47th week of 2012 patent applcation highlights part 48 |
Patent application number | Title | Published |
20120295880 | Compounds With Modifying Activity Enhanced Under Hypoxic Conditions - Compositions and methods for modifying one or more biologic targets are provided. Suitable targets include cells, DNA, proteins, enzymes, and/or a subject in need thereof. The compositions may exist as a monomer or multimer and are active in a biologic environment with enhanced activity in hypoxic environments and, thus, exhibit improved specificity for hypoxic biologic targets (e.g., tumorigenic cells and those undergoing uncontrolled cell growth). A composition typically comprises a complex with an overall charge of 2+ or greater having at least one ruthenium atom attached to a redox active ligand. The redox active ligand helps maintain separation of more than one ruthenium atom. Suitable compositions may further include a terminal ligand comprising a heterocyclic aromatic compound. When provided to a biologic target, the composition modifies the biologic target and no additional compounds need be provided. Suitable compositions are typically catalytic and regenerative in the presence of a reducing agent. | 2012-11-22 |
20120295881 | TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to tetraline and indane derivatives of the formula (I) | 2012-11-22 |
20120295882 | Tricyclic Derivatives and Their Pharmaceutical Use and Compositions - This application relates to tricyclic compounds of Formula I: | 2012-11-22 |
20120295883 | COMPOUNDS - The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases. | 2012-11-22 |
20120295884 | Complement pathway modulators and uses thereof - The present invention provides a compound of formula I: | 2012-11-22 |
20120295885 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula I: | 2012-11-22 |
20120295886 | ANTIVIRAL COMPOUNDS AND THEIR METHODS OF USE - The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): | 2012-11-22 |
20120295887 | PHARMACEUTICALLY ACCEPTABLE SALTS OF PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USE THEREOF - Pharmaceutically acceptable salts of pyrrolo-nitrogenous heterocyclic derivatives, preparation method and medical use thereof are disclosed. More specifically, pharmaceutically acceptable salts of (R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-methylene)-5-(2-hydroxy-3-morpholinyl-4-yl-propyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one presented by formula (I), the preparation method and the use thereof as therapeutic agents, especially as protein kinase inhibitors, are disclosed. | 2012-11-22 |
20120295888 | USE OF AN ADRENAL HORMONE-MODIFYING AGENT - The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): | 2012-11-22 |
20120295889 | 3-Arylamino Pyridine Derivatives - The invention provides novel, substituted 3-arylamino pyridine compounds | 2012-11-22 |
20120295890 | GLYCOSAMINOGLYCAN INHIBITORS - Provided herein are chondroitin sulfate inhibitors, including modulators of glycosylation, and/or sulfation of galactose or N-acetyl galactosamine glycosaminoglycans. | 2012-11-22 |
20120295891 | NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted triazole derivatives of Formula (I) | 2012-11-22 |
20120295892 | GABAERGIC RECEPTOR SUBTYPE SELECTIVE LIGANDS AND THEIR USES - Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases. | 2012-11-22 |
20120295893 | COMPOSITIONS AND METHODS OF COUNTERACTING RESIDUAL SEDATIVE EFFECTS OF SLEEP/ HYPNOTIC DRUGS - The present invention provides pharmaceutical compositions comprising a flumazenil, and methods of alleviating or counteracting residual effects (e.g. drowsiness) associated with the administration of sleep/hypnotic drugs or alleviating effects of alcohol intoxication, using self administration modes of delivery. | 2012-11-22 |
20120295894 | PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF - Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease. | 2012-11-22 |
20120295895 | COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS - A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: | 2012-11-22 |
20120295896 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I) and (IA): | 2012-11-22 |
20120295897 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. | 2012-11-22 |
