Abstract: The present application relates to novel difluorophenol derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: Disclosed is an agent for use in the treatment or prevention of inflammatory bowel disease. Also disclosed is an agent for inhibiting the production of TNF-?. A therapeutic or prophylactic agent for inflammatory bowel disease comprising at least one amino acid selected from the group consisting of lysine, histidine, phenylalanine, methionine, tryptophan, glutamine, glycine, cysteine, cystine and threonine, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day; and a TNF-? production inhibitor comprising an amino acid selected from the group consisting of histidine, phenylalanine and tryptophan, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: A product to reduce and method of reducing the risk of inhalation of harmful substances by applying a formulation composition to a substrate or the skin in close proximity of one or more nostrils. This formulation, when applied creates an electrostatic field having a charge. The electrostatic field attracts airborne particulates of opposite charge to the substrate that are in close proximity to the substrate close to the skin and a biocidic agent renders microorganisms coming in contact the substrate or skin less harmful.

Abstract: Methods and compositions for treating a complication associated with aneurysmal subarachnoid hemorrhage (SAH), the method comprising administering an effective amount of a nitric oxide precursor to a subject in need thereof. Methods and compositions for treating vasospasm, the method comprising administering an effective amount of a nitric oxide precursor to a subject in need thereof.

Abstract: An oral preparation for the prophylaxis or improvement of dry skin accompanied by atopic dermatitis, xeroderma, chapped hand, chapped skin and the like is provided. The present invention can provide an oral preparation for the prophylaxis or improvement of dry skin, which comprises citrulline or a salt thereof as an active ingredient.

Abstract: The subject invention provides therapeutic compositions, and uses thereof for the treatment or amelioration of injury to small intestine mucosa. In preferred embodiments, the composition comprises one or more nutrients and/or electrolytes that acquire or retain considerable absorptive capacity.

Abstract: This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R1 and R2 are hydrogen, alkyl, or aryl radicals.

Abstract: A method of treatment of cystic fibrosis and other pulmonary diseases identified by nitric oxide deficiency, comprising administration of a nebulized solution of citrulline and/or another nitric oxide precursor as an inhalable aerosol or an inhalable dry powder for targeted delivery into conducting and central airways. Citrulline or another nitric oxide precursor is formulated as a composition having predetermined limited volume, salinity, pH and osmolality. The composition is nebulized into an aerosol having a mass median aerodynamic diameter (MMAD) between 2 ?m and 6 ?m.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Abstract: A feline pet food comprising a dietary level of protein and a supplemental amount of at least one amino acid in an amount sufficient to provide a feline lean body mass protection equivalent to about a 50% protein feline pet food.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: The invention relates to (among other things) oligomer-amino acid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated amino acid compounds.

Abstract: The present invention features compounds useful for and methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.

Abstract: The present invention relates to a composition containing bifeprunox or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, including Parkinson's disease and restless leg syndrome.

Abstract: The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients.

Abstract: The invention relates to methods of treating or preventing acquired or congenital mitochondrial diseases or disorders, including treating cell proliferation related disorders or diseases, such as cancer. The invention further relates to pharmaceutical compositions for treating such disorders or diseases.

Abstract: The subjects of the current invention are compounds, which exhibit arginase inhibiting activity (including difluoromethylornithine (DFMO) and L-norvaline, but not limited to them), and which can be used as therapeutically active agents for the treatment and prevention of depression and/or depression-related conditions. Other subjects of the present invention are the use of said arginase inhibiting compounds as therapeutically active agents for the manufacture of pharmaceutical compositions for human and veterinary application, pharmaceutical composition comprising said arginase inhibiting compound and a method for treatment and prevention of depression and/or depression-related conditions. Also, a method for identifying compounds suitable for use as therapeutically active agents for treatment and/or prevention of depression and/or depression-related conditions is disclosed.

Abstract: Provided are compositions comprising beta-alanylhistidine peptides and/or beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: A method for increasing the bioabsorption of amino acids in a human or animal is disclosed. The method includes administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Arginine, Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, and Valine.

