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10th week of 2014 patent applcation highlights part 68
Patent application numberTitlePublished
20140066436PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - The present invention relates to a compound of formula (VII)I, or pharmaceutically acceptable salt or ester thereof, wherein: X is NR2014-03-06
20140066437OXATHIAZINE DERIVATIVES WHICH ARE SUBSTITUTED WITH BENZYL OR HETEROMETHYLENE GROUPS, METHOD FOR PRODUCING THEM, THEIR USE AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND THE USE THEREOF - The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.2014-03-06
20140066438DOPAMINE RECEPTOR D2 ANTAGONIST FOR PREVENTION AND TREATMENT OF FLAVIVIRUS INFECTION - Methods for preventing and/or treating flavivirus infection are disclosed. The method comprises administering to a subject in need thereof a composition comprising: a) a dopamine D2 receptor antagonist in an amount effective for preventing and/or treating flavivirus infection; and b) a pharmaceutically acceptable carrier. The dopamine D2 receptor antagonist may be selected from the group consisting of prochlorperazine or a salt thereof, and haloperidol.2014-03-06
20140066439OSTEOCLAST ACTIVITY - Described are medicaments and methods of treating or preventing metabolic bone diseases, such as Critical Illness Related Metabolic Bone Disease or of critical illness induced Osteopenia secondary to ICU Admission by sufficient autophagy inducing compound to inhibit or suppress critical illness enhanced osteoclastogenesis or increased osteoclast differentiation. The methods include administering of an autophagy activating compound to a mammal to: treat or prevent a bone degenerative disorder; slow bone deterioration; restore lost bone; maintain bone mass and/or bone quality or inhibit bone resorption in particularly by inhibiting or reducing a process by which osteoclasts break down bone and release the minerals resulting in a transfer of calcium from bone fluid to the blood. Also described are methods for administering the autophagy activating compound to treat a bone disorder of hyperresorption of bone and/or enhanced activation of osteoclasts.2014-03-06
20140066440Highly Concentrated Stable Meloxicam Solutions for Needleless Injection - A method for treating pain, inflammation, fever and respiratory complaints in mammals comprising administering by needleless injection to a mammal in need of such treatment an aqueous cyclodextrin-free solution of meloxicam containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base.2014-03-06
20140066441AEROSOLIZED FLUOROQUINOLONES AND USES THEREOF - Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.2014-03-06
20140066442Pyridinylcarboxylic Acid Derivatives as Fungicides - Pyridinylcarboxylic acid derivatives of the formula (I)2014-03-06
20140066443AMINOMETHYL BIARYL BENZOTRIAZOLE DERIVATIVES - The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.2014-03-06
20140066444Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.2014-03-06
20140066445Composition and Methods for Modulating a Kinase Cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relates to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.2014-03-06
201400664462,5-DISUBSTITUTED ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.2014-03-06
20140066447IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-P- HTHALAZIN-1-ONE - The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.2014-03-06
20140066448SUBSTITUTED DIAMINO-PYRIMIDINE AND DIAMINO-PYRIDINE DERIVATIVES AS PI3K INHIBITORS - The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R2014-03-06
20140066449DIPYRIDINIUM DERIVATIVES - Compounds of Formula (I): α-x-β (I) and pharmaceutically acceptable salts and solvates thereof, wherein α, x, and β have the meanings as indicated in the specification, are useful for treating a disease or disorder characterised by pathologically proliferating cells, particularly cancer. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.2014-03-06
20140066450NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT2014-03-06
20140066451THIOXANTHENE DERIVATIVES FOR THE TREATMENT OF INFECTIOUS DISEASES - The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.2014-03-06