20120295898 | Antiviral Therapy - The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 2012-11-22 |
20120295899 | BENZYLPYRROLIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MCP-1 or CCR-2 of formula | 2012-11-22 |
20120295900 | 1,3-OXAZINES AS BACE 1 AND/OR BACE2 INHIBITORS - The present invention provides compounds of formula I | 2012-11-22 |
20120295901 | NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) | 2012-11-22 |
20120295902 | Hetaryl-[1,8]naphthyridine derivatives - Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) | 2012-11-22 |
20120295903 | FLAVIN DERIVATIVES - The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives. | 2012-11-22 |
20120295904 | HEMATOPOIETIC GROWTH FACTOR MIMETIC SMALL MOLECULE COMPOUNDS AND THEIR USES - The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders. | 2012-11-22 |
20120295905 | NEW ANTI-MALARIAL AGENTS - The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation. | 2012-11-22 |
20120295906 | PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE-AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R | 2012-11-22 |
20120295907 | INSECTICIDAL COMPOUNDS - The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them. | 2012-11-22 |
20120295908 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to claim | 2012-11-22 |
20120295909 | ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The invention relates to compounds corresponding to the general formula (I): | 2012-11-22 |
20120295910 | New Phenylsulfamoyl Benzamide Derivatives as Bradykinin Antagonists - The present invention relates to new sulfonamide derivatives of formula (I), wherein R | 2012-11-22 |
20120295911 | Novel Compounds and Compositions for Treatment of Breathing Control Disorders or Diseases - The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. | 2012-11-22 |
20120295912 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 2012-11-22 |
20120295913 | BICYCLIC PYRAZOLE COMPOUNDS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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. | 2012-11-22 |
20120295914 | COMBINATION OF ADRENERGIC RECEPTOR AGONIST ALPHA-1 OR ALPHA-2, PREFERABLY BRIMONIDINE WITH FILLERS, PREFERABLY HYALURONIC ACID - A combination of a quantity of adrenergic receptor agonist α-1 or α-2, and preferably product known as brimonidine, with fillers, and preferably with hyaluronic acid, for decreasing skin or cutaneous reactions is described. | 2012-11-22 |
20120295915 | AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS - Disclosed are compounds having Formula (I), | 2012-11-22 |
20120295916 | ORODISPERSIBLE TABLET CONTAINING COMPACTED SILDENAFIL BASE - The invention relates to a process for the preparation of a pharmaceutical intermediate, comprising the steps of (i) mixing (a-i) sildenafil base, (b-i) wicking agent, (c-i) disintegrant, (d-i) optionally glidant; (ii) compacting the mixture; and (iii) milling the compacted material; and to an intermediate obtainable by that process. In addition, the invention relates to a process for the preparation of an orally dispersible tablet (hereinafter also referred to as an “orodispersible tablet”) comprising the intermediate of the invention, and to orodispersible tablets obtainable by that process. | 2012-11-22 |
20120295917 | IMATINIB DICHLOROACETATE AND ANTI-CANCER AGENT COMPRISING THE SAME - The present invention relates to imatinib dichloroacetate and an anti-cancer agent comprising the same. The imatinib dichloroacetate of the present invention can inhibit tyrosine kinase as well as induce cancer cells to kill themselves via apoptosis, thereby inhibit growth of cancer cells and lead to their destruction, and show significantly enhanced anti-cancer effects by synergy between imatinib and dichloroacetic acid. | 2012-11-22 |
20120295918 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 2012-11-22 |
20120295920 | 5-AMINO-4-HYDROXYPENTOYL AMIDES - HIV inhibitors of formula | 2012-11-22 |
20120295921 | PYRIDYL PIPERIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to pyridyl piperidine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2012-11-22 |
20120295922 | Compounds For Use In Treatment Of Mucositis - The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same. | 2012-11-22 |
