40th week of 2014 patent applcation highlights part 64 |
Patent application number | Title | Published |
20140296231 | AMINO-SUBSTITUTED IMIDAZOPYRIDAZINES - The present invention relates to amino-substituted imidazopyridazine compounds of general formula (I): in which A, R1, R3 and n are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 2014-10-02 |
20140296232 | COMPOUNDS FOR THE TREATMENT OF MYCOBACTERIAL INFECTIONS - The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof: | 2014-10-02 |
20140296233 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2014-10-02 |
20140296234 | PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 2014-10-02 |
20140296235 | 1H-BENZIMIDAZOLE-4-CARBOXAMIDES SUBSTITUTED WITH PHENYL AT THE 2-POSITION ARE POTENT PARP INHIBITORS - Compounds having formula (I) | 2014-10-02 |
20140296236 | QUINOLINES AS FGFR KINASE MODULATORS - The invention relates to new quinoline derivative compounds of formula (I), 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. Formula (I) | 2014-10-02 |
20140296237 | PICOLINAMIDE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. | 2014-10-02 |
20140296238 | Dihydropyrazoles - Novel dihydropyrazole derivatives of formula (I) | 2014-10-02 |
20140296239 | Biaryl-propionic acid derivatives and their use as pharmaceuticals - The present invention relates to compounds of the formula I, | 2014-10-02 |
20140296240 | SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS - The present invention provides a compound of formula I′; | 2014-10-02 |
20140296241 | THE USE OF (2R, 6R)-HYDROXYNORKETAMINE, (S)-DEHYDRONORKETAMINE AND OTHER STEREOISOMERIC DEHYDRO AND HYDROXYLATED METABOLITES OF (R,S)- KETAMINE IN THE TREATMENT OF DEPRESSION AND NEUROPATHIC PAIN - The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment. | 2014-10-02 |
20140296242 | COMPOUNDS FOR TREATING CANCER, FOR ADMINISTERING, AND FOR PHARMACEUTICAL COMPOSITIONS - Some embodiments of this invention include methods for treating disease and methods for administering a compound of the invention. In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of the invention. Pharmaceutical compositions of some embodiments of the present invention comprise a compound of the invention. | 2014-10-02 |
20140296243 | BROMODOMAIN INHIBITORS AND USES THEREOF - The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. | 2014-10-02 |
20140296244 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years. | 2014-10-02 |
20140296245 | BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain. | 2014-10-02 |
20140296246 | BENZIMIDAZOLONE DERIVATIVES AS BROMODOMAIN INHIBITORS - This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) | 2014-10-02 |
20140296248 | METHODS AND COMPOSITIONS FOR PREDICTING RESISTANCE TO ANTICANCER TREATMENT - The instant application provides methods and related compositions pertaining to the identification of resistance to anticancer treatment in a patient. In a particular embodiment, the invention provides biomarkers for the identification of resistance to anticancer treatment in a lung cancer patient, wherein a reduced expression of a MEDIATOR and/or SW1/SNF complex gene in the lung cancer cells of the patient indicates that the lung cancer cells in the patient may be resistant to treatment with a receptor tyrosine kinase inhibitor, such as gefitinib and/or erlotinib. In some embodiments, the invention relates to methods and related compositions for predicting resistance to anticancer treatment by detecting the expression levels of one or more TGF-beta pathway nucleic acids and/or proteins. | 2014-10-02 |
20140296249 | 4-PHENYLPIPERAZINE DERIVATIVES WITH FUNCTIONALIZED LINKERS AS DOPAMINE D3 RECEPTOR SELECTIVE LIGANDS AND METHODS OF USE | 2014-10-02 |
20140296250 | TRAZODONE AND TRAZODONE HYDROCHLORIDE IN PURIFIED FORM - A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride. | 2014-10-02 |
20140296251 | MULTIFUNCTIONAL QUINOLINE DERIVATIVES AS ANTI-NEURODEGENERATIVE AGENTS - Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases. | 2014-10-02 |