20140066452TRANSDERMAL DELIVERY OF BENEFICIAL SUBSTANCES EFFECTED BY A HOSTILE BIOPHYSICAL ENVIRONMENT - The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may be delivered, according to certain embodiments, through the stratum corneum of the skin into the body. Beneficial substances include, but are not limited to, pharmaceutical agents, drugs, vitamins, co-factors, peptides, dietary supplements, and others. The beneficial effects disclosed include, for instance, relief of pain and inflammation, prevention and healing of ulcers of the skin, relief of headache, improved sexual function and enjoyment, growth of hair on the scalp, improving muscle size and/or function, removing body fat and/or cellulite, treating cancer, treating viral infections and others. A hostile biophysical environment may also be used in conjunction with systems and methods for increasing local blood flow, according to one set of embodiments. For example, by using a nitric oxide donor such as L-arginine, local blood flow may be increased, e.g., by transdermally delivering the nitric oxide precursor. The nitric oxide donor may be the sole cause of increased blood flow, or it may be supplemented with an adjunct such as theophylline.2014-03-06
20140066453SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein R2014-03-06
20140066454Antibiotic Tolerance Inhibitors - The present disclosure relates to benzimidazole-benzamide derivatives, and the use thereof, e.g., to treat infections.2014-03-06
20140066455NOVEL COMPOUNDS - There is provided a compound of formula (I):2014-03-06
20140066456COMBINATION THERAPY IN TREATMENT OF CANCER AND FIBROTIC DISEASES - The invention relates to new methods for the treatment of oncological and fibrotic diseases comprising the combined administration of a receptor tyrosine kinase inhibitor in conjunction with a thrombin inhibitor.2014-03-06
20140066457INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.2014-03-06
20140066458METHODS FOR TREATING VASCULAR LEAK SYNDROME - Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.2014-03-06
20140066459TETRAHYDROQUINOLINE DERIVATIVES USEFUL AS BROMODOMAIN INHIBITORS - Tetrahydroquinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.2014-03-06
20140066460SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-PYRROLIDIN-3YLVINYL)PYRIMIDINE - The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.2014-03-06
20140066461METHODS FOR DIAGNOSING AND TREATING SCHIZOPHRENIA - Genetic markers of schizophrenia (SCZ) are presented herein, as are methods for using same for assessing risk of developing SCZ and diagnosing SCZ. Methods for choosing a therapeutic regimen and predicting and/or determining efficacy of a therapeutic regimen based on these genetic markers are also encompassed herein.2014-03-06
20140066462TREATMENT OF POLYCYSTIC DISEASE - The present invention provides methods of treating polycystic disorders. In particular, methods include the use of inhibitors targeting certain protein kinases, such as mTOR, to treat polycystic disease.2014-03-06
20140066463SOLID FORMS OF PEMETREXED - There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof.2014-03-06
20140066464METHODS OF DIAGNOSING AND TREATING CANCER - A method of determining the susceptibility of a cancer in a subject to treatment with an antimetabolite includes obtaining a sample of cancer cells from the subject, measuring the level of UDG expression in the cancer cells, and comparing the measured levels of UDG expression in the cancer cells to a control level.2014-03-06
20140066465CANCER TREATMENT USING TYROSINE KINASE AND NF-kB INHIBITORS - A method of treating cancer by administering to a subject in need thereof a therapeutically effective amount of a tyrosine kinase inhibitor and an NF-κB inhibitor is described. The method is useful for treating subjects having cancer that has developed resistance to tyrosine kinase inhibitors.2014-03-06
20140066466Necroptosis Inhibitors and Methods of Use Therefor - Described herein are compositions that inhibit the production of TNFα downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNFα production or CD40 activation.2014-03-06
20140066468AMORPHOUS FORM OF LOPINAVIR AND RITONAVIR MIXTURE - The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it.2014-03-06
20140066469TREATMENT OF DISEASES ASSOCIATED WITH INFLAMMATION - Compositions and methods are provided for preventing or treating the pre-clinical early-stages of inflammatory diseases, including autoimmune diseases, degenerative inflammatory diseases, metabolic inflammatory diseases, chronic infection associated with inflammation, cancer associated with inflammation, and other inflammatory diseases by administration to an individual of an effective dose of a synergistic combination of active agents comprising or consisting essentially of an aminoquinoline, e.g. hydroxychloroquine, and a statin, e.g. atorvastatin. Each or both of the active agents can be formulated in various ways, including without limitation a solid oral dosage form.2014-03-06
