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36th week of 2013 patent applcation highlights part 36
Patent application numberTitlePublished
20130231261RNASE H-BASED RNA PROFILING - Methods for determining the presence, absence and/or amount and/or identity of RNA in a biological or other sample employs capturing and separating a DNA:RNA hybrid formed by a DNA probe and the RNA of interest from unhybridized DNA and RNA with an RNase H under conditions wherein the nuclease activity of the RNase H is inhibited, releasing the DNA probe by altering the conditions so that the nuclease activity is restored, and determining the presence or amount, and, for multiplex samples, nature of the DNA released. The method can be used to determine RNA of various types, including RNA comprising transcriptomes.2013-09-05
20130231262ENGINEERED PROTEIN: "2-COLOR SERCA", AN ION-MOTIVE ATPase FUSED TO CERULEAN AND YELLOW FLUORESCENT PROTEIN - A method and engineered proteins for use therewith suitable for studying SERCA that are capable of being used in vivo and do not require protein purification or chemical labeling of SERCA, or reconstitution into artificial membranes. The engineered protein for calcium handling within human cells includes a two-color SERCA construct having three component proteins fused together. The three component proteins include a blue fluorescent protein (cerulean), SERCA2a and a yellow fluorescent protein (YFP), or a red fluorescent protein (tagRFP acceptor), SERCA and a green fluorescent protein (GFP). The method of determining SERCA activity for optimization of cardiac function includes resolving structure changes of the two-color SERCA construct. The two-color SERCA constructs are catalytically active and able to pump calcium following the step of resolving structure changes.2013-09-05
20130231263METHODS FOR SELECTING COMPETENT OOCYTES AND COMPETENT EMBRYOS WITH HIGH POTENTIAL FOR PREGNANCY OUTCOME - The present invention relates to a method for selecting a competent oocyte or a competent embryo.2013-09-05
20130231264Ultra-High Throughput Screening Methods to Detect Synergistic Drug Interactions - Synergy occurs when combined agents induce a response greater than the sum of their individual effects. The present invention provides new high throughput screening methods to detect agents acting synergistically in orthogonally pooled mixtures. Computational de-convolution of the pooled data with software reveals single-actives in the pools with twice the statistical power and with much greater efficiency than common high throughput screening approaches. Cross-correlating the orthogonal data reveals pools with activity that cannot be ascribed to any single compound. The components of such ‘Orphan’ activity pools are then tested individually and in all possible combination-pairs to identify and confirm synergy. The high throughput screening invention disclosed, which we name “Ultra-High Throughput Screening for Synergy (uHTSS)”, is applicable for more efficiently discovering nucleic acids, proteins and small molecules that act synergistically without having to systematically test each possible pair, as is required by known screening practices.2013-09-05
20130231265TYROSINE KINASE BIOSENSORS AND METHODS OF USE - Disclosed are compositions and methods for measuring tyrosine kinase activity.2013-09-05
20130231266METHODS AND COMPOSITIONS REDUCING TARGET GENE EXPRESSION USING COCKTAILS OF siRNAS OR CONSTRUCTS EXPRESSING siRNAS - The present invention concerns methods and compositions involving the production or generation of siRNA mixtures or pools capable of triggering RNA-mediated interference (RNAi) in a cell. Compositions of the invention include kits that include reagents for producing or generating siRNA pools. The present invention further concerns methods using polypeptides with RNase III activity for generating siRNA mixtures or pools that effect RNAi, including the generation of a number of RNA molecules to the same target gene.2013-09-05
20130231267ADENOVIRAL ASSEMBLY METHOD - Methods of assembling modified adenoviruses, libraries of adenoviral gene modules and compositions thereof are provided herein.2013-09-05
