| 36th week of 2014 patent applcation highlights part 37 |
| Patent application number | Title | Published |
|---|
| 20140249119 | Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments - The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis. | 2014-09-04 |
| 20140249120 | NEUROACTIVE 13, 17-SUBSTITUTED STEROIDS AS MODULATORS FOR GABA TYPE-A RECEPTORS - The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds. | 2014-09-04 |
| 20140249121 | METHODS AND KITS FOR DETECTING CARDIAC REMODELING IN SUBJECTS WITHOUT CLINICAL SIGNS OF HEART FAILURE - The present relates to a method for detecting cardiac remodeling in a subject without clinical signs of heart failure comprising determining the level of the NGAL-MMP9 complex in a blood sample obtained from the patient. | 2014-09-04 |
| 20140249122 | ANTI-DIABETIC AMINOSTEROID DERIVATIVES - The present invention relates to novel aminosteroid derivatives substituted in position | 2014-09-04 |
| 20140249123 | EXTENDED RELEASE BIODEGRADABLE OCULAR IMPLANTS - Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer. | 2014-09-04 |
| 20140249124 | PHARMACEUTICAL DELIVERY SYSTEMS FOR HYDROPHOBIC DRUGS AND COMPOSITIONS COMPRISING SAME - A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided. | 2014-09-04 |
| 20140249125 | HIGH ENHANCER-LOADING POLYACRYLATE FORMULATION FOR TRANSDERMAL APPLICATIONS - A polyacrylate formulation suitable for delivery of drug to through a body surface of an individual. By loading the drug and permeation enhancers at a high concentration into a polyacrylate proadhesive that has inadequate adhesive properties for typical adhesive application on the skin, a formulation with desirable adhesive characteristics and effective therapeutic properties can be made. The proadhesive has higher glass transition temperature than typical pressure sensitive adhesives. | 2014-09-04 |
| 20140249126 | ANTIBACTERIAL COMPOUNDS - The present invention relates to cephalosporin antibacterial compounds of Formula (I): | 2014-09-04 |
| 20140249127 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 2014-09-04 |
| 20140249128 | TRIAZINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted triazine carboxamides of Formula I: | 2014-09-04 |
| 20140249129 | Substituted Bicyclic Dihydropyrimidinones And Their Use As Inhibitors Of Neutrophil Elastase Activity - This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 | 2014-09-04 |
| 20140249130 | BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer. | 2014-09-04 |
| 20140249131 | Substituted 7-Oxo-Pyrido[2,3-d]Pyrimidines and Methods of Use - The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer. | 2014-09-04 |
| 20140249132 | USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS - The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: | 2014-09-04 |
| 20140249133 | SUBSTITUTED BENZYLINDAZOLES FOR USE AS BUB1 KINASE INHIBITORS IN THE TREATMENT OF HYPERPROLIFERATIVE DISEASES - Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 2014-09-04 |
| 20140249134 | TRIAZOLYL PDE10 INHIBITORS - The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 2014-09-04 |
| 20140249135 | PIM KINASE INHIBITORS AND METHODS OF THEIR USE - New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer. | 2014-09-04 |
| 20140249136 | Parenteral Formulations of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 2014-09-04 |
| 20140249137 | PYRIMIDINE COMPOUNDS AS TUBERCULOSIS INHIBITORS - The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the inventions and | 2014-09-04 |
| 20140249138 | AZAINDOLES USEFUL AS INHIBITORS OF JAK AND OTHER PROTEIN KINASES - The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2014-09-04 |
| 20140249139 | Quinazoline Derivatives - The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X | 2014-09-04 |
| 20140249140 | Nerve Agent Antidotes - The present invention includes compositions that are useful in treating, ameliorating, or preventing nerve agent poisoning. The present invention also includes methods of preventing, treating or ameliorating nerve agent poisoning in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also includes methods of preventing, treating or ameliorating a seizure induced by a disease or disorder in a subject in need thereof, the method comprising administering to the subject an effective amount of a composition of the invention. The present invention also comprises a kit comprising compositions of the invention. | 2014-09-04 |