20140066470NOVEL FORMULATIONS OF WATER-INSOLUBLE CHEMICAL COMPOUNDS AND METHODS OF USING A FORMULATION OF COMPOUND FL118 FOR CANCER THERAPY - Provided are compositions, methods of making the compositions, and methods of using the compositions. The compositions can be provided as pharmaceutical preparations for use in disease treatment, such as cancer therapy. The compositions include novel pharmaceutical preparations which contain effective concentrations of a chemical compound. One compound used is 10H-1,3-Dioxolo[4,5-g]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-8,11(7H,12H)-dione, 7-ethyl-7-hydroxy-, (S)-. The invention also provides methodologies for preparing pharmaceutical preparations for use in intravenous and oral pharmaceutical preparations that contain drug compounds that are difficult to dissolve in water.2014-03-06
20140066471EXTERNAL PREPARATION COMPOSITION COMPRISING FATTY ACID-BASED IONIC LIQUID AS ACTIVE INGREDIENT - Disclosed is an external preparation composition having good transdermal absorbability. An external preparation composition having excellent transdermal absorbability can be produced by dissolving a medicinal substance or a salt thereof in a fatty acid-based ionic liquid to form a composite ionic composition of the medicinal substance. The external preparation composition can be used as a liquid preparation, an ointment, a cream, a plaster or the like, and enables to provide a preparation having excellent transdermal absorbability.2014-03-06
20140066472METHODS OF PREVENTING THE DEVELOPMENT OF MUCOSITIS AND RELATED DISORDERS - Disclosed is a method of preventing the development of mucositis in a subject undergoing radiation therapy or chemotherapy for a disease in need thereof comprising administering an effective amount of a mammalian target of rapamycin (mTOR) inhibitor, such as rapamycin, to the subject. Further disclosed is a method of increasing the lifespan of a normal oral keratinocyte and/or reducing oxidative stress in a normal epithelial cell, wherein the method comprises administering an effective amount of an mTOR inhibitor to a subject undergoing radiation therapy or chemotherapy for a disease in need thereof.2014-03-06
20140066473MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS - A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.2014-03-06
20140066474COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND A MTOR INHIBITOR - The present invention relates to a pharmaceutical combination comprising a phosphatidylinositol-3-kinase (PI3K) inhibitor compound which is a 2-carboxamide cycloamino urea derivative or a pharmaceutically acceptable salt thereof and at least one mammalian target of rapamycin (mTOR) inhibitor or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising such a combination; and the uses of such a combination in the treatment proliferative diseases, more specifically of mammalian target of rapamycin (mTOR) kinase dependent diseases.2014-03-06
20140066475Method For Treating Pruritus - Benzomorphan compounds are found to be useful for treating, ameliorating or preventing pruritus, and in particular pruritus associated with (including induced by) the administration of opioids. Antipruritic activity is believed to be mediated through the dual action of the compounds as mu opioid receptor antagonists and kappa opioid receptor agonists. Pharmaceutical compositions contain therapeutically effective amounts of these useful compounds, optionally in combination with second therapeutic agents, such as opioid or non-opioid analgesics or other compounds.2014-03-06
20140066476MODULATORS OF CELLULAR ADHESION - The present invention provides compounds having formula (I):2014-03-06
20140066477Benzazole Derivatives, Compositions, and Methods of Use as Beta-Secretase Inhibitors - The present invention is directed to benzazole compounds that inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.2014-03-06
20140066478Beta2-Adrenoreceptor Agonists - Compounds of formula2014-03-06
20140066480METHODS AND MATERIALS FOR ASSESSING RESPONSIVENESS TO LENALIDOMIDE, THALIDOMIDE, AND/OR OTHER THALIDOMIDE ANALOGS - This document provides methods and materials related to assessing responsiveness to lenalidomide, thalidomide, and/or other IMiDs (structural and functional analogues of thalidomide that represent a promising new class of immunomodulators). For example, methods and materials for using CRBN levels to determine whether or not cancer cells (e.g., multiple myeloma cells) are susceptible to lenalidomide, thalidomide, and/or other IMiDs are provided.2014-03-06
20140066481Water-Free Pharmaceutical Compositions Suitable for Local Anaesthetics - The present invention relates to a water-free pharmaceutical composition comprising one or more local anaesthetics in base form and which is suitable for topical administration. The composition further comprises a lipid vehicle comprising long-chain triglycerides (LCT) and at least 10% by weight of medium-chain monoglycerides (MCM) selected so the composition has an at least semi-solid appearance at the body temperature at the site of administration. The invention further relates to methods of producing and sterilizing the compositions.2014-03-06
