efficiency caused by utilizing only a specific wavelength in existing organisms or artificial vesicles was improved, and the wavelength region can be enlarged to the all wavelength ranges of visible light.

Abstract: Fusion peptide comprising: i) an amino acid sequence as defined in SEQ ID No.: 1 or a related homolog having at least 90% identity with SEQ ID No.: 1 and having the ability of the sequence SEQ ID No.: 1 to inhibit the kinase-independent function of PI3K?, and ii) a peptide having the ability to penetrate a cell.

Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed under low to moderate pressure at an elevated temperature.

Abstract: Lysine-depleted variants of fragment crystallizable (Fc) regions of immunoglobulins are disclosed. Also disclosed are fusion proteins comprised of N-terminal targeting or active peptide domains fused with such lysine-depleted variant IgG-Fc domains. Polynucleotides encoding such proteins, compositions and kits containing such proteins, and methods of using such proteins are also disclosed.

Abstract: The present invention relates to a short peptide-based therapeutic agent and a medicinal composition including the same for inhibiting activities of cancer cells, which includes at least one short peptide listed as SEQ ID NOs: 1 and 2, either of which is unglycosylated and has no more than 40 amino acid residues, thereby specifically reducing or inhibiting activities of cancer cells such as the cancer cell proliferation, cancer stemness, cell migration, cancer cell invasion, metastasis or drug resistance.

Abstract: The present invention relates to compositions comprising factor VIII coagulation factors linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of making and using such compositions in treatment of factor VIII-related diseases, disorders, and conditions.

Abstract: The present invention relates to processes of obtaining Apo A-1 from an Apo A-1 containing protein fraction (A), comprising suspending the Apo A-1 containing protein fraction (A) in a buffer solution (B), removing impurities from the suspension while keeping the Apo A-1 proteins solubilized, followed by precipitating Apo A˜I from the suspension and collecting the Apo A-1 precipitate. Apo A-I obtained by such processes, reconstituted HDL obtained from such Apo A-1, and pharmaceutical compositions comprising such Apo A-I and/or reconstituted HDL also are provided.

Abstract: Described herein is a new antidote for the rapid elimination of carbon monoxide from hemoglobin, including brain, heart, and red cell hemoglobin. The disclosed therapy involves the use of modified human globins, particularly neuroglobins modified at residue 64 and cytoglobins modified at residue 81, which bind carbon monoxide with extremely high affinity. The monomeric mutant globins are infused into blood, where they rapidly and irreversibly sequester carbon monoxide, and thus limit toxic effects of carbon monoxide on cellular respiration and oxygen transport and utilization.