48th week of 2015 patent applcation highlights part 21 |
Patent application number | Title | Published |
20150336924 | AMIDOALKYLENYL AND AMIDOARYL ESTERS, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE - The invention provides ester compounds for treating ophthalmic diseases. The esters of the invention are particularly advantageous due to their stability in aqueous solutions. | 2015-11-26 |
20150336925 | SUBSTITUTED BENZOFURAN, BENZOTHIOPHENE AND INDOLE MCL-1 INHIBITORS - The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. | 2015-11-26 |
20150336926 | FLUORINATION OF ARYL COMPOUNDS - The invention provides compositions and methods of using the compositions in fluorinating aryl precursors containing a leaving group replaceable by a fluorine atom. The compositions include a metal ion source, a electrophilic fluorine source, a base, and a compound, which is an aryl precursor of the aryl fluoride, and which has a leaving group replaceable by the fluorine atom. Exemplary methods of the invention make use of such compositions and methods to prepare an aryl fluoride compound. In an exemplary embodiment, the electrophilic fluorine source is a source of | 2015-11-26 |
20150336927 | SUBSTITUTED DIOXOPIPERIDINYL PHTHALIMIDE DERIVATIVES - This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent. | 2015-11-26 |
20150336928 | Heterocyclic Compounds And Methods Of Use Thereof - Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. | 2015-11-26 |
20150336929 | PROCESSES FOR THE PREPARATION OF PESTICIDAL COMPOUNDS - The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds. | 2015-11-26 |
20150336930 | 1',3'-Disubstituted-4-Phenyl-3,4,5,6-Tetrahydro-2H,1'H-[1,4']Bipyridinyl-2- '-Ones - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 2015-11-26 |
20150336931 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds of general formula I: | 2015-11-26 |
20150336932 | MULTIFUNCTIONAL NITROXIDE DERIVATIVES AND USES THEREOF - Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction. | 2015-11-26 |
20150336933 | Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof - The present invention relates to compounds of general formula (I) | 2015-11-26 |
20150336934 | 2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME - The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase. | 2015-11-26 |
20150336935 | SHIP1 MODULATORS AND METHODS RELATED THERETO - Compounds of formula (I): where, n, R | 2015-11-26 |
20150336936 | NOVEL COMPOUNDS - Compounds of formula (I): | 2015-11-26 |
20150336937 | CARBAZOLE COMPOUND AND ORGANIC LIGHT EMITTING DEVICE INCUDING THE SAME - A carbazole compound represented by Formula 1 | 2015-11-26 |
20150336938 | METHOD FOR PREPARATION OF JUSTICIDIN A DERIVATIVES OF ARYLNAPHTHALENE LIGNAN STRUCTURE - The present disclosure relates to a novel method for preparing an arylnaphthalene lignan compound. In synthesis of arylnaphthalene lignan compounds and derivatives according to the present disclosure, a naphthalene backbone may be constructed first and an aryl group may be introduced at the final stage. Through this, various kinds of derivatives that could not be prepared from the existing methods can be synthesized effectively. Further, the synthesis method according to the present disclosure is appropriate for large-scale production. | 2015-11-26 |
20150336939 | LFA-1 INHIBITOR AND METHODS OF PREPARATION AND POLYMORPH THEREOF - Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed. | 2015-11-26 |
20150336940 | THERAPEUTIC SUBSTITUTED PYRROLES - Disclosed herein are compounds of the formula: | 2015-11-26 |
20150336941 | THERAPEUTIC ISOXAZOLE COMPOUNDS - The invention provides a compound of formula I: | 2015-11-26 |
20150336942 | Aminopyridine derived compounds as LRRK2 inhibitors - The present invention is directed to aminopyridine derived compounds of formula (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinson's disease or cancer. | 2015-11-26 |
20150336943 | NOVEL BENZODIOXANE-PIPERIDINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS FOR TREATING NEUROPSYCHIATRIC DISORDERS - The present invention concerns benzodioxane-piperidine with general formula I: | 2015-11-26 |
20150336944 | Sodium Channel Blockers, Preparation Method Thereof and Use Thereof - The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD). | 2015-11-26 |
