19th week of 2014 patent applcation highlights part 51 |
Patent application number | Title | Published |
20140128367 | CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS - The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R | 2014-05-08 |
20140128368 | SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. | 2014-05-08 |
20140128369 | NOVEL BENZYL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2014-05-08 |
20140128370 | Tetrahydro-Pyrido-Pyrimidine Derivatives - The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), | 2014-05-08 |
20140128371 | CHEMICAL COMPOUNDS 542 - The present invention relates to compounds of Formula (I): | 2014-05-08 |
20140128372 | Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2014-05-08 |
20140128373 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 2014-05-08 |
20140128374 | HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS - The present invention provides, in part, compounds of Formula I: | 2014-05-08 |
20140128375 | BENZAZEPINE COMPOUNDS AS CGRP RECEPTOR ANTAGONISTS - Compounds of formula I: | 2014-05-08 |
20140128376 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2014-05-08 |
20140128377 | METHODS OF TREATING REFRACTORY REPETITIVE SEIZURES - The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus. | 2014-05-08 |
20140128378 | METHODS OF TREATING EPILEPTOGENESIS - The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus. | 2014-05-08 |
20140128379 | NASAL FORMULATIONS OF BENZODIAZEPINE - The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal. | 2014-05-08 |
20140128380 | METHODS OF MODULATING THE ACTIVITY OF THE MC1 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR - The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain. | 2014-05-08 |
20140128381 | Intranasal Benzodiazepine Pharmaceutical Compositions - The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition. | 2014-05-08 |
20140128382 | 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO- AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed. | 2014-05-08 |
20140128383 | INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES - The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV. | 2014-05-08 |
20140128384 | TUMOR TARGETED DRUG COMBRETASTATIN A4 DERIVATIVE - The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect. | 2014-05-08 |
20140128385 | BACE-2 INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased β cell mass and/or function. | 2014-05-08 |
20140128386 | Hydroxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2014-05-08 |
20140128387 | CERTAIN PROTEIN KINASE INHIBITORS - Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof. | 2014-05-08 |
20140128388 | TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX - Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro. | 2014-05-08 |
20140128389 | DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds. | 2014-05-08 |
20140128390 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases. | 2014-05-08 |
20140128391 | SELECTIVE HDAC1 AND HDAC2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV. | 2014-05-08 |
20140128392 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds of Formula IIa: | 2014-05-08 |
20140128393 | Methods of Treating Cancer - The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 2014-05-08 |
20140128394 | PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE - This invention relates to a piperazine compound represented by Formula (I), | 2014-05-08 |
20140128395 | Novel Method - There is provided inter alia a compound which is an NK-1 receptor antagonist for use in the treatment or prevention of CNV. There is also provided a compound which is an NK-1 antagonist for use in the treatment of chemical burns of the eye particularly alkali burns of the eye. There is also provided a pharmaceutical composition for topical administration to the eye comprising an NK-1 antagonist and an antibiotic agent. | 2014-05-08 |
20140128396 | PYRIMIDINYL PYRIDAZINONE DERIVATIVES - Compounds selected from the group according to Claim | 2014-05-08 |
20140128397 | SYNTHETIC LETHAL TARGETING OF GLUCOSE TRANSPORT - The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells. | 2014-05-08 |
20140128398 | COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OXIDATIVE DNA DAMAGE DISORDERS - Compounds, compositions, and formulations, and accompanying methods useful for treating disorders arising from oxidative DNA damage, including oxidative DNA damage resulting from ionizing radiation or other therapy are described herein. | 2014-05-08 |