| 20140249141 | 1,4-DIAZABICYCLO[3.2.2]NONANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (CNS). | 2014-09-04 |
| 20140249142 | DISCOVERY OF A SOMATIC MUTATION IN MYD88 GENE IN LYMPHOPLASMACYTIC LYMPHOMA - Diagnostic assays for facilitating the diagnosis of lymphoplasmacytic lymphoma (LPL) are provided. The method comprises assessing a biological sample of the subject for the presence of a mutation at position 38182641 in chromosome 3p22.2, wherein presence of the mutation is indicative that the subject has LPL. Also, provided are targeted therapies, methods for monitoring the progression or recurrence of LPL, and a sensitive and inexpensive real-time allele specific polymerase chain reaction assay for reliable and quantitative assessments of the mutation. | 2014-09-04 |
| 20140249143 | Compounds And Methods For Enhancing Innate Immune Responses - Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections. | 2014-09-04 |
| 20140249144 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT - Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R | 2014-09-04 |
| 20140249145 | SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS - Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) | 2014-09-04 |
| 20140249146 | 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS - The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them. | 2014-09-04 |
| 20140249147 | Substituted Bicyclic Aza-Heterocycles and Analogues as Sirtuin Modulators - Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2014-09-04 |
| 20140249148 | SELECTIVE HDAC3 INHIBITORS - Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof. | 2014-09-04 |
| 20140249149 | Compounds with Nematicidal Activity - The present invention relates to the use of known pyridyl carboxamide derivatives and novel pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes. | 2014-09-04 |
| 20140249150 | ACTIVATORS OF PYRUVATE KINASE M2 AND METHODS OF TREATING DISEASE - The invention described herein features methods, compositions, and kits that utilize activators of pyruvate kinase M2 (PKM2) for the treatment or amelioration of disorders related to PKM2 function and characterized by abnormally low levels of serine. | 2014-09-04 |
| 20140249151 | BICYCLIC HETEROCYCLIC COMPOUND - [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11β-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. | 2014-09-04 |
| 20140249152 | TREATMENT FOR GASTROPARESIS USING SEPIAPTERIN - The present invention discloses that diabetic rats showed a reduction in nitrergic relaxation of the gastric, impaired nNOS dimerization, decreased BH4 and GTPCH1 levels and thus, are more susceptible to develop diabetic gastroparesis. The use of tetrahydrobiopterin and its derivatives and sex steroid hormones as disclosed herein provides a novel strategy for therapeutic intervention of diabetic gastroparesis and any other gut-related diseases. Additionally, the present invention also discloses methods to determine risk of developing gastroparesis in an individual that are drawn to detecting variations in the activity and levels of GCH gene and in gene encoding sex steroid hormone receptor. | 2014-09-04 |
| 20140249153 | FIXED DOSE COMBINATION OF BIMATOPROST AND BRIMONIDINE - The present invention is directed to compositions comprising combinations of brimonidine and bimatoprost useful for lowering intraocular pressure in a patient and for the treatment of glaucoma. | 2014-09-04 |
| 20140249154 | SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION - Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus. | 2014-09-04 |
| 20140249155 | SPECTINAMIDES AS ANTI-TUBERCULOSIS AGENTS - Novel 3′-deoxy-3′-acylaminospectinomycin compounds are described. Also described are methods of using the 3′-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections. | 2014-09-04 |
| 20140249156 | Treatment Of Blood Lipid Abnormalities And Other Conditions - There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist. | 2014-09-04 |
| 20140249157 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2014-09-04 |
| 20140249158 | Therapeutic Nanoparticles Comprising a Therapeutic Agent and Methods of Making and Using Same - The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles. | 2014-09-04 |
