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06th week of 2015 patent applcation highlights part 51
Patent application numberTitlePublished
20150038492BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.2015-02-05
20150038493COMPOUNDS THAT TRAP ALPHA-OXOALDEHYDES AND ALPHA-BETA-UNSATURATED ALDEHYDES, META-COMPOUNDS CONTAINING SUCH COMPOUNDS, AND USE OF SAID COMPOUNDS IN TREATING ILLNESSES RELATED TO THE ACCUMULATION OF AGES AND ALES - The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.2015-02-05
20150038494Thiazolopyrimidine Modulators as Immunosuppressive Agents - The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R2015-02-05
20150038495THERAPEUTIC AGENT FOR PAIN - To provide a cancer pain therapeutic and/or prophylactic agent which can be administered to a patient for a long period of time from the early stage to the final stage of the cancer pain therapy, instead of conventional non-opioid analgesic agents or opioid analgesic agents.2015-02-05
20150038496METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF TH2 MEDIATED DISEASES - The present invention relates to methods and pharmaceutical composition for the treatment of T-helper type 2 (Th2)-mediated diseases. More particularly, the present invention relates to an inhibitor of the Suv39h1-HP1a silencing pathway for use in the treatment of a T-helper type 2 (Th2)-mediated disease, in particular allergic asthma.2015-02-05
20150038497BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I:2015-02-05
20150038498THROMBIN INHIBITORS - Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2015-02-05
20150038499METHODS OF ADMINISTERING MONOMETHYL FUMARATE AND PRODRUGS THEREOF HAVING REDUCED SIDE EFFECTS - Methods of improving patient safety and reducing undesirable side effects for patients considering therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed. In particular, a method of treating a disease in a patient in need of such treatment is provided. The method comprises testing the patient for a propensity for a deficiency in tissue glutathione S-transferase theta 1 enzyme (GSTT1) levels. Thereafter, a therapeutically effective amount of a compound selected from monomethyl fumarate (MMF), a prodrug of monomethyl fumarate, and combinations thereof is administered to the patient. During the treatment of the disease, blood lymphocyte concentration is periodically tested in the patient at a predetermined time interval length that is based on the enzyme level propensity testing result.2015-02-05
20150038500PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING OPHTHALMIC DISORDERS - The invention relates to a pharmaceutical composition for preventing or treating an ophthalmologic disease comprising a compound of formula (1) as defined in the specification, or a pharmaceutically acceptable salt or isomer thereof as an active ingredient. Also, the invention relates to a composition for cleansing or preserving a contact lens comprising the above active ingredient.2015-02-05
20150038501INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.2015-02-05
20150038502ISOXAZOLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.2015-02-05
20150038503DERIVATIVES OF 6-SUBSTITUTED TRIAZOLOPYRIDAZINES AS REV-ERB AGONISTS - The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.2015-02-05
20150038504FORMULATION OF SYK INHIBITORS - Disclosed are pharmaceutical compositions comprising a compound having the formula:2015-02-05
20150038505POLYMORPH OF SYK INHIBITORS - Polymorphs of a bis-mesylate salt of a compound of Formula I:2015-02-05
20150038506BICYCLIC HETEROARYL DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF - The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.2015-02-05
20150038507Antiprotozoal Compounds - The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.2015-02-05
20150038508TREATMENT OF LUPUS NEPHRITIS USING LAQUINIMOD - This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.2015-02-05
20150038509Chemokine Receptor Binding Heterocyclic Compounds With Enhanced Efficacy - The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).2015-02-05
20150038510CINNOLINE DERIVATIVES - Disclosed are compounds of Formula 1,2015-02-05
20150038511TREATMENT OF IMMUNE-RELATED AND INFLAMMATORY DISEASES - Provided herein are methods of using compounds and compositions for modulating leukocytic activity, including activity of B cells and/or T cells monocytes, macrophages, and other lymphoid or myeloid-derived cell types, in immune-related diseases or inflammatory diseases. Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.2015-02-05