20140296252 | 1,2,4-TRIAZOL-5-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 2014-10-02 |
20140296253 | DIPHENYLMETHYL PIPERAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION USING SAME - The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I) | 2014-10-02 |
20140296254 | NOVEL DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED DISEASES - Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases. | 2014-10-02 |
20140296255 | LYSINE DEMETHYLASE INHIBITORS FOR THROMBOSIS AND CARDIOVASCULAR DISEASES - The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. | 2014-10-02 |
20140296256 | PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITOR - The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. | 2014-10-02 |
20140296257 | High-Loading Water-Soluable Carrier-Linked Prodrugs - The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment. | 2014-10-02 |
20140296258 | TRISUBSTITUTED TRIAZOLOPYRIMIDINES FOR USE IN PLATELET AGGREGATION INHIBITON - The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation. | 2014-10-02 |
20140296259 | 4-Amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives, their manufacture and their use as antiviral active substances - The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula I | 2014-10-02 |
20140296260 | 3-Aryl-2-((Arylamino)Methyl)Quinazolin-4-(3H)-Ones - The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3Kδ, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3Kδ, are disclosed. | 2014-10-02 |
20140296261 | KINASE MODULATING COMPOUNDS, COMPOSITIONS CONTAINING THE SAME AND USE THEREOF - The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition. | 2014-10-02 |
20140296262 | Method to Treat Premature Ejaculation in Humans - The present invention belongs to the fields of pharmacology, medicine and medicinal chemistry, and provides methods and compositions for treating sexual dysfunction; more particularly, the invention relates to treatment of premature ejaculation in humans. | 2014-10-02 |
20140296263 | SUBSTITUTED XANTHINE DERIVATIVES - The present invention in one embodiment relates to a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein: each of R | 2014-10-02 |
20140296264 | MGMT INHIBITOR COMBINATIONS FOR THE TREATMENT OF NEOPLASTIC DISORDERS - A method of treating a neoplastic disease in a subject includes administering to neoplastic cells of the subject an MGMT inhibitor and at least one of an antimitotic agent or a DNA damaging agent. | 2014-10-02 |
20140296265 | Method of Treating Lymphoma Using Pyridopyrimidinone Inhibitors of PI3K/mTOR - The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I: | 2014-10-02 |
20140296266 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 2014-10-02 |
20140296267 | SOLID DISPERSIONS OF A ERB2 (HER2) INHIBITOR - A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein. | 2014-10-02 |
20140296268 | THERAPEUTIC METHODS AND COMPOSITIONS INVOLVING ALLOSTERIC KINASE INHIBITION - The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state. | 2014-10-02 |
20140296269 | COMPOSITION AND METHOD FOR CONTROLLING PLANT DISEASES - The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of compounds selected from the group (A) consisting of kresoxim-methyl, azoxystrobin, pyraclostrobin, picoxystrobin, enestrobin, trifloxystrobin, dimoxystrobin, fluoxastrobin, orysastrobin, famoxadone, fenamidone, metominostrobin, a compound represented by a formula (II) and pyribencarb: shows an excellent controlling efficacy on plant diseases. | 2014-10-02 |
20140296270 | STAT3 Inhibitors - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein. | 2014-10-02 |
20140296271 | KINASE INHIBITOR - There is provided a compound of formula I, | 2014-10-02 |
20140296272 | THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS - The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity. | 2014-10-02 |
