Abstract: Compounds derived from a transduction complex that enhance memory in mammals and methods of enhancing memory using said compounds are disclosed.

Abstract: The invention provides a method for inhibiting melanin formation composition by applying a glycine derivative, having a structure shown in the following general equation (I): wherein R1 represents a C1˜C4 alkyl group; R2 represents a hydrogen atom or a methyl group; and n represents an integer of 1˜6.

Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.

Abstract: AV?6 peptide ligands, functional variants thereof and their nucleic acids encoding them are disclosed with their uses in the treatment and imaging of AV?6 mediated diseases.

Abstract: The present invention relates to an ecPNA having the general structure: H2N—X—B—Y—COOH and uses thereof, wherein X is A or C and Y is A or C with the proviso that when X is A, Y is C, and when X is C, Y is A; A represents an oligopeptide structure, the sequence of which comprises a sequence which renders the compound able to enter the nucleus of a cell; B represents a peptide nucleic acid (PNA) structure at least 12 nucleotides in length, the sequence of which is capable of hybridizing with a DNA within the nucleus of the cell, which DNA is within a promoter region of a gene; C represents an oligopeptide structure; and each — represents a chemical linkage between the structures at each side thereof, which may be the same as or different from each other such linkage.

Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.

Abstract: The present invention provides a novel therapeutic or preventive method, a pharmaceutical composition and use thereof, that exhibit superior anti-obesity effects (body weight-reducing (losing) effects and/or body fat mass-reducing effects). Specifically, the present invention provides a pharmaceutical composition comprising the combination of a dipeptidyl peptidase 4 inhibitor and a sweetener having a GLP-1 secretion-stimulating action, as well as use thereof for the manufacture of a medicament. The present invention also provides a method for treating or preventing obesity, comprising administering an effective amount of (a) a dipeptidyl peptidase 4 inhibitor and (b) a sweetener having a GLP-1 secretion-stimulating action to a patient suffering from symptoms of obesity.

Abstract: The invention provides intradialytic parenteral nutrition (IDPN) compositions with low carbohydrate for the treatment of malnutrition in dialysis subjects. In some embodiments, the IDPN compositions are advantageous for the treatment of malnutrition in subjects who are diabetic or suffer from other glucose management related pathologies or subjects who benefit from strict fluid management.

Abstract: Novel compounds and methods of using the same to inhibit glycolysis and treat cancer and other diseases are provided herein.

Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Abstract: There are provided methods of generating antibodies in a mammal against recombinant antigens using DNA plasmids capable of expressing said antigens in cells of said mammal, comprising: injecting into tissue of said mammal a DNA plasmid comprising an encoding sequence operably linked to a promoter, electroporating said tissue with an electroporation device capable of delivering an electrical pulse effective to electroporate cells of said tissue to allow entry of said DNA plasmid and expression of said antigen, and allowing said mammal to respond to said expressed antigen in order to generate antibodies to said antigen. Furthermore, there are provided methods of isolating antibodies specific against desired antigens wherein said antibodies are generated in a mammal using DNA plasmids capable of expressing said antigens.

Abstract: This invention relates to nucleic acid aptamers that recognize and bind the complement protein C3 or its biologically active proteolytic products and methods of their use. Particularly preferred are bi-functional aptamer construct that binding specifically with C3b or iC3b, and another target protein. Use of these molecular constructs for commandeering the opsonization process is also described herein.

Abstract: Described herein are methods and compositions for the inhibition of retroviral integration and replication. The methods and compositions inhibit the activity of one or more components of the SET complex or base excision repair enzymes and induce autointegration of retroviral double-stranded nucleic acid.

Abstract: Oligonucleotide compounds modulate expression and/or function of Vascular Endothelial Growth Factor (VEGF) polynucleotides and encoded products thereof. Methods for treating diseases associated with Vascular Endothelial Growth Factor (VEGF) comprise administering one or more Oligonucleotide compounds designed to inhibit the VEGF natural antisense transcript to patients.