20130231268Stabilized Acid Precursor and Acid-Enzyme Formulations for Drilling Mud Cake Removal - Enzyme formulations should stay active and devoid of all possible inactivation processes during transport and long-term storage. The stabilization of enzymatic activity, especially in presence of critical functional components for specialized application, has been a long-standing obstacle when stored over an extended period of time. One such obstacle is the stability of enzyme in presence of weak acids in formulation, which is often desired to efficiently break down biopolymer filtercake embedded in a carbonate matrix, in the open-hole section of a horizontal well, for hydrocarbon production. The invention comprises methods and compositions to enhance the long-term storage stability of an enzyme formulation consisting of an in-situ acid precursor system, where in-situ generated precursors are mainly ester compounds that dissociate by slow hydrolysis to generate organic acid, shifting the pH of the formulation outside the pKa of the enzyme protein. The methods and compositions include the addition of high concentrations of metal halide salts, a pH control additive, and a water activity reducing agent. The methods and compositions of the invention provide a high degree of stability for enzyme formulation at long-term storage conditions.2013-09-05
20130231269Multicomponent Viscoelastic Surfactant Fluid and Method of Using as a Fracturing Fluid - There is a viscoelastic fluid. The fluid has one or more cationic surfactants selected from the group consisting of certain quaternary salts, certain amines, and combinations thereof; one or more anionic polymers/anionic surfactants; one or more of certain zwitterionic/amphoteric surfactants; and water. There is also a method of fracturing a subterranean formation. The viscoelastic fluid is pumped through a wellbore and into a subterranean formation at a pressure sufficient to fracture the formation. There is also a method for gravel packing a subterranean formation.2013-09-05
20130231270Superabsorbing Gel for Actinide, Lanthanide, and Fission Product Decontamination - The present invention provides an aqueous gel composition for removing actinide ions, lanthanide ions, fission product ions, or a combination thereof from a porous surface contaminated therewith. The composition comprises a polymer mixture comprising a gel forming cross-linked polymer and a linear polymer. The linear polymer is present at a concentration that is less than the concentration of the cross-linked polymer. The polymer mixture is at least about 95% hydrated with an aqueous solution comprising about 0.1 to about 3 percent by weight (wt %) of a multi-dentate organic acid chelating agent, and about 0.02 to about 0.4 molar (M) carbonate salt, to form a gel. When applied to a porous surface contaminated with actinide ions, lanthanide ions, and/or other fission product ions, the aqueous gel absorbs contaminating ions from the surface.2013-09-05
20130231271PHOTORESIST RESIDUE AND POLYMER RESIDUE REMOVING LIQUID COMPOSITION - Provided are a photoresist residue and polymer residue removing liquid composition, and a method of removing the residue used therewith, for removing photoresist residue and polymer residue produced during a process of manufacturing a semiconductor circuit element having metallic wiring. Specifically, the composition does not contain nitrogen-containing organic hydroxyl compounds, ammonia or fluorine compounds, and contains an aliphatic polycarboxylic acid having a melting point of 25° C. or higher with an excellent residue removing property and having a metallic oxide main component as the residue removing component. The photoresist residue and polymer residue removing liquid composition, and the method of removing the residue used therewith, is capable of preventing the aliphatic polycarboxylic acid from being recrystallized by evaporation of water after a solution has adhered around a cleaning device liquid ejecting nozzle or a cleaning tank and a chamber. In the photoresist residue and polymer residue removing liquid composition containing the aliphatic polycarboxylic acid with a melting point of 25° C. or higher, the removing liquid contains an organic solvent that is miscible with water and has a vapor pressure of 17 mm Hg or less at 25° C. and a hydroxyl group within the structure.2013-09-05
20130231272GLYCOL DILEVULINATES AS COUPLING AGENTS IN CLEANING FORMULATIONS - The present invention provides water-based cleaning formulations comprising one or more organic solvents having low solubility in water and an alkylene glycol dilevulinate for coupling the organic solvent with water.2013-09-05
20130231273SHORTENED TETRANECTIN-APOLIPOPROTEIN A-1 FUSION PROTEIN, A LIPID PARTICLE CONTAINING IT, AND USES THEREOF - Herein is reported a shortened tetranectin-apolipoprotein A-I fusion protein and a lipid particle comprising the shortened tetranectin-apolipoprotein A-I fusion protein as well as uses thereof.2013-09-05