20150336945 | QUINOLINE AND QUINAZOLINE AMIDES AS MODULATORS OF SODIUM CHANNELS - The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: | 2015-11-26 |
20150336946 | NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment. | 2015-11-26 |
20150336947 | PYRROLOQUINOLINE ALKALOIDS AS ANTIMALARIAL AGENTS AND PROCESS FOR THE PREPARATION THEREOF - The patent provides novel compounds with potential anti-malarial activity and process of synthesis thereof. Further, the process for the synthesis of known antimalarial natural products marinoquinazolinone A-F, aplidiopsamine A and their potential antimalarial analogues is disclosed. | 2015-11-26 |
20150336948 | Isotopically Labeled Biaryl Urea Compounds - The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers. | 2015-11-26 |
20150336949 | 3-(Pyrazolyl)-1H-Pyrrolo[2,3-b]Pyridine Derivatives as Kinase Inhibitors - The present application relates to novel 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. | 2015-11-26 |
20150336950 | CRYSTAL FORM OF COMPOUND USED AS MINERALOCORTICOID RECEPTOR ANTAGONIST AND PREPARATION METHOD THEREFOR - The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases. | 2015-11-26 |
20150336951 | Process For The Preparation Of A DPP-IV Inhibitor - The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I | 2015-11-26 |
20150336952 | Imidazo[4,5-c]quinolin-2-one Compounds and Their Use in Treating Cancer - The specification generally relates to compounds of Formula (I): | 2015-11-26 |
20150336953 | NEW PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS (PDE-10) - The present invention relates to novel pyrimidine derivatives of formula (I) | 2015-11-26 |
20150336954 | Process for Manufacturing a Naphthyridine Derivative - The invention relates to a process and synthetic intermediates that can be used for manufacturing the compound of formula (1-6) which is a synthetic intermediate useful in the preparation of antibiotic compounds. | 2015-11-26 |
20150336955 | PIPERIDINO-PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS - This invention relates to piperidino-pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. | 2015-11-26 |
20150336956 | AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 2015-11-26 |
20150336957 | NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed. | 2015-11-26 |
20150336958 | SUBSTITUTED ACETYL-COA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I) | 2015-11-26 |
20150336959 | Electronic Device - The present application relates to an electronic device comprising a heteroaromatic compound of a formula (I) as functional material, in particular as electron-transport material and as matrix material for emitter compounds. | 2015-11-26 |
20150336960 | ARYL-SUBSTITUTED FUSED BICYCLIC PYRIDAZINE COMPOUNDS - The present invention provides a compound of formula (I) as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula (I), and pharmaceutical compositions comprising such compounds. | 2015-11-26 |
20150336961 | PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF - The present invention relates to process for the preparation of tofacitinib and intermediates thereof. | 2015-11-26 |
20150336962 | 5-CHLORO-2-DIFLUOROMETHOXYPHENYL PYRAZOLOPYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein. | 2015-11-26 |
20150336963 | LIVER 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. | 2015-11-26 |
20150336964 | FUSED HETEROAROMATIC PYRROLIDINONES - Disclosed are compounds of Formula 1, | 2015-11-26 |
20150336965 | NOVEL ANTIVIRAL COMPOUNDS - The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection. | 2015-11-26 |
20150336966 | SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer. | 2015-11-26 |
20150336967 | Novel Benzimidazole Derivatives as Kinase Inhibitors - The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders. | 2015-11-26 |
20150336968 | QUARTERNARY AMMONIUM PERFLUOROALKOXY SALTS FOR PREPARATION OF PERFLUOROPOLYETHERS - The present invention relates to anhydrous tetraalkyl pnictogen perfluoroalkoxy salts and a process to produce anhydrous tetraalkyl pnictogen perfluoroalkoxy salts. The process involves contacting a hydrofluoroether and an amine to produce a tetraalkyl pnictogen perfluoroalkoxy salt in the presence of a solvent. The present invention also relates to processes of preparing fluoroalkyl ether acid fluoride polymers using tetraalkyl pnictogen perfluoroalkoxy salt. The present invention further relates to some novel fluorinated alkyl polyether polymers. | 2015-11-26 |