20140128400 | BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 2014-05-08 |
20140128401 | 8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS - 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X | 2014-05-08 |
20140128402 | PHARMACEUTICAL COMBINATION - The present invention discloses a pharmaceutical combination comprising Hydroxychloroquine and a DPP-IV inhibitor or their pharmaceutically acceptable salts, solvates or prodrugs thereof, for preventing, slowing the progression of, delaying, improving, restoring, or treating a condition or a disease resulting from metabolic disorders. | 2014-05-08 |
20140128403 | USE OF 10H-BENZO[G]PTERIDINE-2,4-DIONE DERIVATIVES - Use of 10H-benzo[g]pteridine-2,4-dione derivatives as photosensitizers in the inactivation of microorganisms. | 2014-05-08 |
20140128404 | 1, 2, 4-Thiadiazol-5-Ylpiperazine derivatives useful in the treatment of neurodegenerative diseases - The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. | 2014-05-08 |
20140128405 | Composition and use for phosphodiesterase inhibitors - Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt. | 2014-05-08 |
20140128406 | MICROBIOCIDAL HETEROCYCLES - The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R | 2014-05-08 |
20140128407 | FAST DISSOLVING AZAPERONE GRANULATE FORMULATION - The present invention relates to a fast dissolving granulate formulation containing the veterinary drug azaperone and a method for preparing said granulate formulation. | 2014-05-08 |
20140128408 | HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed. | 2014-05-08 |
20140128409 | MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES - The present invention relates to the use of indolinones of general formula | 2014-05-08 |
20140128410 | TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 2014-05-08 |
20140128411 | FUNGICIDAL COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a fungicidal composition useful as an agricultural and horticultural fungicide having remarkably improved controlling effects against plant diseases, and a method for controlling plant diseases using the composition. A fungicidal composition comprising, as active ingredients, (a) 3-(2,3,4-trimethoxy-6-methylbenzoyl)-5-chloro-2-methoxy-4-methyl-pyridine (pyriofenone) or its salt and (b) at least one fungicide selected from the group consisting of bixafen, fluxapyroxad, penflufen, isopyrazam, fluopyram, ametoctradin, fenpyrazamine and sedaxane, and a method for controlling plant diseases, which comprises applying the fungicidal composition to plants. | 2014-05-08 |
20140128412 | COMBINATION OF AN ANTIPSYCHOTIC AND AN ANTI-INFLAMMATORY AGENT - The present invention relates to a pharmaceutical composition comprising an antipsychotic in combination with an anti-inflammatory agent, and to the use thereof in the treatment of psychotic disorder, and in particular, of schizophrenia. | 2014-05-08 |
20140128413 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2014-05-08 |
20140128414 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2014-05-08 |
20140128415 | EXCIPIENT DRUG COMPOSITION - A excipient drug composition is disclosed. The excipient drug composition may include a vegetable cellulose or a fruit cellulose, an active ingredient and a genetically modified organism free starch. The vegetable cellulose or fruit cellulose may be derived from wood free vegetable pulp and the fruit cellulose is a wood pulp free cellulose. The genetically modified organism free starch may be selected from the group consisting of a genetically modified organism free rice starch, a genetically modified organism free potato starch or a genetically modified organism free pea starch. | 2014-05-08 |
20140128416 | MEDICAL DEVICES INCORPORATING COLLAGEN INHIBITORS - Provided herein are implantable or insertable biomedical devices comprising a substrate and a collagen inhibitor on or in said substrate, and methods of treatment using the same. In some embodiments, the device is a urethral, ureteral, or nephroureteral catheter or stent. In some embodiments, the device is an absorbable esophageal or tracheal stent. Wound closure devices are also provided herein, including a substrate and a collagen inhibitor on or in the substrate. Also provided are surgical packings, including a substrate and a collagen inhibitor on or in the substrate. A barrier material for preventing adhesions in a subject is further provided, including a preformed or in situ formable barrier substrate and a collagen inhibitor on or in the substrate. Kits comprising the coated substrates are also provided. | 2014-05-08 |
