Abstract: The present inventions provide combination therapies, kits, and methods for providing relief and/or for improving one or more symptoms associated with an auditory system disorder in a subject diagnosed with the auditory system disorder, comprising an effective amount of at least one pharmaceutical agent and at least one auditory system disorder device, as well as methods for using at least one pharmaceutical agent and/or at least one auditory system disorder device in the manufacture of said kits.

Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.

Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: A composition and method for treatment of osteoarthritis is disclosed. The composition includes at least one soluble injectable biocompatible carrier having a viscosity within prescribed limits and an amount of a calcium-channel blocker chosen in relation to the viscosity of the carrier. The concentration of the calcium-channel blocker in the joint synovial fluid is controlled according to the invention whereby effective treatment of osteoarthritis is provided.

Abstract: A method and chemical composition for modifying and dissolving atherosclerotic plaques formed in a patient's blood vessels is provided. A chemical composition comprising one or more of an organic substance, an inorganic substance, and a bioactive substance is administered at sites of the plaques. The chemical composition comprises one or more of d-limonene, propylene glycol, octanoic acid, 2-octane, glycerine, acetylsalicylic acid, acetic acid, omega-3 fatty acids, ethanol, methanol, ezetimibe, rosuvastatin, resveratrol, lactic acid, gluconic acid, chloroform, carbon disulfide, dichloromethane, toluene, lauryldimethyl hydroxysultaine, and any combination thereof. The chemical composition enables modification of plaques by altering their composition. The modification comprises partial dissolution, complete dissolution, or elimination of the plaques, and makes the plaques amenable to different forms of plaque treatment. The modified plaques are eliminated from the patient's body.

Abstract: Various agents are described to denerve, modulate, or otherwise affect the renal nerves and other neural tissue. Also, various delivery devices are described to deliver an agent locally to the renal nerves. The delivery devices are positioned in the renal artery and penetrate into the wall of the renal artery to deliver the agent to the renal nerves. The delivery devices may be used to deliver the agent according to longitudinal position, radial position, and depth of the renal nerves relative to the renal artery. In addition, various methods are described to denervate, modulate, or otherwise affect the renal nerves and other neural tissue.

Abstract: The present invention relates to an in-vitro method for the formation of megamitochondria in cells, wherein the cells are grown in a suitable fermentation medium acidulated with lactic acid to pH values between 5.3 and 6.7. The invention further concerns H+ ionophores, ionophores which catalyze the electroneutral exchange of K+ for H+ and inhibitors of actin polymerisation for the prevention or treatment of a disease in which inhibiting or reducing the formation of megamitochondria has a beneficial effect.

Abstract: Provided is a method of treating or preventing a cardiomyopathy associated with activation of at least one kinase in the MAP kinase signaling pathway in heart tissue by providing to a subject an inhibitor of at least one kinase in the ERK signaling pathway or in the JNK signaling pathway, or both. In some embodiments, the cardiomyopathy is associated with one or more mutations in the LMNA gene, which encodes A-type nuclear lamins, or in the EMD gene, which encodes an inner nuclear membrane protein.

Abstract: A medicament for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the production of such a medicament, and a method for the treatment of such phantom phenomena

Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.

Abstract: Dual suppression of the MAP kinase and PI3K/Akt pathways showed synergistic or greatly enhanced anti-melanoma cell effects, compared to suppression of a single pathway, including the inhibition of cell proliferation, transformation and invasion, induction of G0/G1 cell cycle arrest and, importantly, cell apoptosis. Remarkably, suppression of either pathway induces the expression of thyroid iodide-handling genes and dual suppression of the two pathways synergistically and robustly induces expression of these genes, accompanied by uptake of radioiodine in the cells. These genes include sodium/iodide symporter, thyroid-stimulating hormone receptor, thyroglobulin, thyroperoxidase, pendrin gene, thyroid transcription factors (e.g., TTF-1, TTF-2, PAX8) and other thyroid genes.

Abstract: A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.

Abstract: The present invention provides compositions and methods featuring microRNA polynucleotides for the diagnosis, treatment or prevention of neoplasia.

Abstract: The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kine-toplastid or apicomplexan protozoan with tyrosine kinase inhibitors.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.

Abstract: A method of combating breast cancer in a mammalian individual, the method comprising administering to the individual an agent which reduces the function of the gamma secretase (GS) complex.

Abstract: The present invention relates to a method of treating hepatitis comprising administering a serotonin blocker, and the use of such blockers in said treatment and in the manufacture of medicaments for treating hepatitis.

Abstract: Compositions and methods for the treatment and diagnosis of cancer are disclosed.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.

Abstract: The invention relates to the use of at least on inhibitor selected from the group consisting of raf-, protein kinase C(PKC)-, MEK1/2-, or ERK1/2-inhibitors, for the manufacturing of a medicament to be administrated from 1 up to 12 hours after initiation of an ischemic disease.

Abstract: The invention consists in that substances acting as cascade inhibitors of the Raf/MEK/ERK signaling pathway, in particular MEK inhibitors, are used for the production of a drug for the preventive and antiviral therapy against DNA and RNA viruses, in particular against intranuclear-replicating negative strand RNA viruses, for instance influenza or Borna disease viruses.

Abstract: The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor.

