20th week of 2015 patent applcation highlights part 52 |
Patent application number | Title | Published |
20150133428 | NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS - The invention provides compounds of Formula (I): | 2015-05-14 |
20150133429 | METHOD OF TREATMENT USING SUBSTITUTED PYRAZOLO[1,5-a] PYRIMIDINE COMPOUNDS - Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or | 2015-05-14 |
20150133430 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 2015-05-14 |
20150133431 | GGA DERIVATIVES - This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives. | 2015-05-14 |
20150133432 | SUBSTITUTED 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, | 2015-05-14 |
20150133433 | BENZOTHIOPHENE COMPOUND - A method for preventing or treating a disease selected from the group consisting of visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia in a subject in need thereof, comprising administering to said subject an effective amount of the compound of the following formula (I) or a salt thereof: | 2015-05-14 |
20150133434 | Compositions and Methods for Reactivating Latent Immunodeficiency Virus - The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual. | 2015-05-14 |
20150133435 | PYRROLOBENZODIAZEPINES - Pyrrolobenzodiazepine (PBDs) having a (1-methyl-1H-pyrrol-3-yl)phenyl based amino residue were found to be highly effective compounds having improved cytotoxicity ad DNA binding properties. | 2015-05-14 |
20150133436 | Bromodomain Inhibitors For Treating Autoimmune And Inflammatory Diseases - The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions. | 2015-05-14 |
20150133437 | Tetrahydro[1,8]naphthyridine Sulfonamide and Related Compounds for Use as Agonists of RORy and the Treatment of Disease - The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections. | 2015-05-14 |
20150133438 | Heterocyclic Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds - Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, | 2015-05-14 |
20150133439 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 2015-05-14 |
20150133440 | DIFLUORO-HEXAHYDRO-CYCLOPENTAOXAZINYLS AND DIFLUORO-HEXAHYDRO-BENZOOXAZINYLS AS BACE1 INHIBITORS - The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease. | 2015-05-14 |
20150133441 | THERAMUTEIN MODULATORS - This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein. | 2015-05-14 |
20150133442 | METHODS AND COMPOSITIONS FOR THE INHIBITION OF PIN1 - The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels. | 2015-05-14 |
20150133443 | Thiazolyl- And Oxazolyl-Isoquinolinones And Methods For Using Them - The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders. | 2015-05-14 |
20150133444 | MELAMPOMAGNOLIDE B DERIVATIVES - The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans. | 2015-05-14 |
20150133445 | SYNTHESIS AND USE OF DUAL TYROSYL-DNA PHOSPHODIESTERASE I (Tdp1) - TOPOISOMERASE I (Top1) INHIBITORS - The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds. | 2015-05-14 |
20150133446 | IMIDAZOTHIADIAZOLE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION - The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, R | 2015-05-14 |
20150133447 | Triazolopyrazine - The present invention encompasses compounds of general formula (I) | 2015-05-14 |
20150133448 | NOVEL PYRAZOLE DERIVATIVE - It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates. | 2015-05-14 |
20150133449 | NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5-DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES - The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them. | 2015-05-14 |
20150133450 | METHODS AND COMPOSITIONS USEFUL FOR TREATING DISEASES INVOLVING BCL-2 FAMILY PROTEINS WITH QUINOLINE DERIVATIVES - The present invention relates to compositions and methods for cancer treatment comprising compounds of Formulae I, II, and III. In some aspects, the invention relates to the treatment of B-cell Lymphoma or other hematopoietic cancers. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as, for example, B-cell lymphoma, using a combination of one or more compounds of Formulae I, II, and III. Combination therapy with, for example, 26S proteasome inhibitors, such as, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formulae I, II, and III. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease. | 2015-05-14 |
20150133451 | HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): | 2015-05-14 |
20150133452 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to claim | 2015-05-14 |
20150133453 | PYRROLOTRIAZINONE DERIVATIVES - Compounds of the formula I | 2015-05-14 |