20140296273 | Method and Compositions for Treatment or Prevention of Inflammatory Conditions - Pharmaceutical compositions and methods for treating or preventing an inflammatory condition in a patient are disclosed. The pharmaceutical compositions and methods include the use of vincamine or a vincamine derivative, either alone or in combination with one or more additional therapeutic agents, including a steroid (preferably a corticosteroid), an angiotensin II receptor (type 1) antagonist, an angiotensin-converting enzyme (ACE) inhibitor, and a non-steroidal anti-inflammatory drug. | 2014-10-02 |
20140296277 | PHARMACEUTICAL PREPARATION CONTAINING OXYCODONE AND NALOXONE - The invention concerns a storage stable pharmaceutical preparation comprising oxycodone and naloxone for use in pain therapy, with the active compounds being released from the preparation in a sustained, invariant and independent manner. | 2014-10-02 |
20140296278 | 5-NONYLOXYTRYPTAMINE AND RELATED INTRACELLULAR PH ACIDIFIERS FOR THE TREATMENT AND PREVENTION OF CANCER - Provided herein are compositions for lowering intracellular pH in a cell or population of cells from a subject comprising contacting the cell or population of cells with a therapeutically effective amount of 5-nonyloxytryptamine or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivatives thereof. These compounds are useful for acidification of cells, including cancer cells, which induces apoptosis and cell necrosis. Methods of use of these compounds, including in pharmaceutical compositions in conjunction with other biologically active agents, in treatment of cancers, including glioblastoma and related neuronal cancers are also included. | 2014-10-02 |
20140296279 | INTRAVASCULAR DELIVERY OF NANOPARTICLE COMPOSITIONS AND USES THEREOF - The present invention provides methods of delivering a composition comprising nanoparticles that comprise a macrolide and an albumin by directly injecting the nanoparticle composition into the blood vessel wall or the tissue surrounding the blood vessel wall. The methods can be used for inhibiting negative remodeling or vascular fibrosis in the blood vessel and are useful for treating various diseases. | 2014-10-02 |
20140296280 | PURES-(-)-9-FLUORO-6,7-DIHYDRO-8-(4-HYDROXYPIPERIDIN-1-YL)-5-METHYL-1-OXO-- 1H,-5H-BENZO[I,J]QUINOLIZINE-2- CARBOXYLIC ACID L-ARGININE SALT TETRAHYDRATE AND A PROCESS FOR ITS PREPARATION - Pure S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate and a process for its preparation is disclosed. | 2014-10-02 |
20140296281 | METHODS FOR SCREENING A BRCA1 LOSS-OF-FUNCTION IN A SUBJECT SUFFERING FROM A CANCER - The present invention relates to a method for screening a BRCA1 loss-of-function in a subject comprising the step consisting of determining the level of serine 211 phosphorylated glucocorticoid receptor (GR P-Ser211) expression in a tissue sample obtained from said subject. | 2014-10-02 |
20140296282 | COMPOSITIONS OF A POLYORTHOESTER AND AN APROTIC SOLVENT - Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release. | 2014-10-02 |
20140296283 | Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to azole bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these 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. | 2014-10-02 |
20140296284 | CRYSTALLINE FORMS OF KINASE INHIBITORS - Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer. | 2014-10-02 |
20140296285 | PREPARATION AND APPLICATION OF THE NEW ANTIBACTERIAL AND ANTICANCER COMPOUNDS AND THEIR DERIVATIVES - A method of inhibiting microorganism growth comprising administering an effective amount of a composition including a compound selected from the group consisting of | 2014-10-02 |
20140296286 | COMPOUNDS WITH INCREASED SPECIFICITY FOR THE TREATMENT OF GLIOMA - Disclosed are compounds for the treatment of cancer. Compounds disclosed herein are particularly effective for the selective inhibition of glioma cells. | 2014-10-02 |
20140296287 | METHODS FOR TREATING COGNITIVE DISORDERS USING 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS - Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 | 2014-10-02 |