20150038512COMPOSITIONS AND METHODS COMPRISING A BIOCIDAL POLYAMINE - Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, or reduce biofilms, or to inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.2015-02-05
20150038513ASSOCIATION BETWEEN N-HYDROXY-4-BENZAMIDE AND FOLFOX - Association between N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-yl-carbonylamino]ethoxy}benzamide of formula (I):2015-02-05
20150038514SODIUM AND CALCIUM SALTS OF DIHYDROQUINAZOLINE DERIVATIVE AND USE THEREOF AS ANTIVIRAL AGENTS - The invention relates to sodium and calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treatment and/or prophylaxis of virus infections and to the use thereof for producing drugs for use in methods of treatment and/or prophylaxis of diseases, more particularly the use thereof as antiviral agents, more particularly against cytomegaloviruses.2015-02-05
20150038515INHIBITORS OF HEPATITIS B VIRUS CONVALENTLY CLOSED CIRCULAR DNA FORMATION AND THEIR METHOD OF USE - Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.2015-02-05
20150038516Inhibitors of Protein Kinases - Compounds of general Formula I:2015-02-05
20150038517Indole Derivative Modulators of the alpha 7 nAChR - This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof:2015-02-05
20150038518METHODS FOR THE TREATMENT OF SOLID TUMORS - Described herein are combinations of ACK inhibitors and HDAC inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.2015-02-05
20150038519ORGANIC COMPOUNDS - The invention provides a new method of treating diseases or conditions characterized by reduced dopamine D1 receptor signaling activity, such as Parkinson's disease, depression, and cognitive impairment of schizophrenia, comprising administering an effective amount of a 1,3,5,-substituted, 6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one to a patient in need thereof.2015-02-05
20150038520Molecular Biomarkers for Predicting Response to Tyrosine Kinase Inhibitors in Lung Cancer - The invention relates to methods for determining the clinical outcome of patients suffering lung cancer and being under treatment with an EGFR inhibitor. The methods are based on the detection of the presence of mutations in the EGFR gene conferring resistance to inhibitors of the EGFR tyrosine kinase activity, wherein the appearance of said mutations in the biofluid of the patient is indicative of a high probability that the patient suffers a relapse of the disease. The invention also provides therapeutic methods for said patients.2015-02-05
20150038521TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS - The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I)2015-02-05
20150038522COMBINED ANTICANCER DRUG SENSITIVITY-DETERMINING MARKER - To provide an anti-cancer agent sensitivity determination marker, which marker can determine whether or not the patient has a therapeutic response to the anti-cancer agent, and novel cancer therapeutic means employing the marker.2015-02-05
20150038523INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3 - The invention relates to compounds of formula (I): wherein R2015-02-05
20150038524CRYSTALLINE NALOXOL-PEG CONJUGATE - Naloxol-polyethylene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.2015-02-05
20150038525NOVEL METHYSERGIDE DERIVATIVES - Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders or symptoms thereof, such as, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are methods for antagonizing the 5-HT2015-02-05
20150038526FLUORINE-CONTAINING 5-[2-(PYRID-3-YL)-ETHYL]-2,3,4-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES AS AGENTS FOR REDUCING UNCONTROLLED PROTEIN AGGREGATION - The claimed fluorine-containing substituted 5-[2-(pyrid-3-yl)-ethyl]-2,3,4-tetrahydro-1H-pyrido[4,3-b]indoles and hydrochlorides and hydrobromides thereof, which have the general formula (I), as agents for reducing uncontrolled protein aggregation in the nervous system, the pharmacological agent based thereon and the method for using same relate to the field of medicine and solve the problem of increasing the range of agents for combating the development of destructive processes in the central and peripheral nervous system.2015-02-05
20150038527FUROPYRIDINE DERIVATIVES - Compounds of the formula I2015-02-05
201500385284 -HYDROXY- ISOQUINOLINE COMPOUNDS AS HIF HYDROXYLASE INHIBITORS - The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.2015-02-05
20150038529CRYSTALLINE FORMS OF A PROLYL HYDROXYLASE INHIBITOR - The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.2015-02-05
20150038530COMPOSITIONS AND METHODS FOR THE PREVENTION AND TREATMENT OF MAST CELL-INDUCED VASCULAR LEAKAGE - Disclosed herein are methods of diagnosing and treating infectious disease characterized by a pathology that involves hemorrhaging or pathological vascular leakage.2015-02-05
