39th week of 2012 patent applcation highlights part 49 |
Patent application number | Title | Published |
20120245110 | VASCULAR LEAKAGE INHIBITOR - The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present disclosure inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, enhances the cortical actin ring structure, and improves the stability of the tight junctions (TJs) between vascular cells, thereby inhibiting vascular leakage. The vascular leakage inhibitor of the present disclosure has the activity of not only reducing vascular permeability but also recovering the integrity of damaged blood vessels. Accordingly, the vascular leakage inhibitor of the present disclosure can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present disclosure is synthesized from commercially available or easily synthesizable cholesterols, it has remarkably superior feasibility of commercial synthesis. | 2012-09-27 |
20120245111 | FLAVANONES-CONTAINING FOOD COMPOSITIONS - The present invention relates to food products comprising flavanones. In particular, it relates to food products comprising hesperidin having improved stability. The present invention also concerns processes for the manufacturing of food products comprising said flavanones, especially hesperidin and to the use of the food products in the manufacture of compositions for the improvement of bone and skin health. Said flavanones are subjected to heating in water to a temperature of at least 138° C. | 2012-09-27 |
20120245112 | SYNTHESIS AND IDENTIFICATION OF NOVEL RSK-SPECIFIC INHIBITORS - A composition comprising an SL0101 [kaempferol 3-O-(3″,4″-di-O-acetyl-α-L-rhamnopyranoside)] derivative compound that has enhanced ability to inhibit RSK activity, relative to the parent compound is provided. The compounds have utility for treating any disease or conditions characterized or associated with excess or undesirable RSK activity. For example the RSK inhibitors of the present invention can be used to reduce the proliferation of neoplastic cells or for inhibiting the establishment or maintenance of an intracellular pathogenic infection by pathogens whose pathogenicity derives in part from the pathogen's ability to impede endosomal/phagosomal maturation in the host cell. | 2012-09-27 |
20120245113 | CLERODANE DERIVATIVES FOR MODULATION OF LEUKOTRIENE RECEPTOR ACTIVITY AND RELATED DISEASES - The use or methods of use of extracts comprising one or more special clerodane compounds against inflammatory (including allergic) diseases or conditions, as well as novel compounds of this type, said clerodane derivatives for use against inflammatory (including allergic) diseases or conditions, pharmaceutical formulations comprising them especially for use against inflammatory disease or conditions, and related embodiments; said extract and/or compound(s) for use in the treatment or in the preparation of a medicament (including a nutraceutical) for the prophylactic and/or therapeutic treatment of said disease or condition, as well as their preparation; pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in said prophylactic and/or therapeutic treatment, and related embodiments. | 2012-09-27 |
20120245114 | METHOD FOR THE PROTECTION OF TREES - The present invention provides a method for the prevention/treatment of bark beetle and/or wood borer infestation of trees comprising treatment of the tree with a composition comprising a macroyclic lactone. | 2012-09-27 |
20120245115 | 1-Methylnicotinaide Derivatives and Formulations of Treatment of Lipoprotein Abnormalities - The present invention is directed to nicotinamide derivatives, and their use in treating lipoprotein abnormalities, alone or in combination with a statin. | 2012-09-27 |
20120245116 | Inhibiting GS-FDH to Modulate No Bioactivity - Patients needing NO donor therapy or inhibition of pathologically proliferating cells or increased NO bioactivity are treated with a therapeutically effective amount of an inhibitor of glutathione-dependent formaldehyde dehydrogenase. | 2012-09-27 |
20120245117 | METHODS OF TREATING SQUAMOUS CELL LUNG CANCER WITH 4-IODO-3-NITROBENZAMIDE IN COMBINATION WITH GEMCITABINE AND CARBOPLATIN - In one aspect, the present invention provides a method of treating squamous cell lung cancer in an individual comprising administering to the individual having lung cancer an effective amount of 4-iodo-3-nitrobenzamide or a metabolite thereof or pharmaceutically acceptable salt thereof; gemcitabine; and carboplatin. | 2012-09-27 |
