Abstract: This invention provides compounds that are true antagonists of the leptin receptor, in the presence and the absence of native leptin or another leptin receptor binder. These compounds may be used to inhibit leptin receptor activity, promote growth arrest or death of leptin receptor-positive cancer cells, or monitor or detect a leptin receptor-positive cell, in vitro or in vivo. These compounds may also be used to treat a weight-loss nutritional disorder, osteoporosis, rheumatoid arthritis, osteoarthritis, or inflammatory bowel disease. Also included in the invention are methods for detecting leptin receptor-positive cells, for arresting cell growth or killing cancer cells in vivo, for monitoring or detecting a leptin receptor-positive cell in vitro or in vivo, for treating a weight-loss nutritional disorder, for treating osteoporosis, for treating rheumatoid arthritis, for treating osteoarthritis, or for treating inflammatory bowel disease.

Abstract: Peptides activating dermatopontin in the skin and cosmetic compositions including such peptide, in a physiologically suitable medium, are described. Methods of treating the cutaneous signs of aging and photoaging, and in particular wrinkles, sagging, and loss of volume and elasticity of the skin are also described.

Abstract: The present invention relates to pharmaceutical compositions containing targetable bioconjugates of hydralazine, a direct vasodilating agent previously shown to decrease tumor blood flow, oxygenation and interstitial fluid pressure in solid tumors. These bioconjugates are hydralazine prodrugs that contain hydralazine conjugated to biocompatible carrier molecules which specifically bind to sites that are expressed on a diverse variety of tumor cell types. These hydralazine prodrugs are preferably conjugated through an acid-labile hydrazone link that is designed to be stable in plasma and release hydralazine through acid-catalyzed hydrolysis in the acidic environment of the target tumor. Because these prodrugs are stable at physiological pH and in plasma, they are devoid of systemic vasoactive activity; however, they are acid-labile conjugates that can be hydrolyzed upon reaching the more acid environment of the tumor where the vasoactive activity of hydralazine is restored.

Abstract: The present invention is directed to metabolites of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of cancer.

Abstract: The present invention includes methods for the treatment of autoimmune disorders such as autism, schizophrenia, and type 1 diabetes. Flavonoids, luteolin, diosmin, and diosmin's aglycone form, diosmetin, were found to inhibit activation/phosphorylation of STAT3 induced by IL-6 in cultured neuronal cells. Furthermore, mice treated with diosmin showed a significant reduction of autistic phenotype induced by IL-6 through inhibition of STAT3 activation.

Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, cyclic ketoenols or other acaricidally active compounds and, secondly, further insecticidally active compounds from the group of the anthranilamides, which combinations are highly suitable for controlling animal pests, such as insects and unwanted acarids.

Abstract: Disclosed are levoisovalerylspiramycin I, II or III, preparations, preparing methods and uses thereof. The preparations comprise levoisovalerylspiramycin I, II or III and pharmaceutically acceptable carrier and/or adjuvant, wherein the purity of levoisovalerylspiramycin I, II or III is above 90 wt %. The levoisovalerylspiramycin I, II or III has a good antibacterial activity, and the preparations include solution for injection, powder for injection or lyophilized powder for injection.

Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.

Abstract: Disclosed are methods and pharmaceutical compositions for inducing pancreatic hormone production.

Abstract: Compounds, compositions and methods are provided for modulating the expression of eIF4E-BP1. The compositions comprise oligonucleotides, targeted to nucleic acid encoding eIF4E-BP1. Methods of using these compounds for modulation of eIF4E-BP1 expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E-BP1 are provided.

Abstract: The present invention relates to an anticancer agent containing a TMPRSS4 (transmembrane protease, serine 4) inhibitor as an effective ingredient, more precisely an anticancer agent containing an inhibitor of TMPRSS4 activity as an effective ingredient. The anticancer agent of the present invention can be used effectively for the treatment of cancer by inhibiting TMPRSS4 expression in cancer cells and thereby inhibiting cancer cell invasion and cancer cell growth.

Abstract: Double-stranded RNA (dsRNA) induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). Using a Drosophila in vitro system, we demonstrate that 19-23 nt short RNA fragments are the sequence-specific mediators of RNAi. The short interfering RNAs (siRNAs) are generated by an RNase III-like processing reaction from long dsRNA. Chemically synthesized siRNA duplexes with overhanging 3? ends mediate efficient target RNA cleavage in the lysate, and the cleavage site is located near the center of the region spanned by the guiding siRNA. Furthermore, we provide evidence that the direction of dsRNA processing determines whether sense or antisense target RNA can be cleaved by the produced siRNP complex.