20150336969 | NMDA Receptor Modulators and Uses Thereof - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 2015-11-26 |
20150336970 | MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R | 2015-11-26 |
20150336971 | PROCESS FOR THE PREPARATION OF MORPHINE ANALOGS VIA METAL CATALYZED N-DEMETHYLATION/FUNCTIONALIZATION AND INTRAMOLECULAR GROUP TRANSFER - The present application is directed to an efficient conversion of C-14 hydroxylated morphine alkaloids to various morphine analogs, such as naltrexone, naloxone and nalbuphone. One feature of this process is an intramolecular functional group transfer from the C-14 hydroxyl to the N-17 nitrogen atom following a palladium-catalyzed N-demethylation. | 2015-11-26 |
20150336972 | TRANSITION METAL-CATALYZED PROCESSES FOR THE PREPARATION OF N-ALLYL COMPOUNDS AND USE THEREOF - The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine. | 2015-11-26 |
20150336973 | MONOCLINIC CRYSTALLINE FORM OF ASENAPINE MALEATE WITH A SPECIFIC PARTICLE SIZE DISTRIBUTION - A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60° C.; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof. | 2015-11-26 |
20150336974 | Cyclic Sulfonamides as Sodium Channel Blockers - The present disclosure provides cyclic sulfonamides of Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R | 2015-11-26 |
20150336975 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - The present disclosure provides a series of compounds of the formula (I) | 2015-11-26 |
20150336976 | DIPICOLYLAMINE DERIVATIVES AND THEIR PHARMACEUTICAL USES - Dipicolylamine compounds of Formula (I) set forth herein. Also disclosed are pharmaceutical compositions containing metal ions and these compounds. Further disclosed is a method for treating a condition associated with cells containing inside-out phosphatidylserine, with these compounds. | 2015-11-26 |
20150336977 | Coumestan, Coumestrol, Coumestan Derivatives and Processes of Making the Same and Uses of Same - The present invention provides new coumestans compounds and processes for the preparation of coumestans, pharmaceutical compositions having a coumestan as an active pharmaceutical ingredient, and methods of utilizing coumestans as selective estrogen receptor modulators (SERMs) for treating estrogen dependent diseases such as breast cancer. | 2015-11-26 |
20150336978 | IMPROVED METHOD FOR MANUFACTURING 1,4:3,6-DIANHYDROHEXITOL DI(ALKYL CARBONATE)S - The present invention relates to a process for the manufacturing of pure and substantially oligomers-free 1,4:3,6-dianhydrohexitol di(alkyl carbonate)s which comprises the steps of: a) Preparing a reaction mixture consisting of at least one dianhydrohexitol, at least 2 molar equivalents with respect to the amount of dianhydrohexitol present, of at least one dialkyl carbonate of formula R—O—C(═O)—O—R, where R has the same meaning indicated above, and from 0.01 to less than 0.1 molar equivalents of a transesterification catalyst with respect to the amount of dianhydrohexitol present; and b) Heating the reaction mixture up to its reflux temperature in a reactor preferably equipped with a rectification column comprising a number of theoretical distillation plates sufficient to separate continuously from the reaction mixture by fractional distillation the alcohol obtained or the azeotrope which the alcohol forms with the dialkyl carbonate present in the reaction mixture. The process comprises further recovering the transesterification catalyst from the reaction mixture and isolating the 1,4:3,6-dianhydrohexitol di(alkyl carbonate). | 2015-11-26 |
20150336979 | ISOMANNIDE DERIVATIVES AS INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE - The present invention relates to compounds of the formula (I), wherein R1, R11, R12 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are highly potent and selective soluble epoxide hydrolase inhibitors and are suitable, for example, for the therapy and prophylaxis of renal failure, diabetic nephropathy, type 2 diabetes mellitus, inflammation or could show beneficial effects in pain, dyslipidemia and atherosclerosis. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them. | 2015-11-26 |