20140066482Pharmaceutical Formulation Comprising Metformin and Repaglinide - The invention is related to a pharmaceutical composition comprising repaglinide in combination with metformin or a salt thereof in unit dosage form wherein a pre-formulation of the repaglinide has a pH independent dissolution profile and a relative humidity of less than about 25% prior to mixing with the metformin or a salt thereof; and optionally one or more pharmaceutically acceptable excipients and to a method for its preparation.2014-03-06
20140066483METHOD OF ACTIVATING REGULATORY T CELLS WITH ALPHA-2B ADRENERGIC RECEPTOR AGONISTS - Disclosed herein is a method of upregulating regulatory T-cells, and treating diseases that would benefit from such upregulation, by administering an alpha 2 receptor agonist.2014-03-06
20140066484METHODS OF ADMINISTERING PIRFENIDONE THERAPY - The disclosure relates to improved methods of administering pirfenidone therapy when ciprofloxacin is administered concomitantly.2014-03-06
20140066485MEDICAMENTS CONTAINING FAMOTIDINE AND IBUPROFEN AND ADMINISTRATION OF SAME - A method for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine, in admixture, is administered three times per day.2014-03-06
20140066486REL INHIBITORS AND METHODS OF USE THEREOF - This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.2014-03-06
20140066487ANTIVIRAL COMPOUNDS AND METHODS - The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.2014-03-06
20140066488Inhibitors of Memapsin 2 Cleavage for the Treatment of Alzheimer's Disease - Proteases such as memapsin 2 are important enzymes, playing roles in a variety of diseases including Alzheimer's Disease. The inventors have developed inhibitors of memapsin 2 and methods of use therefore in the treatment of disease.2014-03-06
20140066489DECREASING OR PREVENTING SUB-SURFACE GEOLOGICAL MATTER CONTAMINATION BY AGROCHEMICALS - Method of exposing agricultural substrates (plant matter 2014-03-06
20140066490SYSTEM AND METHOD FOR MODIFYING DEOXYRIBOZYMES - A system and method for programming DNAzymes to be utilized as programmable drugs, which are active only in the presence of specific input combinations and/or certain conditions.2014-03-06
20140066491CHEMICAL MODIFICATION MOTIFS FOR MIRNA INHIBITORS AND MIMETICS - The present invention provides polynucleotides having chemistry patterns that provide for improved stability, potency, and/or toxicity relative to their use as miRNA inhibitors or miRNA mimetics. The invention further provides pharmaceutical compositions and formulations comprising the polynucleotides, and methods for treating patients having a condition associated with miRNA or mRNA expression.2014-03-06
20140066492SPINAL MUSCULAR ATROPHY (SMA) TREATMENT VIA TARGETING OF SMN2 SPLICE SITE INHIBITORY SEQUENCES - The present invention is directed to methods and compositions capable of blocking the inhibitory effect of a newly-identified intronic inhibitory sequence element, named ISS-N1 (for “intronic splicing silencer”), located in the SMN2 gene. The compositions and methods of the instant invention include oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target the SMN2 ISS-N1 site in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The ISS-N1 blocking agents of the invention cause elevated expression of SMN protein, thus compensating for the loss of SMN protein expression commonly observed in subjects with spinal muscular atrophy (SMA).2014-03-06
20140066493COMPOSITIONS AND METHODS FOR TREATMENT OF EAR DISORDERS - The present invention relates to pharmaceutical compositions useful for topical, non-invasive delivery of an oligonucleotide to the ear and to methods for the treatment of an ear disorder, including hearing loss arising from chemical-induced ototoxicity, acoustic trauma and presbycusis; and microbial infections. The method comprises topically administering to the ear of a subject in need thereof a pharmaceutical composition comprising an inhibitory oligonucleotide, a permeability enhancer and a pharmaceutically acceptable carrier, wherein the oligonucleotide reduces or inhibits expression of a gene associated with the ear disorder in the subject.2014-03-06
20140066494ACNE TREATMENT - The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.2014-03-06
20140066495TRANSMUCOSAL ADMINISTRATION OF TAXANES - The present invention provides a pharmaceutical composition for delivering an active agent taxane through transmucosal administration, more particularly through the buccal mucosa or sublingual mucosa. The present invention provides a method for treating cancer by buccal or sublingual administration of the pharmaceutical composition to a subject. The pharmaceutical composition comprises a taxane, a non-ionic surfactant, a viscosity enhancing agent, an adhesive agent, and an alcohol solvent at pH 4-6.2014-03-06
