09th week of 2015 patent applcation highlights part 47 |
Patent application number | Title | Published |
20150057259 | STABILIZED COMPOSITIONS CONTAINING ALKALINE LABILE DRUGS - A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion. Various functional excipients can be included in the carrier system to improve process performance and/or improve the chemical or physical properties of the HME composition. | 2015-02-26 |
20150057260 | ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0): | 2015-02-26 |
20150057261 | AZETIDINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - The present invention relates to azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2015-02-26 |
20150057262 | CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (Ia): | 2015-02-26 |
20150057263 | Quinazoline Compounds And Their Use In Therapy - This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect. | 2015-02-26 |
20150057264 | BICYCLIC PYRAZINONE DERIVATIVES - Compounds of the formula I | 2015-02-26 |
20150057265 | FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS - The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases. | 2015-02-26 |
20150057266 | Pharmaceutical Composition Having Improved Dissolution Profiles For Poorly Soluble Drugs - Pharmaceutical compositions having improved dissolution profiles for drugs therein are disclosed. | 2015-02-26 |
20150057267 | Methods and Compositions for Treating Viral Diseases - The invention provides a method for treating viral infections and coinfections through the use of inhibitory agents that prevent a unique viral structural protein motifs from binding to host proteins from the clathrin adaptor proteins family and subsequently preventing viral replication. | 2015-02-26 |
20150057268 | COMPOSITION AND METHOD FOR NEUROPEPTIDE S RECEPTOR (NPSR) ANTAGONISTS - Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor. | 2015-02-26 |
20150057269 | COMPOSITIONS AND METHODS FOR THE MODULATION OF SPECIFIC AMIDASES FOR N-ACYLETHANOLAMINES FOR USE IN THE THERAPY OF INFLAMMATORY DISEASES - The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH | 2015-02-26 |
20150057270 | CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS - The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spiro-cyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation in vivo. Methods of synthesis and biological methods and data are also provided. | 2015-02-26 |
20150057271 | DIHYDROBENZOXAZINE AND TETRAHYDROQUINOXALINE SODIUM CHANNEL INHIBITORS - The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. | 2015-02-26 |
20150057272 | BENZIMIDAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2015-02-26 |
20150057273 | KINASE INHIBITORS - Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract. | 2015-02-26 |
20150057274 | TRIAZOLOTHIENOPYRIMIDINE COMPOUND INHIBITORS OF UREA TRANSPORTERS AND METHODS OF USING INHIBITORS - Provided herein are small molecule triazolothienopyrimidine compounds that inhibit urea transport activity of solute transporters, particularly the UT-B transporter. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating refractory edema associated with cardiovascular, renal, and metabolic diseases, disorders, and conditions. | 2015-02-26 |
20150057275 | METHODS AND MATERIALS FOR GENETIC ANALYSIS OF TUMORS - This invention relates generally to methods and materials for rapid detection of mutations for tumor genotyping. | 2015-02-26 |
20150057276 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. | 2015-02-26 |
20150057277 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Chemical entities that are quinoxaline kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. | 2015-02-26 |
20150057278 | AMIDO COMPOUNDS AS RORyT MODULATORS AND USES THEREOF - Amido compounds are disclosed that have a formula represented by the following: | 2015-02-26 |
20150057279 | HETEROARYL COMPOUNDS WITH A-CYCLIC BRIDGING UNIT - This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such 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. This invention also relates to pharmaceutical compositions and kits comprising the compounds. | 2015-02-26 |
20150057280 | N-substituted pyridinylidene compounds and derivatives for combating animal pests - The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. | 2015-02-26 |
20150057281 | MODULATORS OF HEC1 ACTIVITY AND METHODS THEREFOR - Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases. | 2015-02-26 |
20150057282 | OXAZOLE TYROSINE KINASE INHIBITORS - The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar | 2015-02-26 |