20150133454 | NANOSTRUCTURED MUCOADHESIVE MICROPARTICLES - Provided is a nanostructured mucoadhesive microparticle including a biocompatible polymer, the microparticle having a surface with a nanostructure formed thereon. The present nanostructured mucoadhesive microparticle having an increased retention time on the mucous as well as with a minimized irritation to the surface can be advantageously used as a drug delivery vehicle. Thus the increased bioavailability of a therapeutic agent administered by the present microparticle leads to an increased therapeutic efficacy, reduced dosage and reduced number of administration as well as significant cost savings and improved patient convenience resulted therefrom. | 2015-05-14 |
20150133455 | FOLIC ACID RAMIPRIL COMBINATION: CELL PROTECTIVE, NEUROPROTECTIVE AND RETINOPROTECTIVE OPHTALMOLIGIC COMPOSITIONS - The invention relates to a cellprotective, neuroprotective and retinoprotective composition. In an embodiment of the invention, said composition comprises (i) Ramipril or Ramiprilate and (ii) folic acid. The composition of the invention can be used, in particular, for the prevention of loss of vision, or even for improving visual acuity and visual field in normal subjects, as well as for treating ophthalmologic pathologies, in particular: glaucoma, diabetic retinopathy, age related macular degeneration, hereditary dystrophy of the retina, uveitis, ammetropia (myopia, presbyopia). This combination of active principles could also be used in general conditions for treating general pathologies (cancer . . . ). | 2015-05-14 |
20150133456 | FLUOROERGOLINE DERIVATIVES AND USES THEREOF - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 2015-05-14 |
20150133457 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways. | 2015-05-14 |
20150133458 | Orally Active, Cell-Penetrating Homing Peptide and Methods of Using Same - Disclosed are compositions and methods useful for oral delivery of targeted therapies for pulmonary diseases, fibrotic disorders and cancer. The compositions and methods are based on peptide sequences that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. The disclosed targeting is useful for oral delivery of therapeutic and detectable agents to diseased tissue in an animal. | 2015-05-14 |
20150133459 | SILDENAFIL SUBLINGUAL SPRAY FORMULATION - The invention is directed to sublingual spray formulations containing sildenafil. The invention is further directed to methods of treating male sexual dysfunction or pulmonary arterial hypertension by administering sublingual spray formulations containing sildenafil to patients in need of such treatments. | 2015-05-14 |
20150133460 | LACTATE SALT OF 4-[6-METHOXY-7-(3-PIPERIDIN-1-YL-PROPOXY)QUINAZOLIN-4-YL]PIPERAZINE-1-CAR- BOXYLIC ACID(4-ISOPROPOXYPHENYL)-AMIDE AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF CANCER AND OTHER DISEASES OR DISORDERS - This invention provides a compound of formula (I): | 2015-05-14 |
20150133461 | PHARMACEUTICAL COMPOSITION CONTAINING AN ANTIVIRALLY ACTIVE DIHYDROQUINAZOLINE DERIVATIVE - The invention relates to pharmaceutical compositions, particularly for intravenous administration, containing {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid in combination with at least one of the cyclodextrin excipients, lysine and arginine; the method for its production; and its use in methods of treatment of and/or as a prophylactic for illnesses, particularly its use as an antiviral, preferably against cytomegaloviruses. | 2015-05-14 |
20150133462 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF BCR-ABL POSITIVE LYMPHOBLASTIC LEUKEMIAS - In one aspect, the invention relates to compositions comprising BCR-ABL tyrosine kinase inhibitors and artemisinin analogues, derivatives thereof, or related compounds, which are useful as in treating Philadelphia chromosome positive leukemias; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with BCR-ABL dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2015-05-14 |
20150133463 | MULTICOMPONENT CRYSTALS COMPRISING DASATINIB AND SELECTED CO-CRYSTAL FORMERS - Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(−)-menthol. | 2015-05-14 |
20150133464 | Injectable particle - The present invention generally relates to an novel injectable particle composition essentially consisting of: (a) a population of domains, wherein each domain essentially consists of a drug matrix and a population of subdomains, wherein the subdomains are evenly distributed in the drug matrix, wherein each subdomain essentially consists of an ionizable excipient, and (b) a rate controlling matrix comprising a biocompatible polymer and optionally an excipient. The particle is for the use of cancer therapy. | 2015-05-14 |
20150133465 | ANTIMICROBIAL AGENTS - The invention provides compounds of formula (I): | 2015-05-14 |