20140066496Composition and Methods for Anti-Macrofouling Treatment of Polymers - There is herein provided a composition comprising azadirachtin, preferably neem oil, and methods of use thereof for inhibiting macrofouling on a polymer in an aquatic environment.2014-03-06
20140066497TREATMENT OF IMMUNE DYSREGULATION USING CANNABINOID DERIVATIVES - This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.2014-03-06
20140066498TRITERPENOID DERIVATIVES, BENZENOID DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME - The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II):2014-03-06
20140066499PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES - An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.2014-03-06
20140066500CYCLOALKYLMETHYLAMINES - The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.2014-03-06
20140066501Anhydrous and Hemihydrate Crystalline Forms of an (R)-Baclofen Prodrug, Methods of Synthesis and Methods of Use - Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.2014-03-06
20140066502Use of Stabilized Granules Containing Glyceryl Trinitrate for Arteriogenesis - The present invention inter alia relates to a method of treating or preventing an arterial insufficiency, wherein an NO donor is administered in an intermitting manner to a subject in an amount effective for the induction of arteriogenesis, and wherein the NO donor is a solid pharmaceutical preparation with the active substance glyceryl trinitrate for oromucosal or oral administration characterized in that it contains between 0.05 and 2 weight % glyceryl trinitrate (GTN), at least one diluent, one carrier material, and at least one substance that reduces the volatility of GTN, whereby this substance is a non-volatile ester stabilizer whose melting point is not higher than 60° C.2014-03-06
20140066503METHODS FOR TREATING TACHYCARDIA AND/OR CONTROLLING HEART RATE WHILE MINIMIZING AND/OR CONTROLLING HYPOTENSION - A method of treating tachycardia while minimizing and/or controlling hypotension associated with such treatment includes administering a therapeutically effective amount of a pharmaceutical composition comprising the S-isomer of esmolol to a subject in need thereof.2014-03-06
20140066504ANALOGS AND PRODRUGS OF BUMETANIDE; COMPOSITIONS AND METHODS OF USE - Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus.2014-03-06
20140066505Utilization of Dialkylfumarates - The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.2014-03-06
20140066506METHOD FOR TREATING MACULAR DEGENERATION - Disclosed is a method for treating macular degeneration in a mammalian subject, which includes administering to the subject in need thereof an effective amount of a 15-keto-prostaglandin compound such as 13,14-dihydro-15-keto-20-ethyl-prostaglandin F2014-03-06
20140066507COSMETIC COMPOSITIONS COMPRISING EPA AND SALICYLIC ACID AND METHODS OF MAKING AND USING SAME - The present disclosure is directed generally to cosmetic compositions comprising EPA free acid and salicylic acid. In some embodiments, the cosmetic compositions have a cosmetically acceptable odor.2014-03-06
20140066508METABOLIC SYNDROME AMELIORATING AGENT - A method for ameliorating metabolic syndrome may include administering, to a patient in need thereof, an effective amount of a monounsaturated fatty acid having 22 carbons or a salt or an ester thereof and/or an effective amount of a monounsaturated fatty acid having 20 carbons or a salt or an ester thereof.2014-03-06
20140066509COSMETIC COMPOSITIONS COMPRISING EPA AND GLA AND METHODS OF MAKING AND USING SAME - The present disclosure is directed generally to cosmetic compositions comprising EPA free acid and GLA free acid. In some embodiments, the cosmetic compositions have a cosmetically acceptable odor.2014-03-06
20140066510OAT EXTRACTS: REFINING, COMPOSITIONS AND METHODS OF USE - A simple and efficient method for the production of stable, clear, high-potency oat extracts is disclosed. The method employs the use of differential dissociation constants and ultrafiltration to stabilise extracts, prevent hazing, and prevent the loss of functional activity as an anti-irritant and anti-oxidant. Also disclosed are compositions of oat extracts derived from whole oat grains and oatmeal. Further disclosed are compositions of oat extracts for use in cosmetic, nutraceutical, therapeutic medical and veterinary preparations.2014-03-06