20120245118 | METHODS AND COMPOSITIONS FOR ALLEVIATING STUTTERING - Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of gamma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexyl)isoindolin- | 2012-09-27 |
20120245119 | METHOD FOR SEPARATING SIALYLLACTOSE MATERIAL - A method for easily and efficiently separating a sialyllactose material from a milk material is disclosed. The method comprises removing proteins from the milk material to obtain a protein-free liquid, adjusting the pH of the protein-free liquid to obtain a pH-adjusted liquid, and concentrating the pH-adjusted liquid by an ultrafiltration (UF) membrane. Since the method also allows separation of sialyllactose from lactose and minerals, sialyllactose can be obtained with high purity, making the sialyllactose material highly useful for food, pharmaceutical, and other applications. | 2012-09-27 |
20120245120 | ZINC SUCROSE OCTASULFATES, THEIR PREPARATION, AND PHARMACEUTICAL AND COSMETIC USES THEREOF - The present invention relates to a zinc sucrose octasulfate of the general formula I, a process for preparing same and its use in the pharmaceutical and/or cosmetic field | 2012-09-27 |
20120245121 | METHODS FOR IMPROVING BONE HEALTH IN INFANTS USING LONG CHAIN POLYUNSATURATED FATTY ACIDS - Disclosed are methods for improving bone health, strength and formation in an infant who may be susceptible to developing bone health issues from conception through adolescence. The methods include administration of a nutritional formulation including at least one LCPUFA to a woman during pregnancy and optionally during lactation and breastfeeding of an infant. | 2012-09-27 |
20120245122 | CAROTENOID-CONTAINING COMPOSITIONS AND METHODS - The present invention is directed to carotenoid-containing compositions and methods for improving bone or respiratory health in a subject comprising administering to the subject a combination of lycopene, beta-carotene, and beta-cryptoxanthin. | 2012-09-27 |
20120245123 | METHODS FOR IMPROVING BONE HEALTH IN INFANTS USING PREBIOTICS - Disclosed are methods for improving bone health, strength and formation in an infant who may be susceptible to developing bone health issues from conception through adolescence. The methods include administration of a nutritional formulation including a prebiotic to a woman during pregnancy and optionally during lactation and breastfeeding of an infant. | 2012-09-27 |
20120245124 | TRPV3 Modulators - Disclosed herein are modulators of TRPV3 of formula (I) | 2012-09-27 |
20120245125 | PYRIDAZINE COMPOUNDS, COMPOSITIONS AND METHODS - The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications. | 2012-09-27 |
20120245126 | DIVALENT AND OXABRIDGED HETEROCYCLIC NEONICOTINOID COMPOUNDS AND PREPARATION METHODS THEREOF - Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as | 2012-09-27 |
20120245127 | Methods of Treating Cell Proliferative Disorders - The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a Syk kinase or Syk/Flt-3 kinase inhibitor. Cell proliferative disorders treatable by the methods include, hematopoietic neoplasms and virally associated tumors. The compounds are also directed to therapeutic or prophylactic inhibition of tumor metastasis. | 2012-09-27 |
20120245128 | RAPID DETECTION AND QUANTIFICATION OF MODIFICATION OF MEDICINAL COMPOUNDS AND DRUG RESISTANCE ACTIVITY - The present disclosure in general relates to methods, systems, and apparatus for identifying modification of a medicinal compound exposed to a sample for use in determining which treatment to provide to a subject in need thereof. | 2012-09-27 |
20120245129 | USE OF S1P RECEPTOR MODULATOR - Use of an S1P receptor modulator in the treatment or prevention of a disease or condirion dependent on brain-derived neurotrophic factor (BDNF) expression. | 2012-09-27 |
20120245130 | Methods of Using Substituted Tetracycline Compounds to Modulate RNA - A method for modulating RNA with tetracycline compounds is described. | 2012-09-27 |
20120245131 | 6-SUBSTITUTED ESTRADIOL DERIVATIVES FOR USE IN REMYELINATION OF NERVE AXONS - Disclosed is a method of remyelinating axons with 6-substituted estradiol compounds of the formula | 2012-09-27 |