Abstract: The present invention embraces microRNA-antagonists and activators of homeobox D10 protein; Zinc finger, MYND domain containing 11 protein; or RB1-inducible coiled-coil 1 protein for use in decreasing glial tumor cell proliferation and treating glioma.

Abstract: The present invention relates to non-invasive methods for treating diseases, disorders and injury to the central nervous system (CNS), and in particular to otic compositions and to methods of use thereof.

Abstract: The present invention relates to USP47 (ubiquitin specific protease 47) inhibitors and methods for inducing apoptosis or cell death in a target cell. In certain embodiments, the invention relates to methods and kits to screen for related agents that induce apoptosis. Additionally, the invention relates to assays for screening compounds capable of acting as USP47 inhibitors.

Abstract: A method is provided for treating individuals suffering from cancer characterized by tumor cells which are telomerase negative, do not have telomerase activity or have L1RT expression or alternative lengthening of telomeres. The method includes administering to an individual in need of treatment thereof, and having the aforementioned cancer, a therapeutically effective amount of a nucleoside analog selected from one or more of the group consisting of: 3?-azido-2?,3?-dideoxythymidine (AZT), 2?,3?-dideoxyinosine (ddI) and 2?,3?-didehydro-3?-deoxythymidine (d4T).

Abstract: A method of treating an adult patient in need of bowel evacuation via the administration of one or more doses of a bowel evacuant consisting of a total of from about 180 g to about 220 g of lactulose in a dosing regimen suitable to achieve bowel evacuation prior to a diagnostic, therapeutic or surgical procedure is disclosed.

Abstract: Interstitial cystitis and related GAG-deficient conditions of the bladder and urinary tract are treated by instillation of high dose chondroitin sulfate, such as 400 mg/20 mL. The higher dose of chondroitin is effective for the rapid reduction of symptoms, particularly in patients with severe and otherwise recalcitrant cystitis.

Abstract: Methods for applying injectable fillers are provided. In some embodiments, the methods can extend effectiveness of the injectable filler. In some embodiments, the methods can provide for an elevated level of effectiveness of the injectable filler. In some embodiments, the methods can prolong the effectiveness of the injectable filler.

Abstract: The invention relates to concentrated liquid cleansing compositions in lamellar phase which possess a lotion-like appearance conveying signals of enhanced moisturization. The use of a specific ratio of synthetic anionic surfactant(s) and co-surfactant(s) to fatty acid(s) in a structured liquid product was found to improve lather production by moderating or eliminating the increase in viscosity upon dilution. In a further embodiment, specific small hydrophobic molecules were found to improve freeze/thaw stability and thereby cause the inventive composition to maintain noticeable moisturization signals.

Abstract: A polyamine-depleted food compositions is provided for preparing foods, intended for humans or animals, for preventing or treating heart rate anomalies.

Abstract: This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallization.

Abstract: The disclosure provides compounds and methods to treat a microbial or a bacterial pathogenesis, and demonstrates that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract: Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.

Abstract: A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

Abstract: A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

Abstract: A method is disclosed for administering a DHEA derivative or a physiologically acceptable salt, ester or ether thereof for one of decreasing body weight, reducing adipose tissue, increasing endurance, as an anti-aging compound and generating production of red blood cells.

Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolid

Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferab

Abstract: Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.

Abstract: Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

Abstract: An amoxicillin product comprising: at least one modified release component(s), wherein the at least one modified release component(s) comprises at least amoxicillin and a pharmaceutically acceptable carrier; and wherein when administered to a patient or subject in the fed state said amoxicillin product exhibits a pharmacokinetic profile for amoxicillin in the plasma characterized as follows: (1) the ratio of the portion of the AUC as measured from 2 hours post-administration to 5 hours post-administration to the portion of the AUC as measured from administration to 2 hours post-administration is at least 2.0:1; and (2) the ratio of the portion of the AUC as measured from 5 hours post-administration to 12 hours post-administration to the portion of the AUC as measured from administration to 2 hours post-administration is at least 1.1:1.

Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.

Abstract: This invention relates to novel indolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.

Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.

Abstract: This invention provides compounds of formula (I) wherein R1, R2, X, p, q, m, n, and Ring C have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or an alkyl group; R2 represents an alkyl group; R3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterized by cognitive deficits.

Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.

Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.

Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.

Abstract: This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazole boronic acid compounds for treating cancer.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C 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 HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.