20150133466 | SENSITIZATION OF CANCER CELLS TO DNA DAMAGE BY INHIBITING KINASES ESSENTIAL FOR DNA DAMAGE CHECKPOINT CONTROL - The invention provides methods for overriding cell cycle arrest in a tumor cell, which comprise inducing DNA damage in the cell, and contacting the cell with an amount of bosutinib or a bosutinib isomer effective to inhibit one or more kinase constituents of a DNA damage checkpoint pathway. The invention also provides novel bosutinib isomers, as well as compositions of the novel isomers and the bosutinib isomer 3,5-dichloro-4-methoxyaniline. | 2015-05-14 |
20150133467 | SCREENING METHOD, PROTEIN INSTABILITY AND/OR STABILITY INDUCERS, AND PROTEIN ACTIVITY ASSESSMENT - Provided is a screening method with which it is possible to determine the cause of a decrease or an increase in the amount of a target protein that is expressed by a cell. One or a plurality of embodiments include: conducting cultivation that includes bringing an assay cell into contact with a test substance, and measuring a relative amount (A) of the target protein in relation to an internal standard; conducting cultivation in which an assay cell is not brought into contact with a test substance, and measuring a relative amount (B) in relation to an internal standard; comparing the relative amount (A) and the relative amount (B); and, based on the comparison, selecting a candidate substance that induces instability and/or stability in the target protein. The assay cell is a cell that is able to express mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression, or a cell having a means for expressing mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression. | 2015-05-14 |
20150133468 | METHANETHIONE COMPOUNDS HAVING ANTIVIRAL ACTIVITY - A compound of formula (I) is useful as an antiviral agent, in particular for the treatment of influenza. A method for preparing the compound of formula (I) and a composition including the compound of formula (I) are described. | 2015-05-14 |
20150133469 | EARLY DETECTION OF TUBERCULOSIS TREATMENT RESPONSE - The present invention includes methods for early detection of a treatment response in a patient suspected of being infected with | 2015-05-14 |
20150133470 | SUBSTITUTED N-ACETYL-L-CYSTEINE DERIVATIVES AND RELATED COMPOUNDS - Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction. | 2015-05-14 |
20150133471 | COMPOUNDS AND THEIR USE AS BACE INHIBITORS - The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 2015-05-14 |
20150133472 | PHARMACEUTICAL COMPOSITION - The present invention relates to a pharmaceutical composition comprising voriconazole and an aqueous, non-aqueous, or oily vehicle, or a mixture thereof, and optionally one or more pharmaceutically acceptable excipients; to a process for preparing such a composition, and to the use of such a composition for the prevention or treatment of fungal infections. | 2015-05-14 |
20150133473 | NOVEL RING-SUBSTITUTED N-PYRIDINYL AMIDES AS KINASE INHIBITORS - The present invention provides a compound of formula (A): | 2015-05-14 |
20150133474 | GHRELIN O-ACYL TRANSFERASE INHIBITOR - The present invention provides novel GOAT inhibitors and their salts and pharmaceutical compositions thereof. | 2015-05-14 |
20150133475 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF PERIODONTITIS AND RHEUMATOID ARTHRITIS - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of periodontitis and rheumatoid arthritis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. | 2015-05-14 |
20150133476 | Polymorphic forms of 4-phenylamino quinazoline derivative, the preparation method and uses thereof - The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof. | 2015-05-14 |
20150133477 | Methods for Reducing Uric Acid Levels Using Barbiturate Derivatives - Methods for reducing uric acid levels in blood or serum of a subject employing metabolites of merbarone as active agents. Methods for treating or preventing disorders of uric acid metabolism are also provided. The metabolites can be formulated as pharmaceutical compositions comprising the metabolites and a pharmaceutically acceptable carrier for use in these methods. | 2015-05-14 |
20150133478 | C-RAF MUTANTS THAT CONFER RESISTANCE TO RAF INHIBITORS - Nucleic acids and proteins having a mutant C-RAF sequence, and methods of identifying patients having cancer who are likely to benefit from a combination therapy and methods of treatment are provided. | 2015-05-14 |
20150133479 | PYRIMIDINYLPIPERIDINYLOXYPYRIDONE ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds. | 2015-05-14 |