20150336980 | Pseudopolymorphic Forms Of A HIV Protease Inhibitor - New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed. | 2015-11-26 |
20150336981 | MODIFIED POLYPHENOLS AND MODIFIED POLYPHENOL COMPOSITIONS - This invention relates to polyphenolic compounds, in particular ethoxylated polyphenolic compounds and the use of such compounds in disease prevention, disease treatment, and life extension in humans and animals. The invention also relates to methods of preparing ethoxylated polyphenolic compounds, and preparation of compositions comprising the compounds, including dietary supplements and foods. The inventors describe how modified C-glycosidic ellagitannins are safe, palatable and effective at medium and high doses, and produce broad and profound health outcomes in mammals. | 2015-11-26 |
20150336982 | Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof - A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer. | 2015-11-26 |
20150336983 | ANTIMICROBIAL COMPOUNDS - Provided are compounds which are useful for controlling microorganisms in aqueous or water-containing systems or in systems which are exposed to moisture, including at elevated temperature. The antimicrobial compounds are of the formula I: | 2015-11-26 |
20150336984 | BENZOXAZINE OXAZOLIDINONE COMPOUND, PREPARATION METHOD AND APPLICATION THEREOF - Disclosed are a benzoxazine oxazolidinone compound shown by a general formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a preparation method thereof, and an application thereof in preparing a drug for treating an infectious disease and in particular, an infectious disease caused by multidrug resistant bacteria. | 2015-11-26 |
20150336985 | FUNGICIDAL HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, | 2015-11-26 |
20150336986 | TRICYCLIC COMPOUNDS FOR INHIBITING THE CFTR CHANNEL - The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2015-11-26 |
20150336987 | NOVEL MONOPHOSPHITE LIGANDS HAVING A CARBONATE GROUP - A monophosphite ligand having a carbonate group is useful for hydroformylation. | 2015-11-26 |
20150336988 | NOVEL MONOPHOSPHITE LIGANDS HAVING A TERT-BUTYLOXYCARBONYL GROUP - A novel monophosphite ligand having a tert-butyloxycarbonyl group is useful as a ligand in hydroformylation of an olefin. | 2015-11-26 |
20150336989 | MIXTURE CONTAINING A MONOPHOSPHITE LIGAND AND THE USE THEREOF FOR CATALYSIS OF A HYDROFORMYLATION REACTION - A mixture containing a monophosphite ligand is useful for the catalysis of a hydroformylation reaction. | 2015-11-26 |
20150336990 | PRODUCTION OF LITHIUM DIPHENYLPHOSPHIDE - Lithium diphenylphosphide solutions in a solvent, e.g., diethoxymethane (DEM), that are more stable than when tetrahydrofuran (THF) is used as a solvent. Methods of producing them are also disclosed. | 2015-11-26 |
20150336991 | NOVEL GLUCOKINASE ACTIVATOR COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT - Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. | 2015-11-26 |
20150336992 | OXAZOLIDINONE-QUINOLONE HYBRID ANTIBIOTICS - The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria: | 2015-11-26 |
20150336993 | MITOCHONDRIA-TARGETED THERANOSTIC AGENTS - Mitochondria-targeted theranostic agents and methods of using them diagnostically and therapeutically are disclosed. In particular, the invention relates to theranostic agents comprising F16, or analogues thereof, conjugated to alkyltriphenylphosphonium lipophilic cations, and their uses in medical imaging and treatment of diseases associated with mitochondrial dysfunction, including cancer. | 2015-11-26 |
20150336994 | BCL-2/BCL-XL INHIBITORS AND THERAPEUTIC METHODS USING THE SAME - Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed. | 2015-11-26 |
20150336995 | PROCESS FOR PREPARING 2,2'-BIPHENOLS USING SELENIUM DIOXIDE AND HALOGENATED SOLVENT - 2,2′-biphenol is prepared in a process using selenium dioxide and a halogenated solvent. | 2015-11-26 |