20120295923 | Aminocyclohexanes and Aminotetrahydropyrans and Related Compounds As Gamma-Secretase Modulators - Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I | 2012-11-22 |
20120295924 | THIENOPYRIMIDINEDIONE DERIVATIVES AS TRPA1 MODULATORS - The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. | 2012-11-22 |
20120295925 | SUBSTITUTED DERIVATIVES OF BICYCLIC [4.3.0] HETEROARYL COMPOUNDS - This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier. | 2012-11-22 |
20120295926 | SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME - Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: | 2012-11-22 |
20120295927 | METHODS OF USING SELECTIVE CHEMOTHERAPEUTIC AGENTS FOR TARGETING TUMOR CELLS - A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor. | 2012-11-22 |
20120295928 | METHODS FOR DETECTING AND REDUCING IMPURITIES OF LAPATINIB AND SALTS THEREOF - Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: | 2012-11-22 |
20120295929 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses. | 2012-11-22 |
20120295930 | NOVEL PROCESS FOR THE PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE - The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients. | 2012-11-22 |
20120295931 | SPIROINDOLINE COMPOUNDS FOR USE AS ANTHELMINTHICS - This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds. | 2012-11-22 |
20120295932 | METHOD FOR THE TREATMENT OF CANCER - Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. Also provided is a method of sensitizing a cancer cell from a solid tumor from a male patient other than a prostate cancer cell to treatment with a chemotherapeutic agent comprising administering an effective amount of
| 2012-11-22 |
20120295933 | TREATMENT OF COPD, GASTRO-ESOPHAGEAL REFLUX DISEASE (GERD), FOOD ALLERGIES AND OTHER GASTROINTESTINAL CONDITIONS AND DISORDERS AMELIORATED BY PROPER HISTAMINE MANAGEMENT USING A COMBINATION OF HISTIDINE DECARBOXYLASE INHIBATORS, LRA DRUGS, ANTI-H1 AND/OR ANTI-H2 DRUGS - The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor. | 2012-11-22 |
20120295934 | New Hexahydrocyclopentapyrrolone, Hexahydropyrrolopyrrolone, Octahydropyrrolopyridinone and Octahydropyridinone Compounds - The invention provides novel compounds having the general formula (I) | 2012-11-22 |
20120295935 | MIXED AMINAL PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - Described herein are pharmaceutical compositions for the administration of one or more mixed aminals, as defined herein, including salubrinal and analogs and derivatives of salubrinal, and methods for treating diseases or disorders arising from apoptosis, particularly for treating diseases or disorders arising from integrated stress response-induced apoptosis, such as occurs in bone diseases, injuries, and defects. | 2012-11-22 |
20120295936 | COMPOSITIONS AND METHODS FOR TREATING SEIZURE DISORDERS - Disclosed are methods of treating a seizure disorder by administering to a patient in need of such treatment a compound having the following formula: | 2012-11-22 |
20120295937 | NITROXIDE THERAPY FOR THE TREATMENT OF VON HIPPEL - LINDAU DISEASE (VHL) AND RENAL CLEAR CELL CARCINOMA (RCC) - The invention provides therapeutic methods that include administering a stable nitroxide to a subject that has, is suspected to have, or is at risk for having a condition associated with reduced VHL or elevated HIF-2α. | 2012-11-22 |
20120295938 | ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together. | 2012-11-22 |
20120295939 | ANTI-VIRAL AGENT - A method of suppressing the proliferation of virus comprises administering an antiviral agent comprising as an effective component at least one member selected from the group consisting of 5,7,4′-trihydroxy-3′,5′-dimethoxyflavone, 3-hydroxypyridine, p-hydroxybenzaldehyde and vanillin to one in need of suppressing of viral proliferation. | 2012-11-22 |
20120295940 | COMPOSITIONS FOR TREATING MASTITIS - The present disclosure relates to compositions that are effective in controlling or in preventing mastitis in an domesticated animal. The disclosed compositions comprise a biocidal system, comprising a primary biocide and a pH buffer component; a skin conditioner and moisturizer; a cationic or ionic surfactant having an HLB of from about 5 to about 30; an emollient system comprising an extradermal penetrating agent and an emollient base; a thickening agent; and an aqueous based carrier. | 2012-11-22 |