| 20140249159 | HETEROCYCLIC COMPOUNDS - The invention relates to compounds of Formula I: wherein Ar | 2014-09-04 |
| 20140249160 | TREATMENT OF HEARING AND BALANCE IMPAIRMENTS WITH REDOX-ACTIVE THERAPEUTICS - Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing or balance impairments involving neuronal damage, loss, or degeneration, by administration of a therapeutically effective amount of a redox-active therapeutic. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect in combination with a therapeutically effective amount of a redox-active therapeutic to treat the ototoxicity. | 2014-09-04 |
| 20140249161 | STILBENE ANALOGS AND METHODS OF TREATING CANCER - Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring. | 2014-09-04 |
| 20140249162 | NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME - The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS). | 2014-09-04 |
| 20140249163 | MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS - The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes. | 2014-09-04 |
| 20140249164 | COMPOUNDS - The present invention relates to compounds of formula (I) | 2014-09-04 |
| 20140249165 | PURINE DERIVATIVES FOR TREATMENT OF CYSTIC DISEASES - Provided herein are methods of treatment of a cystic disease by administering a compound of Formula I. In certain embodiments, the compound for use in the methods provided herein is roscovitine or an analog thereof. | 2014-09-04 |
| 20140249166 | METHODS OF TREATING PATIENTS SUFFERING FROM MOVEMENT DISORDERS - The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A | 2014-09-04 |
| 20140249167 | Administration of NEDD8-Activating Enzyme Inhibitor - Disclosed are methods for the treatment of patients with diseases, disorders or conditions responsive to the inhibition of NAE (Nedd8-activating enzyme), e.g., cancer. The methods comprise administering a clinically effective amount of the NAE-inhibitor ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) according to an intermittent dosing regimen in which there is a rest period of at least two days between each administration. | 2014-09-04 |
| 20140249168 | Trifluoromethyl-substituted fused pyrimidines and their use - The present application relates to novel trifluoromethyl-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2014-09-04 |
| 20140249169 | 1-PYRAZOLYL-3- (4- ((2 -ANILINOPYRIMIDIN- 4 - YL) OXY) NAPTHTHALEN- 1- YL) UREAS AS P38 MAP KINASE INHIBITORS - There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD. | 2014-09-04 |
| 20140249170 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYSNTHESIS FOR BACTERIAL INFECTIONS - The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections. | 2014-09-04 |
| 20140249171 | ORAL FORMULATIONS AND LIPOPHILIC SALTS OF METHYLNALTREXONE - The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration. | 2014-09-04 |
| 20140249172 | INTRANASAL NALTREXONE - A stable transmucosal composition consisting essentially of naltrexone hydrochloride in water is provided. The composition is surprisingly stable at room temperature and can be used for simple, rapid and effective opioid overdose rescue. | 2014-09-04 |
| 20140249173 | GLUTAMATE AGENTS IN THE TREATMENT OF MENTAL DISORDERS - Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided. | 2014-09-04 |
| 20140249174 | ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE - The present invention relates to compounds defined by formula I | 2014-09-04 |
| 20140249176 | PROTEIN SYNTHESIS REQUIRED FOR LONG-TERM MEMORY IS INDUCED BY PKC ACTIVATION ON DAYS PRECEDING ASSOCIATIVE LEARNING - The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC. | 2014-09-04 |
| 20140249177 | SALT FORMS OF BICYCLIC HETEROCYCLIC DERIVATIVES - The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2014-09-04 |
| 20140249178 | COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES - Substituted perhydro pyrrolopyridines and methods for their use in the treatment of HIV infections, AIDS, and AIDS-related diseases, and in the treatment of BVDV infections are described herein. Also, pharmaceutical compositions comprising the substituted perhydro pyrrolopyridines are useful for the treatment of HIV infections, AIDS, and AIDS-related diseases. The compositions include one or more carriers, diluents, or excipients, or a combination thereof. | 2014-09-04 |