20140128417 | ALKYNE SUBSTITUTED QUINAZOLINE COMPOUND AND METHODS OF USE - The invention provides alkyne substituted quinazoline compounds, such as compounds of the formula (I), which are irreversible ErbB kinase inhibitors. The compounds are useful in the treatment of diseases and disorders where ErbB kinase activity is implicated such as a hyperproliferative disorder (e.g., cancer). | 2014-05-08 |
20140128418 | PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND COMPOSITION FOR PREVENTING AND TREATING OSTEOPOROSIS CONTAINING SAME - The present invention provides a pyrazole derivative compound and a pharmaceutically acceptable salt thereof. The compound of the invention is remarkably effective for preventing and treating osteoporosis. | 2014-05-08 |
20140128419 | Rifaximin - Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa. | 2014-05-08 |
20140128420 | NUTRITIONAL SUPPLEMENT COMPOSITIONS - Dietary supplement compositions containing one or more compounds such as arginine, selenium, calcium, calcium sources, morphine precursors (e.g., reticuline), morphine, and morphine-6β-glucuronide are provided. | 2014-05-08 |
20140128421 | CAMPTOTHECIN COMPOUND CONTAINING STABLE 7-MEMBERED LACTONE RING, PREPARATION METHOD AND USE - Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R | 2014-05-08 |
20140128422 | NEW THERAPEUTICAL COMPOSITION CONTAINING APOMORPHINE AS ACTIVE INGREDIENT - A pharmaceutical composition contains apomorphine as the active pharmaceutical ingredient, a water-miscible co-solvent, an antioxidant, and water. The solution has a pH greater than 4. The pharmaceutical composition is suitable for parenteral administration for the treatment of Parkinson's disease. The process for the manufacture of the pharmaceutical composition includes weighing the apomorphine and introducing it into a container with the co-solvent and the antioxidant under agitation until complete dissolution takes place. | 2014-05-08 |
20140128423 | Acridone Compounds - A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia. | 2014-05-08 |
20140128424 | Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2014-05-08 |
20140128425 | Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use - The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2014-05-08 |
20140128426 | Antiviral Drugs for Treatment of Arenavirus Infection - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the | 2014-05-08 |
20140128427 | 5-CARBAMOYL-ADAMANTAN-2-YL AMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND PREPARATION PROCESS THEREOF - Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11β-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11β-hydroxystreroid dehydrogenase type 1. | 2014-05-08 |
20140128428 | COLD MENTHOL RECEPTOR ANTAGONISTS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2014-05-08 |
20140128429 | NEW IMIDAZOLYLKETONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 2014-05-08 |
20140128430 | AMINE SALTS OF LAQUINIMOD - The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine. | 2014-05-08 |
20140128431 | PHARMACEUTICAL COMPOSITION WITH IMPROVED BIOAVAILABILITY, SAFETY AND TOLERABILITY - The invention relates to solid dispersions of poorly soluble compounds formed by coprecipitation, resulting in improved bioavailability, safety and tolerability. The invention also relates to Purified Eudragit L100-55 used to prepare such solid dispersions. | 2014-05-08 |
20140128432 | ANAPLASTIC THYROID CANCERS HARBOR NOVEL ONCOGENIC MUTATIONS OF THE ALK GENE - The present invention relates to diagnostic, therapeutic and prognostic methods for thyroid cancers. In one embodiment, the present invention provides a method for treating a an anaplastic thyroid cancer (ATC) patient comprising the step of administering to the patient an effective amount of an anaplastic lymphoma kinase (ALK) inhibitor. In another embodiment, a method for diagnosing ATC in patient comprises the step of performing an assay on a biological sample from the patient to identify the presence or absence of a C3592T and/or a G3602A mutation in exon 23 of the ALK gene according to SEQ ID NO:6, wherein the presence of either of both of the mutations correlates with a diagnosis of ATC in the patient. | 2014-05-08 |
20140128433 | METHODS FOR THE ADMINISTRATION OF ILOPERIDONE - The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms. | 2014-05-08 |