20120245132 | Composition Comprising Benzoic Acid in Combination with Organic Acid Preservatives as Active Ingredients and the Use Thereof - The present invention relates to the use of low content of benzoic acid and/or sodium salt thereof in combination with one or more organic acid preservatives as active ingredients in the manufacture of a vaginal composition, wherein the composition has weak inhibition effect on normal vaginal lactobacilli while has strong inhibition effect on vaginal fungi and/or pathogenic vaginal lactobacilli, the organic acid preservatives are selected from the group consisting of dehydroacetic acid and/or sodium salt thereof, propionic acid and/or a salt thereof, sorbic acid and/or a salt thereof. The composition of the present invention is particularly useful in inhibiting vaginal fungi, and/or inhibiting pathogenic vaginal lactobacilli, and/or promoting normal vaginal lactobacilli, and/or maintaining normal vaginal acidity, and/or modulating vaginal microecosystem, and/or modulating vaginal microbials, and/or selectively decontaminating vagina. | 2012-09-27 |
20120245133 | METHODS FOR THE TREATMENT OF A TRAUMATIC CENTRAL NERVOUS SYSTEM INJURY - Methods of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury, are provided. The methods comprise a therapy comprising a constant or a two-level dosing regime of progesterone. In one method, a subject in need thereof is administered at least one cycle of therapy, wherein the cycle of therapy comprises administering a therapeutically effective two-level intravenous dosing regime of progesterone. The two-level dosing regime comprises a first time period, wherein a higher hourly dose of progesterone is administered to the subject, followed by a second time period, wherein a lower hourly dose of progesterone is administered to the subject. | 2012-09-27 |
20120245134 | ANDROGEN PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING DEPRESSION - The present invention relates to methods, kits, combinations, and compositions for treating, preventing or reducing the risk of developing a depressive disorder, or the symptoms associated with, or related to a depressive disorder in a subject in need thereof. The present invention also relates to a method of administering a steroid in the testosterone synthetic pathway, for example testosterone, to a subject in need thereof. In addition, the methods, kits, combinations and compositions may be used in conjunction with other pharmaceutical agents including agents effective at treating, preventing, or reducing the risk of developing a depressive disorder in a subject. | 2012-09-27 |
20120245135 | Gallium Complexes, Pharmaceutical Compositions And Methods Of Use - The present invention provides complexes of gallium with a ligand, methods of making the complexes, methods of using the complexes and pharmaceutical gallium compositions comprising the complexes, in particular those compositions suitable for therapeutic oral administration. | 2012-09-27 |
20120245136 | CHROMAN-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2012-09-27 |
20120245137 | ARYL SULPHONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I). | 2012-09-27 |
20120245138 | N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 2012-09-27 |
20120245139 | INHIBITORS OF THE HEDGEHOG PATHWAY - The present invention is directed to a compound of Formula I | 2012-09-27 |
20120245140 | N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS - N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors. | 2012-09-27 |
20120245141 | ACTIVATORS OF HUMAN PYRUVATE KINASE - Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R | 2012-09-27 |
20120245142 | 3-OXO-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES AS PARP INHIBITORS - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds. | 2012-09-27 |
20120245143 | 3-0X0-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES WITH SELECTIVE PARP-1 INHIBITION - There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. | 2012-09-27 |
20120245144 | BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE - Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 2012-09-27 |
