32nd week of 2014 patent applcation highlights part 58 |
Patent application number | Title | Published |
20140221385 | COMBINATIONS OF SEROTONIN RECEPTOR AGONISTS FOR TREATMENT OF MOVEMENT DISORDERS - The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention. | 2014-08-07 |
20140221386 | COMBINATIONS OF AKT INHIBITOR COMPOUNDS AND ERLOTINIB, AND METHODS OF USE - The invention provides A combination of a) a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and b) erlotinib or a pharmaceutically acceptable salt thereof for the prophylactic or therapeutic treatment of a hyperproliferative disorder, such as cancer. | 2014-08-07 |
20140221387 | COMPOSITIONS AND METHODS USEFUL FOR TREATING DISEASES - The present invention relates to a compositions for and methods of cancer treatment in which compounds of Formula I or Formula II. In some aspects, the treatment of B-cell Lymphoma or other hematopoietic cancers is encompassed. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds of Formula I or Formula II. Combination therapy with, for example, a class of therapeutics known as 26S proteasome inhibitors, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formula I or Formula II. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease. | 2014-08-07 |
20140221388 | CARBOSTYRIL DERIVATIVES AND SEROTONIN REUPTAKE INHIBITORS FOR TREATMENT OF MOOD DISORDERS - The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder. | 2014-08-07 |
20140221389 | USE OF 4-AMINO-5-FLUORO-3-[6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL- ]-1H-QUINOLIN-2-ONE IN THE TREATMENT OF CANCER IN MODERATE HEPATIC IMPAIRED PATIENTS - The present invention relates to a method of treating a cancer in patient in need thereof by administering 4-amino-5 fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one, or a tautomer thereof, or a salt of any one of them, wherein the patient is a moderate hepatic impaired patient. | 2014-08-07 |
20140221390 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - Provided is a compound useful in the prevention and treatment of non-alcoholic steatohepatitis. A prophylactic and/or therapeutic agent for non-alcoholic steatohepatitis which contains, as the active ingredient, 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, an acid-addition salt thereof, or a solvate of the same. | 2014-08-07 |
20140221391 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 2014-08-07 |
20140221392 | CYCLOHEXANE DERIVATIVE COMPOUND - To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R | 2014-08-07 |
20140221393 | Itraconazole Analogs and Use Thereof - Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs. | 2014-08-07 |
20140221394 | HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 - The invention provides an acid addition salt of a compound of the formula ( | 2014-08-07 |
20140221395 | Deuterium-Enriched Alkyl Sulfonamides and Uses Thereof - The present invention is concerned with deuterium-enriched sulfonamides of formula 1, their pharmaceutically acceptable salts and methods of use thereof for the treatment of anxiety disorders including, General Anxiety Disorder (GAD), Panic Disorder (PD), Post-Traumatic Stress Disorder (PTSD), Social Phobia (SP), Health Anxiety (Hypochondriasis), depression, major depressive disorders, unipolar depression, bipolar I depression disorder, bipolar II depression disorder, treatment-resistant depression, single episodic and recurrent major depressive disorders, depression in the medically ill, attention deficit hyperactivity disorder (ADHD), attention deficit disorder (ADD), Obsessive-Compulsive Disorder (OCD), Obsessive-Compulsive Personality Disorder (OCPD), Autism Spectrum Disorder (ASD), schizophrenia, psychosis, epilepsy, seizures, hot flashes due to menopause, age-related macular degeneration (AMD), premature ejaculation, male erectile dysfunction, sexual dysfunction, obesity, eating disorders, bulimia nervosa, anorexia nervosa, angina, migraine, pain, nociception, sleep disorders, insomnia, fibromyalgia, alcohol withdrawal, autism, Rett's syndrome, cyclothymic disorder, neural injury, neurodegenerative diseases, Parkinson's disease, Parkinson's disease psychosis, Huntington disease, Alzheimer's disease, frontotemporal dementia, cognitive impairment associated with age-related dementia, Alzheimer's disease, schizophrenia, psychosis, depression, pain or discomfort associated with surgery and pain or discomfort associated with medical illness. | 2014-08-07 |
