Abstract: The present invention relates to a solid oral dosage form comprising a therapeutically effective amount of aliskiren or a pharmaceutically acceptable salt thereof, a therapeutically effective amount of HCTZ and a hydrophilic filler selected from the group a carbohydrate or combinations thereof, e.g. sugars, sugar alcohols and starches or combinations of these.

Abstract: The present invention relates to a pharmaceutical oral fixed dose combination comprising a) a therapeutically effective amount of Aliskiren, or a pharmaceutically acceptable salt thereof, b) a therapeutically effective amount of Amlodipine, or a pharmaceutically acceptable salt thereof, wherein the pharmaceutical oral fixed dose combination shows an in vitro dissolution of component (a) of 60% or less after 10 minutes and 98% or less after 20 minutes, and a dissolution profile of component (b) of 50% or more after 20 minutes, and 70% or more after 30 minutes at pH 2, said pharmaceutical oral fixed dose combination being bioequivalent, or close to reaching bioequivalence, to a free dose combination of Aliskiren and Amlodipine.

Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.

Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: The invention relates to the use of a compound of Formula I for the treatment of protease-activated receptor mediated diseases by the administration of a compound of Formula I or a prodrug or metabolite thereof.

Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.

Abstract: A biocidal composition comprising 2,2-dibromomalonamide and sodium ortho-phenylphenol, and its use for the control of microorganisms in aqueous and water-containing systems.

Abstract: This invention pertains to methods and compositions for the diagnosis and treatment of cardiovascular conditions. More specifically, the invention relates to isolated molecules that can be used to diagnose and/or treat cardiovascular conditions including cardiac hypertrophy, myocardial infarction, stroke, arteriosclerosis, and heart failure.

Abstract: There is provided a process for the preparation of Lacosamide (which is a useful medicament) of formula I, which comprises an enantioselective enzymatic acylation.

Abstract: The present invention relates to a method for treating a subject having or at risk of a diabetes-related disorder. In a preferred embodiment, the method involves increasing the level or activity of Hypoxia Induced Factor 1 (HIF-1?) in pancreatic-?-cells or insulin-sensitive tissues in the subject by administering to the subject an inhibitor of a protein that decreases the level or activity of HIF-1?. The present invention also relates to a method of transplanting pancreatic islet cells in a subject.

Abstract: The present invention comprises methods and pharmaceutical compositions for intranasal delivery of effective amounts of DFO directly to the CNS, in particular the brain treatments that inhibit GSK3b in patients with psychiatric disorders including, but not limited to, bipolar disorder, depression, ADHD and schizophrenia. In addition a treatment composition is disclosed which comprises DFO and in certain embodiments combines DFO with one or more of the psychotropic drug types, i.e., antipsychotics, mood stabilizers and antidepressants. Moreover, a treatment for treating impairment of neural plasticity through inhibition of GSK3b is provided as well as prevention of apoptosis of cells through inhibition of GSK3b.

Abstract: Methods for treating eye diseases associated with inflammation and/or vascular proliferation in subjects are disclosed. The methods include administering therapeutically effective amounts of a tranilast compound, in particular (E)-2-[[3-(3-Methoxy-4-propargyloxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or (E)-2-[[3,4-Bis(difluoromethoxy)phenyl)-1-oxo-2-propenyl]amino]benzoic acid or pharmaceutically acceptable salts or solvates thereof.

Abstract: An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G1)-Q1 or —C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.

Abstract: Methods and compositions for improving the delivery and/or efficacy of a therapy (e.g., a cancer therapy) are disclosed. In one embodiment, methods and compositions for treating or preventing a cancer (e.g., a solid tumor such as a desmoplastic tumor) by administering to a subject an anti-hypertensive agent, as a single agent or in combination with a microenvironment modulator and/or a therapy, e.g., a cancer therapy (for example, a therapeutic agent or therapy, including immunotherapy (e.g., antibodies, vaccine, cell-based), nanotherapeutics, radiation therapy, photodynamic therapy, low molecular weight chemotherapeutics, molecularly targeted therapeutics and/or oxygen radical) are disclosed.

Abstract: Salts of kukoamine B, their preparation method and their pharmaceutical use in preparation of drugs for preventing and treating sepsis. Experiments indicate that salts of kukoamine B have a good effect on antagonizing the key factors inducing sepsis, and can be used in the preparation of drugs for preventing and treating sepsis. Under the current circumstances of the lack of effective measures for the treatment of sepsis in clinical practice, the medicinal formulations, which comprise the salts of kukoamine B, pharmaceutically acceptable carrier and/or diluent, provide a new approach for the prevention and treatment of sepsis.