20120245145 | METHOD AND COMPOSITIONS FOR TREATMENT AND PREVENTION OF BROAD SPECTRUM VIRUS AILMENTS COMPRISING A CALCIUM CHANNEL BLOCKER OR A CALMODULIN BLOCKER - In the broadest aspect, the invention provides a composition for and a method of prophylactic and/or therapeutic treatment of a animal/mammal for any viral disease, mixed bacterial and viral infections, bacterial infections, bacterial endotoxins, bacterial exotoxins, autoimmune diseases, and cellular or humoral mediated allergic conditions that is caused by any virus that relies on the maintenance of specific calcium ion concentrations for the post ribosomal RNA synthesis processing of viral protein translation, transportation and processing of viral structural components by utilizing a therapeutic amount of a blocker selected from the group consisting of a calcium channel blocker, a metabolite thereof, a calmodulin blocker and a metabolite thereof, and a pharmaceutical acceptable diluent or carrier; and/or is caused by damage to the animal/mammal by a pathological immune response to antigens. | 2012-09-27 |
20120245146 | METHOD OF TREATMENT OF HORMONE DEPLETION INDUCED VASOMOTOR - The invention provides a method to effectively wean a woman from hormone therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for a limited period of a duration between 3 and 8 months. | 2012-09-27 |
20120245147 | INHIBITORS OF THAPSIGARGIN-INDUCED CELL DEATH - Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death. | 2012-09-27 |
20120245148 | TETRAHYDROQUINOXALINE UERA DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application. | 2012-09-27 |
20120245149 | NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS - The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): | 2012-09-27 |
20120245150 | NOVEL (HETEROCYCLE/TETRAHYDROPYRIDINE)-(PIPERAZINYL)-1-ALCANONE AND (HETEROCYCLE/DIHYDROPYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE DERIVATIVES, AND USE THEREOF AS p75 INHIBITORS - The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): | 2012-09-27 |
20120245151 | BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS - Disclosed are compounds of Formula (I) or prodrugs thereof; | 2012-09-27 |
20120245152 | 3-(BIARYOXY)PROPIONIC ACID DERIVATIVE - A compound of the general formula (I): | 2012-09-27 |
20120245153 | MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof. | 2012-09-27 |
20120245154 | SUBSTITUTED AMINOTHIAZINE DERIVATIVE - The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid β protein, for example, a compound of formula (I), wherein, R | 2012-09-27 |
20120245155 | FUSED HETEROCYCLIC COMPOUND HAVING AMINO GROUP - The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-βproteins. | 2012-09-27 |
20120245156 | ORAL LYOPHILIZED COMPOSITIONS - The present invention relates to a method for preparing an oral lyophilizate composition comprising:
| 2012-09-27 |
20120245157 | OXAZINE DERIVATIVES - The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins. | 2012-09-27 |
20120245158 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I. | 2012-09-27 |
20120245159 | COMPOSITION AND METHOD FOR CONTROLLING ARTHROPOD PESTS - The present invention provides: an arthropod pests control composition comprising, as active ingredients, a condensed heterocyclic compound and a neonicotinoid compound; a method for controlling arthropod pests which comprises applying effective amounts of a condensed heterocyclic compound and a neonicotinoid compound to the arthropod pests or a locus where the arthropod pests inhabit; and so on. | 2012-09-27 |
20120245160 | POLYMORPHOUS FORMS III AND IV OF N-BENZOYL - STAUROSPORINE - The present invention relates to a crystalline form III and a crystalline form IV of N-benzoyl staurosporine. N-benzoyl staurosporine is also known as Midostaurin or PKC412. | 2012-09-27 |
20120245161 | INDOLYL-PIPERIDINYL BENZYLAMINES AS BETA-TRYPTASE INHIBITORS - The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula | 2012-09-27 |
20120245162 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 2012-09-27 |
20120245163 | TRPV1 Antagonists - Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, | 2012-09-27 |
20120245164 | DIPHENYL-PYRAZOLOPYRIDINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF AS NUCLEAR RECEPTOR NOT MODULATORS - The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3. | 2012-09-27 |
20120245165 | NOVEL BENZOFURAN TYPE DERIVATIVES, A COMPOSITION COMPRISING THE SAME FOR TREATING OR PREVENTING COGNITIVE DYSFUNCTION AND THE USE THEREOF - The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder. | 2012-09-27 |
20120245166 | TREATMENT OF NEURODEGENERATIVE DISEASES, CAUSATION OF MEMORY ENHANCEMENT, AND ASSAY FOR SCREENING COMPOUNDS FOR SUCH - Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning. | 2012-09-27 |