20120295941 | Method For Producing Intermediates For The Production Of Macrocycles That Are Inhibitors Of The Proteasomic Degradation of P27, Such As Argyrin And Derivatives Thereof - The present invention relates to an improved method for the synthesis of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof. | 2012-11-22 |
20120295942 | Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists - There are described 4-difluoromethoxyphenyl pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF | 2012-11-22 |
20120295943 | CYCLOALKYLAMINE DERIVATIVES - Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): | 2012-11-22 |
20120295944 | TREATMENT OF HYPERPROLIFERATIVE DISORDERS WITH DIARYLHYDANTOIN COMPOUNDS - The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer. | 2012-11-22 |
20120295945 | BUCCAL, POLAR AND NON-POLAR SPRAY CONTAINING ONDANSETRON - Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant. | 2012-11-22 |
20120295946 | Agents Useful for Reducing Amyloid Precursor Protein and Treating Dementia and Methods of Use Thereof - The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production. | 2012-11-22 |
20120295947 | PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROC- YCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF - The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis). | 2012-11-22 |
20120295948 | INDIRUBIN-3'-OXIME DERIVATIVES AS POTENT CYCLIN DEPENDENT KINASE INHIBITORS - The present invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor with anti-cancer activity. More particularly, this invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor having excellent anti-cancer activity against human lung cancer cell, human fibro sarcoma cell, human colon cancer cell, human leukemia cell, human stomach cancer cell, human nasopharyngeal cancer cell and/or human breast cancer cell. | 2012-11-22 |
20120295949 | MICRORNA-BASED METHODS AND COMPOSITIONS FOR THE DIAGNOSIS, PROGNOSIS AND TREATMENT OF TUMOR INVOLVING CHROMOSOMAL REARRANGEMENTS - Provided are novel methods and compositions for the diagnosis, prognosis and treatment of tumor involving a chromosomal rearrangement, in particular a tumor or neoplasia of the thyroid gland. In addition, methods of identifying anti-tumor agents are described. | 2012-11-22 |
20120295950 | RBP4 IN INSULIN SENSITIVITY/RESISTANCE, DIABETES, AND OBESITY - Methods for screening molecules that modulate the activity of Retinol Binding Protein 4 (RBP4) and their use in treatment of insulin resistance are described. Also described are methods of diagnosing insulin resistance and related conditions by detecting modulation of RBP4 activity. | 2012-11-22 |
20120295951 | GENETIC CHANGES IN ATM AND ATR/CHEK1 AS PROGNOSTIC INDICATORS IN CANCER - The present invention relates to the discovery that, in human cancer, an 11q deletion of ATM together with an increase in ATR and CHEK1 expression correlates with resistance to ionizing radiation which could be overcome by inhibition of the ATR/CHEK1 pathway. It provides for methods of identifying patients unlikely to exhibit an adequate response to radiation therapy and/or chemotherapy who may benefit from ATR/CHEK1 pathway inhibition, as well as methods of treating said patients. | 2012-11-22 |
20120295952 | TREATMENT OF FILAGGRIN (FLG) RELATED DISEASES BY MODULATION OF FLG EXPRESSION AND ACTIVITY - The present invention relates to antisense oligonucleotides and/or compounds that modulate the expression of and/or function of Filaggrin (FLG), in particular, by targeting natural antisense polynucleotides of Filaggrin (FLG). The invention also relates to the identification of these antisense oligonucleotides and/or compounds and their use in treating diseases and disorders associated with the expression of FLG. | 2012-11-22 |
20120295953 | TREATMENT OF TUMOR PROTEIN 63 (P63) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO P63 - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Tumor Protein 63 (p63), in particular, by targeting natural antisense polynucleotides of Tumor Protein 63 (p63). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of p63. | 2012-11-22 |