Abstract: The present invention includes a combination comprising: a) mecamylamine; and b) an ACE inhibitor, an AT2 receptor inhibitor, a renin inhibitor, or a combination thereof.

Abstract: A compound represented by Formula (1): The compound can be used as insecticides.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

Abstract: The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic and/or serotonin neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.

Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract: Proteases such as memapsin-1 are import enzymes, playing roles in a variety of diseases including diabetes. The inventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease.

Abstract: A modified release formulation of lacosamide suitable for once-daily administration.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.

Abstract: A modified release formulation of lacosamide.

Abstract: A 3-aminooxalylaminobenzamide compound is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide compound is represented by formula [1]: in which, for instance, R1 and R2 each represent a C1 to C3 alkoxy group or a C1 to C3 haloalkoxy group; R3 and R4 each represent a C1 to C8 alkyl group or a C1 to C8 haloalkyl group; R5 represents a C1 to C5 haloalkyl group; R6 and R7 each represent a hydrogen atom or a C1 to C5 alkyl group; Y represents a hydrogen atom or a halogen atom; Z represents a hydrogen atom; n is an integer ranging from 0 to 4; and m is an integer ranging from 0 to 2.

Abstract: The present invention relates to a method for selectively crystallizing Z isomer of iopromide of formula (I) comprising a) dissolving a crude iopromide comprising a mixture of E and Z isomers or a concentrate thereof in an alcohol, and b) heating the resulting alcohol solution to obtain crystalline of Z isomer of iopromide; and a method for preparing a composition comprising the crystalline Z isomer of iopromide.

Abstract: The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.

Abstract: The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein R1 is phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, R2 is hydrogen or methyl, and R3 and R4 have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.

Abstract: Embodiments of the invention relate to methods and compositions for treating symptoms related to inflammatory conditions and to methods and compositions for treating inflammatory components of common cold, utilizing various method of administration of X-ray contrast media (CM).

Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Abstract: An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G1)-Q1 or —C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.

Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.

Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.

Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.

Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.

Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.

Abstract: The present invention relates to novel compounds of general formula (I) and (II) for their use in gene therapy as non-viral vehicles and their use for the preparation of a medicament. It also discloses the process of synthesis of said compounds of general formula (I) and (II).

Abstract: Disclosed are a novel therapeutic agent and a novel treatment method for cancer. Specifically disclosed are: a targeting agent for a cell selected from the group consisting of a cancer cell and a cancer-associated fibroblast, which comprises a retinoid and/or derivative thereof; a substance delivery carrier for the cell, which comprises the targeting agent; an anti-cancer composition utilizing the targeting agent or the carrier; an anticancer-associated fibroblast composition; and a method for treatment of cancer.

Abstract: It is intended to provide a novel compound that has an excellent ?-secretase inhibitory effect and specifically inhibits A? production. The present invention provides a compound of the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a linear or branched alkyl group having 1 to 4 carbon atoms or a phenyl group; R2 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more phenyl or halogenophenyl groups; R3 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more hydroxyl groups; R4 represents a linear or branched alkyl group having 1 to 4 carbon atoms; and the symbol “*” represents a chiral center.

Abstract: The present invention provides methods for the prevention of, delay progression to overt to, or the treatment of diastolic dysfunction or diastolic heart failure which method comprises administering to a warm-blooded animal a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with (i) an ACE inhibitor or a pharmaceutically acceptable salt thereof; or (II) an angiotensin II receptor blocker or a pharmaceutically acceptable salt thereof.

Abstract: A vascular embolization gelling agent for sustained release of drugs for treating tumors having a drug and a drug carrier. The drugs are antitumor drugs. The drug carrier includes poloxamer polymer and polyvinylpyrrolidone or gel made of the combination, and may be purified before use. The drug carrier accounts for 5-65% of the gel. The particle size of the gel is in the range of 10 nm-150 ?m. The embolization agent is a liquid gel at normal temperature, to facilitate direct transcatheter injection, and is rapidly solidified to the gel state in body with the increase of the temperature; it is used to encapsulate different drugs on demand, and can achieve dual efficacy of embolization and drug treatment through local sustained release of the drug. The present invention can be used as the embolization agent for endovascular interventional therapy for transcatheter arterial chemoembolization of various benign and malignant tumors.

Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the phthalic diamides, and which are highly suitable for controlling animal pests such as insects and undesired acarids.

Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].

Abstract: Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.

Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more diamide compound(s) selected from Group (A) shows an excellent controlling activity on a pest.

Abstract: An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and an additive dispersed in the mouth-stable polymer matrix. The oral product is adapted to release the additive from the body when the body is received within the oral cavity and exposed to saliva.

Abstract: The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate.