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10th week of 2015 patent applcation highlights part 65
Patent application numberTitlePublished
20150065453COMBINATION OF AN OXIDANT AND A PHOTOACTIVATOR FOR THE HEALING OF WOUNDS - There is provided a wound healing composition which comprises at least one oxidant, at least one photoactivator capable of activating the oxidant and at least one healing factor chosen from hyaluronic acid, glucosamine and allantoin in association with a pharmaceutically acceptable carrier. In addition, a method of topically treating wounds using at least one oxidant and at least one photoactivator capable of activating the oxidant followed by illumination of said photosensitizer is disclosed.2015-03-05
20150065454Solution aqueuse homogene de chitosane injectable - The present invention relates to a homogeneous aqueous solution of injectable chitosan containing a chitosan having a degree of acetylation lower than 20%, said solution containing between 0.1 and 3.5% by weight of chitosan, said solution presenting a pH lower than 6.2, and said aqueous solution being capable of forming crystalline particles of chitosan after injection. The present invention also relates to compounds containing such a homogeneous aqueous solution of chitosan. The invention also relates to such compounds for their use as dermatological or cosmetic compounds, or for their use as a medical device, advantageously as a bioresorbable implant.2015-03-05
20150065455METHODS OF ASSESSING SUSCEPTIBILITY TO DRUG-INDUCED THROMBOCYTOPENIA - The invention relates to assessing the FcγRIIIa-158 polymorphism in a subject in order to determine susceptibility of the subject to drug induced thrombocytopenia, as well as therapies and therapeutic compositions based on the use of this biomarker.2015-03-05
20150065456AGENT FOR TREATMENT AND PREVENTION OF CANCER - The invention provides methods of treating or preventing in a subject a cancer, tumor, or neoplasm, including malignancies or metastases thereof, using a direct Factor Xa inhibitor. The methods particularly involve the treatment of human patients afflicted with a malignant cancer, tumor, or neoplasm with an effective amount of the Factor Xa inhibitor. In an embodiment, the Factor Xa inhibitor is the small molecule edoxaban p-toluenesulfonate monohydrate, also termed “DU-176b”. The invention provides methods of administering a Factor Xa inhibitor to effectively reduce or suppress, or otherwise abrogate, the growth of cancers, tumors, or neoplasms in a subject who has, or is at risk for, cancer and, optionally, who also has, or is at risk for, thrombotic disease or embolism. The methods of the invention can also reduce the incidence of migration or invasion of metastatic or malignant cancers in a human subject by administration of a Factor Xa inhibitor.2015-03-05
20150065457METHOD OF USING CYCLODEXTRIN - Described are methods for using cyclodextrin to treat, inhibit, prevent, ameliorate, or cure diabetes or conditions relating to diabetes.2015-03-05
20150065458Composition for Inactivating an Enveloped Virus - The present invention relates generally to the field of prevention of diseases caused by enveloped viruses. More particularly, this invention concerns a composition for inactivating an enveloped virus comprising at least one non phospholipid Lipid Vesicle (nPLV) able to interact with said enveloped virus and an agent that enhances the lipid exchange between said nPLV and the membrane of said enveloped virus.2015-03-05
20150065459BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.2015-03-05
20150065460Biomarkers Related to Insulin Resistance and Methods Using the Same - Biomarkers relating to pancreatic Beta-cell function, pancreatic Beta-cell glucose sensitivity, insulin resistance, and/or pancreatic Beta-cell-related disorders are provided. Methods based on the same biomarkers are also provided.2015-03-05
20150065461Vesicular Formulations for Use in the Treatment of Pain or Reduced Mobility of a Joint - The present invention relates to vesicular formulations for use in the treatment of pain and/or reduced mobility associated with a loss of lubrication and/or structural integrity and/or swelling of a collagen structure. It also relates to a method of treating pain such as joint pain or tendonitis comprising topically administering a vesicular formulation according to the invention.2015-03-05