20150133480 | FLUOROETHYL THIAMINE OR SALTS THEREOF AND APPLICATION THEREOF IN PREPARATION OF ANTICOCCIDIAL DRUGS - The present invention discloses a fluoroethyl thiamine or salts thereof and application thereof in preparation of anticoccidial drugs. The structural formula of the fluoroethyl thiamine or salts thereof is shown as Formula (I). The fluoroethyl thiamine or salts thereof of the present invention have a remarkable anticoccidial effect, particularly on some coccidia which had resistance to other anticoccidial drugs, therefore the fluoroethyl thiamine or salts thereof of the present invention can be applied to preparation of anticoccidial drugs. Thus, the present invention provides conditions for development of new anticoccidial drugs. | 2015-05-14 |
20150133481 | CRYSTALLINE FORMS OF AN ANDROGEN RECEPTOR MODULATOR - Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity. | 2015-05-14 |
20150133482 | FORMULATIONS OF RIFAXIMIN AND USES THEREOF - The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods. | 2015-05-14 |
20150133483 | Dihydroetorphines and Their Preparation - The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, | 2015-05-14 |
20150133484 | METHOD OF PREPARING OXYMORPHONE - The invention relates to an improved method of preparing oxymorphone or a salt thereof from oripavine. In particular, the invention relates to a method of preparing oxymorphone with a content of alpha-beta-unsaturated ketones (ABUK) <10 ppm, wherein the content of 8,14-dihydroxydihydromorphinone in the prepared oxymorphone is >10 ppm. | 2015-05-14 |
20150133485 | COMPOSITIONS AND METHODS OF USING THREOHYDROXYBUPROPION FOR THERAPEUTIC PURPOSES - This disclosure relates to methods administering threohydroxybupropion or a prodrug thereof in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and threohydroxybupropion or a prodrug of threohydroxybupropion are also disclosed | 2015-05-14 |
20150133486 | BUPROPION AS A MODULATOR OF DRUG ACTIVITY - This disclosure relates to methods administering bupropion or a prodrug thereof in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and bupropion or a prodrug of bupropion are also disclosed | 2015-05-14 |
20150133487 | TRITOQUALINE FOR USE IN THE TREATMENT OF CYSTIC FIBROSIS - This invention relates to tritoqualine for use in the treatment of cystic fibrosis or any one of its complications. The invention also relates to the method for the treatment of cystic fibrosis or any one of its complications by administering tritoqualine. The invention can be used to improve the condition of individuals with cystic fibrosis. | 2015-05-14 |
20150133488 | COMPOSITIONS AND METHODS FOR TREATING EPILEPSY - Compositions and methods for treating epilepsy and epileptic syndromes are described herein. The compositions and methods include therapeutically effective amounts of one or more dimebolins, or pharmaceutically acceptable salts thereof. | 2015-05-14 |
20150133489 | COMPACTED MOXIFLOXACIN - The invention relates to a process for the preparation of tablets containing moxifloxacin, comprising the steps of (i) providing moxifloxacin, pharmaceutically acceptable salts, solvates or hydrates thereof, optionally mixed with one or more pharmaceutical excipients; (ii) compacting it into a slug; (iii) granulating the slug; and (iv) compressing the resulting granules into tablets; and also tablets, granules and compacted material containing compacted moxifloxacin. | 2015-05-14 |
20150133490 | INHIBITOR OF JAK1 AND JAK2 - The present invention provides an amino pyrazole compound, which is 3-[(1R)-6-fluoro-2,3-dihydro-1H-inden-1-yl]-N-(3-methyl-1H-pyrazol-5-yl)-3H-imidazo[4,5-b]pyridin-5-amine, or a pharmaceutically acceptable salt thereof, that inhibits JAK1 and JAK2 and, therefore may be useful in treating cancer. | 2015-05-14 |
20150133491 | COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY - Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases. | 2015-05-14 |
20150133492 | N-desmethyldauricine, A Novel Autophagic Enhancer for Treatment of Cancers and Neurodegenerative Conditions Thereof - This invention is directed to the use of N-desmethyldauricine, a novel autophagy enhancer, in treating cancers or neurodegenerative conditions. | 2015-05-14 |
20150133493 | COUMARIN-BASED COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND CANCER - Compounds including those of the Formula I | 2015-05-14 |
20150133494 | Method of Treating Cancer - This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF. | 2015-05-14 |
20150133495 | Substituted Acyloxyamidines as HCV NS3/4A Inhibitors - Disclosed herein is a compound of Formula I | 2015-05-14 |
20150133496 | Treatment of CNS Disorders Associated with Mutations in Genes Encoding Lysosomal Enzymes - Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase. | 2015-05-14 |