20150038531USE OF A NOVEL AMINOPYRIDINE DERIVATIVE TO PREVENT OR TREAT CANCER - An aminopyridine derivative of Formula 1 and a method of preventing or treating cancer using the same. Formula 1:2015-02-05
20150038532Pharmaceutical Composition Of A Potent HCV Inhibitor For Oral Administration - A pharmaceutical composition of the following Compound (1), a potent hepatitis C viral (HCV) inhibitor, or a pharmaceutically acceptable salt thereof, for oral administration.2015-02-05
20150038533PHACETOPERANE FOR THE TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER - The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.2015-02-05
20150038534COMPOUNDS AND METHODS - Disclosed are compounds having the formula:2015-02-05
20150038535Thiophene-carboxamides useful as inhibitors of protein kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.2015-02-05
20150038536TYROSINE KINASE INHIBITORS - The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.2015-02-05
20150038537Agents For The Control Of Parasites On Animals - The invention relates to agents for the control of parasites on animals, comprising an active substance from the group of the phenylpyrazoles and vitamin E or a derivative thereof, such as particularly vitamin E acetate, as well as optionally a further active substance from the group of the pyrethroids and/or optionally additionally further active and/or auxiliary substances. In particular, the invention relates to the use of such agents for the control of ectoparasites such as, in particular, fleas, ticks and sand flies in pets such as, in particular, in dogs, cats and ferrets.2015-02-05
20150038538THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS - The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly neurodegenerative diseases, inflammatory and autoimmune diseases and cardiovascular disorders. Additionally, there is provided a process for preparing such compounds, as well as pharmaceutical compositions comprising them.2015-02-05
20150038539METHOD OF INCREASING THE EXTENT OF ABSORPTION OF TIZANIDINE - An article and method for increasing the extent of tizanidine absorption in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release tablet composition at or around the time food is consumed. The composition may be packaged in a container for distribution.2015-02-05
20150038540INSTANTLY WETTABLE ORAL FILM DOSAGE FORM WITHOUT SURFACTANT OR POLYALCOHOL - An instantly wettable and rapidly disintegrating oral film dosage form without a surfactant and without a polyalcohol was achieved by combining at least one water soluble polymer that is not a copolymer of vinylpyrrolidone, at least one active agent, a copolymer of vinylpyrrolidone and titanium dioxide. In certain embodiments, the film comprises hydroxypropyl cellulose or a combination of hydroxypropyl cellulose and a polymer or copolymer of vinylpyrrolidone or a substituted vinylpyrrolidone as the water soluble polymer(s). A plasticizer, and optional additives selected from synthetic sweeteners, natural sweeteners, flavorants, antioxidants, colorants, and opacifiers, can be added to the disclosed film oral dosage forms.2015-02-05
20150038541COMPOSITION AND METHODS FOR CELL MODULATION - Composition and methods for affecting cell proliferation, metabolism or sensitization, including the potentiation of proteasome inhibitor therapy for the treatment of disease caused by deregulation of ubiquitin-proteasome systems, in a cell or subject. The composition includes a compound in combination with a ubiquitin-proteasome inhibitor. In one embodiment, the compound has the formula C42H35N5O3 and the ubiquitin-protease inhibitor is a proteasome inhibitor or an inhibitor of another component of the ubiquitin-proteasome pathway such as an E3 ubiquitin ligase. In one embodiment of the method, the compound is administered to a cell or subject and a therapeutically effective amount of a ubiquitin-protease inhibitor is also administered. In another embodiment, the compound is administered to a cell or subject to inhibit cell proliferation. In yet another embodiment, the compound is administered to a cell or subject to increase, or augment, glucose utilization.2015-02-05
20150038542USES OF SELECTIVE INHIBITORS OF HDAC8 AND TREATMENT OF INFLAMMATORY CONDITIONS - Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.2015-02-05
20150038543ANTI-GLYCATION PROPERTIES OF OXINDOLE DERIVATIVES - This invention provides a series of new oxindole derivatives 1-21, evaluated for their antiglycation potential by using in vitro BSA-MG glycation model. These derivatives showed a varying degree of antiglycation activity with IC2015-02-05