20150336996 | MANGANESE-BASED MAGNETIC RESONANCE CONTRAST AGENTS - Manganese coordination complexes with utility as magnetic resonance probes and as biological reductant sensors are disclosed. In one embodiment, ligands can stabilize both the Mn | 2015-11-26 |
20150336997 | MANGANESE-BASED MAGNETIC RESONANCE CONTRAST AGENTS - Manganese coordination complexes with utility as magnetic resonance probes and as biological reductant sensors are disclosed. In one embodiment, ligands can stabilize both the Mn | 2015-11-26 |
20150336998 | MAGNETIC SUBSTANCE - The present disclosure relates to a ferromagnetic substance containing a crystal of a metal complex molecule in which a heterocycle is bonded to metal, the metal of the metal complex molecule is bonded to the metal of another metal complex via oxygen as a electron donor, and the ferromagnetic substance has a ferromagnetic property balanced with stability of crystals based on a metal—electron donor—metal bond angle that is from 130° to 160°. The present disclosure also relates to a drug containing, as a principal component, the crystal of the metal complex molecule. | 2015-11-26 |
20150336999 | PROCESS FOR THE PRODUCTION OF SOPHOROSE STARTING FROM SOPHOROLIPIDS - The present invention concerns a process for the production of sophorose starting from sophorolipid, in which a step for the hydrolysis of sophorolipid is carried out in an aqueous medium in the presence of an acidic compound. | 2015-11-26 |
20150337000 | Mannose-Receptor Selective Lysinylated Cationic Amphiphiles and a Process for Preparation Thereof - The present invention relates to the mannose-receptor selective lysinylated cationic amphiphile and a process for preparation thereof. The compounds of the present invention can target DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterparts in genetic immunization in mice. The present invention discloses that immunization with electrostatic complexes (lipoplexes) of DNA vaccines encoding melanoma antigens (gp100 and tyrosinase) and liposome of the presently described novel lysinylated cationic amphiphiles with mannose-mimicking shikimoyl head-groups provides long-lasting (100 days post melanoma tumor challenge) protective immunity in all immunized mice. Cationic amphiphiles with mannose-mimicking shikimoyl head-groups described in the present invention are likely to find future applications in the field of genetic immunization. | 2015-11-26 |
20150337001 | ASTER GLEHNI EXTRACTS, FRACTIONS OR COMPOUNDS ISOLATED THEREFROM FOR THE TREATMENT OR PREVENTION OF HYPERURICEMIA OR GOUT - The present invention relates to an | 2015-11-26 |
20150337002 | NUCLEOSIDE AND NUCLEOTIDE HAVING SULFONAMIDE STRUCTURE - The present invention provides compounds shown by the formula: | 2015-11-26 |
20150337003 | ABIRATERONE AND ANALOGS THEREOF FOR THE TREATMENT OF DISEASES ASSOCIATED WITH CORTISOL OVERPRODUCTION - Novel analogs of abiraterone and methods of treating diseases associated with the overproduction of cortisol, such as Cushing's syndrome, obesity, headache depression, hypertension, diabetes mellitus type II, metabolic syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, stroke or incidentalomas, by administering an effective amount of abiraterone or analogs thereof to a patient in need thereof are described. | 2015-11-26 |
20150337004 | NOVEL BETULINIC ACID PROLINE DERIVATIVES AS HIV INHIBITORS - The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases. | 2015-11-26 |
20150337005 | ESTERS OF GLYCYRRHETINIC ACID, PREPARATION AND COSMETIC APPLICATIONS THEREOF - An ester of glycyrrhetinic acid with (poly)glycerol-sorbitol and cosmetic compositions thereof is described. The introduction of sorbitol in the (poly)glycerol chain determines an increase in solubility of the ester of the invention increasing solubility in water and the possibility of using glycyrrhetinic acid in cosmetic applications. | 2015-11-26 |
20150337006 | PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF - The present invention further provides method of preparing nanocrystals or microcrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma). | 2015-11-26 |
20150337007 | PROCESS FOR THE PREPARATION OF UNSATURATED TRIFLUOROMETHANESULFONATE STEROID DERIVATIVES - Disclosed is a method for the conversion of a compound of formula 3 to a compound | 2015-11-26 |