20150057283 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 2015-02-26 |
20150057284 | METHOD AND IMPROVED PHARMACEUTICAL COMPOSITION FOR ENHANCING TRANSDERMAL DELIVERY OF PDE-5 INHIBITOR - The present disclosure relates to the use of an agent that enhances transdermal delivery of a PDE-5 inhibitor. More particularly, the present disclosure provides improved method and composition that promotes transdermal delivery of a PDE-5 inhibitor for the treatment of the PDE-5 mediated conditions and/or diseases. | 2015-02-26 |
20150057285 | BENZYL SUBSTITUTED TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS - The invention provides triazine compounds and methods of their use to modulate protein kinases and to treat diseases mediated by said protein kinases. | 2015-02-26 |
20150057286 | NEW BIS-AMIDO PYRIDINES - This invention relates to bis-amido pyridines of general formula (I) | 2015-02-26 |
20150057287 | METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 2015-02-26 |
20150057288 | PEST CONTROL AGENTS FOR HONEYBEE PARASITIC PESTS, AND PEST CONTROL METHOD FOR HONEYBEE PARASITIC PESTS USING THE PEST CONTROL AGENTS - A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof. | 2015-02-26 |
20150057289 | BICYCLO[3.2.1.]OCTYL AMIDE DERIVATIVES AND USES OF SAME - The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): | 2015-02-26 |
20150057290 | METHOD OF USING FLIBANSERIN FOR NEUROPROTECTION - The present invention relates to the use of 1-[2-(4-(3-trifluoromethyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one, optionally in the form of its pharmaceutically acceptable acid addition salts and optionally in the form of its hydrates or solvates, for preparing a pharmaceutical composition with a neuroprotective activity. | 2015-02-26 |
20150057291 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer. | 2015-02-26 |
20150057292 | SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer. | 2015-02-26 |
20150057293 | NEW COMPOUNDS - The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 2015-02-26 |
20150057294 | 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS - The present invention relates to the 1H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain. | 2015-02-26 |
20150057295 | New 6-Alkynyl Pyridine - This invention relates to 6-alkynyl-pyridine of general formula (I) | 2015-02-26 |
20150057296 | NOVEL PHARMACEUTICAL DOSAGE FORMS COMPRISING VALGANCICLOVIR HYDROCHLORIDE - The present invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms. | 2015-02-26 |
20150057297 | HALOFUGINOL DERIVATIVES AND THEIR USE IN COSMETIC AND PHARMACEUTICAL COMPOSITIONS - The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions. | 2015-02-26 |
20150057298 | NOVEL COMPOUNDS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, | 2015-02-26 |
20150057299 | Methods of Using Diaminopyrimidine P2X3 and P2X 2/3 Receptor Modulators for Treatment of Acute and Sub-Acute Cough, Urge to Cough and Chronic Cough, in Respiratory Diseases - Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): | 2015-02-26 |
20150057300 | SUBSTITUTED PIPERIDINES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted piperidines or pyrrolidines having Formula IA: | 2015-02-26 |
20150057301 | Pro-Neurogenic Compounds - This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death. | 2015-02-26 |
20150057302 | 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. | 2015-02-26 |
20150057303 | SYNTHESIS OF (R)-N-METHYLNALTREXONE - This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use. | 2015-02-26 |
20150057304 | Extruded Immediate Release Abuse Deterrent Pill - The present disclosure relates to an oral, immediate release, abuse deterrent pill containing at least one active pharmaceutical ingredient susceptible to abuse which is homogenously spread throughout a carrier matrix used to deter abuse. The pill is prepared using hot melt extrusion and a forming unit through a continuous process. The formed pill is abuse deterrent to parenteral administration due at least to particle size, viscosity, or purity limitations. | 2015-02-26 |
20150057305 | PHARMACEUTICAL COMPOSITION - Disclosed in the present invention is a pharmaceutical composition, comprising a weight ratio of 1:120 to 1:1000 of camptothecin compound of formula I and β-cyclodextrin or derivatives thereof, and an acidic buffer to adjust the pH=3.5-6.0. The composition can be used to treat solid tumours, such as melanoma, pancreatic cancer, hepatoma etc. The pharmaceutical composition of the present invention is miscible with a water-miscible co-solvent system in any proportion, and can be used as an intravenous infusion solvent, and has no obvious hemolysis or vascular stimulation; the pharmaceutical composition has a better tumour inhibiting rate than solubilisation of surfactants. | 2015-02-26 |