20120245167 | ARTHROPOD PEST CONTROL METHOD AND COMPOSITION - Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A | 2012-09-27 |
20120245168 | Composition, Synthesis, and Use of New Substituted Pyran and Pterin Compounds - The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency. | 2012-09-27 |
20120245169 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 2012-09-27 |
20120245170 | PYRAZOLOPYRIDINE DERIVATIVES AS ANTICANCER AGENT - The present invention concerns compounds of following general formula (I): (Formula I) and their pharmaceutically acceptable salts, their method of preparation and their uses, notably as anticancer agent. | 2012-09-27 |
20120245171 | BENZPYRAZOLE DERIVATIVES AS INHIBITORS OF PI3 KINASES - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 2012-09-27 |
20120245172 | HETEROCYCLIC AMINE DERIVATIVES - The present invention relates to compounds of formula I | 2012-09-27 |
20120245173 | INHIBITION OF ACTIVATED CDC42-ASSOCIATED KINASE 1 - Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided. | 2012-09-27 |
20120245174 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer. | 2012-09-27 |
20120245175 | MK2 INHIBITORS - The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases. | 2012-09-27 |
20120245176 | NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS - A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: | 2012-09-27 |
20120245177 | CRYSTALLINE LEVOFOLINIC ACID AND PROCESS FOR ITS PREPARATION - The present invention relates to stable crystalline (6S)—N(5)-formyl-5,6,7,8-tetrahydrofolic acid, commonly referred to as levofolinic acid, in essentially pure 6S diastereomeric form, and to a process for its preparation. | 2012-09-27 |
20120245178 | CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR - Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor. | 2012-09-27 |
20120245179 | Method Of Therapeutic Administration of DHE To Enable Rapid Relief Of Migraine While Minimizing Side Effect Profile - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 2012-09-27 |
20120245180 | COMBINATION - The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer. | 2012-09-27 |
20120245182 | CRYSTALLINE FORMS OF 3-(2,6-DICHLORO-3,5-DIMETHOXY-PHENYL)-1--1-METHYL-UREA AND SALTS THEREOF - The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them. | 2012-09-27 |
20120245183 | MACROCYCLIC LACTONE DERIVATIVES FOR THE TREATMENT OF CANCER - The present invention provides compounds represented by formula (1): wherein, R | 2012-09-27 |
20120245184 | SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION - The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity. | 2012-09-27 |
20120245185 | ARYL AND HETEROARYL SULFONES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. | 2012-09-27 |
20120245186 | COMBINATION CANCER THERAPY WITH HSP90 INHIBITORY COMPOUNDS - Disclosed is a method for treating a subject with cancer, comprising administering to the subject an effective amount of paclitaxel or a paclitaxel analogue and an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein. | 2012-09-27 |
20120245187 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I) | 2012-09-27 |
20120245188 | METHODS OF TREATING MEMORY LOSS AND ENHANCING MEMORY PERFORMANCE - The present invention provides methods and compositions for enhancing working memory impaired due to aging, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), Parkinson's disease, alcoholism or alcohol withdrawal or Huntington's disease using p38 MAPK inhibitor such as SB239063. | 2012-09-27 |
20120245189 | CRYSTALLINE CDC7 INHIBITOR SALTS - The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide. | 2012-09-27 |
20120245190 | AUTOPHAGY INDUCING COMPOUND AND THE USES THEREOF - The present invention relates to a composition comprising compounds of formula (I-V), | 2012-09-27 |
20120245191 | NEW AZASPIRODECANONE COMPOUNDS - The invention provides novel compounds having the general formula (I) | 2012-09-27 |
20120245192 | PHARMACEUTICAL FORMULATIONS CONTAINING RIFAXIMIN, PROCESSES FOR THEIR OBTAINMENT AND METHOD OF TREATING INTESTINAL DISEASE - Disclosed herein are methods of treating a patient having an intestinal disorder, the methods comprising: administering to a patient in need thereof a pharmaceutical composition comprising a hydrate or solvate form of rifaximin in polymorphic form β, alone or in a mixture with other crystalline, hydrate, solvate or amorphous forms of rifaximin, in gastroresistant microgranules, wherein the rifaximin is administered at a dose of at least 800 mg per day for a period of at least 7 days. | 2012-09-27 |