20140296288 | IMINO-SUGAR C-GLYCOSIDES, PREPARATION AND USE THEREOF - The present disclosure relates to iminosugar derivatives and processes for the preparation thereof. The disclosed compounds have glycosidase inhibiting properties, and are useful in the treatment of various diseases, such as type 2 diabetes, neurodegenerative diseases or lysosomal storage disorders. The present disclosure also relates to pharmaceutical compositions containing the disclosed compounds and to their use as biochemical tools. | 2014-10-02 |
20140296289 | Thiazolyl Oxime Ethers and Hydrazones as Crop Protection Agents - Thiazolyl oxime ethers and hydrazones of the formula (I), | 2014-10-02 |
20140296290 | THERAPEUTIC USES OF COMPOUNDS HAVING AFFINITY TO THE SEROTONIN TRANSPORTER, SEROTONIN RECEPTORS AND NORADRENALIN TRANSPORTER - Therapeutic uses of | 2014-10-02 |
20140296291 | NOVEL CRYSTALLINE FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE - The invention relates to novel crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms. | 2014-10-02 |
20140296292 | METHODS AND COMPOSITIONS ASSOCIATED WITH THE GRANULOCYTE COLONY-STIMULATING FACTOR RECEPTOR - Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders. | 2014-10-02 |
20140296293 | PHARMACEUTICAL COMPOSITIONS COMPRISING A LOCAL ANAESTHETIC SUCH AS BUPIVACAINE FOR LOCAL ADMINISTRATION TO THE MOUTH OR THROAT - The present invention relates to compositions comprising a lipophilic local anaesthetic, preferably bupivacaine or a pharmaceutically active salt thereof, which are formulated for local administration to the mouth or throat of a subject. The compositions are useful in the treatment or alleviation of pain, burning or xerostomia of the oral cavity, pharynx, oral mucosa and pharyngeal mucosa or for use in providing local anesthesia of the oral cavity, pharynx, oral mucosa and pharyngeal mucosa. In particular in the treatment of pain, burning or xerostomia, which is caused by a disease such as oral mucositis, Burning Mouth Syndrome, Sjogren's syndrome, xerostomia, periodontitis, toothache, tonsillectomy, throat infection or mononucleosis, canker sores and aphthous stomatitis. | 2014-10-02 |
20140296294 | NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES - Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: | 2014-10-02 |
20140296295 | 2-ALKOXY-SUBSTITUTED DICYANOPYRIDINES AND THEIR USE - The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders. | 2014-10-02 |
20140296296 | Biaryl-Propionic Acid Derivatives and their Use as Pharmaceuticals - The present invention relates to compounds of the formula I, | 2014-10-02 |
20140296297 | Materials Having Embedded Insecticides and Additives - The present invention concerns polymeric material containing at least an embedded insecticidally active ingredient and an additive, which are released at room temperature. It similarly concerns materials produced from this polymer, for example in the form of self-supporting film/sheet, threads, wovens, fabrics, textiles, nets, curtains and pellets. The invention further concerns processes for producing such polymeric material and also the use of the self-supporting film/sheet, threads, wovens, fabrics, textiles and nets and curtains produced from the material for protecting humans, animals and plants and buildings, machines and packaging against arthropods, particularly for controlling insects. | 2014-10-02 |
20140296298 | COMPOSITION AND METHOD FOR CONTROLLING HARMFUL ARTHROPODS - The present invention provides a composition for controlling harmful arthropods having an excellent controlling harmful arthropods comprising an amide represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of pyrazole compounds selected from the group (A) consisting of chlorantraniliprole, cyantraniliprole and a compound represented by a formula (II), shows an excellent controlling efficacy on harmful arthropods. | 2014-10-02 |
20140296299 | METHODS AND COMPOSITIONS FOR LOCALLY INCREASING BODY FAT - Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention. | 2014-10-02 |
20140296300 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION CONTAINING PIRFENIDONE IN SUSTAINED-RELEASE TABLET FORM AND ITS APPLICATION IN THE REGRESSION OF HUMAN CHRONIC RENAL FAILURE, BREAST CAPSULAR CONTRACTURE AND HEPATIC FIBROSIS - The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis. | 2014-10-02 |