20150057306 | COMPOSITIONS COMPRISING SCOPOLAMINE AND KETAMINE IN THE TREATMENT OF DEPRESSION - Described are compositions and methods for administering scopolamine and ketamine in the treatment of depression (e.g., Major Depressive Disorder and Treatment-Resistant Depression). | 2015-02-26 |
20150057307 | NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS - Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided. | 2015-02-26 |
20150057308 | Fluorinated 3-(2-Oxo-3-(3-Arylpropyl)Imidazolidin-1-yl)-3-Arylpropanoic Acid Derivatives - The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3 -arylpropyl)imidazolidin-1-yl)-3 -arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described. | 2015-02-26 |
20150057309 | 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 C-MET PROTEIN, ETC - The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them. | 2015-02-26 |
20150057310 | Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. | 2015-02-26 |
20150057311 | Heterocyclic GSK-3 Allosteric Modulators - The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein GSK-3 is involved, such as neurodegenerative diseases, inflammatory diseases, cancer, diabetes, and to promote various regenerative processes. | 2015-02-26 |
20150057312 | SUBSTITUTED QUINOLINES AS BRUTON'S TYROSINE KINASES INHIBITORS - The present invention is directed to novel quinolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. The disclosed substituted quinolines include Bruton's tyrosine kinase (Btk) inhibitors. | 2015-02-26 |
20150057313 | MODULATING AFFERENT SIGNALS TO TREAT MEDICAL CONDITIONS - This document provides methods and materials for modulating afferent nerve signals to treat medical conditions such as CHF, CHF respiration, dyspnea, peripheral vascular disease (e.g., peripheral arterial disease or venous insufficiency), hypertension (e.g., age-associated hypertension, resistant hypertension, or chronic refractory hypertension), COPD, sleep apnea, and chronic forms of lung disease where muscle dysfunction is a part of the disease pathophysiology. For example, methods and materials involved in using electrical and/or chemical techniques to block or reduce afferent nerve signals (e.g., nerve signals of group III and/or IV afferents coming from skeletal muscle and/or the kidneys) are provided. | 2015-02-26 |
20150057314 | COMPOSITION COMPRISING A COMBINATION OF OMEPRAZOLE AND LANSOPRAZOLE, AND A BUFFERING AGENT, AND METHODS OF USING SAME - The present disclosure relates to pharmaceutical compositions comprising omeprazole, lansoprazole and sodium bicarbonate. Methods of using such compositions are also provided | 2015-02-26 |
20150057315 | Methods for Treatment of 16P11.2 Microdeletion Syndrome - Subjects that have a 16p11.2 microdeletion syndrome are treated by administering compositions that include mGluR inhibitors, including mGluR antagonists that include mGluR negative allosteric modulators. Administration of compositions employed in the methods of the invention can treat psychiatric, including neuropsychiatric disorders, cognitive impairments, attention, obesity, intellectual disability and seizure disorders. | 2015-02-26 |
20150057316 | NOVEL SULFONATE-BASED TRIMEBUTINE SALTS - The present description relates to compounds of Formula I (A | 2015-02-26 |
20150057317 | GABR-A2 DIAGNOSTIC - The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs. | 2015-02-26 |
20150057318 | USE OF SUCCINATE DEHYDROGENASE INHIBITORS (SDHIS) FOR CONTROLLING WOOD DISEASES IN GRAPE - The invention relates to the use of succinate dehydrogenase SDH inhibitors (SDHIs), in particular bixafen, penflufen or fluopyram for controlling wood diseases in grape, to a method for treating plants or plant parts for controlling wood diseases in grape and to a method for controlling wood diseases in grape plants and plant parts, and in plants which grow from the seedlings, grafts and cuttings, by treating them with SDHIs. | 2015-02-26 |
20150057319 | NOVEL CHOLINE COCRYSTAL OF EPALRESTAT - The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients. | 2015-02-26 |
20150057320 | TRANSTHYRETIN LIGANDS CAPABLE OF INHIBITING RETINOL-DEPENDENT RBP4-TTR INTERACTION FOR TREATMENT OF AGE-RELATED MACULAR DEGENERATION, STARGARDT DISEASE, AND OTHER RETINAL DISEASE CHARACTERIZED BY EXCESSIVE LIPOFUSCIN ACCUMULATION - A method for treating a disease characterized by excessive lipofuscin accumulation in the retina of a mammal afflicted therewith comprising administering to the mammal an effective amount of a transthyretin (TTR) ligand. | 2015-02-26 |