20140221396 | TUBULIN INHIBITORS - Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V). | 2014-08-07 |
20140221397 | FIBROSIS INHIBITOR - [Object] The main object of the present invention is to provide a fibrosis inhibitor. | 2014-08-07 |
20140221398 | PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS - The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts. | 2014-08-07 |
20140221399 | METHOD OF TREATING FUNCTIONAL SOMATIC SYNDROMES WITH COMBINATION OF FAMCICLOVIR AND CELECOXIB - The present invention relates to methods of treating fibromyalgia by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib. | 2014-08-07 |
20140221400 | USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection. | 2014-08-07 |
20140221401 | METHODS AND COMPOSITIONS FOR TREATING PAIN - The present application relates to compounds and methods for treating pain, incontinence and other conditions. | 2014-08-07 |
20140221402 | QUINAZOLINE DERIVATIVE AND APPLICATION THEREOF - This invention provides a class of quinazoline compounds, as represented by formula (I), and their pharmaceutically acceptable salts, | 2014-08-07 |
20140221403 | QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. | 2014-08-07 |
20140221404 | FUSION GENE OF Kif5b GENE AND Ret GENE, AND METHOD FOR DETERMINING EFFECTIVENESS OF CANCER TREATMENT TARGETING FUSION GENE - In order to identify a gene that can serve as an indicator for predicting the effectiveness of a drug treatment of cancer and to provide a novel method for predicting the effectiveness of a drug treatment targeting said gene, lung adenocarcinomas were subjected to whole-transcriptome sequencing. As a result, in-frame fusion transcripts between the KIF5B gene and the RET gene were identified. The KIF5B-RET gene fusions were detected in 6 out of 319 (2%) LADC specimens from Japanese individuals and 1 out of 80 (1%) LADC specimens from U.S.A. individuals. None of the seven subjects revealed known activating mutations such as EGFR, KRAS or ALK oncogenes; thus, said gene fusions were found to be responsible mutations (driver mutations) for oncogenesis. Since said gene fusions are considered to induce constitutive activation of RET tyrosine kinase protein, it was found that treatments with RET tyrosine kinase inhibitors are effective in patients with detection of said gene fusions. | 2014-08-07 |
20140221405 | PLATELET ADP RECEPTOR INHIBITORS - Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof. | 2014-08-07 |
20140221406 | QUINAZOLINE-7-ETHER COMPOUNDS AND METHODS OF USE - The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination. | 2014-08-07 |
20140221407 | USE AND APPLICATION OF A PHARMACEUTICAL COMPOSITION CONTAINING A MIXTURE OF NATURAL-ORIGIN HETEROCYCLICAL GUANIDINE, FOR COSMETOLOGY, WOUND HEALING, FOCAL DYSTONIA AND MUSCULAR SPASM- RELATED CLINICAL PATHOLOGIES - Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided. | 2014-08-07 |
20140221408 | PESTICIDAL PYRIMIDINE COMPOUNDS - Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description. | 2014-08-07 |
20140221409 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): | 2014-08-07 |
20140221410 | Fluorinated 3-(2-Oxo-3-(3-Arylpropyl)Imidazolidin-1-yl)-3-Arylpropanoic Acid Derivatives - The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described. | 2014-08-07 |
20140221411 | 2-HYDROXYARYLAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER CONTAINING SAME AS ACTIVE INGREDIENT - The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells. | 2014-08-07 |
20140221412 | THERAPEUTIC COMPOUNDS AND METHODS - The invention provides compounds of formula I: and salts thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer using compounds of formula I. | 2014-08-07 |