20150133497 | GLYCINE REUPTAKE INHIBITOR AND USE THEREOF - Disclosed are a glycine reuptake inhibitor and the use thereof. The glycine reuptake inhibitor is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is one or more groups selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy; R2 is selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy; and each of R3 and R4 is independently selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. | 2015-05-14 |
20150133498 | BENZOFURAN COMPOUNDS, COMPOSITIONS, KITS AND/OR METHODS THEREOF - Benzofuran compound, composition thereof, kit thereof, and/or method thereof. A benzofuran-2-carboxamide moiety may be N-arylated and/or N-alkylated, and the resulting benzofuran compound may be a sigma receptor ligand that binds to, e.g., a σ1 receptor and/or a σ2 receptor with relatively high affinity and/or selectivity. For example, the benzofuran compound may be 5,6-dimethoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, or 6-methoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide. The composition may include the benzofuran compound and a pharmaceutically acceptable carrier. | 2015-05-14 |
20150133499 | PHARMACEUTICAL COMPOSITIONS OF 5-HYDROXYTRYPTOPHAN AND SEROTONIN-ENHANCING COMPOUND - This invention relates to novel pharmaceutical compositions comprising a therapeutically effective amount of a slow-release formulation of 5-hydroxytryptophan (5-HTP) and a serotonin-enhancing compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating CNS disorders, including depressive disorders, bipolar disorders, anxiety disorders, obesity and pain. | 2015-05-14 |
20150133500 | BENZIMIDAZOLE DERIVATIVES AND USE THEREOF - The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: | 2015-05-14 |
20150133501 | ALFENTANIL COMPOSITION FOR THE TREATMENT OF ACUTE PAIN - There is provided pharmaceutical compositions for the treatment of pain e.g. short-term pain, which compositions comprise a mixture comprising:
| 2015-05-14 |
20150133502 | MEANS TO FACILITATE FOOD INTAKE AND FOOD RETENTION - The disclosure provides for means for a method to facilitate food intake and food retention in a mammal by applying a sufficient dose of a local anesthetic drug in the lumen of the pharyngeal-esophageal-gastric-duodenal tract before or during or after eating. The local anesthetic can be amethocaine, articaine, benzocaine, bupivacaine, chloroprocaine, cinchocaine, cyclomethycaine, dibucaine, diethocaine, etidocaine, larocaine, levobupivacaine, lidocaine, lignocaine, mepivacaine, novocaine, piperocaine, prilocaine, procaine, proparacaine, propoxycaine, QX-222, QX-314, ropivacaine, tetracaine, trimecaine, menthol, eugenol or a safe pharmaceutical formulations of tetrodotoxin, saxitoxin, or neosaxitoxin. The disclosure is useful for patients having problems with food intake or food retention. | 2015-05-14 |
20150133503 | PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING TUBERCULOSIS - The present invention relates to a pharmaceutical composition for preventing or treating tuberculosis, comprising: (a) a pharmaceutically effective amount of a compound represented by the following chemical formula 1; and (b) a pharmaceutically acceptable carrier. Chemical formula 1 The compound contained as an active ingredient of the present invention inhibits the expression and activity of CO-DH in tubercle | 2015-05-14 |
20150133504 | PHARMACEUTICAL COMPOSITIONS FOR DIRECT SYSTEMIC INTRODUCTION - The invention relates to pharmaceutical compositions for direct systemic introduction, are also known as DSI pharmaceutical compositions, for used as human veterinary pharmaceutical compositions. In one embodiment, the invention relates to a pharmaceutical composition for direct system introduction comprising bovine gelatin, mannitol, an optional surfactant, an optional flavorant, and an active pharmaceutical ingredient. A DSI pharmaceutical composition of the invention has a disintegration time of 7 seconds or less in deionized water maintained at 37.0° C.±0.5° C. The invention also relates to a method of delivering an active pharmaceutical ingredient to an animal comprising the step of placing a DSI pharmaceutical composition of the invention into a mucosal cavity of an animal to be treated with the active pharmaceutical ingredient and to the corresponding methods of treatment. | 2015-05-14 |
20150133505 | Arylethynyl derivatives - The present invention relates to ethynyl derivatives of formula I | 2015-05-14 |
20150133506 | 1-ARYL-5-ALKYL PYRAZOLE DERIVATIVE COMPOUNDS, PROCESSES OF MAKING AND METHODS OF USING THEREOF - Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): | 2015-05-14 |