20120295954 | TREATMENT OF INTERFERON REGULATORY FACTOR 8 (IRF8) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO IRF8 - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Interferon Regulatory Factor 8 (IRF8), in particular, by targeting natural antisense polynucleotides of Interferon Regulatory Factor 8 (IRF8). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with The expression of IRF8. | 2012-11-22 |
20120295955 | RNA ANTAGONIST COMPOUNDS FOR THE MODULATION OF HER3 - The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment. | 2012-11-22 |
20120295956 | PREVENTION OF TISSUE ISCHEMIA AND RELATED METHODS - Provided herein are methods for preventing, ameliorating, and/or reducing tissue ischemia and/or tissue damage due to ischemia, increasing blood vessel diameter, blood flow and tissue perfusion in the presence of vascular disease including peripheral vascular disease, atherosclerotic vascular disease, coronary artery disease, stroke and influencing other conditions, by suppressing CD47 and/or blocking TSP1 and/or CD47 activity or interaction. Influencing the interaction of CD47-TSP1 in blood vessels allows for control of blood vessel diameter and blood flow, and permits modification of blood pressure and cardiac function. Under conditions of decreased blood flow, for instance through injury or atherosclerosis, blocking TSP1-CD47 interaction allows blood vessels to dilate and increases blood flow, tissue perfusion and tissue survival. | 2012-11-22 |
20120295957 | PREVENTION OF TISSUE ISCHEMIA AND RELATED COMPOSITIONS - Provided herein are compositions for preventing, ameliorating, and/or reducing tissue ischemia and/or tissue damage due to ischemia, increasing blood vessel diameter, blood flow and tissue perfusion in the presence of vascular disease including peripheral vascular disease, atherosclerotic vascular disease, coronary artery disease, stroke and influencing other conditions, by suppressing CD47 and/or blocking TSP1 and/or CD47 activity or interaction. Influencing the interaction of CD47-TSP1 in blood vessels allows for control of blood vessel diameter and blood flow, and permits modification of blood pressure and cardiac function. Under conditions of decreased blood flow, for instance through injury or atherosclerosis, blocking TSP1-CD47 interaction allows blood vessels to dilate and increases blood flow, tissue perfusion and tissue survival. | 2012-11-22 |
20120295958 | MODULATION OF GLUCAGON RECEPTOR EXPRESSION - Compounds, compositions and methods are provided for modulating the expression of glucagon receptor. The compositions comprise oligonucleotides, targeted to nucleic acid encoding glucagon receptor. Methods of using these compounds for modulation of glucagon receptor expression and for diagnosis and treatment of disease associated with expression of glucagon receptor are provided. | 2012-11-22 |
20120295959 | 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 polynucleotides 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. | 2012-11-22 |
20120295960 | TREATMENT REGIMEN FOR PARKINSON'S DISEASE - Provided is an improved treatment for Parkinson's Disease where the efficacy of L-Dopa treatment is increased by including gene therapy in the treatment regimen. The combination therapy results in long-term improvements in response to L-Dopa and diminished side effects caused by L-Dopa. | 2012-11-22 |
20120295961 | MODULATION OF HEPATITIS B VIRUS (HBV) EXPRESSION - Disclosed herein are antisense compounds and methods for decreasing HBV mRNA, DNA and protein expression. Such methods, compounds, and compositions are useful to treat, prevent, or ameliorate HBV-related diseases, disorders or conditions. | 2012-11-22 |
20120295962 | TARGETING MICRORNAS FOR THE TREATMENT OF LIVER CANCER - Provided herein are methods for the treatment of liver cancer. These methods encompass the administration of a compound comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Also provided herein are compositions for the treatment of liver cancer. Such compositions include compounds comprising a modified oligonucleotide, wherein the modified oligonucleotide is targeted to a miRNA. Certain miRNAs have been identified as overexpressed in liver cancer, such as, for example, hepatocellular carcinoma, and are thus selected for targeting by modified oligonucleotides. Further, certain miRNAs have been identified as overexpressed in hepatocellular carcinoma cells exposed to dioxin, and are thus selected for targeting by modified oligonucleotides. Antisense inhibition of certain of these miRNAs has been found to inhibit cell proliferation and induce apoptosis. | 2012-11-22 |