20150337008 | METHOD FOR PRODUCING FIBROIN POWDER FROM SILK PRODUCTS OR FILAMENTS - Method for producing a fibroin powder from silk products or filaments without sericin and dyes having the following phases: a) introduction of products or filaments into a very tightly-woven sealed bag with high filtering capacity to allow the treatment liquid but not the silk fibrils to exit; b) introduction of the bag into a tank; with fresh and hot water with a mixer, in which soda is added to the water for a time of some hours; c) a rinsing phase of which the last is made with acetic acid in such a way as to make the fibre acceptable to the cutis as originally; d) phase of centrifugation and drying tumbler; e) tumbling phase, first opening the bags to throw away the material dried in the tumblers by pulverizing the fibre with a homogenous fragmentation in such a way as to keep the fibrils whole. | 2015-11-26 |
20150337009 | TOLL-LIKE RECEPTOR 2-AGONISTIC LIPOPEPTIDES, AND METHOD OF MAKING THE SAME - The present disclosure is directed to a novel class of toll-like receptor 2-agonistic (TLR2) lipopeptide compounds having specific structures, and synthetic methods of making the compounds. These compounds provide high potency of agonistic activities with human, other than murine, TLR2, and are useful as vaccine adjuvants. Vaccines are perhaps one of the most successful medical interventions against infectious disease. | 2015-11-26 |
20150337010 | Method for treating or preventing liver related diseases - This invention discloses an isolated peptide containing an amino acid sequence of SEQ ID No.1. The isolated peptide is capable of providing the effects in suppressing hepatocyte apoptosis, attenuating hepatic triglyceride accumulation, suppressing the expression of inflammatory cytokines, inhibiting expression of pro-apoptotic proteins, enhancing expression of survival factor and inhibiting the expression of biomarker of hepatic fibrosis. Therefore, this invention discloses the peptide as the effective ingredient in a composition for treating or preventing liver related diseases. | 2015-11-26 |
20150337011 | DENDRIMERIC PEPTIDES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Novel peptide compounds and pharmaceutical compositions thereof are disclosed that have a formula represented by the following formula (I) wherein L | 2015-11-26 |
20150337012 | EGFR-BINDING PEPTIDE - Provided are a substance capable of binding to EGFR specifically with a high affinity and a pharmaceutical agent containing the substance. A peptide which contains at least an amino acid sequence is represented by the formula (1), (2) or (3), as described in the specification, and is composed of 12 to 50 amino acids: | 2015-11-26 |
20150337013 | NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS - The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against | 2015-11-26 |
20150337014 | Theragnostic Particles - The present invention provides viral-based nanoparticles for therapeutic and diagnostic use, and methods for making and using the nanoparticles. Specifically, such nanoparticles comprise decoration-competent viral particles shells such as expanded capsids of phages, stabilized with engineered decoration proteins that have been linked to one or more compounds not naturally occurring on a wild type viral capsid. | 2015-11-26 |
20150337015 | ANTIVIRAL RIFT VALLEY FEVER VIRUS PEPTIDES AND METHODS OF USE - The invention entails synthetic short peptides based on Rift Valley Fever Virus (RVFV) fusion protein. The peptides are broad-spectrum antivirals, and are useful for prophylactic treatment against or therapeutic treatment of infection by hemorrhagic fever viruses, such as RVFV, Ebola Virus, and Andes Virus, as well as vesicular stomatitis virus. | 2015-11-26 |
20150337016 | Methods and Compositions for Targeting Heterologous Integral Membrane Proteins to the Cyanobacterial Plasma Membrane - This disclosure pertains to the functional localization of heterologous integral plasma membrane proteins (HIPMPs) lacking cleavable signal sequences into the plasma membrane (PM) of cyanobacterial hosts, e.g., JCC138 ( | 2015-11-26 |