20150057321 | SOFT CHEWABLE PHARMACEUTICAL PRODUCTS - A soft chewable pharmaceutical product for delivery of a pharmaceutically acceptable active ingredient to an animal comprising pamoic acid or a pharmaceutically acceptable salt and a process for the manufacture of such soft chewable pharmaceutical product. | 2015-02-26 |
20150057322 | COMPOUNDS CONTAINING S-N-VALERYL-N--VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS - A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi. | 2015-02-26 |
20150057323 | COMPOSITION FOR TREATING OCULAR EFFECTS OF DIABETES - The composition for treating ocular effects of diabetes is a composition that contains an aldose reductase inhibitor in an ophthalmic gel for topical application to the eye. The composition includes a carrier having, by weight, about 0.4% carbomer, 4.0% sorbitol, 0.01% centrimide, 0.01% ethylenediaminetetraacetic acid (EDTA) and effective amounts of sodium chloride and sodium hydroxide for adjusting the pH of the topical carrier to about 7 and to achieve a desired viscosity, with the balance being water. The aldose reductase inhibitor (ARI) is mixed with the topical carrier at about 0.1%-6% by weight of the composition to form an ophthalmic gel. Preferably, the ARI is 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4′-imidazolidine]-2′,5′-dione, referred to as 2-methyl sorbinil, having the structure: | 2015-02-26 |
20150057324 | TABLET CONTAINING 5-HYDROXY-1H-IMIDAZOLE-4-CARBOXAMIDE - The tablet containing (1) 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, and (2) silicon dioxide has a high content of 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof and an easily takable size as a tablet, and shows superior dissolution property. | 2015-02-26 |
20150057325 | COMPOUNDS CAPABLE OF MODULATING/PRESERVING ENDOTHELIAL INTEGRITY FOR USE IN PREVENTION OR TREATMENT OF ACUTE TRAUMATIC COAGULOPATHY AND RESUSCITATED CARDIAC ARREST - The present invention relates to novel uses of compounds that protect the endothelium, particularly prostacyclin and variants and derivatives thereof in the treatment or prevention of acute traumatic coagulopathy (ATC) and of patients resuscitating from cardiac arrest. The invention also relates to a method of identifying individuals at risk of developing ATC. | 2015-02-26 |
20150057326 | Method for Synthesizing Cycloalkanyl[b]indoles, Cycloalkanyl[b]benzofurans, Cycloalkanyl[b]benzothiophenes, Compounds and Methods of Use - A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided. | 2015-02-26 |
20150057327 | KETOROLAC TROMETHAMINE COMPOSITIONS FOR TREATING OR PREVENTING OCULAR PAIN - Compositions comprising ketorolac tromethamine at a therapeutically effective concentration of less than 0.5% are disclosed herein. Methods of treating or preventing ocular pain using said compositions are also disclosed herein. | 2015-02-26 |
20150057328 | PROLINE SULFONAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to (S)-proline sulfonamide compounds of formula (I) | 2015-02-26 |
20150057329 | COMPOUNDS AND METHODS FOR MODULATING EXPRESSION APOB - The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing. | 2015-02-26 |
20150057330 | ANTISENSE OLIGONUCLEOTIDES FOR INDUCING EXON SKIPPING AND METHODS OF USE THEREOF - An antisense molecule capable of binding to a selected target site to induce exon skipping in the dystrophin gene, as set forth in SEQ ID NO: 1 to 202. | 2015-02-26 |
20150057331 | NOVEL CELLULAR TARGETS FOR HIV INFECTION - Methods and compositions are provided for treating HIV infection and for inhibiting HIV infection, and for identifying purinergic receptor antagonists or Panx 1 hemi-channel blockers useful therefor. The invention provides a method of treating a mammalian subject having an HIV infection, or suspected of having been exposed to HIV, comprising administering to the mammalian subject an amount of (i) an antagonist of a Panx 1 hemichannel, or (ii) of an inhibitor of a purinergic receptor, effective to inhibit (a) HIV fusion with a target cell, or (b) HIV replication, or (c) HIV entry into a target cell, or two or more of (a), (b) and (c). | 2015-02-26 |
20150057332 | Methods for the Treatment of Nonalcoholic Steatohepatitis - The present invention relates to the treatment of nonalcoholic steatohepatitis (NASH), in particular to a compound that inhibits miR-21 expression for use in the treatment of nonalcoholic steatohepatitis. | 2015-02-26 |