| 20140249179 | Crystalline Form of (R)-7-Chloro-N-(Quinuclidin-3-YL)benzo[B]thiophene-2-Carboxamide Hydrochloride Monohydrate - Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described. | 2014-09-04 |
| 20140249180 | TAU AGGREGATION INHIBITOR - A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy. | 2014-09-04 |
| 20140249181 | TROPOLONE COMPOUNDS FOR TREATING OR PREVENTING RETROVIRAL INFECTION - Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R | 2014-09-04 |
| 20140249182 | METHOD OF TREATING THERMOREGULATORY DYSFUNCTION WITH PAROXETINE - The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature. | 2014-09-04 |
| 20140249183 | Treatment for Substance Use Disorders and Stress Disorders - Treatments are described for stress disorders and substance use disorders, for example, substance use disorders associated with use of alcohol, cocaine, amphetamines, and the like. | 2014-09-04 |
| 20140249184 | POLYMER-BASED SURGICALLY IMPLATABLE HALOPERIDOL DELIVERY SYSTEMS AND METHODS FOR THEIR PRODUCTION AND USE - Surgically implantable drug delivery systems for long-term delivery of haloperidol containing a biodegradable polymer and haloperidol fabricated into the surgically implantable drug delivery systems via solvent casting and compression molding are provided. Also provided are methods for producing the surgically implantable drug delivery systems and methods for using these systems in the treatment of psychotic disorders such as schizophrenia. | 2014-09-04 |
| 20140249185 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 2014-09-04 |
| 20140249186 | TAXANE COMPOUNDS, COMPOSITIONS AND METHODS - The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation. | 2014-09-04 |
| 20140249187 | COMPOSITION AND METHOD FOR CONTROLLING HARMFUL ARTHROPODS - The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an carboxylic acid represented by a formula (I) wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of pyrazole compounds selected from the group (A) consisting of chlorantraniliprole, cyantraniliprole and a compound represented by a formula (II), shows an excellent controlling efficacy on harmful arthropods. | 2014-09-04 |
| 20140249188 | 5-[5-[2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-2-METHYLPROPANOMETHYLPROPANOYLMET- HYLAMINO]-4-(4-FLUORO-2-METHYLPHENYL)]-2-PYRIDINYL-2-ALKYL-PROLINAMIDE AS NK1 RECEPTOR ANTAGONISTS - The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C | 2014-09-04 |
| 20140249189 | FATTY ACID NIACIN CONJUGATES AND THEIR USES - The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate. | 2014-09-04 |
| 20140249190 | Fast Dissolving Tablet - The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided. | 2014-09-04 |
| 20140249191 | Compositions for Controlling Vascularization in Ophthalmological and Dermatological Diseases - A treatment method for controlling vascularization in a patient's eye or skin includes administering to the patient's eye or skin a pharmaceutical composition having formula (I) or a pharmaceutically acceptable salt, hydrate, enantiomer, diastereomer, racemate or mixtures of stereoisomers thereof. wherein the patient has a disease or disorder associated with vascularization in the eye or skin or wherein said patient is at risk for developing a disease or disorder associated with vascularization of the eye or skin. | 2014-09-04 |
| 20140249192 | COMPOUNDS ACT AT MULTIPLE PROSTAGLANDIN RECEPTORS GIVING A GENERAL ANTI-INFLAMMATORY RESPONSE - The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula | 2014-09-04 |
| 20140249193 | MODULATORS OF MITOCHONDRIAL PROTEIN IMPORT - The present invention provides compounds that modulate protein translocation in mitochondria, compositions thereof, and methods of identifying, making and using these. | 2014-09-04 |
| 20140249194 | OPTICALLY ACTIVE FLUCONAZOLE ANALOGUES CONTAINING THIOPHENES AS ANTIFUNGAL AGENTS - The invention discloses optically active compounds of Formula (1a) or Formula (1b), | 2014-09-04 |
| 20140249195 | 7-AZONIABICYCLO[2.2.1]HEPTANE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF - Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided | 2014-09-04 |
| 20140249196 | N-BENZYLBENZIMIDAZOLE MODULATORS OF PPARG - The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided. | 2014-09-04 |
| 20140249197 | NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 2014-09-04 |