20120295963 | AGENTS, COMPOSITIONS AND METHODS FOR TREATING PATHOLOGIES IN WHICH REGULATING AN ACHE-ASSOCIATED BIOLOGICAL PATHWAY IS BENEFICIAL - The present invention provides agents which are capable of regulating the function of a micro-RNA component which can be used to regulate an AChE-associated biological pathway. In addition, the present invention provides methods and pharmaceutical compositions for the treatment of various pathologies related to AChE-associated biological pathways such as apoptosis, aberrant cholinergic signaling, abnormal hematopoietic proliferation and/or differentiation, cellular stress, exposure to inflammatory response-inducing agents, and/or exposure to organophosphates or other AChE inhibitors. | 2012-11-22 |
20120295964 | RETROGRADE TRANSPORT VIRAL VECTOR SYSTEM HAVING ENVELOPE COMPRISING FUSED GLYCOPROTEIN - Provided is a lentiviral vector system which sustains a high-frequency retrograde transportation ability in animal brain and has a higher titer. A kit for preparing a retrograde transport viral vector, which comprises: (1) a packaging plasmid containing the gag gene and pol gene of HIV-1; (2) a packaging plasmid containing an accessory gene of HIV-1; (3) a transfer plasmid containing a target gene; and (4) an envelope plasmid containing, as an envelope gene, a gene encoding a fused polypeptide comprising the extracellular domain of rabies virus glycoprotein (RV-G), the transmembrane domain of rabies virus glycoprotein (RV-G) or vesicular stomatitis virus glycoprotein (VSV-G) and the intracellular domain of vesicular stomatitis virus glycoprotein (VSV-G). | 2012-11-22 |
20120295965 | FUSED THIOPHENES AS DUAL INHIBITORS OF EGFR/VEGFR AND THEIR USE IN THE TREATMENT OF CANCER - Disclosed are compositions and methods related to identification of modulators of EGFR and VEGFR. | 2012-11-22 |
20120295966 | Chromone Inhibitors of S-Nitrosoglutathione Reductase - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 2012-11-22 |
20120295967 | HIGH CONCENTRATION OLOPATADINE OPHTHALMIC COMPOSITION - The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis. | 2012-11-22 |
20120295968 | Pharmaceutical Composition Comprising Cannabinoids - The present invention relates to a pharmaceutical composition comprising Δ9 Tetrahydrocannabinol (THC), Cannabidiol (CBD), and at least one small molecule selected from Citric Acid, Ascorbic Acid, Citrus Essential Oil(s), Lecithin, one or more sugar(s), Resvertrol, and combinations thereof, wherein the composition exhibits an increased but negated psychoactivity with concurrent enhancement in therapeutic potency of THC and/or CBD. The present invention is further directed to methods of treating one or more disease(s) or disorder(s) modulated by the activation of the Cannabinoid CB1 and/or CB2 receptors, by administering a therapeutically effective amount of the composition of the present invention to a subject in need thereof. | 2012-11-22 |
20120295969 | Novel Muscle Relaxant Using Negatively Charged Gold with Choline - In order to achieve muscle relaxing effect and anti-atrial fibrillation effect, the present invention provides gold nanoparticles complexes. Gold nanoparticles complexes include negatively charged gold nanoparticles bound to choline or spermidine through ionic bonds according to the purpose to be achieved, which form gold nanoparticles-choline complexes or gold nanoparticles-spermidine complexes. The complexes migrate to an acetylcholine receptor and then the ionic bonds of the complexes are broken, thereby inducing gold-sulfur bonds in the Cys loop of an acetylcholine receptor, thus block the ionic path and achieve the effects. | 2012-11-22 |
20120295970 | THERAPEUTIC COMPOSITIONS - Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. | 2012-11-22 |
20120295971 | THERAPEUTIC COMPOSITIONS - Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. | 2012-11-22 |