20150057333 | DOUBLE-STRANDED OLIGONUCLEOTIDES - Antisense sequences, including duplex RNAi compositions, which possess improved properties over those taught in the prior art are disclosed. The invention provides optimized antisense oligomer compositions and method for making and using the both in in vitro systems and therapeutically. The invention also provides methods of making and using the improved antisense oligomer compositions. | 2015-02-26 |
20150057334 | USE OF INHIBITORS OF ZDHHC2 ACTIVITY FOR MODULATION OF ADIPOGENESIS - The present invention concerns Zdhhc2, a new target involved in adipogenesis modulation. Using a siRNA approach, the inventors demonstrated that decrease in Zdhhc2 activity in adipose tissue induces a decrease in adipogenesis. Thus, the present invention relates to modulators of Zdhhc2 activity as well as screening test for identification of modulators of the activity of this target, and their use, especially in pharmaceutical composition, to modulate adipogenesis and thus treat obesity and related disorders. | 2015-02-26 |
20150057335 | NOVEL FUSION GENES IDENTIFIED IN LUNG CANCER - [PROBLEMS] To identify mutations that can serve as indicators for predicting the effectiveness of drug treatments in cancers such as lung cancer; to provide a means for detecting said mutations; and to provide a means for identifying, based on said mutations, patients with cancer or subjects with a risk of cancer, in which drugs targeting genes having said mutations or proteins encoded by said genes show a therapeutic effect. | 2015-02-26 |
20150057336 | RNAi-RELATED INHIBITION OF TNF alpha SIGNALING PATHWAY FOR TREATMENT OF GLAUCOMA - RNA interference is provided for inhibition of tumor necrosis factor α (TNFα) by silencing TNFα cell surface receptor TNF receptor-1 (TNFR1) mRNA expression, or by silencing TNFα converting enzyme (TACE/ADAM17) mRNA expression. Silencing such TNFα targets, in particular, is useful for treating patients having a TNFα-related condition or at risk of developing a TNFα-related condition such as the ocular conditions associated with elevated intraocular pressure (TOP), including glaucoma and ocular hypertension. | 2015-02-26 |
20150057337 | METHODS AND COMPOSITIONS FOR THE SPECIFIC INHIBITION OF KRAS BY ASYMMETRIC DOUBLE-STRANDED RNA - This invention relates to compounds, compositions, and methods useful for reducing KRAS target RNA and protein levels via use of Dicer substrate siRNA (DsiRNA) agents possessing asymmetric end structures. | 2015-02-26 |
20150057338 | TREATMENT OF PANCREATIC DEVELOPMENTAL GENE RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO A PANCREATIC DEVELOPMENTAL GENE - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of a Pancreatic Developmental gene, in particular, by targeting natural antisense polynucleotides of a Pancreatic Developmental gene. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of Pancreatic Developmental genes. | 2015-02-26 |
20150057339 | HIGH MOLECULAR WEIGHT ARGININE-GRAFTED BIOREDUCIBLE POLYMERS - The polymeric carrier for delivering nucleic acid material to a cell is provided herein. The polymeric carrier can include a dendrimer group having 2 to 8 termini, each of the termini having an arginine-grafted bioreducible polymer attached thereto. In one embodiment, only a portion of the termini can have an arginine-grafted bioreducible polymer attached thereto. | 2015-02-26 |
20150057340 | NUCLEIC ACID COMPRISING OR CODING FOR A HISTONE STEM-LOOP AND A POLY(A) SEQUENCE OR A POLYADENYLATION SIGNAL FOR INCREASING THE EXPRESSION OF AN ENCODED THERAPEUTIC PROTEIN - The present invention relates to a nucleic acid sequence, comprising or coding for a coding region, encoding at least one peptide or protein comprising a therapeutic protein or a fragment, variant or derivative thereof, at least one histone stem-loop and a poly(A) sequence or a polyadenylation signal. Furthermore the present invention provides the use of the nucleic acid for increasing the expression of said encoded peptide or protein, particularly for the use in gene therapy. It also discloses its use for the preparation of a pharmaceutical composition, e.g. for use in gene therapy, particularly in the treatment of diseases which are in need of a treatment with a therapeutic peptide or protein, preferably as defined herein. The present invention further describes a method for increasing the expression of a peptide or protein comprising a therapeutic protein or a fragment, variant or derivative thereof, using the nucleic acid comprising or coding for a histone stem-loop and a poly(A) sequence or a polyadenylation signal. | 2015-02-26 |