| 20140249198 | MELATONIN AND ITS USE IN PREVENTING POSTOPERATIVE COMPLICATIONS - The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof and a method for the therapeutic and/or prophylactic treatment of postoperative infectious and/or non-infectious complications induced by surgical interventions. | 2014-09-04 |
| 20140249199 | TAK1 KINASE INHIBITORS, COMPOSITIONS, AND USED RELATED THERETO - The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof. | 2014-09-04 |
| 20140249200 | CO-ADMINISTRATION OF ATORVASTATIN AND ETHYL EICOSAPENTAENOIC ACID OR A DERIVATIVE THEREOF - In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on atorvastatin therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. | 2014-09-04 |
| 20140249201 | BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS - Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds. | 2014-09-04 |
| 20140249202 | TARGETED NANOPARTICLES - Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems. | 2014-09-04 |
| 20140249203 | NANOPARTICLES STABILIZED WITH NITROPHENYLBORONIC ACID COMPOSITIONS - Described herein are carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle. Targeted versions of the described nanoparticles are also described, as are related compositions, methods and systems. | 2014-09-04 |
| 20140249204 | IDENTIFICATION OF A JAK2 MUTATION IN POLYCYTHEMIA VERA - The present invention concerns the V617F variant of the protein-tyrosine kinase JAK2, said variant being responsible for Vaquez Polyglobulia. The invention also relates to a first intention diagnostic method for erythrocytosis and thrombocytosis allowing their association with myeloproliferative disorders, or to the detection of the JAK2 V617F variant in myeloproliferative disorders allowing their reclassification in a new nosological group. | 2014-09-04 |
| 20140249205 | ACTIVATION OF QUIESCIENT STEM CELLS - Compositions and methods are provided for altering the activation of quiescent stem cells by modulating activity of the microRNA miR-489. | 2014-09-04 |
| 20140249206 | OLIGONUCLEOTIDES FOR MODULATION OF TARGET RNA ACTIVITY - The present invention relates to oligonucleotides for modulation of target RNA activity. Thus, the invention provides oligonucleotides that bind to microRNA binding sites of target RNA. The oligonucleotides may activate RNase H or RNAi. In a preferred embodiment, the oligonucleotides prevents a microRNA from binding to its binding site of the target RNA and thereby prevent the microRNA from regulating the target RNA. Such oligonucleotides have uses in research and development of new therapeutics. | 2014-09-04 |
| 20140249207 | MEANS FOR INHIBITING THE EXPRESSION OF ORC-1 - The present invention is related to a nucleic acid molecule comprising a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO: 1, whereby the nucleotide core sequence comprises the nucleotide sequence from nucleotide positions 1755 to 1763 of SEQ ID NO: 1; from nucleotide positions 1904 to 1912 of SEQ ID NO: 1; from nucleotide positions 1905 to 1913 of SEQ ID NO: 1; from nucleotide positions 2548 to 2556 of SEQ ID NO: 1; whereby the first stretch is additionally at least partially complementary to a region preceding the 5′ end of the nucleotide core sequence and/or to a region following the 3′ end of the nucleotide core sequence. | 2014-09-04 |
| 20140249208 | MODIFIED POLYNUCLEOTIDES FOR TREATING PROTEIN DEFICIENCY - The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of polynucleotides, primary transcripts and mmRNA molecules. | 2014-09-04 |
| 20140249209 | METHODS FOR THE TREATMENT AND PREVENTION OF LIVER DISEASE - The presently disclosed invention is directed to the discovery that hepatocyte nuclear factor 4 alpha (HNF4α; also known as NR2A1), a transcription factor, reverses hepatocyte dysfunction in an animal model of cirrhosis, resulting in improvement in hepatic function, treatment of cirrhosis, and prolonged survival. | 2014-09-04 |
| 20140249210 | MODULATION OF PRE-MRNA USING SPLICE MODULATING OLIGONUCLEOTIDES AS THERAPEUTIC AGENTS IN THE TREATMENT OF DISEASE - The present invention encompasses a class of compounds known as splice modulating oligonucleotides (SMOs) that modulate pre-mRNA splicing, thereby affecting expression and functionality of a specific protein in a cell. The present invention further provides compositions and methods for modulating pre-mRNA splicing using a SMO of the invention to abrogate disease-causing mutations in a protein. Accordingly, the present invention provides compositions and methods of treating a subject at risk of, susceptible to, or having a disease, disorder, or condition associated with aberrant or unwanted target pre-mRNA expression or activity. | 2014-09-04 |