20130231274FUSION PROTEIN HAVING TRANSCRIPTION FACTOR TRANSACTIVATION-REGULATING DOMAIN AND PROTEIN TRANSDUCTION DOMAIN, AND TRANSCRIPTION FACTOR FUNCTION INHIBITOR COMPRISING THE SAME - This invention relates to a fusion protein comprising the TMD of the transcription factor and PTD, an inhibitor for transcription factor function comprising the same, and a method for producing the same. Various diseases associated with malfunctions or defects of the transcription factor are effectively treated using the fusion protein according to the present invention.2013-09-05
20130231275AMINIOTHIAZOLES AND THEIR USES - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases particularly bacterial infections.2013-09-05
20130231276Combination Of An Aminoacyl-tRNA Synthetase Inhibitor With A Further Antibacterial Agent For Attenuating Multiple Drug Resistance - Bacterial multidrug resistance is attenuated in a subject by administering an aminoacyl-tRNA synthetase inhibitor and an antibacterial agent to the subject, wherein the aminoacyl-tRNA synthetase inhibitor is distinct from the antibacterial agent.2013-09-05
20130231277CHIMERIC FGF21 PROTEINS WITH ENHANCED BINDING AFFINITY FOR BETA-KLOTHO FOR THE TREATMENT OF TYPE II DIABETES, OBESITY, AND RELATED METABOLIC DISORDERS - The present invention relates to chimeric proteins that include an N-terminus coupled to a C-terminus, where the N-terminus includes an N-terminal portion of fibroblast growth factor 21 (“FGF21”) and the C-terminus includes a C-terminal portion of fibroblast growth factor 19 (“FGF19”). The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, as well as methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, methods of treating a subject in need of increased FGF21-βKlotho-FGF receptor complex formation, methods of causing increased FGF21 receptor agonist-βKlotho-FGF receptor complex formation, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention.2013-09-05
20130231278Peptides containing tryptophan - The present invention relates to a process to produce a composition comprising water-soluble peptides and having a Trp/LNAA ratio of more than 0.15, which comprises hydrolyzing lysozyme, preferably hen eggs lysozyme, to prepare a hydrolysate having a DH of between 5 and 45.2013-09-05
20130231279OXYTOCIN TREATMENT TO IMPROVE MEMORY AND MODIFY BLOOD GLUCOSE - The disclosure provides a method for enhancing memory of a subject, lowering blood glucose levels in a subject, and treating schizophrenia, the methods comprise intranasally administering to the subject an amount of a oxytocin peptide or analogue thereof having a beneficial effect.2013-09-05
20130231280Novel Peptide Involved in Energy Homeostasis - The expression of a mRNA encoding a putative 76 amino acid, secreted protein (“Enho1”) was found to negatively correlate with fasting triglyceride and cholesterol levels. A recombinant adenovirus was used to increase the expression of Enho1 mRNA in two mouse models of obesity, KK-A2013-09-05
20130231281Rapid acting insulin formulation comprising an oligosaccharide - A composition in aqueous solution, including an insulin and at least one oligosaccharide whose average degree of polymerization is between 3 and 13 and whose polydispersity index PDI is above 1.0, the oligosaccharide having partially substituted carboxyl functional groups, the unsubstituted carboxyl functional groups being salifiable.2013-09-05
20130231282METHODS FOR ADMINISTERING HYPOGLYCEMIC AGENTS - The present invention relates to methods of administering hypoglycemic agents and/or GLP-1 agonists.2013-09-05
20130231283NOVEL NEURTURIN CONJUGATES FOR PHARMACEUTICAL USE - The present invention relates to neurturin protein products conjugated to polyols and to pharmaceutical compositions comprising neurturin conjugates as active ingredients, preferably PEGylated neurturin conjugates or variants thereof, having increased bioavailability.2013-09-05
20130231284METHODS OF TREATING CARTILAGE DEFECTS - The present invention provides methods of repairing and regenerating cartilage tissue by administering into the cartilage or the area surrounding the cartilage a composition comprising a therapeutically effective amount of a morphogenic protein.2013-09-05
20130231285Methods for Treating Skin Aging and Scars - It is to provide a method for treating skin aging, or a method for treating skin scar that can exert a sufficient effect. A composition for treating skin aging comprising bFGF for treating aging of the skin that is administered intradermally or subcutaneously, or a composition for treating skin scar comprising bFGF for treating scar of skin that is administered intradermally or subcutaneously is utilized. Preferred examples of aging of skin include skin wrinkle, pigmented spot, sagging skin, rough skin, skin thinning, decrease of skin viscoelasticity, etc., and preferred examples of scar include keloid, hypertrophic scar, scar contracture, etc.2013-09-05