20150038544ANIMAL FEED COMPOSITION - Disclosed is an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. Also disclosed is a method for enhancing animal growth by feeding the animal with a composition according to the invention. Further disclosed is the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow-growing animals. Disclosed is the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular, immunocompromised or slow-growing animals. A composition may be in the form of a food or feed supplement.2015-02-05
20150038545HYDROXYPHENYL PYRROLE COMPOUNDS CONTAINING AN HYDROXAMIC ACID AS HDAC INHIBITORS AND MEDICINAL APPLICATIONS THEREOF - The present invention refers to compounds derived from hydroxyphenyl 1H-pyrrole rings, which have the following formula (I):2015-02-05
20150038546SUBSTITUTED CHROMAN COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS - The present invention provides calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention.2015-02-05
20150038547Biological Basis of Adult Wellness - This disclosure is of a lowered absorption of nutrients within the adult digestive tract, more specifically, a decreased mechanical absorption of certain specific amino acids over time; said decreased nutritional uptake decreasing wellness of the individual by the mechanism of depletion of bodily reserves; said lowered uptake being mitigated by a patently unique method to intercede in the nutrient absorption process.2015-02-05
20150038548OLIGONUCLEOTIDE INHIBITORS OF DNA METHYLTRANSFERASES AND THEIR USE IN TREATING DISEASES - Modified oligonucleotides comprising CpG sites, wherein the cytosine is replaced by cytosine analogs are provided as well as methods of making the oligonucleotides and their use in treating cancer, tumorigenesis and hyper-proliferative disorders.2015-02-05
20150038549Methods and Compositions for Modulating Gene Expression Using Components That Self Assemble in Cells and Produce RNAi Activity - Compositions and methods for downmodulating expression of target nucleic acids are disclosed.2015-02-05
20150038550Targeting MicroRNAs for Metabolic Disorders - Provided herein are methods and compositions for the treatment of metabolic disorders. Also provided herein are methods and compositions for the reduction of blood glucose level, the reduction of gluceoneogenesis, the improvement of insulin resistance and the reduction of plasma cholesterol level. In certain embodiments, the methods comprise inhibiting the activity of miR-103. In certain embodiments, the methods comprise inhibiting the activity of miR-107. In certain embodiments, the activity of both miR-103 and miR-107 is inhibited. In certain embodiments, such methods comprise administering a compound comprising an oligonucleotide targeted to a microRNA.2015-02-05
20150038551Pharmaceutical Composition for Preventing or Treating Diabetes Containing TENC1 Expression or Activity Suppressor - The present invention relates to a pharmaceutical composition for preventing or treating diabetes or a complication of diabetes, which includes a TENC1 (tensin like C1 domain-containing phosphatase) expression or activity suppressor, and, more specifically, relates to a pharmaceutical composition for preventing or treating diabetes or a complication of diabetes, which either suppresses the degradation of IRS-1 (insulin receptor substrate-1) or suppresses the phosphorylation of IRS-1 due to the PTPase activity of TENC1. The pharmaceutical composition according to the present invention, which is for preventing or treating diabetes or a complication of diabetes and comprises the TENC1 expression or activity suppressor as an active ingredient, can be expected to be widely usable in preventing and treating diabetes or a complication of diabetes since the pharmaceutical composition can effectively prevent the muscular dystrophy and reduction in sugar adsorption that occur due to reduction in IRS-1 by suppressing degradation of IRS-1 caused by TENC1.2015-02-05