20140221413 | PREOPERATIVE TREATMENT OF POST OPERATIVE PAIN - A method of treating postoperative pain in a patient undergoing a surgery is described. The method is based on preoperative administration of a buprenorphine-containing transdermal dosage form. The dosage form can be administered to the patient, for example, 1-4 days prior to surgery. Alternative embodiments of the invention include subsequent transdermal dosage forms to treat the postoperative pain. | 2014-08-07 |
20140221414 | SOLID DISPERSION OF RIFAXIMIN - A solid dispersion of rifaximin comprising rifaximin and pharmaceutically acceptable carrier. A pharmaceutical composition comprising the solid dispersion of rifaximin. | 2014-08-07 |
20140221415 | Method of Treating Dyskinesia - Methods of treating patients with dyskinesias, by administering a therapeutically effective amount of a dual-action mu-opioid receptor antagonist/kappa-opioid receptor agonist or prodrug thereof to a subject in need thereof, sufficient to mitigate the dyskinesia. Alternatively, a combination of both a mu-opioid receptor antagonist or prodrug thereof, and a kappa-opioid receptor agonist or prodrug thereof can be administered, either together or separately. | 2014-08-07 |
20140221416 | Tamper Resistant Pharmaceutical Formulations - Disclosed in certain embodiments is a solid oral dosage form comprising a heat-labile gelling agent; a thermal stabilizer; and a drug susceptible to abuse. | 2014-08-07 |
20140221417 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 2014-08-07 |
20140221418 | HYALURONIC ACID BASED COPOLYMERS - Hyaluronic acid (HA) conjugates or crosslinked HAs compositions for coating an implantable device are provided. The implantable device can be used for treating a disorder such as atherosclerosis, thrombosis, restenosis, high cholesterol, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, and combinations thereof. | 2014-08-07 |
20140221419 | BENZOMORPHAN ANALOGS AND THE USE THEREOF - The present invention is directed to Benzomorphan Analog compounds of the Formula I-ID as shown below, wherein R | 2014-08-07 |
20140221420 | CCR5 ANTAGONISTS FOR TREATING HIV - Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described. | 2014-08-07 |
20140221421 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 2014-08-07 |
20140221422 | NOVEL THIENOPYRIDINE COMPOUNDS, AND METHODS OF USE THEREOF - The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF). | 2014-08-07 |
20140221423 | Agents And Methods For Treating Ischemic And Other Diseases - This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma. | 2014-08-07 |
20140221424 | PHARMACEUTICAL COMPOSITIONS FOR USE IN THE TREATMENT OF CYSTIC FIBROSIS - The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and pharmaceutical compositions thereof for the treatment of cystic fibrosis, in patients, including kits and/or products thereof. | 2014-08-07 |
20140221425 | Quinolyl-containing Hydroxamic Acid Compound and Preparation Method Thereof, and Pharmaceutical Composition Containing This Compound and Use Thereof - Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc. | 2014-08-07 |
20140221426 | SELECTIVE METABOLIC APPROACH TO INCREASING ORAL BIOAVAILABILITY OF PHENYLEPHRINE AND OTHER PHENOLIC BIOACTIVITIES - Presystemic metabolism in intestine of bioactives such as phenylephrine is avoided by administering a subject (human or animal) the bioactive (e.g., phenylephrine) in combination with one or more inhibitors of sulfation (e.g., sulfotransferase enzymes aka SULTs). This can also be enhanced be co-administering inhibitors of monoamine oxidases aka, MAOs, and uridine diphosphate glucoronysl transferases, aka UGTs. Preferably the inhibitors are GRAS compounds. The one or more inhibitor compounds inhibit the enzymes responsible for rapid presystemic metabolism, thus allowing the bioactives (e.g., phenylephrine) to be more readily absorbed intact into the circulatory system. | 2014-08-07 |
20140221427 | ISOTOPOLOGUES OF POMALIDOMIDE - Provided herein are pomalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided. | 2014-08-07 |
20140221428 | ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 2014-08-07 |