20140296301 | TOPICAL OPHTHALMOLOGICAL PHARMACEUTICAL COMPOSITION CONTAINING REGORAGENIB - The present invention relates to topical ophthalmological pharmaceutical compositions containing regorafenib, a hydrate, solvate or pharmaceutically acceptable salt thereof or a polymorph thereof and its process of preparation and its use for treating ophthalmological disorders. | 2014-10-02 |
20140296302 | Methods For Treating Inflammation - The present invention provides methods for treating or limiting development of inflammatory disorders. | 2014-10-02 |
20140296303 | Use of Pyridoxamine to Treat and/or Prevent Disease Processes - Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. | 2014-10-02 |
20140296304 | Pharmaceutically Active Disubstituted Pyridine Derivatives - The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase. | 2014-10-02 |
20140296305 | Use of Quaternary Pyridinium Salts as Vasoprotective Agents - The invention relates to the use of quaternary pyridinium salts of formula (I), | 2014-10-02 |
20140296306 | AMIDE COMPOUND AND MEDICINAL USE THEREOF - A compound of formula [I-W]: | 2014-10-02 |
20140296307 | POTENT ANALOGUES OF THE C-MYC INHIBITOR 10074-G5 WITH IMPROVED CELL PERMEABILITY - The present invention relates compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. The compounds exhibit increased inhibitory activity against c-Myc relative to the known c-Myc inhibitor small-molecule benzofurazan N-([1,1′-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (10074-G5). | 2014-10-02 |
20140296308 | DRUGS FOR INHIBITING P38 AND USES THEREOF - The present invention relates to compounds with a benzoxadiazolyl amine structure which are capable of inhibiting the activation or the biological activity of p38 mitogen-activated protein kinase (MAPK) and the use thereof in the treatment of a disease that can be alleviated by means of inhibiting the activation or the biological activity of said p38 MAPK, for example, an inflammatory disease or a disease presenting with pain. | 2014-10-02 |
20140296309 | MODIFIED RELEASE COMPOSITIONS OF EPALRESTAT OR A DERIVATIVE THEREOF AND METHODS FOR USING THE SAME - Modified release pharmaceutical compositions of epalrestat are provided. Methods of manufacturing the tablets and treating various diseases and conditions, including diabetes and diabetic complications, by administering the modified release compositions to patients in need thereof are also provided. | 2014-10-02 |
20140296310 | METHODS OF TREATING BACTERIAL INFECTIONS WITH 1,2-BENZISOTHIAZOLINONE AND ISOINDOLINONE DERIVATIVES - Methods of treating, preventing and ameliorating bacteria! infections with 1,2-benzisothiazolinone and isoindolinone derivatives are disclosed. Pharmaceutical compositions containing 1,2-benzisothiazolinone and isoindolinone derivatives are useful for treating bacteria! infections caused by drug resistant strains of bacteria, including but not limited to methicillin and vancomycin bacterial organisms. | 2014-10-02 |
20140296311 | GAMMA SECRETASE MODULATORS - Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease. | 2014-10-02 |
20140296312 | TREATMENT OF BREAST CANCER - The disclosure describes the use of one or more compounds that fall within the scope of one or more of structural formulae I, II, III, IV, V, or VI for treating triple negative breast Compounds useful for treating breast cancer include those compounds of formulae I, II, III, IV, V, or VI that inhibit proliferation of breast cancer cells and/or lead to the death of breast cancer cells, especially triple negative breast cancer. | 2014-10-02 |
20140296313 | (4-Phenylimidazol-2-yl) Ethylamine Derivatives Useful As Sodium Channel Modulators - The present invention is directed to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole Na | 2014-10-02 |