20150065462CONJUGATES OF A PHOSPHOLIPID AND A DRUG FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE - Conjugates of drugs suitable for use in the treatment of inflammatory bowel disease and phospholipids, and their use in the treatment of inflammatory bowel disease, are disclosed. The disclosed conjugates serve as targeted prodrugs which are suitable for oral administration, and which are capable of releasing the drug selectively at the diseased tissue upon activation by PLA2015-03-05
20150065463PHOSPHONATE DERIVATIVES AND METHODS OF USE THEREOF IN THE TREATMENT OF ALZHEIMER'S DISEASE - Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided.2015-03-05
20150065464AMIDE COMPOUNDS, COMPOSITIONS AND APPLICATIONS THEREOF - The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them. These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Fatty Acid Amide Hydrolase (FAAH), such as pain including acute and post operative pain, chronic pain, cancer pain, cancer chemotherapy induced pain, neuropathic pain, nociceptive pain, inflammatory pain, back pain, pain due to disease of various origin such as: diabetic neuropathy, neurotropic viral disease including human immunodeficient virus (HIV), herpes zoster such as post herpetic neuralgia; polyneuropathy, neurotoxicity, mechanical nerve injury, carpal tunnel syndrome, immunologic mechanisms like multiple sclerosis; sleep disorders, anxiety and depression disorders, inflammatory disorders, weight and eating disorders, Parkinson's disease, addiction, spasticity, hypertension or other disorders. The disclosure also relates to the process of preparation of the amide compounds.2015-03-05
20150065465IMIDAZOTRIAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I)2015-03-05
20150065466NOVEL DXR INHIBITORS FOR ANTIMICROBIAL THERAPY - The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group.2015-03-05
20150065467USE OF LIPID CONJUGATES IN THE TREATMENT OF DISEASES OR DISORDERS OF THE EYE - In one embodiment, the invention provides a method of treating, reducing the incidence, reducing the severity or pathogenesis of an eye disease or disorder in a subject, including, inter alia, retinal detachment, macular degeneration, glaucoma or retinopathy, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a contact lens solution comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.2015-03-05
20150065468BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF - Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.2015-03-05
20150065469SALICYLIC ACID DERIVATIVES USEFUL AS GLUCOCEREBROSIDASE ACTIVATORS - Compounds of Formula (I) and the pharmaceutically acceptable salts thereof are disclosed. The variables. R2015-03-05
20150065470Steroid Sulfatase Inhibitor Regimen for the Treatment of Endometriosis - The present invention is related to a dosage regimen of a steroid sulfatase inhibitor, E2MATE, for use in the prevention or treatment of endometriosis. The present invention further relates to a method for preventing or treating endometriosis.2015-03-05
20150065471SALTS OF 5-[(1R)-2-(AMINO)-1-HYDROXYETHYL]-8-HYDROXYQUINOLIN-2(1H)-ONE - The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.2015-03-05
20150065472INTRAUTERINE APPLICATION OF 18-METHYL-15SS,16SS-METHYLENE-19-NOR-20-SPIROX-4-EN-3-ONE SYSTEMS, INTRAUTERINE SYSTEMS CONTAINING 18-METHYL-15SS,16SS-METHYLENE-19-NOR-20-SPIROX-4-EN-3-ONE, AS WELL AS THE USE THEREOF IN CONTRACEPTION AND GYNAECOLOGICAL THERAPY - The present invention describes intrauterine use of 18-methyl-15β,16β-methylene-19-nor-20-spirox-4-en-3-ones of the general formula (1)2015-03-05
20150065473METHOD FOR VISUAL ENHANCEMENT AND POST PROCEDURE TREATMENT PROTOCOL - A new and novel method for determining post procedural treatment is disclosed herein. In one embodiment, a method for a treating a patient following a surgical procedure on at least one eye comprises determining a depth at which the surgical procedure is to be performed or was performed, and providing instructions for administering medication for a length of time to the at least one eye of the patient, the length of time based at least in part upon the depth.2015-03-05
20150065474DEXAMETHASONE FORMULATIONS IN A BIODEGRADABLE MATERIAL - Effective treatments of acute pain for extended periods of time are provided. Through the administration of an effective amount of dexamethasone at or near a target site, one can relieve pain cause by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discongenic back pain and joint pain as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least twenty-five days. In some embodiments, the relief can be for 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.2015-03-05