20140221429 | HETEROCYCLIC SCHIFF'S BASES AS NOVEL AND NEW ANTIGLYCATION AGENTS - The invention provides that heterocyclic Schiff bases posses protein antiglycation potential in hyperglycemia. The novel antiglycation agents 3-6 showed a moderate to potent antiglycation activity. | 2014-08-07 |
20140221430 | Solid Forms of 3-(6-(1-(2,2-Difluorobenzo[D][1,3]Dioxol-5-yl)Cyclopropanecarboxamido)-3-- Methylpyridin-2-yl)Benzoic Acid - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 2014-08-07 |
20140221431 | NOVEL HISTONE DEACETYLASE INHIBITOR OF BENZAMIDES AND USE THEREOF - Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof. | 2014-08-07 |
20140221432 | 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 amide compound 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 neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods. | 2014-08-07 |
20140221433 | N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl- )phenyl]acetamide mesylate monohydrate - The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions. | 2014-08-07 |
20140221434 | ALTERING PHARMACOKINETICS OF PIRFENIDONE THERAPY - The invention relates to methods for reducing adverse events in patients receiving pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. | 2014-08-07 |
20140221435 | AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to amide compounds of formula I and I′ or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 2014-08-07 |
20140221436 | COMPOSITIONS FOR AN ORALLY ACTIVE 1,2,4-OXADIAZOLE FOR THE TREATMENT OF DISEASE - The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations. | 2014-08-07 |
20140221437 | N-HETERO-RING-SUBSTITUTED AMIDE DERIVATIVE - Compounds having an excellent hypoglycemic effect and β cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 2014-08-07 |
20140221438 | NOVEL SOLID FORMS OF EPALRESTAT - The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic. | 2014-08-07 |
20140221439 | POLYUNSATURATED FATTY ACIDS FOR THE TREATMENT OF DISEASES RELATED TO CARDIOVASCULAR, METABOLIC AND INFLAMMATORY DISEASE AREAS - The present disclosure relates to lipid compounds of the general formula (I): | 2014-08-07 |
20140221440 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising a carboxylic acid compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and one or more kinds of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and met conazole, shows an excellent controlling efficacy on plant diseases. | 2014-08-07 |
20140221441 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and one or more kinds of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and metconazole, shows an excellent controlling efficacy on plant diseases. | 2014-08-07 |
20140221442 | USE OF DIANHYDROGALACTITOL AND ANALOGS AND DERIVATIVES THEREOF TO TREAT GLIOBLASTOMA MULTIFORME - The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N | 2014-08-07 |
20140221443 | NOVEL HYDROGEN SULFATE SALT - The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation. | 2014-08-07 |
20140221444 | Novel crystals and process of making 5-(-methyl)-2-methoxy-benzoic acid - The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. | 2014-08-07 |
20140221445 | AQUEOUS OPHTHALMIC SOLUTIONS OF PHENTOLAMINE AND MEDICAL USES THEREOF - The invention provides aqueous ophthalmic solutions of phentolamine or pharmaceutically acceptable salts thereof, medical kits, and methods for using such ophthalmic solutions to improve visual performance in a patient. Exemplary aqueous ophthalmic solutions include those containing phentolamine mesylate, mannitol, sodium acetate, and water. | 2014-08-07 |
20140221446 | METHODS AND COMPOSITIONS FOR DAILY OPHTHALMIC ADMINISTRATION OF PHENTOLAMINE TO IMPROVE VISUAL PERFORMANCE - The invention provides methods, compositions, and kits containing phentolamine for improving visual performance. In particular, the invention provides improvement in visual performance, such as improvement in visual acuity, by daily ophthalmic administration of a phentolamine solution to an eye of a patient at or near the bedtime of the patient for an extended duration while minimizing the occurrence of adverse side effects, such as eye redness during the patient's waking hours. | 2014-08-07 |