20150038552ESOPHAGEAL MICRORNA EXPRESSION PROFILES IN EOSINOPHILIC ESOPHAGITIS - Methods and compositions disclosed herein generally relate to methods of treating eosinophilic esophagitis (EE) and eosinophilic disorders by providing or enhancing a diagnosis of EE and eosinophilic disorders. In particular, the invention relates to obtaining a sample from a patient, then quantifying from the sample an amount of one or more microRNAs (miRNAs) associated with EE, wherein an altered level of the miRNA correlates with a positive diagnosis of EE. An EE diagnosis can then be provided or enhanced, based upon the quantifying step, and an appropriate treatment can be administered to the patient. The invention further relates to diagnostic kits, tests, and/or arrays that can be used to quantify the one or more miRNAs associated with EE, as well as treatments developed to up-regulate or down-regulate one or more miRNAs and/or their downstream pathways relevant to EE or asthma. The invention further relates to the use of IGF1 and IGF1R inhibitors for the treatment of EE and eosinophilic disorders.2015-02-05
20150038553TREATMENT OF ATONAL HOMOLOG 1 (ATOH1) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO ATOH1 - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Atonal homolog 1 (ATOH1), in particular, by targeting natural antisense polynucleotides of Atonal homolog 1 (ATOH1). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of ATOH1.2015-02-05
20150038554Extended Dicer Substrate Agents and Methods for the Specific Inhibition of Gene Expression - The invention provides compositions and methods for reducing expression of a target gene in a cell, involving contacting a cell with an isolated double stranded nucleic acid (dsNA) in an amount effective to reduce expression of a target gene in a cell. The dsNAs of the invention possess a single stranded extension (in most embodiments, the single stranded extension comprises at least one modified nucleotide and/or phosphate back bone modification). Such single stranded extended Dicer-substrate siRNAs (DsiRNAs) were demonstrated to be effective RNA inhibitory agents compared to corresponding double stranded DsiRNAs.2015-02-05
20150038555Extended Dicer Substrate Agents and Methods for the Specific Inhibition of Gene Expression - The invention provides compositions and methods for reducing expression of a target gene in a cell, involving contacting a cell with an isolated double stranded nucleic acid (dsNA) in an amount effective to reduce expression of a target gene in a cell. The dsNAs of the invention possess a single stranded extension (in most embodiments, the single stranded extension comprises at least one modified nucleotide and/or phosphate back bone modification). Such single stranded extended Dicer-substrate siRNAs (DsiRNAs) were demonstrated to be effective RNA inhibitory agents compared to corresponding double stranded DsiRNAs.2015-02-05
20150038556CFTR MRNA COMPOSITIONS AND RELATED METHODS AND USES - Materials, formulations, production methods, and methods for delivery of CFTR mRNA for induction of CFTR expression, including in the mammalian lung are provided. The present invention is particularly useful for treating cystic fibrosis.2015-02-05
20150038557METHODS AND COMPOSITIONS FOR TREATMENT OF RETINAL DEGENERATIVE DISEASES - The present invention relates to an isolated nucleic acid molecule comprising i) a nucleotide sequence coding for a hyperpolarizing light-gated ion channel or pump gene from an archeon or for a light-active fragment of said gene, or the nucleotide sequence and ii) a nucleotide sequence coding for a neurotrophic factor for use in the treatment of a retinal degenerative disease.2015-02-05
20150038558RNA Containing Modified Nucleosides and Methods of Use Thereof - This invention provides RNA, oligoribonucleotide, and polyribonucleotide molecules comprising pseudouridine or a modified nucleoside, gene therapy vectors comprising same, methods of synthesizing same, and methods for gene replacement, gene therapy, gene transcription silencing, and the delivery of therapeutic proteins to tissue in vivo, comprising the molecules. The present invention also provides methods of reducing the immunogenicity of RNA, oligoribonucleotide, and polyribonucleotide molecules.2015-02-05
20150038559Pharmaceutical Composition and Method for the Treatment of Neurodegenerative Diseases, in Particular Amyotrophic Lateral Sclerosis - A pharmaceutical composition and method for therapy of neurodegenerative diseases including amyotrophic lateral sclerosis, the composition comprising an adenoviral vector, expressing a human angiogenesis factor gene; an effective amount of the adenoviral vector in the form of a non-replicating nanoparticle based on a genome of human adenovirus type 5 with an insertion of a human angiogenin gene which produces the human angiogenesis in a human body; a non-replicating nanoparticle based on the genome of human adenovirus type 5 with an insertion of a human vascular endothelium growth factor gene; and a formulating buffer; wherein the human angiogenin factor gene and the human vascular endothelium growth factor gene are cloned in two expression cassettes within one non-replicating nanoparticle based on the genome of human adenovirus type 5.2015-02-05