20150133507 | PHARMACEUTICAL COMPOSITIONS COMPRISING GLITAZONES AND NRF2 ACTIVATORS - The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis. | 2015-05-14 |
20150133508 | Use of Quaternary Pyridinium Salts as Vasoprotective Agents - The invention relates to the use of quaternary pyridinium salts of formula (I), | 2015-05-14 |
20150133509 | TREE TRUNK INJECTION - The present invention provides a tree trunk injection agent whereby pathogenic fungi and/or pests in trees can be effectively controlled merely by a short-time application in a low chemical dose, and a method for controlling tree diseases using the tree trunk injection agent. According to one embodiment of the present invention, the tree trunk injection agent is obtained by adding, to an aqueous solution of an insecticidal component such as acetamiprid, a hardly soluble fungicidal component such as thiophanate-methyl so as to suspend the hardly soluble fungicidal component, wherein a particle size based on 50% volume of the fungicidal component is 4 μm or less, or adding thereto at least one fungicidal component selected from a group consisting of triflumizole and metconazole. | 2015-05-14 |
20150133510 | TERTIARY AMINES FOR USE IN THE TREATMENT OF CARDIAC DISORDERS - The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP185) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl)amine structure. | 2015-05-14 |
20150133511 | N-ALKYLTRIAZOLE COMPOUNDS AS LPAR ANTAGONISTS - Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis . . . . | 2015-05-14 |
20150133512 | N-ARYLTRIAZOLE COMPOUNDS AS LPAR ANTAGONISTS - Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis. | 2015-05-14 |
20150133513 | PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF PARKINSONS DISEASE - Pharmaceutical compositions are provided for treatment of Parkinson's disease comprising a pharmaceutically acceptable carrier and a fixed dose combination of two active agents selected from compounds having either neuroprotective or symptomatic effects, or both, in Parkinson's disease patients, wherein the molar ratio of the two compounds is in the range of 1:1 to 1:100. The compositions are formulated for immediate release, controlled release, or both immediate and controlled release. | 2015-05-14 |
20150133514 | PROTEIN DISULFIDE ISOMERASE INHIBITING ANTICANCER AGENTS - Protein disulfide isomerase inhibitors according to formula I | 2015-05-14 |
20150133515 | METHOD FOR INTEGRIN LIGAND DISCOVERY - This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery based upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions. | 2015-05-14 |
20150133516 | Methods and Compositions for Treating ADHD - The present invention provides compositions and methods of using α2 adrenergic receptor agonists as treatments for ADHD. The α2 adrenergic receptor agonist for use with these methods is a benzimidazole derivative, and may be specifically N-(4,5-Dihydro-1H-imidazol-2-yl)-7-cyano-4-methyl-1H-benzimidazol-5-amine acetate. Formulations and routes of administration are also described. | 2015-05-14 |
20150133517 | ONDANSETRON SUBLINGUAL SPRAY FORMULATION - The invention is directed to sublingual spray formulations containing ondansetron or a pharmaceutically acceptable salt thereof and water. The invention is further directed to methods for treating or preventing nausea and emesis associated with cancer treatments by administering sublingual spray formulations containing ondansetron or a pharmaceutically acceptable salt thereof to a patient in need thereof. | 2015-05-14 |
20150133518 | CRYSTALLINE FORMS OF AN ALKOXYIMIDAZOL-1-YLMETHYL BIPHENYL CARBOXYLIC ACID - The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension. | 2015-05-14 |
20150133519 | NOVEL DIESTER AND TRIESTER BASED LOW MOLECULAR WEIGHT, BIODEGRADEABLE CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY - The instant invention provides for novel cationic lipids of Formula A that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain coupled with inclusion of hydrolysable functionality in the lipid chains to enhance the efficiency and tolerability of in vivo delivery of siRNA. | 2015-05-14 |
20150133520 | COMPOSITIONS AND METHODS FOR INDUCING MYOBLAST DIFFERENTIATION AND MYOTUBE FORMATION - Provided herein are methods of inducing differentiation of a mammalian myoblast into a mammalian myocyte that include contacting a mammalian myoblast with an oligonucleotide that decreases Mitogen-activated protein kinase kinase kinase kinase 4 (Map4k4) mRNA expression in a mammalian myoblast or myocyte. Also provided are methods of inducing mammalian myoblasts or myocytes to form a myotube that include contacting two or more mammalian myoblasts or two or more mammalian myocytes with an oligonucleotide that decreases Map4k4 mRNA expression in a mammalian myoblast or myocyte. Also provided are methods of identifying a candidate agent useful for inducing muscle formation, and compositions containing an oligonucleotide that decreases Map4k4 mRNA expression in mammalian myoblast or myocyte and one or more additional muscle therapeutic agents and/or muscle-building neutraceuticals. | 2015-05-14 |