20140066511TOPICAL DELIVERY OF L-ARGININE TO CAUSE BENEFICIAL EFFECTS - A preparation is disclosed for producing enhanced blood flow in tissue thus causing beneficial effects such as promoting hair growth on scalp tissue lacking sufficient hair, restoring normal sexual function in males with erectile dysfunction. Specifically, this is a preparation which provides local delivery of the amino acid L-arginine, an important biological precursor to the main substance which is responsible for relaxation of blood vessels permitting enhancement of blood flow. In the preferred embodiments, the L-arginine is provided so that it can be topically applied to the scalp or penis. The preparation also contains an agent which aids in the transfer of L-arginine into the tissue. In the preferred embodiments this agent overcomes the resistance to transfer caused by the high charge density of L-arginine. In the preferred embodiments this means is high ionic strength created by addition of choline chloride, magnesium chloride and sodium chloride. This preparation when applied nightly to scalp tissue lacking sufficient hair for a period of time causes substantial growth of hair on the scalp. Further, when applied to the penis of a subject with erectile dysfunction causes restoration of normal sexual function.2014-03-06
20140066512ORAL COMPOSITIONS COMPRISING CREATINE - The present invention relates to rehydration and nutritional products comprising creatine and/or its salts, or analogues or precursors thereof, in ready to use aqueous oral compositions, such as gels, pastes and the like, and products for reconstitution in water, for use by humans and animals, together with processes for their preparation and uses thereof.2014-03-06
20140066513METHODS FOR COMPOSITIONS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME - A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I:2014-03-06
20140066514Veterinary Compositions For Controlling Ecto- And Endoparasites In Bovines, Use Of These Compositions, Use Of IGR Substances Associated With Microminerals, Method For Controlling Ecto- And Endoparasites In Bovines And Kit - Veterinary compositions are described for controlling ecto- and endo-parasites in animals, such as bovine. The compositions contain an IGR compound(s) or a benzoyl substituted urea(s) along with a mineral mix and at least one carrier.2014-03-06
20140066515METHODS FOR TREATING CHANNELOPATHIES - The present invention is directed to the use of a class of peptide compounds for treating diseases associated with hyperexcitability. The present invention is also directed to the use of a class of peptide compounds for treating diseases associated with dysfunction of an ion channel.2014-03-06
20140066516Novel Method - The present invention is directed to a novel method for reducing intrapatient variability in pharmaceutically active agent which is suitably not absorbed in the stomach, such as paracetamol, containing formulations in patients having gastric dysmotility, or a method of improving analgesia in a diabetic patient, or improving absorption of an active agent is a patient with gastric dysmotility, which methods comprises administering orally to said patient in need thereof a pharmaceutical dosage form comprising a first active agent, calcium carbonate, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, a super disintegrant, and a second active agent.2014-03-06
20140066517USE OF CALIXARENES ASSOCIATED WITH AN ANTIBOTIC IN THE TREATMENT OF BACTERIAL INFECTIONS - A product comprising a calixarene for its use in the treatment of pathologies involving at least one bacterial strain having a resistance to at least one defined antibiotic, on patients undergoing simultaneous or sequential treatment with a given antibiotic to which said bacterial strain optionally has a resistance.2014-03-06
20140066518USE OF A SPRAYABLE COMPOSITION COMPRISING AMBROXOL - The present invention relates to ambroxol hydrochloride for the treatment of acute pharyngitis, wherein ambroxol hydrochloride as a sprayable composition comprising up to 30 mg/ml ambroxol hydrochloride is administered locally in a dose of 1 to 20 mg.2014-03-06
20140066519USE OF XANTHOHUMOL AND/OR ISOXANTHOHUMOL AS AN AGENT FOR PREVENTING AND/OR COMBATING LIVER DISEASES - Method for the prevention and/or control of liver diseases, such as non-alcoholic steatohepatitis (NASH) even when eating a high fat diet. Prevention of NASH can be accomplished by preventing the liver from becoming a fatty liver even when eating a high fat diet by providing xanthohumol as a supplement to the high fat diet.2014-03-06
20140066520NOVEL ANTI-INFLAMMATORY CYCLOOXYGENASE INHIBITORS - Disclosed is a pharmaceutical composition including a therapeutic quantity of a COX-2 inhibitor having an IC50-WHMA COX-2/COX-1 ratio ranging from about 0.23 to about 3.33 with reduced gastrointestinal and cardiovascular toxicity. Also disclosed are methods for treating osteoarthritis, rheumatoid arthritis or acute pain with less side-effects and faster onset of action utilizing the disclosed pharmaceutical composition.2014-03-06