Abstract: Described herein are methods for identification of alternative safe molecular targets and novel regulators in complex molecular networks using a novel fault diagnosis engineering approach. For example, in this invention we claim new molecular targets that could be effectively targeted for changing the activity of CREB, and therefore for treatment of learning and memory related disorders. Learning and memory dysfunction is a major clinical manifestation of a number of human disorders, such as Alzheimer Disease (AD), schizophrenia, dementias, autism, etc. More specifically, we claim that composition and compounds that can target the activity of L AND/OR P/Q-, N-type calcium channels, G?i, G??, PP2A and CaMKII and IV are effective therapeutics for the treatment of disorders manifested by learning and memory dysfunction.

Abstract: Compounds of formula (I), in which R1 and R2 are independently a substituted phenyl group, where the substituents are as defined in the claims and with the proviso that at least one of the substituents is a cyano, carboxy or (C1-4)alkoxycarbonyl group, are inhibitors of CCR9 activity useful for therapeutic treatment, particularly of irritable bowel disease.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: A method for treating cerebral vascular diseases in a human or non-human animal is disclosed. The method involves inhibiting 20-HETE synthesizing enzyme activity sufficiently to increase or prevent a decrease in cerebral blood flow in the human or non-human animal.

Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.

Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.

Abstract: The invention relates to benzotriazol-1-yl-aminoacetonitrile compounds and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.

Abstract: The present invention provides certain monofluoroalkyl derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of Formula (I).

Abstract: Provided is a method of formulating hydrophobic pesticides comprising emulsifying an aqueous phase and a water-immiscible phase to form a formulation; wherein the aqueous phase is comprised of water and optionally a freeze/thaw agent, one or more emulsifiers, or combinations thereof, and the water-immiscible phase comprises the hydrophobic pesticide and one or more emulsifiers.

Abstract: A regime or regimen for loosening/slackening and/or relaxing cutaneous and/or subcutaneous human skin tissue, advantageously for cosmetically/therapeutically treating skin wrinkles and fine lines, comprises administering to a candidate subject in need of such treatment, a thus-effective amount of at least one inhibitor of at least one calcium channel.

Abstract: A method and device are disclosed which prevents the decay and deterioration of wooden objects caused by pests by using a controlled release device. This controlled release device utilizes polymers which incorporate pesticides. In the disclosed method, the controlled release device is placed in contact with the wood of the wooden object. The pesticide is gradually released from the device and absorbed into the wood structure. The pesticide absorbed by the wood creates a barrier or an exclusion zone to penetration by inserts. The controlled release device maintains a minimal effective level of pesticide in the barrier or exclusion zone for a predetermined period of time.

Abstract: The present invention is directed to methods of treating, preventing, and/or managing abnormal increases in gastrointestinal motility, and intestinal conditions that cause the same. Such conditions include, but are not limited to, irritable bowel syndrome (IBS), infectious diseases of the small and large intestines, and symptoms of any of the foregoing. In particular, the present invention discloses methods of using enriched (R)-verapamil, as well as compositions and formulations containing the same.

Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is H, chlorine, or bromine; R2 is electron attractive groups selected from the group consisting of CF3, CN, fluorine, CH3SO3, CF3SO3, and NO2; R3 is linear or branched alkyl having 1 to 10 carbon atoms, linear or branched alkoxyalkyl having 2 to 10 carbon atoms, aliphatic alcohol having 1 to 10 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms. The invention also relates to methods for preparing the said compounds and the composition comprising the same. The compounds of the present invention have the effect of &bgr;2-receptor agonist and can be used for the treatment of asthma and bronchitis.

Abstract: Compounds of formula (I) 1

Abstract: A method for resolving enantiomers of a compound containing the structure of the formula: 1

Abstract: Novel methods of treating bone diseases or disorders are provided.

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: Carriers for use in the preparation of mixtures for inhalation powders intended for pulmonary administration of micronized drugs by means of a dry powder inhaler and the method for their preparation are described.

Abstract: To provide novel nitrogen-containing compounds having antagonism to CXCR4 and remedies for disease, such as rheumatism, cancer metastasis, etc., based on the CXCR4 antagonism.

Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically compatible, water-soluble salts thereof 1

Abstract: This invention relates to chemical uncouplers with a broader safety window making the use of them in treating obesity and, consequently, in the treatment of obesity related diseases and conditions such as atherosclerosis, hypertension, diabetes, especially type 2 diabetes (NIDDM (non-insulin dependent diabetes mellitus)), impaired glucose tolerance, dyslipidemia, coronary heart disease, gallbladder disease, osteoarthritis and various types of cancer such as endometrial, breast, prostate and colon cancers and the risk for premature death as well as other conditions, such as diseases and disorders, which conditions are improved by an increase in mitochondrial respiration, more attractive.

Abstract: The present invention relates to the use of specific compounds for the treatment and/or prophylaxis of inflammatory conditions. Furthermore, the present invention relates to the use of inhibitors for treating viral infections, particularly to the use of MEK inhibitors, especially MEKI inhibitors, for prophylaxis and/or treatment of virally induced hemorrhagic fever and/or hemorrhagic shock syndromes, for the treatment of virally induced TNF-∝ mediated diseases, and for regulating and/or inhibiting of virally induced TNF-∝ production. Furthermore, methods for preventing and/or treating of virally induced hemonrhagic fevers and/or hemorrhagic shock syndromes, for regulating and/or inhibiting virally induced TNF-∝ production, and for the treatment of virally induced TNF-÷ medicated diseases are disclosed together with pharmaccutical compositions useful within said methods.

Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of Formula (1).