20150057341 | Composition with Pharmacological Effect for Vaporizing and Method - A composition is provided that includes a cannabinoid capable of inducing a pharmacological effect, an ester, a condensation aerosol, and a carrier liquid solution of food grade materials. The cannabinoid may include a bio-active ingredient receivable by a cannabinoid receptor and/or an acetylcholine receptor. The pharmacological effect may be produced by reception of tetrahydrocannabinol, cannabidiol, or mixtures thereof. The composition may also include ethanol, flavoring agents, and aromatherapy agents. The composition is deliverable to a user via vaporization. A method is provided for creating a pharmacological effect using the composition. | 2015-02-26 |
20150057342 | COMPOSITIONS FOR COMBINED IMMEDIATE AND SUSTAINED RELEASE OF CANNABINOIDS, METHODS OF MANUFACTURE AND USE THEREOF - Provided are oral pharmaceutical compositions comprising sustained release or a combination of sustained and immediate release formulation of cannabinoids, a process for their preparation and methods of use thereof. | 2015-02-26 |
20150057343 | AGONISTS OF THE AhR RECEPTOR PATHWAY HAVING SEBOSUPPRESSIVE ACTIVITY AND A METHOD FOR IDENTIFYING SAID AGONISTS - The subject invention provides a method of treating acne in a subject which comprises topically and periodically applying to the subject's acne a composition comprising 3-phenyl-1-benzo[f]chromen-1-one and a pharmaceutically acceptable carrier, wherein the 3-phenyl-1-benzo[f]chromen-1-one is present in an amount effective to treat the subject's acne. The subject invention also provides a method of treating a skin condition associated with abnormal sebum secretion or abnormal sebaceous gland function in a subject, compositions in such methods and a sorting method for identifying agonists of AhR pathway, useful in such methods and compositions. | 2015-02-26 |
20150057344 | PELTATIN FOR THE TREATMENT OF CHRONIC INFLAMMATORY DISORDERS - The present invention generally relates to health benefits of natural compounds. In particular, the present invention relates peltatins, a group of natural compounds that can be used to treat, prevent or alleviate chronic inflammatory disorders. For example, the present invention concerns a composition comprising at least one peltatin for use in the treatment or prevention of chronic inflammatory disorders. | 2015-02-26 |
20150057345 | METHOD FOR IMPROVING ECONOMIC PERFORMANCE IN POULTRY HUSBANDRY - Method for improving the feed efficiency in poultry husbandry wherein poultry is provided with a compound directly upon hatching, the compound being selected from a lactylate in accordance with formula 1, or a Na, K, Ca, Mg, Fe(II), Zn, NH4, or Cu(II) salt thereof, | 2015-02-26 |
20150057346 | METHODS OF MAINTAINING INTRAMUSCULAR MYOGLOBIN LEVELS, MAINTAINING MAXIMAL AEROBIC CAPACITY, AND ENHANCING THE OXIDATIVE CAPACITY OF MUSCLE IN A SUBJECT - Methods of maintaining intramuscular myoglobin levels, maintaining maximal aerobic capacity, and enhancing the oxidative capacity of muscle in a subject in need thereof are provided. Generally, the methods include administering an effective amount of β-hydroxy-β-methylbutyrate to the subject. The β-hydroxy-β-methylbutyrate may be administered as part of a nutritional composition. | 2015-02-26 |
20150057347 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION AND LIPID DISORDERS - The invention relates to the compounds of formula I and formula II 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 or formula II; and methods for treating or preventing inflammation and lipid disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hypertriglyceridemia, steatohepatitis, cystinosis and inflammatory diseases. | 2015-02-26 |
20150057348 | METHODS FOR TREATING INFLAMMATORY DISEASES WITH COMPOSITIONS COMPRISING POLYUNSATURATED FATTY ACID MONOGLYCERIDES OR DERIVATIVES THEREOF - There are provided methods for treating an inflammatory diseases chosen from inflammatory bowel diseases, asthma, acute respiratory distress syndrome, chronic obstructive pulmonary disease, acute lung injury, bronchopulmonary dysplasia, cystic fibrosis, bronchitis, bronchiolitis, arthritis, osteoarthritis, ankylosing spondylitis and rheumatism. The method comprise administering to a subject in need thereof an effective amount of at least one lipid and an effective amount of at least one compound chosen from compounds of the present disclosure. Such compounds are polyunsaturated fatty acid monoglycerides or derivatives thereof. | 2015-02-26 |