20150065475Turfgrass Fungicide Formulation with Pigment - Oil-in-water fungicidal formulations are prepared having pigment dispersed therein, the pigment being stable within the oil-in-water emulsion as a result of the addition of suitable silicone surfactants and suitable emulsifiers. The formulations can be prepared either as a 2-pack formulation or as a single formulation. In the case of the single formulation polyethylene glycol is also added. In either case, the formulations show a synergistic effect through the addition of the pigment, the resulting formulations having an increased efficacy. Further, the formulations show a synergistic effect when mixed with conventional chemical fungicides, both being added in reduced amounts compared to recommended rates.2015-03-05
20150065476Scalp Care Composition - A scalp care composition comprising from 1% to 99% of a volatile carrier; from 0.05% to 10% of a polymeric rheology modifier and mixtures thereof; from 0.03% to 1% of particulate scalp benefit agent wherein the composition is shear thinning and has (1) a zero shear viscosity value measured at 0.01 Pa of greater than about 1,500 Pa s; (2) a moderate stress viscosity value measured at 1 Pa viscosity of greater than about 1,000 Pa s; and (3) a high shear rate viscosity value measured at 100 1/s of less than about 0.5 Pa s.2015-03-05
20150065477CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R2015-03-05
20150065478Amino-Derivatives As Novel Inhibitors Of Histone Deacetylase - This invention comprises the novel compounds of formula (I)2015-03-05
20150065479METHOD FOR ENHANCING ANTI-TUMOR EFFECT OF A MICROTUBULE-TARGETING DRUG, AND A METHOD FOR TREATMENT OF TUMOR - A method for treating a tumor by combining a piperidine compound of formula (I) or salt thereof and a microtubule-targeting drug, in which the microtubule-targeting drug is administered once per 7 days or more one cycle, and the piperidine compound is administered once or more per day for 4 days or more:2015-03-05
20150065480MIF INHIBITORS AND THEIR USES - The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.2015-03-05
20150065481MICROBIOCIDAL PYRAZOLE DERIVATIVES - Compounds of the formula I wherein the substituents areas defined in claim 2015-03-05
20150065482ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0):2015-03-05
20150065483Substituted 6,5-Fused Bicyclic Heteroaryl Compounds - The present invention relates to substituted 6,5-fused 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.2015-03-05
20150065484SUSTAINED RELEASE DOSAGE FORMS FOR A JAK1 INHIBITOR - This invention relates to sustained release dosage forms comprising {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and doses and methods related thereto.2015-03-05
20150065485SUBSTITUTED POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE - This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.2015-03-05
20150065486METHODS FOR TREATING POLYCYSTIC KIDNEY DISEASE - Methods for treating autosomal dominant polycystic kidney disease (ADPKD) are described herein. More particularly, methods described herein relate generally to administering glutaminase1 inhibitors to subjects afflicted with ADPKD. Accordingly, the use and application of compounds or agents that inhibit glutaminase1 for treating ADPKD or for use in a medicament for treating ADPKD are encompassed herein.2015-03-05
20150065487MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.2015-03-05
20150065488METHODS OF TREATING DISORDERS ASSOCIATED WITH PROTEIN POLYMERIZATION - The present invention relates to methods of treatment of clinical disorders associated with protein polymerization comprising administering, to a subject, an effective amount of carbamazepine, oxcarbazepine or another carbamazepine-like compound. It is based, at least in part, on the discovery that, in cells having a genetic defect in α1-antitrypsin, carbamazepine was able to decrease levels of the mutant protein. Furthermore, carbamazepine reduced the hepatic load of mutant α1-antitrypsin and the toxic effect of that mutant protein accumulation, hepatic fibrosis, in vivo using a mouse model of the disease. As patients having this defect in α1-antitrypsin exhibit toxic accumulations of the protein, treatment according to the invention may be used to ameliorate symptoms and signs of disease.2015-03-05