20140128434 | METHOD OF ADMINISTRATION AND TREATMENT - This invention relates to a method of treating cancer in a human in need thereof by determining the presence or absence of a detectable amount of a gene product of the Neurofibromin-2 (NF2) gene in a sample from the human, and administering to the human an effective amount of a focal adhesion kinase (FAK) inhibitor, or a pharmaceutically acceptable salt thereof, if no gene product or no isoform 1 gene product is detected. This invention also relates to a method of treating cancer in a human in need thereof, comprising determining the presence or absence of a detectable amount of a functional isoform 1 protein of the NF2 gene, or a functional fragment thereof, in a sample from the human, and administering to the human an effective amount of a focal adhesion kinase (FAK) inhibitor, or a pharmaceutically acceptable salt thereof, if no gene product or no isoform 1 gene product is detected. | 2014-05-08 |
20140128435 | SUBSTITUTED PYRAZOLES AS ESTROGEN RECEPTOR LIGANDS - The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R | 2014-05-08 |
20140128436 | PRODRUGS OF INHIBITORS OF PLASMA KALLIKREIN - The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula: | 2014-05-08 |
20140128437 | HETEROCYCLIC INHIBITORS OF NECROPTOSIS - The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. | 2014-05-08 |
20140128438 | Methods for Treating Gout Flares - Methods of treating gout flares comprising administering a composition comprising a first urate-lowering agent are disclosed. In some aspects, the first urate-lowering agent is (−)-halofenate, (−)-halofenic acid, or a pharmaceutically acceptable salt thereof. Other aspects provide for methods of reducing the number, duration, frequency or intensity of gout flares experienced by a subject. | 2014-05-08 |
20140128439 | Methods for Treating Gout Flares - Methods of treating gout flares comprising administering a composition comprising a first urate-lowering agent are disclosed. In some aspects, the first urate-lowering agent is (−)-halofenate, (−)-halofenic acid, or a pharmaceutically acceptable salt thereof. Other aspects provide for methods of reducing the number, duration, frequency or intensity of gout flares experienced by a subject. | 2014-05-08 |
20140128440 | MICROBICIDAL COMPOSITION - Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one. | 2014-05-08 |
20140128441 | NOVEL EP4 AGONIST - Provided is a compound represented by the formula (1): | 2014-05-08 |
20140128442 | PREPARATION OF AND FORMULATION COMPRISING A MEK INHIBITOR - The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound. | 2014-05-08 |
20140128443 | Liquid Formulations Of Bendamustine - Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described. | 2014-05-08 |
20140128444 | NOVEL CRYSTALLINE SALTS OF ASENAPINE WITH ORGANIC DI-ACIDS AND TRI-ACIDS - Novel crystalline salts of Asenapine (I) with organic di-acids and tri-acids and to methods of their preparation are disclosed along with related pharmaceutical compositions and methods of treating psychotic diseases or disorders. | 2014-05-08 |
20140128445 | POLYMERIC BENZYL CARBONATE-DERIVATIVES - The present invention relates to polymeric derivatives, which can be conjugated to an amino-containing drug to improve its in vivo properties. The polymeric derivative can subsequently be released to yield the drug in its native form. Methods of preparing and using these polymeric derivatives and drug conjugates are described. | 2014-05-08 |
20140128446 | 2-Methylthiopyrrolidines and Their Use for Modulating Bacterial Quorum Sensing - Compounds of Formula (I) are disclosed herein and their use in inhibiting quorum sensing in bacteria. | 2014-05-08 |
20140128447 | NOVEL NON-PRIMATE HEPACIVIRUS - The invention is directed to immunogenic compositions and methods for inducing an immune response against Non-Primate Hepacivirus in an animal. In another aspect, the invention relates to antibodies that bind Non-Primate Hepacivirus polypeptides. In yet another aspect, the invention relates to methods for preventing, or reducing NPHV infection in an animal. | 2014-05-08 |
20140128448 | NUCLEIC ACID/POLYSACCHARIDE COMPLEX - An object of the present invention is to provide a highly stable nucleic acid-polysaccharide complex of an siRNA and schizophyllan. A nucleic acid-polysaccharide complex is formed by adding polydeoxyadenine in which at least part of the phosphodiester link portion is phosphorothioated to an siRNA and allowing the siRNA and schizophyllan to form a complex. | 2014-05-08 |