20150038560METHODS AND COMPOSITIONS FOR TREATING NEUROPATHIES - Methods of treating or preventing axonal degradation in neuropathic diseases in mammals are disclosed. The methods can comprise administering to the mammal an effective amount of an agent that acts by increasing sirtuin activity in diseased and/or injured neurons. The methods can also comprise administering to the mammal an effective amount of an agent that acts by increasing NAD activity in diseased and/or injured neurons. Also disclosed are methods of screening agents for treating a neuropathies and recombinant vectors for treating or preventing neuropathies.2015-02-05
20150038561MITOCHONDRIAL TARGETED RNA EXPRESSION SYSTEM AND USE THEREOF - Described herein is a mitochondrial-targeted RNA expression system (mtTRES) for delivery of RNA molecules to mitochondria. mtTRES vectors generate RNAs in vivo that are un-capped, non-polyadenylated, and actively directed to mitochondria. The disclosed vectors are capable of delivering either non-coding RNA molecules or RNA molecules encoding a protein of interest to the mitochondria. In particular, the disclosed vectors include (1) an RNAPIII initiation (promoter) sequence, (2) a non-coding leader sequence (NCL), (3) a mitochondrial translation initiation sequence and an ORF encoding a protein of interest, or a sequence encoding a non-coding RNA, and (4) an RNAPIII termination sequence.2015-02-05
20150038562Modified L-nucleic Acid - A modified L-nucleic acid, containing an L-nucleic acid part conjugated to a non-L-nucleic acid part is described. The conjugate has extended retention time in and demonstrates a delayed elimination from an organism.2015-02-05
20150038563STABLE COMPOSITION COMPRISING AN ANTI-AGEING COMPOUND AND A SOLVENT - A cosmetic composition including diacetylresveratryl thioctate and a solvent. The solvent has a 2015-02-05
20150038564SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF - The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms.2015-02-05
20150038565LONG ACTING COMPOSITIONS - The present invention relates to a long-acting composition for the treatment of an animal in need thereof wherein the composition includes a therapeutically effective amount of a bioactive agent, characterised in that the composition includes a non-aqueous carrier and a solvent system comprising castor oil and at least one cyclic amide.2015-02-05
20150038566REGULATION OF CHOLESTEROL HOMEOSTASIS - The invention provides novel compounds of Formulas (I)-(IV), as described herein. Also provided are compositions of these compounds, method of making the compounds, and methods of using the compounds. The compounds can be used to regulate cholesterol homeostasis and to treat conditions and diseases associated with cholesterol homeostasis, including lysosomal lipid storage disorders such as Niemann-Pick Disease type C.2015-02-05
20150038567Cannabinoid Carboxylic Acids, Salts of Cannabinoid Carboxylic Acids, and the Production and Uses of Same - The invention relates to a compound selected from the group consisting of all stereoisomers and their mixtures of the compounds of general formulas (1)-(4), in which R2015-02-05
20150038568USE OF TOTAL COUMARINS OF CNIDIUM FRUIT IN PREPARING MEDICAMENTS FOR TREATING PSORIASIS - A pharmaceutic composition for treating an allergic skin disorder. It has an active component and a carrier. The active component has a major active ingredient osthol and a group of minor active ingredients: xanthotoxol, xanthotoxin, isopimpinellin, bergapten, and imperatorine. The major active ingredient osthol accounts for at least 90% by weight of the active component, which accounts for 5-35% by weight of the overall pharmaceutic composition.2015-02-05
20150038569Anti-cervical Cancer Compound and Method of Use Thereof - Cervical cancer is one of the most common malignancies and is associated with a dismal prognosis. The most common therapeutic option for cervical cancer consists of surgery in early stages, and chemotherapy or radiotherapy in more advanced stages of the disease. Although treatment options have increased for some patients, overall progress has been modest. This invention relates to a method for treating cancer comprising administering an anti-cancer compound. More particularly, the present invention relates to an anti-cervical-cancer compound for treating human cervical cancer and tumor.2015-02-05