20130231286Use of Prolactin Receptor Antagonist and Chemotherapeutic Drug for Treating Ovarian Cancer - The present invention relates generally to the field of cancer diagnosis and treatment, and more particularly to compositions and methods that may be useful for eliminating cancer cells with stem-like characteristics. The disclosed compositions and methods may also be useful for managing breast cancer, ovarian cancer, cervical cancer or endometrial (uterine) cancer with metastases; and visualizing the cancer cells in patient's body. The compositions of the instant invention include human prolactin receptor antagonist G129R.2013-09-05
20130231287PEGYLATED ALBUMIN POLYMERS AND USES THEREOF - The present invention provides an albumin polymer and a process of making an albumin polymer, the process comprising breaking instrinsic disulfide bridges in albumin with a reducing agent and crosslinking inter- and intra-molecular disulfide bridges so as to form the polymer. The present invention also provides PEGylated albumin polymers and methods of making PEGylated albumin polymers, the methods comprising polymerizing albumin by crosslinking inter- and intra-molecular disulfide bridges, and PEGylating the albumin polymer. The present invention further provides a pharmaceutical composition useful as a blood plasma expander, blood substitute or for drug delivery, and methods of treating blood loss in a subject and of delivering drugs to a subject's tissue, the pharmaceutical composition comprising a therapeutically effective amount of the PEGylated albumin polymer.2013-09-05
20130231288HUMAN PLACENTAL COLLAGEN COMPOSITIONS, AND METHODS OF MAKING AND USING THE SAME - The present invention provides compositions comprising human placental telopeptide collagen, methods of preparing the compositions, methods of their use and kits comprising the compositions. The compositions, kits and methods are useful, for example, for augmenting or replacing tissue of a mammal.2013-09-05
20130231289SYNTHETIC ANALOGUES OF NEURAL REGENERATION PEPTIDES - Embodiments of this invention include synthetic compounds (NRP analogues) of peptides termed neural regeneration peptides (NRPs). NRP analogues are made by substituting amino acids in the native peptide sequence, modifying amino acids chemically, by replacing amino acids with synthetic moieties, by stabilizaing β-turns, acetylation of terminal glycine residues or by cyclization. NRP analogues can be used to treat a variety of conditions involving degeneration of neural cells, and includes treating disorders of the nervous system, including peripheral neuropathy, multiple sclerosis, diabetic peripheral neuropathy, neurotoxin-induced neurodegeneration, and amyotrophic lateral sclerosis.2013-09-05
20130231290METHODS OF DIAGNOSING AND TREATING NEURODEGENERATIVE DISEASES - The present invention relates to methods of diagnosing, treating and prognosing mental disorders, such as Alzheimer's Disease. In one embodiment, the present invention provides a method of treating Alzheimer's Disease by inhibiting dysfunctional signaling of α7 nAChRs in the medial septum region of an individual.2013-09-05
20130231291FERMENTED SOYA BASED MIXTURE COMPRISING ISOFLAVONES- AGLICONES, EQUOL AND LUNASIL, PROCESS FOR THE PREPARATION AND USES THEREOF IN FOOD, MEDICAL AND COSMETIC FIELDS - The present invention concerns a mixture comprising isoflavones-aglicones, such as daidzein, genistein and glycitein, in addition to equol and lunasin, said mixture being based on soya fermented using lactic acid bacteria isolated from food matrices and use of said mixture for protection of skin and similar and of human intestinal cells with particular reference to prevention of inflammatory state and protection of barrier functions and hair loss treatment.2013-09-05
20130231292Synergistic anti-proliferation activity of TAS-108 with mTOR inhibitors against cancer cells - The invention provides methods and compositions for inhibiting tumor growth in a mammal. The methods comprise administering to the mammal a synergistic combination of (7α)-21-[4-[(Diethylamino)methyl]-2-methoxyphenoxy]-7-methyl-19-norpregna-1,3,5(10)-trien-3-ol 2-hydroxy-1,2,3-propanetricarboxylate and a synergistic chemotherapeutic drug. The combination of the compounds more than additively inhibits growth of tumor cells.2013-09-05