Abstract: Provided are RNA aptamer specifically binding to cancer metastasis-inducing domain of CEA (Carcinoembryonic antigen), a composition for prevention and/or inhibition and/or diagnosis of cancer metastasis containing the same as an active ingredient, and a method of prevention and/or inhibition and/or diagnosis of cancer metastasis using the same.

Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc). One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.

Abstract: Novel adeno-associated virus (AAV) vectors in nucleotide and amino acid forms and uses thereof are provided. The isolates show specific tropism for certain target tissues, such as blood stem cells, liver, heart and joint tissue, and may be used to transduce stem cells for introduction of genes of interest into the target tissues. Certain of the vectors are able to cross tightly controlled biological junctions, such as the blood-brain barrier, which open up additional novel uses and target organs for the vectors, providing for additional methods of gene therapy and drug delivery.

Abstract: This invention relates to compounds, compositions, and methods useful for reducing AR target RNA and protein levels via use of dsRNAs, e.g., Dicer substrate siRNA (DsiRNA) agents.

Abstract: The invention provides methods for enhancing the cytotoxicity of DNA damage in cancer cells that express thymine DNA glycosylase, and treating tumors accordingly. The methods comprise inhibiting the expression or biologic activity of thymine DNA glycosylase, and inducing DNA damage in the cancer cells. DNA damage may be induced by administration of bendamustine or gemcitabine to the cancer cells.

Abstract: Use of autophagic activity in regulation of the amount of melanin in a keratinocyte, the control of skin or hair color, or selection of an agent for regulating the amount of melanin in a keratinocyte or an agent for controlling skin or hair color.

Abstract: A method of treating cancerous tumors is presented herein. The method includes injecting an effective dose of a plasmid encoded for IL-12, B7-1 or IL-15 into a cancerous tumor and subsequently administering at least one high voltage, short duration pulse to the tumor. The electroporation pulses may be administered at at least 700V/cm for a duration of less than 1 millisecond. The intratumor treatments with electroporation may be administered in at least a two-treatment protocol with the time between treatments being about 7 days. The intratumor treatments with electroporation may be administered in a three-treatment protocol with a time of four days between the first and second treatments and a time of three days between the second and third treatments. It was found that the intratumor treatments using electroporation not only resulted in tumor regression but also induced an immune memory response which prevented the formation of new tumors.

Abstract: Methods for producing interfering RNA molecules in mammalian cells are provided. Therapeutic uses for the expressed molecules, including inhibiting expression of HIV, are also provided.

Abstract: The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment of bacterial infections.

Abstract: Provided herein are methods of reducing adhesion formation in a subject, for example, post-surgical abdominal and pelvic adhesions. The methods include the step of administering to the subject in need thereof a compound chosen from 2?,3?-cyclic adenosine monophosphate, analogs thereof, and pharmaceutically acceptable salts thereof, able to reduce the formation of adhesions in a subject as compared to adenosine monophosphate, in an amount effective to reduce adhesions.

Abstract: Provided herein are microalgal polysaccharide compositions and. Also provided are methods of using polysaccharides for applications such as topical personal care products, cosmetics, and wrinkle reduction compositions. The invention also provides novel microalgal compositions useful for improving the health and appearance of skin. The invention also includes insoluble polysaccharide particles for application to human skin.

Abstract: A sea cucumber preparation and manufacturing method thereof, comprising steps as follows: put the cut and well-cleaned fresh sea cucumber or soaked sea cucumber into an airtight container; at 70˜130° C., gelatinate for 1 min˜20 h, freeze-dry till the water content is less than 10 wt %, then sequentially carry out coarse, ultra-micro and nanometer crushing till the fineness reaches 10˜1000 nm. Add water into the sea cucumber nanometer powder to carry out proteinase enzymolysis, after the enzymolysis is finished, inactivate the proteinase, separate and take the supernatant and dry to get nanometer sea cucumber extract. Evenly mix the extract with panax pseudo-ginseng saponins extract at the proportion of 99˜70%:1˜30%. The content of the sea cucumber polysaccharide in the mixture is 2.5˜8.0 wt %, the content of panax pseudo-ginseng saponins is 0.3˜21.0 wt %. The compound preparation has complementary and synergistic effects on pharmacological effect.