Abstract: An object of the present invention to obtain a blood flow improving agent composed of natural components, which increase activity or circulation of blood flow and accelerate decomposition, detoxication and elimination of toxic substances and supplement each other, and the production method thereof. The blood flow improving agent of the present invention is prepared by blending a nano-colloidized marine organic compound, more than one of trace elements containing minerals extracted from a mineral ore and nano-colloidized plant minerals and amino acids derived from a fuvic acid in nano-bubble water containing dissolved oxygen.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

Abstract: Described herein are compositions for neutralization and decontamination of toxic chemical and biological agents. In one embodiment, the subject matter discloses a nontoxic, non-corrosive composition capable of neutralizing and decontaminating toxic chemical and biological agents in a very short period of time. The present subject matter finds utility in a great number of occasions, including, but not limited to, military actions or terrorist attacks where chemical or biological agents are utilized.

Abstract: The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.

Abstract: The present invention relates to the field of cardiology. More specifically, the present invention relates to the use of ?3 adrenoreceptor agonists to treat cardiac hypertrophy and heart failure. In a specific embodiment, a method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy. In a more specific embodiment, the method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of the ?3 adrenoreceptor agonist BRL 26830A to a patient diagnosed with cardiac hypertrophy. In a further embodiment, the present invention provides a method for treating a cardiovascular disease or condition associated with cardiac hypertrophy comprising the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy.

Abstract: [Problem] A valine, isoleucine, leucine mixture which is excellent in the reduction of bitter taste and improved dissolution speed is provided. [Solving Means] The above problem is solved by a solid solution composed of three amino acids of valine, isoleucine, leucine, and a solid solution composed of these and at least one of acid selected from the group consisting of neutral aliphatic amino acid, neutral hydroxy amino acid, neutral acid amide amino acid, acidic amino acid, basic amino acid, hydroxy acid.

Abstract: This disclosure demonstrates a novel therapy immunological approach using polyamine-based therapy (PBT) for relieving tumor-induced suppression of the patient's immune system. The demonstration of the pharmacological release from the naturally occurring polyamine-mediated immune suppression offers profound impact on the immunotherapy of cancer together with a variety of diseases caused by the disease-causing vector's ability to evade an immune reaction. This therapeutic approach is equally applicable to disease states whereby immune system suppression by polyamines has been demonstrated including; bacterial infections, parasitic infections including malaria and typanosomiasis, viral infections, peptic ulcers and gastric cancer due to H. Pylori infection together with prevention of pregnancy. With a small molecule drug, used in combination with DFMO, the pharmacological manipulation of polyamine levels for therapeutic benefit in various disease states is possible.

Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.

Abstract: A system for the controlled release of one or more physiologically or pharmacologically active substances, comprising compositions in the form of micro particles or granules, particularly for use in the zootechnical and/or veterinary field. The micro particles include a core which contains one or more substances having a pharmacological action, food supplements or diagnostic media, said one or more substances being characterized by the presence, within their chemical structure, of a basic functional group, specifically including an amine functional group. The core comprises also one or more carboxylic acids and/or their salts and eventually one or more excipients. Said core is coated by an outer layer of fats or waxes, and preferably by a mixture of glyceride of fatty acids.

Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject at least one compound selected from the group consisting of those set forth in Table 1, Table 2, Table 3, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.

Abstract: The present invention relates to compositions suitable for the treatment of pathological conditions distinguished by insufficient or reduced mitochondrial function. The compositions comprise, as principal active ingredients, the amino acids leucine, isoleucine and valine. The compositions may also comprise, as further active ingredients, amino acids threonine and lysine, and optionally, histidine, phenylalanine, methionine, tryptophan, as well as tyrosine and cysteine.

Abstract: The present invention relates to compositions suitable for the treatment of pathological conditions distinguished by insufficient or reduced mitochondrial function. The compositions comprise, as principal active ingredients, the amino acids leucine, isoleucine and valine. The compositions may also comprise, as further active ingredients, amino acids threonine and lysine, and optionally, histidine, phenylalanine, methionine, tryptophan, as well as tyrosine and cysteine.