20130231293COMPOSITIONS AND METHODS FOR THE THERAPY AND DIAGNOSIS OF INFLAMMATORY BOWEL DISEASE - Compositions and methods for the therapy and diagnosis of Inflammatory Bowel Disease (IBD), including Crohn's Disease and Ulcerative Colitis, are disclosed. Illustrative compositions comprise one or more bacterial polypeptides, immunogenic portions thereof, polynucleotides that encode such polypeptides, antigen presenting cell that expresses such polypeptides, and T cells that are specific for cells expressing such polypeptides. The disclosed compositions are useful, for example, in the diagnosis, prevention and/or treatment of IBD.2013-09-05
20130231294TDF-RELATED COMPOUNDS AND ANALOGS THEREOF, ANALOGS AND BIOACTIVE FRAGMENTS - The present invention relates generally to tissue differentiation factor (TDF) analogs. More specifically, the invention relates to structure-based methods and compositions useful in designing, identifying, and producing molecules, which act as functional modulators of TDF-like receptors. The invention further relates to methods of detecting, preventing, and treating TDF-associated disorders.2013-09-05
20130231295LIGNIN DERIVATIVES AND USES THEREOF - An article including a lignin derivative, where the lignin derivative includes a moiety derived from an antimicrobial compound. Also provided are methods of inhibiting microbial growth with an article including a lignin derivative.2013-09-05
20130231296NEW DRUG COMBINATIONS FOR THE TREATMENT OF MALARIA - The present invention relates to pharmaceutical preparations/compositions comprising 3-N-formyl hydroxy amino propyl phosphonic acid derivatives or 3-N-acetyl hydroxy amino propyl phosphonic acid derivatives as active ingredients in combination with Piperaquine.2013-09-05
20130231297DIETARY SUPPLEMENT FOR IMPROVING VISUAL PERFORMANCE - An orally administered composition and method for improving visual performance using the composition is provided. The composition comprises a combination of astaxanthin, saffron, lutein, zeaxanthin and European black currant extract in amounts effective to reduce eye fatigue or enhance at least one of visual acuity, contrast acuity, glare relief and recovery, or high intensity blue light filtration.2013-09-05
20130231298ANTI-BACTERIAL ACTIVITY OF 9-HYDROXY DERIVATIVES OF 6,11-BICYCLOLIDES - The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof:2013-09-05
20130231299METHODS FOR REDUCING NEMATODE DAMAGE - A method of reducing damage to plant propagation material and plant organs which grow at a later time by a representative of the class Nematoda, which method comprises (i) treating the propagation material with (A) a chelating agent, and optionally (B) a macrocyclic lactone compound or another pesticide, before the material is sown or planted, or (ii) applying (A) a chelating agent, and optionally (B) a macrocyclic lactone compound or another pesticide, to the locus of the material or the treated material defined in (i) before its planting, and/or at its planting and/or during its growth.2013-09-05
20130231300Purified Crocetin Compound And Method For Treating, Inhibiting, And/Or Prophylaxis of Cancer, Such As Pancreatic Cancer - A fraction separated from crude crocetin by preparative HPLC, and identified using LC/MS and NMR as crocetinic acid, markedly regressed the proliferation and increased apoptosis in pancreatic cancer cells. Purified crocetinic acid showed more potency than 15 commercial or crude crocetin using proliferation and apoptosis as markers. Purified crocetinic acid also showed significant anti-tumorigenic activity against pancreatic cancer cells in a mouse model of pancreatic cancer. Given crocetinic acid's low toxicity, crocetinic acid could be used as a chemotherapeutic or chemopreventative agent for pancreatic cancer.2013-09-05
20130231301COMBINATION OF CHECKPOINT KINASE I INHIBITORS AND WEE I KINASE INHIBITORS - A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.2013-09-05
20130231302ANTIMICROBIAL SOLUTIONS - The present invention provides antimicrobial solutions that in certain cases comprise a biguanide and a glycol ether and, in some cases, optionally also includes combinations of at least one an alcohol, at least one chelator, glycerol, deoxycholate, and/or at least one alkylpolyglucoside. In certain aspects the invention comprises a biguanide and deoxycholate or a combination of chelator, ethanol, and alkylpolyglucoside. Also provided are methods for rapidly killing and/or reducing bacteria, fungi, or virus from surfaces, for example, including surfaces of indwelling medical devices and organic surfaces such as skin and sutures, and inorganic surfaces such as medical equipment, pipelines etc.2013-09-05