20140296314 | Methods for Treating Conditions Such as Dystonia and Post-Stroke Spasticity with Clonidine - Effective treatments of dystonia and/or post-stroke spasticity for extended periods of time are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relieve dystonia and/or post-stroke spasticity caused by diverse sources. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least five days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days. | 2014-10-02 |
20140296315 | PYRAZOLE-AMIDE COMPOUNDS AND PHARMACEUTICAL USE THEREOF - A compound represented by the following formula: | 2014-10-02 |
20140296316 | HYDRATE AND CRYSTAL OF FLUORENE COMPOUNDS - A compound represented by the formula (J): | 2014-10-02 |
20140296317 | 4R,5S-ENANTIOMER OF 2-(5-METHYL-2-OXO-4-PHENYL-PYRROLIDIN-1-YL)-ACETAMIDE WITH NOOTROPIC ACTIVITY - The invention relates to the 5S,4R-enantiomer of 2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide with cognition enhancing activity of high pharmacological value and to its preparation method which includes the synthesis of 5S-methyl-4R-phenylpyrrolidin-2-one, its N-alkylation with ethyl haloacetate and the treatment of intermediate ethyl 2-(5S-methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetate with ammonia. | 2014-10-02 |
20140296318 | NOVEL TISSUE PROTECTIVE ERYTHROPOIETIN RECEPTOR (NEPOR) AND METHODS OF USE - Methods of determining whether a patient is suitable for erythropoietin (EPO) therapy, including (A) isolating a tissue sample from said patient; (B) determining the level of expression of EPH-B4 in said sample; and (C) correlating a presence of EPH-B4 expression to a negative physiological response to EPO therapy). In addition, methods of enhancing the effectiveness of EPO therapy in a patient by administering to said patient, in conjunction with EPO therapy, an siRNA specific for EPH-B4. | 2014-10-02 |
20140296319 | Composition For Promoting Apoptosis Or Inhibiting Cell Growth, Comprising Epstein-Barr Virus Microrna - Provided is a use of an miRNA of an Epstein-Barr virus (EBV), more specifically, EBV miR-BART4-5p, miR-BART4-3p, miR-BART1-5p, miR-BART15-3p, miR-BART5-5p, miR-BART5-3p, miR-BART16-5p, miR-BART16-3p, miR-BART17-3p, miR-BART21-3p, miR-BART18-5p, miR-BART7-5p, miR-BART9-5p, miR-BART22-5p, miR-BART20-3p, miR-BART13-5p, miR-BART13-3p, miR-BART2-3p, and mimics thereof for promoting apoptosis or inhibiting cell growth. | 2014-10-02 |
20140296320 | Use Of siRNA To Achieve Down Regulation Of An Endogenous Gene In Combination With The Use of A Sense Construct To Achieve Expression Of A Polynucleotide - The present invention relates to the combinatorial use of an siRNA targeted against an endogenous gene to knock out or knock down expression of the endogenous gene in a host and a delivery of a polynucleotide encoding the gene in a delivery vehicle/expression vector to the host to provide expression in the host of the protein encoded by the polynucleotide. | 2014-10-02 |
20140296321 | METHODS AND COMPOSITIONS FOR MANIPULATING TRANSLATION OF PROTEIN ISOFORMS FROM ALTERNATIVE INITIATION OF START SITES - Provided herein are antisense oligonucleotides, compositions comprising antisense oligonucleotides, and methods for the use of antisense oligonucleotides in manipulating translation. Expression of isoforms of proteins expressed from different start codons of the same transcript are inhibited by antisense oligonucleotides, which may also enhance expression of non-target isoforms. | 2014-10-02 |
20140296322 | CONJUGATES, PARTICLES, COMPOSITIONS, AND RELATED METHODS OF USE - Particles and conjugates for delivering nucleic acid agents. Compositions containing the particles, the conjugates, or both. Methods of using the particles, the conjugates, and the compositions. | 2014-10-02 |
20140296323 | TRICYCLO-PHOSPHOROTHIOATE DNA - The present invention relates to a nucleic acid molecule containing a sequence of tricyclo nucleosides joined by internucleoside phosphorothioate linkage. The invention also relates to synthetic antisense oligonucleotides and to methods employing the same. | 2014-10-02 |