Abstract: The invention provides methods for treating or preventing psychiatric and substance abuse disorders, involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.

Abstract: Disclosed herein is the identification of human DNA polymerase ? (pol ?) as the polymerase that mediates repair of DNA containing interstrand cros slinks (ICLs). The mechanism of action of a number of chemotherapeutic and antimicrobial agents is the induction of ICLs. Thus, provided herein is a method of enhancing the efficacy of a chemotherapeutic or antimicrobial agent in a subject, including selecting a subject in need of treatment with an ICL-inducing agent and administering to the subject an ICL-inducing agent and a therapeutically effective amount of an inhibitor of pol ?. Subjects in need of treatment with an ICL-inducing agent, include, for example, subjects diagnosed with a hyperproliferative disease, an autoimmune disease or an infectious disease. Also provided is a composition for treating a hyperproliferative disease, an autoimmune disease or an infectious disease, comprising an ICL-inducing agent and an amount of an inhibitor of pol ? sufficient to enhance the efficacy of the ICL-inducing agent.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy. Carboxylic acid-containing compounds having a terminal cyclic moiety, a carboxylic acid group, and a C3-12 hydrocarbon chain optionally containing at least one double bond, at least one triple bond, or at least one double bond and one triple bond linking the cyclic moiety and the carboxylic acid group are inhibitors of histone deacetylase.

Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.

Abstract: A modification of pharmacokinetics of suramin by use of amino compounds in modification of lipophilicity and protein binding characteristics for tackling the physico-chemical properties of suramin that gives it poor distribution in the body; formulating the resulting product in a form that leads to targeting body fluids like the lymphatic system when administered in a specific way; and determining the route of administration that maximizes targeting with a view to reducing the dosage so as to limit toxicity, hence increase tolerance by patient.

Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

Abstract: The invention involves various embodiments of a method for treating a human being for a condition associated with (1) a clinical state of impairment of carnitine or carnitine esters, or decreased fatty acid metabolism, (2) low energy production or lower ATP production, (3) clinical hyperammonemia, and (4) clinically high pyruvate levels resulting from a deficiency in the biosynthesis of carnitine. The method involves administering a therapeutically effective salt of N-6-trimethyl-L-lysine.

Abstract: The invention involves various embodiments of a method for treating a human being for a condition associated with (1) seizures, myoclonic seizures, epilepsy, refractory epilepsy, hyperkinetic movements or tremors of hands or feet, (2) a state of ataxia, (3) accumulation of neuronal autofluorescent storage bodies in lysosomes or neurons, or regression of motor development, and (4) low alertness, dementia or mental retardation. The method involves administering a therapeutically effective salt of N-6-trimethyl-L-lysine.

Abstract: It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitches” (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies.

Abstract: The presently disclosed and claimed inventive concepts include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and ?2-antiplasmin and abnormal cell proliferation. The presently disclosed and claimed inventive concepts also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed and claimed inventive concepts further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma ?2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.

Abstract: The invention provides antidepressant prodrugs comprising an antidepressant conjugated to one or more amino acids. The invention also relates to pharmaceutical compositions comprising an antidepressant prodrug, and to methods of preparing and using the same.

Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.

Abstract: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.

Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: Compositions based on amino acids are described, in particular for oral or parenteral use, suitable for treating heart insufficiency. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and valine, as active ingredients. Preferably, the compositions also comprise, as further active ingredients, up to 50% of theronine and lysine. Other essential amino acids are preferably also provided (in particular methionine, phenylalanine, histidine, triphtophan) as well as non essential amino acids (in particular tyrosine and/or cyst(e)ine—i.e., cystine and cyst(e)ine). Other amino acids can be added, provided that their sum is in a percentage being lower than 20% with respect to the other active ingredients, and less than 10% for each single amino acid.