20120295972 | Ester Derivatives of Bimatoprost Compositions and Methods - Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same. | 2012-11-22 |
20120295973 | METHODS AND COMPOSITIONS OF DERIVATIVES OF PROBUCOL FOR THE TREATMENT OF DIABETES - This present invention provides methods and pharmaceutical compositions for the treatment or prophylaxis of diabetes and related disorders, comprising the administration of an effective amount of a monoester of probucol, particularly the monosuccinic acid ester, or a pharmaceutically acceptable salt or derivative thereof. | 2012-11-22 |
20120295974 | TRANS-, TRANS-CONJUGATED LINOLEIC ACID COMPOSITIONS AND USE THEREOF - This invention relates generally to trans-,trans-conjugated linoleic acid compositions and use thereof, and in particular to trans-,trans-conjugated linoleic acid produced from photoisomerization of soy oil in the presence of an antioxidant, and used in pharmaceutical, nutraceutical and human and animal food compositions for improved health. The invention also relates generally to a method for treatment and prevention of health-related disorders of obesity by administration of pharmaceutical, nutraceutical and/or food compositions containing and/or prepared from trans-,trans-conjugated linoleic acid-rich soy oil. | 2012-11-22 |
20120295975 | METHODS OF TREATING INFLAMMATORY CONDITIONS - The present invention provides methods of treating a β-arrestin2 mediated and/or GPR120 mediated response in a subject. The β-arrestin2 mediated and/or GPR120 mediated response can be inflammation, including diabetes, inflammation associated with obesity and obesity. The methods can comprise administering to a subject a therapeutically effective amount of a compound predicted to bind a β-arrestin2 molecule and/or GPR120, wherein the compound selectively activates a β-arrestin2-dependent signaling pathway of GPR120. | 2012-11-22 |
20120295976 | COMPOSITION AND/OR METHOD FOR PREVENTING RECURRENCE OF STROKE - By using a composition for preventing onset and/or recurrence of stroke which contains ethyl icosapentate as its effective component, onset and/or recurrence of stroke is prevented, or in particular, the onset and/or recurrence of stroke in a hyperlipidemia patient who has been treated with HMG-CoA RI, or in particular the recurrence of stroke in a patient who is beyond six months after the onset of stroke, is prevented. | 2012-11-22 |
20120295977 | Organosulfur prodrugs for the prevention and treatment of infectious diseases - A method for enhancing the overall beneficial immune system response in a host that works in conjunction with the host's natural immune system response to enhance the host's ability to eliminate infectious microbes while simultaneously suppressing the toxicity of the immune system response to the host. Allium related organosulfur compounds are disclosed which have a various antimicrobial immunomodulatory properties that work together with the host's immune system in the prevention and treatment of disease. Prophylactic and therapeutic treatment is provided by administering an allium related organosulfur compound such that a localized thiosulfinate is caused to be non-enzymatically formed in response to localized generation by activated immune system cells of reactive oxygen species such as hydrogen peroxide. Suitable allium related organosulfur compounds may be administered to the host in an efficient manner through the use of S-AllylMercapto-N-AcetylCysteine (SAMNAC) or similar prodrugs. | 2012-11-22 |
20120295978 | DICLOFENAC GEL - The present invention provides a gel formulation comprising diclofenac sodium which has superior transdermal flux properties, which may be used for the topical treatment of pain, such as in osteoarthritis. | 2012-11-22 |
20120295979 | USE OF SULINDAC FOR PROTECTING RETINAL PIGMENT EPITHELIAL CELLS AGAINST OXIDATIVE STRESS - Compositions and methods described herein are based on the use of the drug sulindac, a non steroidal anti-inflammatory drug (NSAID), for protecting retinal pigment epithelial cells against oxidative stress which is a major component of macular degeneration. Described herein is a new use for sulindac. | 2012-11-22 |
20120295980 | COMPOUNDS AND METHODS FOR DELIVERY OF PROSTACYCLIN ANALOGS - This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula: | 2012-11-22 |