20150065489Substituted Quinolines and Their Use As Medicaments - Disclosed are substituted quinolines of formula 12015-03-05
20150065490ORGANIC COMPOUNDS - Compounds of formula I2015-03-05
20150065491ADMINISTRATION OF BENZODIAZEPINE COMPOSITIONS - The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.2015-03-05
201500654925,6-DIHYDRO-1H-PYRIDIN-2-ONE COMPOUNDS - The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.2015-03-05
20150065493PROCESS FOR PREPARING STERILE BRINZOLAMIDE - Process of preparing sterile brinzolamide using ethylene-oxide gas sterilisation, sterile brinzolamide obtainable by said process and pharmaceutical compositions comprising said sterile brinzolamide.2015-03-05
20150065494AMINOSTYRYLBENZOFURAN DERIVATIVES AS INHIBITORS AGAINST BETA-AMYLOID FIBRIL FORMATION, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.2015-03-05
20150065495SUBSTITUTED- 1H-BENZO[D]IMIDAZOLE SERIES COMPOUNDS AS LYSINE-SPECIFIC DEMETHYLASE 1 (LSD1) INHIBITORS - The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.2015-03-05
20150065496PESTICIDAL COMPOSITIONS COMPRISING BENZOYLUREA COMPOUND AND FURTHER PESTICIDAL COMPOUND AND THEIR USES - The present invention relates to Pesticidal compositions comprising a benzoylurea compound (I) being flufenoxuron or teflubenzuron and further pesticidal compounds (II) and optionally compounds (III) in synergistically effective amounts.2015-03-05
20150065497MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.2015-03-05
20150065498N-LINKED LACTAM M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.2015-03-05
201500654993-AMINOTHIENO[3,2-c]QUINOLINE DERIVATIVES, METHODS OF PREPARATION AND USES - The present invention relates to compounds according to Formula I: and salts thereof, wherein R2015-03-05
20150065500Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.2015-03-05
20150065501N-substituted hetero-bicyclic furanone derivatives for combating animal - The invention relates to N-substituted hetero-bicyclic furanone 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 hetero-bicyclic furanone 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 hetero-bicyclic furanone compounds.2015-03-05
20150065502ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib):2015-03-05
20150065503SALT FORM OF A HUMAN HISTONE METHYLTRANSFERASE EZH2 INHIBITOR - Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.2015-03-05
20150065504ANTIVIRAL COMPOUNDS - Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).2015-03-05
20150065505PYRIMIDINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.2015-03-05
20150065506TETRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I:2015-03-05
20150065507NOVEL COMPOUNDS - The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.2015-03-05
20150065508INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.2015-03-05
20150065509HIGHLY 6-SUBSTITUTED -2,4-DIAMINOPYRIMIDINES AS INHIBITORS OF ANTHRAX - 2,4-diaminopyrimidine compounds of generic Formula 1, where R and R′ may be the same or different and are independently selected from: C2015-03-05
20150065510Rilyazine Derivatives and Compositions for The Treatment of Cancer - The present application discloses Rilyazine analogs, methods for their preparation, and the treatment of cancer by the administration of an effective amount of the Rilyazine analogs to a patient in need thereof.2015-03-05
20150065511Compositions and Methods for the Treatment of Presbyopia - The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably use aceclidine separate or together with a cycloplegic agent and/or with a nonionic surfactant and viscosity enhancer, and or with low concentrations of a selective α-2 adrenergic receptor agonist.2015-03-05
20150065512DIOXA-BICYCLO[3.2.1]OCTANE-2,3,4-TRIOL DERIVATIVES - Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).2015-03-05
20150065513DIOXA-BICYCLO[3.2.1]OCTANE-2,3,4-TRIOL DERIVATIVES - Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).2015-03-05
20150065514Methods And Compositions To Reduce Oxidative Stress - The invention relates to therapeutic applications for compositions that reduce the level of oxidative stress on cells in vivo or in vitro. The invention describes methods for improving the therapeutic properties of stem cells. The invention also provides combination therapies that are useful to balance the oxidative microenvironment of cells in vivo or in vitro.2015-03-05
20150065515LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.2015-03-05