20140128449 | OLIGONUCLEOTIDE MODULATION OF SPLICING - The present invention relates to the selective modulation of pre-mRNA splicing, in particular, for that involving alternative splicing in disease-related proteins such as those involved in Duschenne's Muscular Dystropy and Spinal Muscular Atrophy. | 2014-05-08 |
20140128450 | Cancer Therapy - The present invention provides a method for treating a hyperproliferative disorder characterized by expression of a mutant form of p53 in a subject, the method comprising administering to the subject a therapeutically effective amount of an agent which inhibits promyelocytic leukemia (PML) protein. | 2014-05-08 |
20140128451 | Compositions and Methods for Delivery of MicroRNA to Cells - Provided herein are gold nanoparticles mediated non-viral delivery of miRNAs, siRNAs, genes and drugs. Nanoparticle platforms and combinatorial drug delivery vehicles comprises gold nanoparticles with a plurality of thilolated hyperbranched dendrons conjugated to the nanoparticle surface. The thiolated hyperbranched dendrons comprise chemically-modifiable surface groups, functionalized interior groups and nano-cavities within the hyperbranched structure to which a variety of payload molecules may be conjugated, optionally via a linker. Payload molecules may comprise nucleic acids, anticancer drugs and small molecule inhibitors, optionally with, non-cytotoxic signaling agents, for example, fluoroscein isothiocyanate. Successful manipulation of the degree of PEGylation and the amount of gold nanoparticles in a polyelectrolyte complex to evaluate the best formulation for highest payload delivery of chemically unmodified miRNA duplexes and stemloops is presented. Also provided are methods for delivering one or more therapeutic agents to a cell or tissue or for treating a pathophysiological condition in a subject by delivering the combinatorial drug delivery vehicles to a cell or tissue associated with the pathophysiological condition to facilitate internalization of the vehicle to effect treatment. | 2014-05-08 |
20140128452 | SUGAR CHAIN-RELATED GENE AND USE THEREOF - As a result of dedicated studies, the present inventors succeeded in discovering, for the first time, that fibrogenesis could be suppressed at the physiological tissue level by inhibiting sulfation at position 4 or 6 of GalNAc, which is a sugar that constitutes sugar chains. Furthermore, the present inventors conducted studies using various disease model animals, and as a result, successfully demonstrated that inhibitors of sulfation at position 4 or 6 of GalNAc had therapeutic effects on diseases caused by tissue fibrogenesis (tissue fibrogenic disorders). | 2014-05-08 |
20140128453 | MODULATION OF APOLIPOPROTEIN CIII (APOCIII) EXPRESSION - Provided herein are methods, compounds, and compositions for reducing expression of ApoCIII mRNA and protein in an animal. Also provided herein are methods, compounds, and compositions for increasing HDL levels and/or improving the ratio of TG to HDL and reducing plasma lipids and plasma glucose in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate any one or more of cardiovascular disease or metabolic disorder, or a symptom thereof. | 2014-05-08 |
20140128454 | NUCLEIC ACID MODULATORS OF GLYCOPROTEIN VI - The present invention relates, in general, to a pharmacologic system to modulate the biology of platelets based upon a nucleic acid ligand that can interact with and modulate the activity of platelet glycoprotein GPVI to regulate platelet function. These nucleic acid ligands are also actively reversible using a modulator that inhibits the activity of the nucleic acid ligand to neutralize this pharmacologic effect and thereby restore GPVI function, including collagen binding, platelet adhesion, collagen-induced platelet activation, and collagen-induced platelet aggregation. The invention further relates to compositions comprising the nucleic acid ligand, the ligand and a modulator, methods to generate the nucleic acid ligand and its modulator, as well as methods of using these agents and compositions in medical therapeutic and diagnostic procedures. | 2014-05-08 |