20140066521ANITBACTERIAL OR PRESERVING COMPOSITION CONTAINING 3-BUTOXY-1,2-PROPANEDIOL - The present invention relates to an antibacterial and/or preserving composition which contains 3-butoxy-1,2-propanediol as a preserving agent. The antibacterial or preserving composition according to the present invention has an excellent resistance to microorganisms and has an excellent moisturizing effect, and hardly causes skin troubles.2014-03-06
20140066522EMULSIONS OF PERFLUOROCARBONS - The subject application provides for an emulsion comprising an amount of a perfluorocarbon liquid dispersed as particles within a continuous liquid phase, wherein the dispersed particles have a monomodal particle size distribution and uses thereof. The subject application also provides for a method of manufacturing a perfluorocarbon emulsion, a process for preparing a pharmaceutical product containing a PFC emulsion and a process for validating a batch of an emulsion for pharmaceutical use.2014-03-06
20140066523Drug Delivery Compositions And Methods Of Use - The invention provides moldable drug delivery carriers made up of a suspension of a solid phase and an organic liquid phase for the sustained release of a therapeutic agent. The invention also provides multiphase drug delivery systems made up of a granular hydrophobic solid phase, an organic liquid phase and a hydrogel, for sustained drug delivery at varying rates over the life of the composition.2014-03-06
20140066524COMPOSITIONS, GELS AND FOAMS WITH RHEOLOGY MODULATORS AND USES THEREOF - The present disclosure relates generally to compositions for cosmetic or pharmaceutical application. The compositions include a carrier and rheology modulators.2014-03-06
20140066525METHODS FOR IMPROVING HIGHER ALCOHOL YIELDS FROM SYNGAS BY ALTERING FLOW REGIMES WITHIN A REACTOR - Mixed alcohols are produced from syngas. The syngas is provided to a catalyst in a reactor at selected temperatures and pressures. Reactive products, including mixed alcohols, are removed from the reactor. Non-reactive components are removed from the mixed alcohols of their reaction products. At least part of the non-reactive components are reintroduced in the reactor along with syngas. The non-reactive components are a solvent or a super critical fluid. The non-reactive components can be reintroduced into the reactor with reactive components such as methanol or CO2.2014-03-06
20140066526METHOD AND APPARATUS FOR PRODUCTING LIQUID HYDROCARBON FUELS - A method of converting carbon containing compounds such as coal, methane or other hydrocarbons into a liquid hydrocarbon fuel utilizes a high pressure, high temperature reactor which operates upon a blend of a carbon compound including CO2014-03-06
20140066527Synthesis Gas Reaction and Processing System - A process wherein synthesis gas is reacted to produce desired products, such as alcohols, and wherein by-products, such as methane, are reformed to provide hydrogen and carbon monoxide that is recycled to the feed of synthesis gas. The process also may provide for the recycle of unreacted hydrogen and unreacted carbon monoxide to the feed of synthesis gas.2014-03-06
20140066528ANION EXCHANGE MEMBRANE AND PRODUCING METHOD THEREOF - A graft chain containing an N-vinylimidazole derivative is introduced into a polymer substrate by radiation graft polymerization to obtain an alkyl substituted imidazolium salt by a reaction with an alkyl halide, so that an anion exchange membrane with high alkaline durability, in which a nucleophilic substitution reaction and an elimination reaction are inhibited, is obtained.2014-03-06
20140066529Nanoporous Silica Polyamine Composites with Surface-bound Zirconium (IV) and Methods of Use - Silica polyamine composites (SPC) made from silanized amorphous nano-porous silica gel and poly(allylamine) (BP-1) were functionalized with phosphorus acid using the Mannich reaction, resulting in a phosphonic acid modified composite (BPAP). Zirconium (IV) was immobilized on BPAP. Arsenate anions strongly adsorbed on the ZrBPAP composite in the pH range 2 to 8, while arsenite only adsorbed well at pH 10. Regeneration of the resin was carried out successfully for As(V) and As(III) using 2M-H2014-03-06
20140066530EVA RECYCLING METHOD - A method of recycling scrap ethylene-vinyl acetate (EVA) foam involves foaming and crosslinking a blend containing virgin EVA resin and scrap EVA foam, as well as a crosslinking agent and blowing agent for the EVA resin. The blend further contains a compatibilizer, which is a hydrogenated petroleum resin.2014-03-06