20150038570COMPOSITIONS AND PRODUCTS CONTAINING S-EQUOL, AND METHODS FOR THEIR MAKING - A composition for use in making commercial food and skin products comprising 5-equol or mixtures, including both a non-racemic mixture and a racemic mixture, of S-equol and R-equol. The composition can be used to make articles of commerce such as food supplements, pharmaceuticals, and medicaments. The compositions are useful in a method of delivering S-equol to a mammal to prevent or treat a disease or associated condition, including hormone-dependent diseases or conditions such as cardiovascular disease, lipid disorder, osteopenia, osteoporosis, liver disease, and acute ovarian estrogen deficiency. The S-equol enantiomer can be produced in a biological synthesis from the metabolism of an isoflavone by an organism.2015-02-05
20150038571Antiviral Composition against Flavivirus - The present invention relates to a composition having antiviral activity for prophylaxis or treatment of flavivirus infection or a disease resulting therefrom in humans or animals, characterised in that said composition consisting of baicalein, or analogues, or derivatives thereof. The composition may further comprise a pharmaceutically acceptable carrier. The antiviral activity may include inhibition of virus attachment to host cells, inhibition of intracellular virus replication and direct virucidal activity. The flavivirus may comprise dengue virus type-1, dengue virus type-2, dengue virus type-3, dengue virus type-4 and Japanese encephalitis virus.2015-02-05
20150038573ANTI-OBESITY AGENT COMPRISING COMPOUND CONTAINING BENZOTROPOLONE RING - The object of the present invention is to provide an anti-obesity agent which contains a tea-derived component and which is safe and does not compromise the flavor of foods and beverages.2015-02-05
20150038574Opsin-Binding Ligands, Compositions and Methods of Use - Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.2015-02-05
20150038575MELANOGENESIS-INHIBITORY CONSTITUENTS OF Ligusticum sinense - Melanogenesis-inhibitory constituents of 2015-02-05
20150038576COMPOSITIONS AND THEIR USE FOR SMOKING CESSATION AND OTHER TREATMENTS - A composition includes a liquid. The liquid aerosolizes for delivery to a user by an airway. The liquid includes an agent that activates a TRPV3 channel. The agent includes a terpenoid compound.2015-02-05
20150038577N-ACETYL L-CYSTEINE CHELATES AND METHODS FOR MAKING AND USING THE SAME - A nutritional supplement for a human, the supplement having a chelate comprised of an N-acetyl-L-cysteine ligand bonded to a metal to form a chelate ring. A method for preparing a chelate comprised of N-acetyl-L-cysteine ligand and a metal having the steps of: dissolving an amount of N-acetyl-L-cysteine in an aqueous solution, adding a metal to the aqueous solution, stifling and heating the aqueous solution, and removing the solvent under reduced pressure. A method of treating a human for one or more of oxidative stress, cardiovascular disease, cerebrovascular disease, neurodegenerative diseases, Alzheimer's disease, ADHD, bipolar, schizophrenia, autism, dementia, and HIV in a human comprising administering an effective amount of a composition having N-acetyl-L-cysteine in a chelate formation with a metal. A compound having a chelate formulation with a metal being chelated by an N-acetyl-L-cysteine ligand.2015-02-05
20150038578METHODS AND APPARATUSES FOR SURFACE FUNCTIONALIZATION AND COATING OF NANOCRYSTALS - The present disclosure describes a method and series of compositions for surface functionalization of nanoparticles that eliminates the possibility of ligand loss in alien environments. In particular, the present disclosure provides method and compositions for production of highly-stable surface-functionalized nanorods of noble metals for in-vivo applications as well as use in composite materials.2015-02-05
20150038579Method for Treating Eczema - A method for treating eczema including the steps of applying an isothiocyanate functional surfactant to an area affected by eczema, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.2015-02-05
20150038580Method for Treating Skin Cancer - A method for treating skin cancer including the steps of applying an isothiocyanate functional surfactant to an area affected by skin cancer, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.2015-02-05
20150038581HISTONE DEACETYLASE INHIBITORS - In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.2015-02-05