20140221447 | FORMULATION FOR PREVENTING OR REDUCING BLEEDING AT A SURGICAL SITE - An implantable drug depot useful for preventing, reducing or treating bleeding at a surgical site beneath the skin in a patient is provided. The implantable drug depot comprises a therapeutically effective amount of clonidine or a pharmaceutically acceptable salt thereof, and at least one biodegradable polymer. The drug depot is capable of releasing clonidine or a pharmaceutically acceptable salt thereof over a period of at least three days. | 2014-08-07 |
20140221448 | FUNGICIDAL PYRAZOLES - Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, | 2014-08-07 |
20140221449 | DIVIDABLE GALENICAL FORM ALLOWING MODIFIED RELEASE OF THE ACTIVE INGREDIENT - Dividable galenical form for the modified release of active ingredient, wherein the non-subdivided galenical form and a portion of said form obtained by subdivision have identical dissolution profiles. | 2014-08-07 |
20140221450 | Compositions for the treatment of Fragile X syndrome - The present invention relates to a composition comprising a maxi-K potassium channel opener the use in the treatment of fragile X syndrome. More specifically the present invention relates to a composition comprising a fluoro-oxindole or a chloro-oxindole for use in the treatment of fragile X syndrome. | 2014-08-07 |
20140221451 | IMPLANTS FOR THE TREATMENT OF DOPAMINE ASSOCIATED STATES - Biodegradable implants comprising dopamine modulating compounds are described. | 2014-08-07 |
20140221452 | COMPOSITIONS COMPRISING EICOSAPENTAENOIC ACID AND 5-HTP AND METHODS OF USE THEREOF - The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases. | 2014-08-07 |
20140221453 | D-SERINE TRANSPORTER INHIBITORS AS PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VISUAL SYSTEM DISORDERS - The present invention relates to pharmaceutical compositions comprising D-serine transporter inhibitors and therapeutic methods using such pharmaceutical compositions in methods for the treatment of visual system disorders and the enhancement of the visual function. | 2014-08-07 |
20140221454 | Extended 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 pattern of deoxyribonucleotides (in most embodiments, the pattern comprises at least one deoxyribonucleotide-deoxyribonucleotide base pair) designed to direct the site of Dicer enzyme cleavage within the dsNA molecule. Deoxyribonucleotides of the dsNA molecules of the invention are located within a region of the dsNA that can be excised via Dicer cleavage to generate an active siRNA agent that no longer contains the deoxyribonucleotide pattern (e.g., deoxyribonucleotide-deoxyribonucleotide base pairs). Such DNA-extended Dicer-substrate siRNAs (DsiRNAs) were demonstrated to be more effective RNA inhibitory agents than corresponding double stranded RNA-extended DsiRNAs. DsiRNA agents were also found to tolerate guide strand mismatches. | 2014-08-07 |
20140221455 | DIFFERENTIATION MODULATING AGENTS AND USES THEREFOR - The present invention is directed to methods and agents for modulating the differentiation potential and/or proliferation of preadipocytes. More particularly, the present invention discloses methods and agents for modulating a fibroblast growth factor (FGF) signaling pathway, especially the FGF-1 or FGF-2 signaling pathway, for treating or preventing adiposity-related conditions including, but not limited to, obesity, lipoma, lipomatosis, cachexia or lipodystrophy or the loss of adipose tissue in trauma or atrophic conditions. | 2014-08-07 |