20150065516NEW BIARYL AMIDE DERIVATIVES - The invention provides novel compounds having the general formula (I)2015-03-05
20150065517NEW COMPOUNDS - The present invention provides organic compounds of the following structure;2015-03-05
20150065518METHODS OF TREATING CANCER HAVING AN ACTIVE WNT/BETA-CATENIN PATHWAY - The present invention provides methods of treating a subject having a Wnt/beta-catenin active cancer by administering to said subject a compound that inhibits the expression or activity of YES1, BIRC5 or BCL2L1, a compound that inhibits YAP1-beta-catenin complex formation, a compound that inhibits YAP1-beta-catenin complex binding to DNA, a compound that inhibits YAP1-beta-catenin-TBX5 complex formation, or any combination thereof. The compound can be, for example, a nucleic acid, a peptide, an antibody or a small molecule. Methods of screening for therapeutic targets for treating cancer are included.2015-03-05
20150065519HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.2015-03-05
20150065520SUBSTITUTED 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.2015-03-05
20150065521TRIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 MODULATORS - Compounds of the formula I:2015-03-05
20150065522THERAPEUTIC COMPOUNDS AND USES THEREOF - The present invention relates to compounds formula (I):2015-03-05
20150065523CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I) including stereoisomers or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein X is NH, or O; Q is 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; A is phenyl or a 5-6 heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; B may assume different meanings from A and is phenyl or a 5-6 membered heteroaryl group, which may be substituted by one or more substituents independently selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; and processes for their preparation, pharmaceutical compositions containing them and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.2015-03-05
20150065524KINASE INHIBITOR POLYMORPHS - Polymorphs, hydrates, and solvates of chemical compounds that modulate kinase activity, including mTOR activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mTOR activity, are described herein.2015-03-05
20150065525METHODS FOR IMPROVING DIAPHRAGM FUNCTION - Provided are compositions and methods for improving diaphragm function in a patient by administering to the patient an effective amount of a skeletal muscle troponin activator or a pharmaceutically acceptable salt thereof.2015-03-05
20150065526OVERCOMING ACQUIRED RESISTANCE TO CHEMOTHERAPY TREATMENTS THROUGH SUPPRESSION OF STAT3 - This disclosure relates to methods of treating cancer comprising administering an effective amount of a STAT3 inhibitor, prodrugs, or derivatives thereof, in combinations with an EGFR tyrosine kinase inhibitors, prodrugs, or derivatives thereof, to a subject in need thereof. In certain embodiments, the STAT3 inhibitor is niclosamide or salt thereof. In certain embodiments, the EGFR tyrosine kinase inhibitor is erlotinib or salt thereof.2015-03-05
20150065527BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - A pharmaceutical formulation comprising the compound of formula2015-03-05
20150065528PARALYTIC SHELLFISH POISON - The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal.2015-03-05
20150065529SYNERGISTIC FUNGICIDAL MEXURES FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a compound of Formula I-V and at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, and chlorothalonil provides synergistic control of selected fungi.2015-03-05
20150065530BIOMARKER ASSOCIATED WITH IRRITABLE BOWEL SYNDROME AND CROHN'S DISEASE - The present invention provides compositions and methods for characterizing irritable bowel syndrome. In particular, the present invention provides compositions and methods for determining polymorphisms associated with IBS-D and Crohn's disease. The present invention further provides compositions and methods for determining a treatment course of action in subjects with IBS-D and Crohn's disease.2015-03-05
20150065531COMPOUNDS FOR USE IN CANCER THERAPY - Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.2015-03-05
20150065532PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.2015-03-05
20150065533Benzyl-substituted carbamates and use thereof - The present application relates to novel benzyl-substituted carbamates, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.2015-03-05