20150337017 | Genes Encoding Novel Lipid Transporters and their Use to Increase Oil Production in Vegetative Tissues of Plants - The present invention discloses a novel gene encoding a transporter protein trigalactosyldiacylglycerol-5 (TGD5), mutations thereof and their use to enhance TAG production and retention in plant vegetative tissue. | 2015-11-26 |
20150337018 | USE OF COMPOUNDS THAT SELECTIVELY MODULATE ASTROCYTIC RELEASE OF SUBSTANCES THROUGH HEMICHANNELS OF CONNEXINS AND PANNEXINS, WITHOUT INFLUENCING GAP JUNCTIONS, FOR THE TREATMENT OF PSYCHIATRIC DISORDERS - The present invention is related to the use of compounds or pharmaceutically acceptable salts thereof that modulate astrocytic release of substances through connexin and pannexin hemichannels, for the treatment of psychiatric disorders. Compounds or pharmaceutically acceptable salts thereof used in the present invention comprise any compound that differentially modulates, blocks, opens, inhibits, and/or activates connexin and/or pannexin hemichannels from astrocytes while not affecting gap junctions. The invention is also related to a method for treating psychiatric disorders, comprising administering to a mammal or human a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, that modulates astrocytic release of substances through connexin and pannexin hemichannels. Pharmaceutical compositions and a screening method are also considered in the present invention. Examples are shown for connexin 43, connexin 30 and pannexin 1 hemichannel modulators shown not to affect gap junctions, in the form of both non peptide compounds and peptides which were tested in different models for psychiatric disorders, comprising PTSD, memory, anxiety and depression. | 2015-11-26 |
20150337019 | ANTI-INFLAMMATORY PROTEINS AND PEPTIDES AND METHODS OF PREPARATION AND USE THEREOF - The present disclose relates to anti-inflammatory proteins/peptides, their uses, methods of preparation and methods of their detection. In particular, the invention relates to major royal jelly proteins modified by methylglyoxal and fragments thereof from a | 2015-11-26 |
20150337020 | CCN3 AND CCN3 PEPTIDES AND ANALOGS THEREOF FOR THERAPEUTIC USE - The present invention provides a method for treating a human patient with a pathology by administering to the subject an effective amount of an agent selected from the group of: native full-length CCN3 proteins; analog CCN3 full-length proteins with native cysteine residues substituted by a replacement amino acid; CCNp native peptide fragments having from about 12 to about 20 amino acids; analog CCNp peptide fragments with native cysteine residues substituted with a replacement amino acid; and combinations thereof. | 2015-11-26 |
20150337021 | Molecules, Compositions and Methods to Treat Organ Scarring - The present disclosure provides molecules, compositions and methods for treating scarring in organs. The molecules, compositions and methods treat scarring by modulating the WNT, platelet-derived growth factor receptor (PDGFR), transforming growth factor-beta (TGF3) and/or connective-tissue growth factor (CTGF) signaling pathways. | 2015-11-26 |
20150337022 | SEQUENCE OF NUCLEOTIDES AND PEPTIDES GSE 24.2 OF DYSKERIN, WHICH CAN INDUCE TELOMERASE ACTIVITY, METHOD FOR OBTAINING SAME, THERAPEUTIC COMPOSITIONS AND APPLICATIONS THEREOF - This invention relates to a compound that induces or activates telomerase activity based on the nucleotide sequence of the GSE 24.2 fragment of dyskerin or the protein or peptide sequence encoded by said nucleotide sequence. Another part of the invention relates to vectors that comprise said sequence and cells transformed thereby, and pharmaceutical compositions that contain all these elements. These compositions may be used in the treatment of diseases from the following group: ageing or acceleration of ageing, neurodegenerative diseases and dyskeratosis congenita. | 2015-11-26 |
20150337023 | Colon and Pancreas Cancer Peptidomimetics - The invention relates to a peptidomimetic of an NPC-1 epitope on the MUC5AC protein which is differentially expressed in pancreatic and colorectal cancer, and diagnostic and therapeutic usages. Further, antibodies that selectively bind the NPC-1 epitope peptidomimetics and may be used in diagnostic and therapeutic methods. | 2015-11-26 |