20140221456 | TARGETING p63 TO RE-ACTIVATE DORMANT RESERVE STEM CELLS IN OLFACTORY EPITHELIUM - Disclosed herein is a method for activating a dormant epithelial stem cell, or population thereof, to a state of multipotency comprising, reducing the level of ΔNp63 in the cell(s). The dormant epithelial stem cell(s) may be a horizontal basal cell (HBC) of the olfactory epithelium and the level of ΔNp63 may be reduced by contacting the cell or population with an effective amount of one or more agents that downmodulate ΔNp63. One example of an agent is an RNAi. Also disclosed is a method for treating olfactory dysfunction in a subject, comprising activating HBCs of the subject by reducing the level of ΔNp63 in one or more HBCs of the subject, to thereby treat the olfactory dysfunction. Activated horizontal basal cell (HBCs) are also disclosed. | 2014-08-07 |
20140221457 | AMELIORATING OXIDATIVE STRESS IN NEURODEGENERATIVE DISEASE VIA NOX1 TARGETING - Disclosed herein are methods, compounds and compositions designed for ameliorating oxidative stress in cells. In particular, disclosed are viral vectors that express RNA interfering molecules for inhibiting expression or activity of Nox1 or RAC1. Depending on the location of administration, expression of inhibiting molecules can reduce oxidative stress in neurons associated with a particular neurodegenerative condition. | 2014-08-07 |
20140221458 | METHODS AND MEANS FOR EFFICIENT SKIPPING OF EXON 45 IN DUCHENNE MUSCULAR DYSTROPHY PRE-mRNA - The invention relates to a method for inducing or promoting skipping of exon 45 of DMD pre-mRNA in a Duchenne Muscular Dystrophy patient, preferably in an isolated (muscle) cell, the method comprising providing an isolate muscle cell with a molecule that binds to a continuous stretch of at least 21 nucleotides within said exon. The invention further relates to such molecule used in the method. | 2014-08-07 |
20140221459 | BACTERIALLY-DERIVED, INTACT MINICELLS THAT ENCOMPASS PLASMID-FREE FUNCTIONAL NUCLEIC ACID FOR IN VIVO DELIVERY TO MAMMALIAN CELLS - Intact, bacterially-derived minicells can safely introduce therapeutically effective amounts of plasmid-free functional nucleic acid to target mammalian cells. To this end, functional nucleic acid can be packaged into intact minicells directly, without resort to expression constructs, the expression machinery of the host cell, harsh chemicals or electroporation. | 2014-08-07 |
20140221460 | METHOD FOR IDENTIFYING MODULATORS OF HCV TRANSLATION OR REPLICATION INVOLVING THE NS5B POLYPEPTIDE AND A PSEUDOKNOT - The invention relates to a method for identifying compounds that act as modulators of hepatitis C (HCV) translation and/or replication, and to compounds identified by this method, and their uses in medicine. The invention also relates to an RNA useful for identifying modulators of HCV translation and/or replication. The invention further relates to a method for producing a replication-competent HCV virus. | 2014-08-07 |
20140221461 | NUCLEIC ACID MOLECULES AND USES THEREOF - Provided in this application are formulations of double stranded RNA molecules and Krebs Cycle analogs that improving ribonuclease stability, reducing off-target effects of a double stranded siRNA molecule, or of reducing interferon responsiveness of a double stranded siRNA molecule using such dsRNA. Also disclosed are methods of treating a primary tumor or a metastasis by contacting circulating tumor cells, a primary tumor, or a metastasis with a described formulation. | 2014-08-07 |
20140221462 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CARDIOMYOPATHY DUE TO FRIEDREICH ATAXIA - A method for preventing or treating cardiomyopathy due to energy failure in a subject in need thereof is provided. The method comprises administering to the subject a therapeutically effective amount of a vector which comprises a nucleic acid sequence encoding a gene that can reverse energy failure. An exemplary cardiomyopathy is that which is associated with Friedreich ataxia and an exemplary nucleic acid sequence comprises a nucleic acid that encodes frataxin (FXN). | 2014-08-07 |
20140221463 | METHODS FOR HEART REGENERATION - Methods for heart regeneration are provided. The invention provided herein includes methods of modulating proliferation of cardiomyocytes using small molecules and micro RNAs. In embodiments, the methods provided may be used to increase proliferation or cardiomyocytes. Further provided are methods to be used for the treatment of myocardial infarction. | 2014-08-07 |