20150065534INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1 - The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.2015-03-05
20150065535METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome Type 2 diabetes mellitus atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof.2015-03-05
20150065536Benzoic Acid, Benzoic Acid Derivatives and Heteroaryl Carboxylic Acid Conjugates of Hydrocodone, Prodrugs, Methods of Making and Uses Thereof - The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.2015-03-05
20150065537AZABICYCLIC CARBAMATES AND THEIR USE AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory.2015-03-05
20150065538TRPA1 ANTAGONISTS - Compounds of formula (I)2015-03-05
20150065539Methods for Increasing CFTR Activity - The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.2015-03-05
20150065540Treating Neuropathic Pain with Seh Inhibitors - Provided are methods for treating, reducing, alleviating, and/or inhibiting neuropathic pain by orally, intravenously or intrathecally administering an effective amount of an inhibitor of soluble epoxide hydrolase (“sEH”), to a patient in need thereof. The neuropathic pain treated is selected from the group consisting of post-herpetic neuralgia, trigeminal neuralgia, focal peripheral nerve injury, and anesthesia dolorosa, central pain due to stroke or mass lesion, spinal cord injury, or multiple sclerosis, and peripheral neuropathy due to diabetes, HIV, or chemotherapy.2015-03-05
20150065541Bis(difluoromethyl)pyrazoles as Fungicides - Bis(difluoromethyl)pyrazole derivatives of the formula (I)2015-03-05
20150065542ANTI-VIRAL COMPOUNDS - The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.2015-03-05
20150065543DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds having the formula:2015-03-05
20150065544THERAPEUTIC AGENT AND PREVENTIVE AGENT FOR DEMYELINATING DISEASE - The object of the present invention is to provide a novel therapeutic or preventive agent for demyelinating disease. The present invention is a therapeutic or preventive agent for demyelinating disease, containing as an active ingredient a 2-phenylthiazole compound represented by Formula (I)2015-03-05
20150065545Transdermal Delivery of Anastrozole for Systemic Effect - Formulations and methods for transdermal drug delivery compositions that include anastrozole are disclosed. Transdermal anastrozole compositions of the present disclosure may be indicated for treating testosterone deficiency. Disclosed transdermal anastrozole compositions may include permeation enhancers that may improve penetration of anastrozole in human skin. Permeation enhancers within transdermal anastrozole compositions may include oils from Amazon rainforest such as Pracaxi oil, 2015-03-05
20150065546DIARYLHYDANTOIN COMPOUNDS - The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.2015-03-05
20150065547ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION - An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.36 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. The esterified cellulose ether is useful as an excipient for poorly water-soluble drugs.2015-03-05
20150065548COMPOSITION COMPRISING AN ORGANIC DILUENT AND A CELLULOSE ETHER - A liquid composition comprises an organic diluent and at least one cellulose ether 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 hydroxyl groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.29 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. The liquid composition can be used for preparing a solid dispersion of an active ingredient in a cellulose ether.2015-03-05
20150065549Bendamustine Pharmaceutical Compositions - Provided herein are pharmaceutical formulations of dry-powder bendamustine suitable for pharmaceutical use. Also provided are methods of producing dry-powder bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.2015-03-05
20150065550NEW ALPHA2 ADRENOCEPTOR AGONISTS - Compounds of formula (I), wherein X and R2015-03-05
20150065551Use of Dithiine-tetracarboximides for Controlling Phytopathogenic Fungi - The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.2015-03-05
20150065552Use of Indolyl and Indolinyl Hydroxamates for Treating Heart Failure of Neuronal Injury - Novel use of small molecules, particularly indolyl and indolinyl hydroxamates is disclosed herein. The indolyl and indolinyl hydroxamates are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating a patient suffering from heart failure or neuronal injury.2015-03-05
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