20150133521 | INHIBITORS OF MICRORNAs THAT REGULATE PRODUCTION OF ATRIAL NATRIURETIC PEPTIDE (ANP) AS THERAPEUTICS AND USES THEREOF - The present invention relates to methods, kits and compositions to treat hypertension and other cardiovascular diseases in a subject, in particular, a method of treating or preventing a cardiovascular disease in a subject comprising administering to a subject at least one anti-miR agent to miRNA-425. In some embodiments, an anti-miR agent is a small molecule or an oligonucleotide complementary to at least part of the miR-425 of SEQ ID NO: 1, or an anti-miR complementary to at least part of the miRNA seed sequence AUGACA (SEQ ID NO: 2). Another aspect of the present invention relates to methods, kits and compositions to treat low blood pressure in a subject comprising administering a composition comprising a miR-425 agent to decrease ANP levels in the subject. Other aspects of the present invention relates to assays, methods and systems to identify a subject at risk of hypertension, or identifying a subject suitable to administration of an anti-miR-425 agent for treatment of hypertension, the assay comprising assessing if a subject is homozygous or heterozygous for the major (A) allele of rs5068 SNP, and/or assaying for levels of miR-425 and/or assaying for levels of NT-proANP and/or levels of ANP in the plasma of a subject. | 2015-05-14 |
20150133522 | MANIPULATING MICRORNA FOR THE MANAGEMENT OF NEUROLOGICAL DISEASES OR CONDITIONS AND COMPOSITIONS RELATED THERETO - This disclosure relates to manipulating microRNA for the management of neurological disorders and compositions related thereto. In certain embodiments, the disclosure contemplates inhibition of miR324 or miR324-5p, e.g., the use of nucleobase polymers for antisense disruptions or RNA interference of miR-324 expression or for miR324-5p binding in order to increase Kv4.2 expression. In certain embodiments, the disclosure relates to methods of treating or preventing a neurological disease or condition comprising administering an effective amount of an inhibitor to a subject in need thereto. | 2015-05-14 |
20150133523 | METHOD FOR DOWN-REGULATING GENE EXPRESSION IN FUNGI - The present invention concerns methods for controlling fungus infestation via dsRNA mediated gene silencing, whereby the intact fungus cell(s) are contacted with a double-stranded RNA from outside the fungal cell(s) and whereby the double-stranded RNA is taken up by the intact fungal cell(s). In one particular embodiment, the methods of the invention are used to alleviate plants from fungus pests. Alternatively, the methods are used for treating and/or preventing fungal infestation on a substrate or a subject in need of such treatment and/or prevention. Suitable fungal target genes and fragments thereof, dsRNA constructs, recombinant constructs and compositions are disclosed. | 2015-05-14 |
20150133524 | PYRUVATE DEHYROGENASE KINASES AS THERAEUTIC TARGETS FOR CANCER AND ISCHEMIC DISEASES - The invention provides therapeutic and prophylactic compounds and methods for altering the activity of pyruvate dehydrogenase kinase (e.g. PDK1, PDK2, PDK3, PDK4). Such therapies are useful for the treatment of neoplasia. The invention further provides therapeutic and prophylactic compounds and methods of altering pyruvate dehydrogenase activity to treat or prevent cell death related to ischemia. | 2015-05-14 |
20150133525 | TREATMENT OF RNASE H1 RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO RNASE H1 - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of RNase H1, in particular, by targeting natural antisense polynucleotieds of RNase H1. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of RNASE H1. | 2015-05-14 |
20150133526 | TREATMENT OF DISCS LARGE HOMOLOG (DLG) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO DLG - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Discs large homolog (DLG), in particular, by targeting natural antisense polynucleotides of Discs large homolog (DLG). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorder associated with the expression of DLG. | 2015-05-14 |
20150133527 | REGULATION OF CARDIAC SODIUM CHANNELS BY SIRT1 AND SIRT1 ACTIVATORS - Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation. | 2015-05-14 |