20140221464 | Compositions and Methods for Treating Skeletal Myopathy - The present invention provides a method of preventing or treating a myopathy, such as a skeletal myopathy, comprising administering a modulator of a miRNA. In one embodiment, the skeletal myopathy is centronuclear myopathy. The modulator can be an agonist that promotes the expression, function or activity of a miR-133 family member. The miR-133 family member can be miR-133a or miR-133b. | 2014-08-07 |
20140221465 | MODIFIED POLYNUCLEOTIDES FOR TREATING GALACTOSYLCERAMIDASE PROTEIN DEFICIENCY - The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of polynucleotides, primary transcripts and mmRNA molecules. | 2014-08-07 |
20140221466 | MICRORNA INHIBITORS - The present invention relates to microRNAs (miRNAs) that are associated with obesity. The present invention is directed to methods, compounds, and compositions for preventing and treating obesity, as well as related diseases, using a microRNA inhibitor. | 2014-08-07 |
20140221467 | METFORMIN DERIVATIVES FOR TREATING DIABETES AND DIABETES COMPLICATIONS - The invention provides mutual ternary salts of metformin, lipoic acid and acidic amino acids such as aspartic acid and glutamic acid. The invention further provides treatment of prediabetes, diabetes, diabetic complications and/or other conditions in mammals in a method that comprises administering an effective amount of one or more of the foregoing compositions to a mammal in need of such treatment. | 2014-08-07 |
20140221468 | Compounds that Modulate Store Operated Calcium Channels - Store operated calcium channel modulating compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which modulation of store operated calcium channels is desired. | 2014-08-07 |
20140221469 | PHYTOCANNABINOIDS FOR USE IN THE TREATMENT OF CANCER - The present invention relates to the use of phytocannabinoids in the treatment of cancer. More particularly it relates to the use of phytocannabinoids in the treatment of tumour cell invasion and cell migration or metastases. Cancers, where invasion and cell migration plays a key role in prognosis include brain tumours, more particularly gliomas, and most particularly Glioblastoma multiforme (GBM) and breast cancers. The phytocannabinoids tetrahydrocannabivarin (THCV) and cannabidivarin (CBDV) alone or in combination with each other and/or other phytocannabinoids, particularly cannabidiol (CBD), tetrahydrocannabinol (THC) and cannabigerol (CBG) or their respective acids are of particular use. | 2014-08-07 |
20140221470 | COMPOUND FOR INHIBITING GLUTATHIONE S-TRANSFERASE OMEGA 1 ACTIVITY, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF, AND METHOD FOR SYNTHESIZING THE SAME - A compound for inhibiting activity of glutathione s-transferase omega 1 is provided and is represented by the following Formula 1: | 2014-08-07 |
20140221471 | COMPOSITIONS AND METHODS TO TREAT SKIN DISEASES CHARACTERIZED BY CELLULAR PROLIFERATION AND ANGIOGENESIS - Described herein are compositions and methods for preventing and/or treating skin diseases including, but not limited to, psoriasis and atopic dermatitis as well as providing anti-aging benefits which results in reduced appearance of wrinkles and aged skin, improved skin color, treatment of photodamaged skin, improvement in skin's radiance and clarity and finish, and an overall healthy and youthful appearance of the skin, involving aberrant angiogenesis and hyperplasia employing one or more benzo[c]chromen-6-one derivatives. | 2014-08-07 |
20140221472 | USE OF MYRICETIN OR DERIVATIVES THEREOF AS A CATHEPSIN K INHIBITOR - This invention is directed to a novel inhibitor on collagen degradation caused by the activity of a human cathepsin K rising. In particular, the inhibitor is myricetin or derivatives thereof. The invention also relates to use of the novel inhibitor to manufacture a medicament in a form of pharmaceuticals, foods, nutraceuticals or cosmetics for the prevention, amelioration and/or treatment of pathological symptoms or diseases associated with collagen degradation. Alternatively, the present invention is further directed to addition of the novel inhibitor to a medicament, food, nutraceutical or cosmetics used for the treatment, amelioration and/or prevention of the disease or pathological symptoms associated with collagen degradation by the increased human cathepsin K actively. The invention also provide the methods for treating, ameliorating and/or preventing the symptoms or diseases, comprising administering an effective amount of the medicament to a subject in need thereof. | 2014-08-07 |