201302313035-HALOGENOPYRAZOLE(THIO)CARBOXAMIDES - The present invention relates to novel 5-halogenopyrazole(thio)carboxamides, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.2013-09-05
20130231304BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENT - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.2013-09-05
20130231305Method of Modulating Protein 14-3-3 Functionality By Facilitating or Inhibiting Phosphorylation - The present invention relates to a method of modulating cellular activity. More particularly, the present invention provides a method of modulating apoptosis by modulating protein 14-3-3 phosphorylation and, thereby its functionality. The present invention still further extends to methods for identifying agents capable of modulating protein 14-3-3 phosphorylation. The method and molecules of the present invention are useful, inter alia, in the treatment and/or prophylaxis of conditions characterized by unwanted cellular activity, such as unwanted cell survival.2013-09-05
20130231306AMINO PYRIMIDINE ANTICANCER COMPOUNDS - Compounds of Formula 1, as shown below and defined herein:2013-09-05
20130231307NOVEL ANTIVIRAL ACYCLIC NUCLEOSIDE PHOSPHONATES - Compounds of formula (I) wherein A represents a nucleobase or a derivative thereof, n is equal to 0 or 1 and R′, R″ are carbonic chain, and R2013-09-05
20130231308USE OF AMINOSALICYLATES IN DIARRHOEA-PREDOMINENT IRRITABLE BOWEL SYNDROME - A method for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant irritable bowel syndrome or other non-specific bowel disorder is disclosed comprising administering to a patient in need of such treatment or prophylaxis an effective amount of balsalazide, or a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or a derivative thereof, or a composition comprising balsalazide the modified compound, or a salt or a derivative thereof together with a suitable carrier. Use of balsalazide, a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or derivative thereof, for the manufacture of a medicament for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant Irritable Bowel Syndrome or other non-specific bowel disorder is also disclosed.2013-09-05
20130231309TREATMENT OF INFLAMMATION AND ORGAN DYSFUNCTION - Compositions and methods are disclosed for decreasing the amount and activity of matrix-degrading metalloproteinases (MMPs) in and around cells. The compositions and methods are useful for treating and/or preventing symptoms of diseases including but not limited to Hypertension, Type II Diabetes, and Metabolic Syndrome X. Such treatment is effected by normalizing the blood plasma's protease activity, reducing blood pressure, preventing membrane receptor cleavage, and reducing the levels of insulin resistance and oxygen free radicals in the blood stream.2013-09-05
20130231310MESALAMINE SUPPOSITORY - The present invention relates to a mesalamine rectal suppository designed to provide improved comfort of use. One embodiment of the invention is a mesalamine rectal suppository-comprising mesalamine and one or more pharmaceutically acceptable excipients, wherein the drug load of the suppository ranges from 35% to 50%. Yet another embodiment of the invention is a mesalamine rectal suppository comprising mesalamine having a tap density ranging from about 600 to about 800 g/L (as measured by USP <616>) and a hard fat having an ascending melting point of 32 to 35.5° C. Yet another embodiment is a mesalamine rectal suppository comprising mesalamine particles and one or more pharmaceutically acceptable excipients, where the mesalamine particles have a surface area of from about 0.1 m2013-09-05
20130231311NOVEL FORMULATIONS FOR TREATMENT OF MIGRAINE - Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.2013-09-05
20130231312TREATMENT OF TYPE II DIABETES AND DIABETES-ASSOCIATED DISEASES WITH SAFE CHEMICAL MITOCHONDRIAL UNCOUPLERS - This application discloses methods for treating, preventing and/or alleviating the symptoms of type II diabetes and diabetes-related disorders or complications. The invention provides a novel approach to treating and managing disorders and symptoms related to elevated plasma glucose concentrations and insulin resistance, characterized by few side effects and low toxicity. In particular, the invention provides 2-hydroxy-benzoic anilide compounds and derivatives, and compositions thereof, which can control blood-glucose and increase insulin sensitivity by reducing plasma glucose concentration and cellular energy efficiency.2013-09-05