20140128455 | DIAGNOSIS AND TREATMENT OF FRIEDREICH'S ATAXIA - The present invention is directed to oligonucleotides based on peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences and the use of such oligonucleotides for the dissociation of higher order structures, including triplex-helix DNA structures, in repeated sequences of DNA in Friedreich's ataxia. The dissociation of such structures may be used in the diagnosis and/or treatment of Friedreich's ataxia. Consequently, the present invention is also directed to a method for diagnosing Friedreich's ataxia and the use of peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences in the treatment of Friedreich's ataxia. Preferably, the oligonucleotides comprise a sequence selected from the group consisting of (GAA) | 2014-05-08 |
20140128456 | Compounds and methods for the treatment of inflammatory diseases of the CNS - Inflammatory diseases in the CNS can be treated or alleviated by the administration of an oligonucleotide in an amount sufficient to reduce the influx of mononuclear cells to the central nervous system by down-regulating the expression of at least one cell surface marker. For example multiple sclerosis can be treated or at least alleviated, by the administration of an oligonucleotide in a dose effective to inhibit or reduce the influx of mononuclear and/or autoaggressive cells to the central nervous system. The oligonucleotide can be used alone, or in combination with other treatment strategies. | 2014-05-08 |
20140128457 | THERAPEUTIC RIBONUCLEASES - The present invention relates to the use of ribonucleases (RNases) in the treatment or prevention of disease. | 2014-05-08 |
20140128458 | POLYCYCLIC COMPOUNDS AND METHODS RELATED THERETO - The invention relates to a novel compound of the formula | 2014-05-08 |
20140128459 | SOLID FORMS OF ORTATAXEL - The present invention relates to solid forms of 13-(N-Boc-β-isobutylserinyl)-14-βhydroxybaccatin III 1, 14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water. | 2014-05-08 |
20140128460 | USE OF SMALL MOLECULE INHIBITORS TARGETING EYA TYROSINE PHOSPHATASE - Inhibitors of EYA tyrosine phosphatase are provided herein, as well as pharmaceutical compositions and methods relating thereto. | 2014-05-08 |
20140128461 | USE OF A FOOD COMPOSITION IN THE TREATMENT AND/OR PREVENTION OF NEUROPATHIC PAIN INDUCED BY AN ANTICANCER AGENT - The invention relates to the use of a low-polyamine-content food composition for use in the treatment and/or prevention of neuropathic pain induced by a platinum salt. | 2014-05-08 |
20140128462 | LYOPHILIZED PREPARATION OF CYTOTOXIC DIPEPTIDES - The present invention is directed to novel lyophilized pharmaceutical preparations comprising a cytotoxic dipeptides such as melphalan flufenamide and one or more excipient(s) selected from the group comprising a polysorbate; a polyethylene glycol; β-cyclodextrin; ocyclodextrin; hydroxypropyl-β-cyclodextrin; sulfobutylether-β-cyclodextrin; lactose; benzyl alcohol; disodium succinate; propylene glycol; Cremophor EL; Dimethyl sulfoxide; D-mannitol; Trehalose; Sucrose and an amino acid. This preparation may be further formulated and is useful in cancer therapy. | 2014-05-08 |
20140128463 | AMIDE COMPOUND, PREPARATION METHOD AND USES THEREOF - Disclosed are amide compounds, preparation method and uses thereof, specifically, the compounds represented by formula I or pharmaceutically acceptable salts, wherein R | 2014-05-08 |
20140128464 | COMPOSITIONS AND METHODS FOR TREATING AND/OR PREVENTING CARDIOVASCULAR DISEASE - In various embodiments, the present invention provides pharmaceutical compositions comprising fatty acids and methods for treating subjects using same. | 2014-05-08 |
20140128465 | PRODUCTION AND PURIFICATION OF ESTERS OF POLYUNSATURATED FATTY ACIDS - The present invention includes methods for producing and purifying esters of polyunsaturated fatty acids that include reacting a composition having triglycerides with polyunsaturated fatty acid residues in the presence of an alcohol and a base to produce an ester of a polyunsaturated fatty acid from the triglycerides. The composition can be a polyunsaturated fatty acid-containing composition that has not been conventionally processed. The reacted composition can be further processed by distillation. | 2014-05-08 |
20140128466 | COMPOUNDS FOR USE IN THE TREATMENT OF INFLAMMATORY BOWEL DISEASE - Described are compounds of the structural formula (I): Also provided are pharmacologically acceptable isomers and salts of the compound of (I). The compounds are useful in the treatment of inflammatory bowel disease. | 2014-05-08 |
20140128467 | METHODS OF TREATMENT USING A BCAT1 INHIBITOR - The present invention is directed to methods of using inhibitors of the cytosolic form of BCAT in the treatment of cancer, rheumatoid arthritis, and bone disease. | 2014-05-08 |