20140221473 | Compositions, Methods of Use, and Methods of Treatment - Embodiments of the present disclosure provide compositions including ketamine analogues, salts, and disalts, pharmaceutical compositions including ketamine analogues, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like. | 2014-08-07 |
20140221474 | Method and Formulation for Chemical Peeling - A chemical peeling formulation and a formulation able to increase the efficacy and the tolerability of preparations based on the use of compounds used to carry out chemical peeling, comprising at least one keratolytic agent and dimethyl isosorbide. The composition may additionally comprise dimethyl sulphone. | 2014-08-07 |
20140221475 | PLATINUM(IV) COMPLEXES AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - New platinum(IV) complexes which has a strong antitumor activity and has a feature that a side effect is relatively reduced is provided. The new complex is platinum(IV) complexes with cis,cis-spiro[4,4]nonane-1,6-diamine ligand and is platinum(IV) complexes with optically active cis,cis-spiro[4,4]nonane-1,6-diamine ligand. Especially, the new complex is dichloromalonato((1S,5S,6S)-spiro[4.4]nonane-1,6-diamine)platinum(IV). | 2014-08-07 |
20140221476 | COMPOUND, COMPOSITION AND USES THEREOF - The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications. | 2014-08-07 |
20140221477 | Process For The Preparation Of A Sulfated Derivative Of 3,5-Diiodo-O-[3-Iodophenyl]-L-Tyrosine - The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives. | 2014-08-07 |
20140221478 | DI-FLUORO CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS - The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. | 2014-08-07 |
20140221479 | SARMS AND METHOD OF USE THEREOF - This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds. | 2014-08-07 |
20140221480 | METHODS OF MANAGING BRAIN INFLAMMATION - This disclosure relates to methods of managing brain injury such as inflammation due to trauma induced brain injury and ischemic stroke by administering resatorvid or derivative there of a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating cerebral ischemia comprising administering an effective amount of resatorvid to a subject in need thereof. In certain embodiments, the effective amount is 3 mg/kg. In certain embodiments, resatorvid is administered by injection. | 2014-08-07 |
20140221481 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 2014-08-07 |
20140221482 | TRIHEPTANOIN FOR THE TREATMENT OF GLUCOSE TRANSPORT 1 DEFICIENCY - Provided are methods for treating GLUT1 and related brain energy deficiencies comprising administering odd-carbon fatty acid sources, e.g., C5 or C7 fatty acid sources, and related compositions. | 2014-08-07 |
20140221483 | GIP Elevation Inhibitor - A GIP-increase inhibitor, which may be utilized for producing a medicine, a food, or the like, is provided. The GIP-increase inhibitor contains triacylglycerol in which α-linolenic acid accounts for 10% by mass or more of the constituent fatty acid, as an effective ingredient. | 2014-08-07 |
20140221484 | GENETIC POLYMORPHISMS ASSOCIATED WITH CARDIOVASCULAR DISORDERS AND DRUG RESPONSE, METHODS OF DETECTION AND USES THEREOF - The present invention is based on the discovery of genetic polymorphisms that are associated with cardiovascular disorders, particularly acute coronary events such as myocardial infarction and stroke, and genetic polymorphisms that are associated with responsiveness of an individual to treatment of cardiovascular disorders with statin. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 2014-08-07 |