20130231313SUBSTITUTED PHENYLACETATE AND PHENYLPROPANE AMIDES AND USE THEREOF - The present application relates to novel substituted phenylacetamides and phenylpropanamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.2013-09-05
20130231314METHODS FOR TREATING MULTIPLE MYELOMA WITH 3-(4-AMINO-1-OXO-1,3-DIHYDROISOINDOL-2-YL)PIPERIDINE-2,6-DIONE - Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.2013-09-05
20130231315MODIFIED 4-PHENYL-PYRIDINE DERIVATIVES - Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK2013-09-05
20130231316Drug Combination Comprising a Selective Serotonin Reuptake Inhibitor and a Glucocorticoid Receptor Antagonist for the Treatment of Depression - The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders2013-09-05
20130231317DHEA BIOADHESIVE CONTROLLED RELEASE GEL - The DHEA bioadhesive controlled release gel includes DHEA mixed in a polymeric gel for the purpose of treating atrophic vaginitis, vaginal dryness, dyspareunia, itching, burning, irritation, increase in pH and decreased vaginal flora. The gel adheres to vaginal tissue and protects the DHEA from systemic absorption, which prevents leakage, loss of DHEA, and elevated levels of systemic DHEA. The gel is configured to slowly erode over time so as to deliver a predetermined dose of DHEA to vaginal tissue and thereby promote local intracellular conversion to estrogens, androgens and progesterone so that normal levels of fluid in the vagina is produced. The gel also acts as a moisturizer. An adjustable applicator may also be provided to insure proper placement and dose of the DHEA.2013-09-05
20130231318OCULAR IMPLANT MADE BY A DOUBLE EXTRUSION PROCESS - The invention provides biodegradable implants sized for implantation in an ocular region and methods for treating medical conditions of the eye. The implants are formed from a mixture of hydrophilic end and hydrophobic end PLGA, and deliver active agents into an ocular region without a high burst release.2013-09-05
20130231319Bridged Spiro[2.4]heptane Ester Derivatives - The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.2013-09-05
20130231320SUBSTITUTED AMIDE COMPOUND - A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula:2013-09-05
201302313212-SUBSTITUTED-ETHYNYLTHIAZOLE DERIVATIVES AND USES OF SAME - The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I):2013-09-05
20130231322THERAPEUTIC SUBSTITUTED BETA-LACTAMS - A compound having a structure2013-09-05
20130231323ETHYNYLBENZENE DERIVATIVES - Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R2013-09-05
20130231324SPIRO BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof:2013-09-05
20130231325ALDH-2 INHIBITORS IN THE TREATMENT OF ADDICTION - Disclosed are novel isoflavone derivatives having the structure of Formula I:2013-09-05
20130231326SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.2013-09-05
20130231327Substituted Spiro-Amide Compounds - Substituted spiro-amide compounds corresponding to formula I2013-09-05
20130231328IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same.2013-09-05
20130231329Benzazole Derivatives as Histamine H4 Receptor Ligands - The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.2013-09-05
20130231330IMIDAZOPYRIZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.2013-09-05
20130231331Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.2013-09-05
20130231332SMALL MOLECULE INHIBITORS OF EBOLA AND LASSA FEVER VIRUSES AND METHODS OF USE - The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.2013-09-05
20130231333ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.2013-09-05
20130231334METHODS OF CONTROLLING NEONICOTINOID RESISTANT APHIDS - The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using a trifluoromethylpyri(mi)dine derivative in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects.2013-09-05
20130231335INHIBITORS OF POLO-LIKE KINASE - The present invention provides compounds having a structure according to Formula (I):2013-09-05
20130231336SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS - The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.2013-09-05
20130231337Bicyclic Heteroaryl Compounds - This invention relates to compounds of the general formula:2013-09-05
20130231338BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.2013-09-05
20130231339BENZOFURAN-2-SULFONAMIDES PYRIDINE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.2013-09-05
20130231340PHARMACEUTICAL COMPOUNDS - The invention provides a method of inhibiting a TYK2 kinase, which method comprises bringing into contact with the TYK2 kinase an effective TYK2 kinase-inhibiting amount of a compound having the formula (0):2013-09-05