20140066531HIGHLY REFRACTORY RUBBER COMPOSITION SHEET - To provide a highly refractory rubber composition sheet that retains a fixed shape until the thermal expansion residue formed by the heat of a fire or the like is formed, does not allow the thermal expansion residue from the heat formed by a fire or the like to easily detach and fall off of construction materials, such as steel framing and the like, and can prevent penetration of flames for at least two hours in the case of exposure to the flames of a fire or the like. [Solution] The highly refractory rubber composition sheet is formed from a highly refractory rubber composition that contains a polyhydric alcohol (A), a nitrogen-containing foaming agent (B), a rubber substance (C), a flame resistant foaming agent (D), and titanium dioxide (E). The highly refractory rubber composition sheet is characterized by the nitrogen-containing foaming agent (B), being in a range of 76-80 parts by weight to 100 parts by weight of the rubber substance (C).2014-03-06
20140066532RIGID FOAMS SUITABLE FOR WALL INSULATION - Polyurethane/polyisocyanurate foams having a NFPA 101 Class A rating (ASTM E-84) are produced from a foam-forming reaction mixture that includes: an organic polyisocyanate, an isocyanate-reactive composition that includes at least one polyether polyol or polyester polyol with a nominal hydroxyl functionality of at least 2.0, a blowing agent composition and at least one halogen-free flame retardant. The blowing agent composition includes: (1) up to 5% by weight, based on total weight of the foam-forming composition, of one or more hydrocarbons having an LEL less than 2% by volume in air; and/or (2) a hydrocarbon having an LEL greater than 2% by volume in air; and (3) up to 1% by weight, based on total weight of foam-forming composition, of water.2014-03-06
20140066533CONJUGATED MICROPOROUS MACROMOLECULE CATALYST COMPLEXED WITH COBALT, CHROMIUM, ZINC, COPPER OR ALUMINIUM, PREPARATION AND USE THEREOF - Disclosed are a type of catalyst which can catalyse the ring-addition reaction of CO2014-03-06
20140066534POLYURETHANE FOAM AND METHOD FOR PRODUCING SAME - The invention relates to a method for producing a polyurethane foam, wherein a mixture having the following is discharged from a mixing head through a discharge line: A) a component reactive toward isocyanates; B) a surfactant component; C) a blowing agent component selected from the group comprising linear, branched, or cyclic C1 to C6 hydrocarbons, linear, branched, or cyclic C1 to C6 fluorocarbons, N2, O2, argon, and/or CO2, wherein the blowing agent C) is present in the supercritical or near-critical state; and D) a polyisocyanate component. The component A) has a hydroxyl value=100 mg KOH/g and =1000 mg KOH/g. The blowing agent component C) is present at least partially in the form of an emulsion, and means provided with an opening or several openings are arranged in the discharge line in order to increase the flow resistance during the discharge of the mixture comprising A), B), C), and D), wherein the cross-sectional area of the opening or the sum of the cross-sectional areas of all openings is =0.1% and =99.9% of the inner cross-sectional area of the discharge line.2014-03-06
20140066535METHOD FOR PRODUCING FLEXIBLE POLYURETHANE FOAM MATERIALS - The present invention relates to a method for producing flexible polyurethane foams, wherein an isocyanate component (component B) is used which comprises polyether carbonate polyol, and to the isocyanate component itself. The invention also provides an NCO-terminated, urethane group-comprising prepolymer obtainable by reaction of one or more polyisocyanates (B1) with one or more polyether carbonate polyols.2014-03-06
20140066536POLYMER POLYOLS HAVING IMPROVED QUALITY - This invention relates to polymer polyols comprising one or more base polyols; one or more ethylenically unsaturated monomers in which at least one of the monomers is styrene which contains less than or equal to 1000 ppm of impurities; with one or more preformed stabilizers; in the presence of at least one free radical polymerization initiator; and optionally, one or more chain transfer agents.2014-03-06
20140066537ORGANIC COMPOSITIONS FOR REPEATEDLY ADJUSTABLE OPTICAL ELEMENTS AND SUCH ELEMENTS - The present invention relates an organic liquid composition comprising a mixture of a first polymer with a linear polymeric chain having two photoactive groups as endgroup; and a second polymer with a multifunctional polymeric chain having at least three photoactive groups, that can reversibly and repeatedly crosslink to form a solid polymer network wherein said liquid composition been crosslinked by irradiation with at least one wavelength L1 and been uncrosslinked at least locally by irradiating the network with at least one other wavelength L2 in order to repeatedly adjust shape and optical properties of said composition in its crosslinked state. The composition is applicable as a starting material for intraocular lenses and for other lenses and optical elements.2014-03-06
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