Abstract: The present invention relates to ready-to-use sterile, alginate-based, aqueous compositions for medical use. More particularly, the invention relates to an aqueous composition for medical use that has been sterilized by heat sterilization and having a viscosity at 25° C. of at least 300 cP) (Helipath® T F spindle, 100 rpm at 25° C.), said composition having a pH in the range of 6.5-7.5; containing 0.5-10 wt. % of an alginate salt; and further containing 10-500 mM of one or more dissolved C2-C7 mono- or dicarboxylates that are optionally substituted with up to 2 hydroxyl groups. The alginate-based composition of the present invention has excellent storage stability and is easy to manufacture. The alginate-based aqueous compositions of the present invention can advantageously be used, for instance, to prevent adhesions between a healing trauma site and adjacent surrounding tissue. These compositions can further be used in implants or in pharmaceutical preparations for oral administration.

Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: A composition to be administered to a mammal for treating hearing loss is disclosed herein. The composition consists essentially of a biologically effective amount of vitamin A, vitamin C, vitamin E, and a vasodilator comprising magnesium. The composition optionally includes a withanolide and/or resveratrol. The vitamin A, vitamin C, vitamin E, and the vasodilator comprising magnesium provides an additive effect that is equal to or greater than a sum of the effects of the individual components.

Abstract: A method for the treatment of back pain by injection of an injectable flowable composition in the epidural space, wherein the composition is composed of microparticles of dexamethasone acetate and a polymer, are disclosed.

Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.

Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: To provide a therapeutic agent and a diagnostic agent for mitochondrial dysfunction brain diseases including cerebral infarction as a representative. A therapeutic agent for a mitochondrial dysfunction brain disease, which comprises (A) ?-aminolevulinic acid represented by the formula (1), a derivative thereof, or a salt thereof and (B) an iron compound in combination. R2R1NCH2COCH2CH2COR3??(1) wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryl group, or an aralkyl group; and R3 represents a hydroxy group, an alkoxy group, an acyloxy group, an alkoxycarbonyloxy group, an aryloxy group, an aralkyloxy group, or an amino group.

Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.

Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

Abstract: The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Abstract: The present invention relates to a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof having an excellent effect of inhibiting 11?-hydroxysteroid dehydrogenase type 1: General formula (I) wherein R1 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from substituent group A or a heterocyclic group that may be substituted with 1 to 4 group(s) independently selected from substituent group A; R2 independently represents a halogen atom or a C1-C6 alkyl group; n represents an integer of 0 to 2; and substituent group A represents the group consisting of halogen atoms, C1-C6 alkyl groups, and so forth.

Abstract: The present invention is drawn to transdermal drug formulations, transdermal patches incorporating such formulations, as well as associated methods. The formulations can include about 0.3 wt % to about 5 wt % of a drug, such as alprazolam, about 4 wt % to about 30 wt % water, about 10 wt % to about 40 wt % glycerol, about 0.5 wt % to about 6 wt % oleyl alcohol. Other co-solvents and/or additives can be present to achieve a 100 wt % formulation.

Abstract: The present invention provides a compound of general formulae A useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2, 1-c][1,4]benzodiazepine hybrids of general formulae 6a-g, 10a-o, 14a-g and 18a-o.

Abstract: Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4?, have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.

Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.

Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

Abstract: The present invention relates to benzofuran-2-sulfonamide derivatives with the following formula: or pharmaceutically acceptable salts thereof. The derivatives are useful as modulators of chemokine receptors.

Abstract: EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.

Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.

Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.