20150057349 | 4-OXO-2-PENTENOIC ACID AND THE HEALTH OF THE DIGESTIVE TRACT - The present invention relates generally to compositions with a health benefit. In particular, the invention relates to the field of inflammatory disorders of the digestive tract, for example, ileitis, colitis, rectal inflammation, pharyngitis, leaky gut syndrome, irritable bowel syndrome and inflammatory bowel disease. A subject matter of the invention is a composition comprising 4-oxo-2-pentenoic acid for use in the treatment or prevention of inflammatory disorders of the digestive tract. | 2015-02-26 |
20150057350 | FIBROSIS BIOMARKERS AND METHODS OF USING SAME - Methods and systems for using fibrosis biomarkers associated with a prolonged period of physical inactivity are provided. Also provided is a method of reducing the effect of prolonged physical inactivity on the development of fibrosis in a subject who is experiencing or is expected to experience prolonged physical inactivity in the near future by administering a therapeutically effective amount of a leucine metabolite (e.g., β-hydroxy-β-methylbutyric acid (HMB)) to the subject. | 2015-02-26 |
20150057351 | METHOD FOR TREATING NEUROPATHIC PAIN - A method for treating neuropathic pain in a mammalian subject, which comprises administering an effective amount of a fatty acid derivative, is provided. | 2015-02-26 |
20150057352 | Microorganisms, Compositions, and Methods for Producing Fatty Acids - Methods of producing an unsaturated free fatty acid comprising at least 18 carbon atoms are provided. In some embodiments, the methods comprise culturing an engineered microorganism in a culture medium, wherein the engineered microorganism comprises at least one recombinant enzyme selected from acyl-lipid desaturase delta-9 (EC:1.14.19.1), acyl-lipid desaturase delta-12 (EC:1.14.19.6), acyl-lipid desaturase delta-15 (EC:1.14.19.-), and thioesterase (EC:3.1.2.14). Engineered microorganisms comprising at least one of those recombinant enzymes are also provided. The methods and organisms can be used to produce at least one free fatty acid selected from oleic acid, linoleic acid and α-linolenic acid. | 2015-02-26 |
20150057353 | production of ultrapure EPA and polar lipids form largely heterotrophic culture - Eicosapentaenoic acid (EPA) compositions and EPA-rich polar lipids for prophylactic or therapeutic applications are described. Production from certain cultured micro-organisms (like | 2015-02-26 |
20150057354 | METHOD OF MAINTAINING OR IMPROVING TACTICAL PERFORMANCE AND COGNITIVE FUNCTION THROUGH DIETARY SUPPLEMENTATION - The present invention provides methods of maintaining or improving tactical performance and/or psychomotor performance, wherein the free amino acid beta-alanine, or a salt or ester thereof, is administered to an individual as a human dietary supplement over a period of time in an amount effective to maintain or improve tactical performance and/or psychomotor performance under normally stressful and/or fatiguing high intensity physical activity. | 2015-02-26 |
20150057355 | AMANTADINE COMPOSITIONS AND METHODS OF USE - Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration. | 2015-02-26 |
20150057356 | MELT-EXTRUDED COMPOSITION COMPRISING A CELLULOSE ETHER - A melt-extruded polymer composition comprising a) at least one cellulose ether, b) one or more active ingredients and c) one or more optional additives, wherein said at least one cellulose ether has an MS (hydroxyalkyl) of 0.05 to 0.55 and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.32 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. | 2015-02-26 |
20150057357 | BIS (THIOHYDRAZIDE AMIDE) COMPOUNDS FOR TREATING CANCERS - Methods of treating a subject with cancer characterized by an impaired ability to repair oxidative DNA damage, comprising administering to the subject an effective amount of a bis(thiohydrazide amide) compound are provided. | 2015-02-26 |
20150057358 | NOVEL SUSTAINED RELEASE DOSAGE FORMS - A sustained release dosage form comprises an active ingredient blended with a polymeric matrix. At least a portion of the polymeric matrix is formed by a cellulose ether having an onset dissolution temperature of at least 40° C., having anhydroglucose units joined by 1-4 linkages and having methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydrogluclose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.31 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. | 2015-02-26 |