| 20140249211 | Systemic Gene Replacement Therapy for Treatment of X-Linked MyoTubular Myopathy (XLMTM) - The present invention provides compositions and methods for treating a myopathy. In certain embodiments, the invention provides compositions and methods for treating, improving muscle function, and prolonging survival in a subject with X-linked myotubular myopathy (XLMTM). The present invention provides a method comprising systemic administration of a composition that induces the increased expression of myotubularin in the muscle of a subject. The invention provides sustained regional and global increases in muscle function. | 2014-09-04 |
| 20140249212 | Compositions and Methods for Transient Expression of Recombinant RNA - Compositions for transient but prolonged exogenous mRNA expression through the use of the transcription system of negative strand RNA viruses, and methods of use thereof are disclosed. In some embodiments, the system contains only RNAs and does not include any DNA molecules. The compositions typically include an RNA template unit (rTeUn) that includes a virus regulatory sequences operably linked to a coding sequence of interest. The rTeUn is typically transfected to a host cell's cytoplasm in the presence of virus expression system proteins that mediate replication of the rTeUn and transcription of the transgene. The rTeUn RNA bonded to viral proteins exhibits high resistance to degradation, prolonged duration of expression, and is free of viral genes. The compositions can be used to reprogram cell. For example, the compositions and methods can be used to redirected lymphocytes to target cancer cells, or to dedifferentiate somatic cells into induce pluripotent stem cells. | 2014-09-04 |
| 20140249213 | Acid-Labile Lipophilic Prodrugs of Cancer Chemotherapeutic Agents - The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof. | 2014-09-04 |
| 20140249214 | CO-ADMINISTRATION OF WARFARIN AND ETHYL EICOSAPENTAENOATE - In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on warfarin therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. | 2014-09-04 |
| 20140249215 | NEW SALT OF ABEXINOSTAT, ASSOCIATED CRYSTALLINE FORM, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Abexinostat tosylate of formula (II): | 2014-09-04 |
| 20140249216 | METHODS OF TREATMENT USING MODULATORS OF SIRT2 - The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method. | 2014-09-04 |
| 20140249217 | ENHANCER OF SURVIVAL OF TRANSPLANTED ORGAN - The present invention provides an agent for promoting graft survival which can suppress rejection without use of existing immunosuppressants, an organ preservation solution capable of maintaining the freshness of an organ excised from a donor, and the like. An agent for promoting graft survival or an organ preservation solution is prepared, which comprises 5-aminolevulinic acid (ALA) or a derivative thereof, or a salt of ALA or the derivative and an iron compound as active ingredients. Preferable examples of the ALAs can include ALA and various esters such as methyl ester, ethyl ester, propyl ester, butyl ester, and pentyl ester of ALA, and their hydrochlorides, phosphates, and sulfates. Preferable examples of the iron compound can include sodium ferrous citrate. | 2014-09-04 |
| 20140249218 | ADMINISTRATION OF INGENOL MEBUTATE - The present invention relates to novel crystalline forms of ingenol ingenol-3-angelate and methods of preparation and use thereof. More specifically, the invention relates to a novel crystalline form and purified forms of the compound of Formula 1 (ingenol-3-mebutate; ingenol-3-angelate; isoform ‘b’; PEP005), which is characterized by, for example, attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy, single crystal X-Ray crystallography (XRC), X-ray powder diffraction, and, Differential Scanning Calorimetry (DSC), and methods of preparation and use thereof. | 2014-09-04 |
| 20140249219 | Anti-obesity potential of Calebin A - The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-α), Interleukin-6 (IL-6) and Interleukin-1 (IL-1β). | 2014-09-04 |