20150038582THERAPEUTIC REGIMENS AND METHODS FOR IMPROVING VISUAL FUNCTION IN VISUAL DISORDERS ASSOCIATED WITH AN ENDOGENOUS RETINOID DEFICIENCY - Therapeutic regimes for improving visual function in a subject having a deficiency in endogenously produced 11-cis retinal comprising administering the synthetic retinal derivative as a divided dose over 2-7 days then providing a resting period of 7-28 days after which the second dose of the synthetic retinal derivative is administered. Preferred synthetic retinal derivatives are 9- or 11-cis-retinyl esters. Disorders associated with deficiency in endogenously produced 11-cis retinal include retinitis pigmentosa and Leber congenital amaurosis.2015-02-05
20150038583Orodispersible composition comprising polyunsaturated fatty acids without bad odor or taste - An orodispersible composition without bad odor, smell, or taste comprising polyunsaturated fatty acids (PUFA) and a disintegrant. The disintegrant is a solid dispersion comprising mannitol, xylitol, microcrystalline cellulose, crospovidone and dibasic calcium phosphate. A process of preparing the composition and its use as nutritional or dietary supplement for balancing the blood lipid level, preventing or reducing the risk of the development of atherosclerotic changes, disorders or diseases.2015-02-05
20150038584MATERIALS FOR DISINFECTION PRODUCED BY NON-THERMAL PLASMA - Aspects of the present subject matter are directed to a method comprising contacting an fluid, optionally containing an added organic material, with a non-thermal plasma to form a disinfection composition, wherein the disinfection composition is a liquid, and contacting a surface with the disinfection composition, wherein the surface is at least partially disinfected upon contact with the disinfection composition. Additional aspects of the present subject matter are directed to a method comprising forming a disinfection composition by contacting an organic material with a non-thermal plasma, wherein the disinfection composition is a liquid. A further aspect of the present subject matter is directed to a disinfection composition comprising an organic material contacted by a non-thermal plasma, wherein the disinfection composition is a liquid.2015-02-05
20150038585Treatment of Diseases by Concurrently Eliciting Remyelination Effects and Immunomodulatory Effects Using Selective RXR Agonists - The present specification provides RXR agonists with both remyelination promotion and immunomodulatory activities, compositions comprising such RXR agonists, and methods using such compounds and compositions to treat a demyelination-related disorder by both promoting remyelination of neurons and modulating the immune system.2015-02-05
20150038586USE OF N-ACETYLCYSTEINE AMIDE IN THE TREATMENT OF PENETRATING HEAD INJURY - This disclosure describes methods of use for N-acetylcysteine amide for the treatment of penetrating head injury.2015-02-05
20150038587NOVEL CRYSTALLINE FORMS OF (1S,2R)-2-(AMINO METHYL)-N,N-DIETHYL-1-PHENYL CYCLOPROPANE CARBOXAMIDE - The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.2015-02-05
20150038588COMPOSITIONS AND METHODS OF TREATMENT OF STATUS EPILEPTICUS - The invention provides a method of treating benzodiazepine-resistant status epilepticus in a subject having been exposed to a nerve agent inducing the status epilepticus.2015-02-05
20150038589Nutritional Product Comprising a Biguanide - The present invention relates to a nutritional product comprising a biguanide in a concentration of 20 to 1600 mg per 100 g, based on total weight of the nutritional product, the nutritional product further comprising at least one dietary component selected from the group of (i) digestible carbohydrates, (ii) amino acid sources, such as proteins, peptides, free amino acids including salts of free amino acids, (iii) lipids, and (iv) dietary fibre. The invention further relates to a nutritional product comprising a biguanide for use in a prophylactic or therapeutic treatment of an aging-associated disorder.2015-02-05
20150038590N-CYCLOALKYL-N-[(CYCLOALKENYLPHENYL)METHYLENE]-(THIO)CARBOXAMIDE DERIVATIVES - The present invention relates to fungicidal N-cycloalkyl-N-[(cycloalkenylphenyl)methylene]carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.2015-02-05
20150038591Compounds, compositions and methods for the treatment of tauopathies - Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of tauopathies, such as Alzheimer's disease and Parkinson's disease, and the manufacture of medicaments for such treatment.2015-02-05
20150038592STABLE WATER-IN-OIL EMULSIONS WITH SPREADABLE OILS - The invention comprises a cosmetic and/or dermatological preparation based on water-in-oil emulsions, comprising at least two W/O emulsifiers and at least one oil having a spreadability value of more than 600 mm2015-02-05
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