20140296324 | VECTORS HARBORING TOXIC GENES, METHODS AND USES THEREFOR - The present disclosure describes nucleic acids, and viruses comprising such nucleic acids, for growing a toxic gene in an insect cell. These nucleic acids comprise a sequence encoding a toxic polypeptide, and an intron that interrupts the sequence, whereby the intron is spliced in mammalian cells but not in insect cells. Infection of mammalian cells but not insect cells with the nucleic acids or viruses can lead to expression of toxic levels of the toxic polypeptide in mammalian cells but not in insect cells. Viruses, such as an AAV or a baculovirus comprising a nucleic acid can be grown in insect cell lines in vitro and can be administered to a subject in need of therapy, such as a subject in need of cancer therapy. | 2014-10-02 |
20140296325 | METHODS AND COMPOSITIONS FOR INDUCING BROWN ADIPOGENESIS - Methods and compositions for treating obesity and related disorders. The methods include the use of stem cells treated with BMP-2, -4, -5, -6 and/or -7. | 2014-10-02 |
20140296326 | EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) AND METHODS OF USE IN ADENOVIRAL-ASSOCIATED VIRUS TYPE 6 (AAV6) TRANSDUCTION - Comparative gene analysis (CGA) was combined with pathway visualization software to identify a positive correlation between AAV6 transduction and epidermal growth factor receptor (EGFR) expression. It was found that EGFR is necessary for vector internalization and functions as a co-receptor for AAV6. The identification and characterization of AAV6's requirement of EGFR expression for high transduction activity has allowed construction of recombinant AAV6 vectors which are capable of targeting and killing specific types of head and neck tumors that because of this high EGFR activity, were until now, refractory to current therapies. | 2014-10-02 |
20140296327 | DIAGNOSIS AND TREATMENT OF MESOTHELIOMA - This disclosure provides methods for surveillance, early detection and diagnosis, subtype classification, prediction of recurrence, prognosis and therapy of malignant mesothelioma based on profiles of indicator mutations in disclosed genes. | 2014-10-02 |
20140296328 | 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. | 2014-10-02 |
20140296329 | PHYTOESTROGEN PRODUCT OF RED CLOVER AND PHARMACEUTICAL USES THEREOF - The present invention provides compositions comprising optimized ratios of Red clover phytoestrogens as determined by a proprietary physiologically based pharmacokinetic and pharmacodynamic model. The compositions are useful for modulating bone remodeling, and prevention and treatment of osteoporosis. | 2014-10-02 |
20140296330 | TREATMENT OF CIRCADIAN RHYTHM DISORDERS - Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm. | 2014-10-02 |
20140296331 | TREATMENT OF CIRCADIAN RHYTHM DISORDERS - Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm. | 2014-10-02 |
20140296332 | TREATMENT OF CIRCADIAN RHYTHM DISORDERS - Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm. | 2014-10-02 |
20140296333 | COMPOSITION OF THE TREATMENT OF VASCULAR DISEASES OR KCa3.1 CHANNEL-MEDIATED DISEASES COMPRISING MODAFINIL OR DERIVATIVES THEREOF - The present invention relates to modafinil or derivatives thereof as a medicine for the treatment of vascular diseases or KCa3.1 channel (Ca activated K channel) mediated diseases and a novel use of the same. More specifically, the present invention relates to a pharmaceutical composition for the prevention or treatment of vascular diseases or KCa3.1 channel-mediated diseases comprising modafinil or a derivative of modafinil, or pharmaceutically acceptable salts thereof which relax blood vessels and inhibit KCa3.1 channel currents by increasing intracellular cAMP, a method for treating vascular diseases or KCa3.1 channel-mediated diseases using the composition and a health functional food composition for the prevention or improvement of vascular diseases or the KCa3.1 channel-mediated diseases comprising modafinil or a modafinil derivative compound, or sitologically acceptable salts thereof. | 2014-10-02 |
20140296334 | N-Optionally Substituted Aryl-2-Oligomer-3-Alkoxypropionamides - The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer. | 2014-10-02 |