20130231341N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE - Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.2013-09-05
20130231342ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE - The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).2013-09-05
20130231343COMPOUNDS AND METHODS FOR TREATING MULTIPLE SCLEROSIS - The invention described herein pertains to the treatment of multiple sclerosis. In particular, the invention described herein pertains to the treatment of multiple sclerosis using compounds that modulate the action of acrolein.2013-09-05
20130231344COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.2013-09-05
20130231345Compounds and Method for Treatment of Cancer - The invention relates to a compound of Formula I:2013-09-05
20130231346METHODS OF TREATING CANCER - Methods for treating a human with cancer comprise administering a therapeutically effective amount of at least one MEK inhibitor and at least one mTOR inhibitor to said patient, wherein said patient has at least one mutation in at least one Ras protein or gene encoding at least one Ras protein and/or wherein said patient has at least one mutation, deletion or insertion in LKB1/STK11.2013-09-05
20130231347METHOD OF TREATMENT WITH BRAF INHIBITOR - The disclosure is directed to a method of treating humans suffering from V600 mutant melanoma that incorporates the detection of the presence or absence of at least one mutation in at least one NRAS protein and/or at least one MEK1 protein, or a gene encoding said protein, and subsequently initiating treatment, modifying treatment, or discontinuing treatment with a chemo-therapeutic agent selected from a BRaf inhibitor or other suitable agent based upon the presence or absence of said mutation.2013-09-05
201302313488-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.2013-09-05
20130231349PROTEASE INHIBITORS - Compounds of the formula II:2013-09-05
20130231350SOLID DISPERSION FORMULATIONS AND METHODS OF USE THEREOF - The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.2013-09-05
20130231351SIR2 REGULATION - Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.2013-09-05
20130231352HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls having the general formula (I) and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p1 108 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML), Myelodysplastic syndrome (MDS), myelo-proliferative diseases (MPD), Chronic Myeloid Leukemia (CML), T-cell Acute Lymphoblastic leukaemia (T-ALL), B-cell Acute Lymphoblastic leukaemia (B-ALL), Non Hodgkins Lymphoma (NHL), B-cell lymphoma and solid tumors, such as breast cancer.2013-09-05
20130231353PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI-PROFILERATIVE AGENTS - The present invention concerns the compounds of formula2013-09-05
20130231354SUBSTITUTED AZAINDAZOLE COMPOUNDS - Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.2013-09-05
20130231355QUINAZOLIN-4 (3H)- ONE DERIVATIVES USED AS P13 KINASE INHIBITORS - The present invention relates to the compound of formula (I)2013-09-05
20130231356QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.2013-09-05
20130231357PHARMACEUTICAL COMPOSITIONS CONTAINING PEMETREXED HAVING EXTENDED STORAGE STABILITY - Long term storage stable pemetrexed-containing liquid pharmaceutical compositions are disclosed. The compositions can include pemetrexed or pharmaceutically acceptable salts thereof; an antioxidant selected from lipoic acid, dihydrolipoic acid, methionine and mixtures thereof; a chelating agent selected from lactobionic acid, sodium citrate, tribasic and mixtures thereof; and a pharmaceutically acceptable fluid. The pH of the compositions is in a range of about 8 to about 9.5. The pemetrexed-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 227 nm, after at least about 18 months of storage at a temperature of from about 5° C. to about 25° C. Methods of preparing the formulation as well as methods of treatment of pemetrexed-susceptible diseases using the same are also disclosed.2013-09-05
20130231358PIPERIDINONE CARBOXAMIDE INDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.2013-09-05
20130231359Salt Form of a Multi-Arm Polymer-Drug Conjugate - Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate.2013-09-05
20130231360Beta-Carbolines as Inhibitors of Haspin and DYRK Kinases - The present disclosure is directed to compounds of Formula (I) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.2013-09-05
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