20120245194 | SMALL MOLECULE INHIBITORS OF THE ALPHA4-PAXILLIN INTERACTION - The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5, with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin-alpha.4 interaction. The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition. | 2012-09-27 |
20120245195 | NOVEL MONOHYDRATE OF AZAADAMANTANE DERIVATIVES - The invention relates to a crystalline monohydrate of (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.1 | 2012-09-27 |
20120245196 | 1-SUBSTITUTED 2-AZABICYCLO [3.1.1] HEPTYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS FOR TREATING NEUROLOGIC DISORDERS - This invention provides 2-azabicyclo[3.1.1]heptyl derivatives, and methods for producing them, which are useful therapeutic agents for preventing or treating central nervous system disorders and disease mediated by a Nicotinic Acetylcholine Receptor such as, but not limited to, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, dementia, pain and nicotine addiction. | 2012-09-27 |
20120245197 | PHARMACEUTICAL COMPOSITION CONTAINING TOSUFLOXACIN OR SALT THEREOF - A pharmaceutical composition containing tosufloxacin or a salt thereof, which is excellent in stability and preservative effect and contamination preventing effect is provided. A pharmaceutical composition containing tosufloxacin or a salt thereof, a metal compound comprising aluminum, borax, an alkali metal chloride and a preservative is excellent in stability and preservative effect and contamination preventing effect, and useful especially as eye drops, nasal drops and ear drops. | 2012-09-27 |
20120245198 | COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF CANCER - Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions. | 2012-09-27 |
20120245199 | [4 [4-(AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL- )-METHANONES AND SYNTHESIS THEREOF - The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase. | 2012-09-27 |
20120245200 | CRYSTAL FORM OF QUINOLINE COMPOUND AND PROCESS FOR ITS PRODUCTION - A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula ( | 2012-09-27 |
20120245201 | Isopropylphenidate for Treatment of Attention-Deficit/Hyperactivity Disorder and Fatigue-Related Disorders and Conditions - The present invention relates to the identification of isopropylphenidate as a useful therapeutic agent in the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) as well as various fatigue causing disease and disorders and medication induced fatigue. | 2012-09-27 |
20120245202 | METHODS AND PRODUCTS FOR TREATING INFLAMMATION - Pharmaceutical compositions comprising an isolated form of a compound of Formula I or IA (e.g., anatabine or S-(−)-anatabine) or a salt thereof can be used to treat disorders comprising an inflammatory component, including chronic, low-level inflammation. Compounds of Formula I also can be provided, for example, in other vehicles such as beverage products and consumer products such as lotions and creams. | 2012-09-27 |
20120245203 | METHODS FOR TREATING HEARTBURN AND/OR PREVENTING GASTRIC BLEEDING OR HEMORRHAGE IN PATIENTS RECEIVING CLOPIDOGREL THERAPY - The present invention relates to methods of treating heartburn in a patient receiving clopidogrel therapy. In another aspect, the present invention relates to methods of preventing gastric bleeding or hemorrhage in patients receiving clopidogrel therapy. | 2012-09-27 |
20120245204 | Unknown - Heteroarylpiperidine and -piperazine derivatives of the formula (I) | 2012-09-27 |
20120245205 | COMPOSITIONS AND METHODS FOR INHIBITING HAIR GROWTH - A method for inhibiting hair growth in mammals using compositions containing FP receptor antagonists (e.g., prostaglandin F analogs that are block activation of the FP receptor). The compositions can be applied topically to the skin and/or hair. The compositions can arrest hirsutism or hypertrichosis, reverse hirsutism and hypertrichosis, and further prevent hair growth. These compositions can also be used to protect hair from chemical or radiation-induced alopecia or hair loss. These compositions can also be used to inhibit pigmentation of the hair or skin. | 2012-09-27 |
20120245206 | MULTI-CYCLIC COMPOUNDS AND METHODS OF USE - The present invention relates to compounds of Formulas I and II, | 2012-09-27 |
20120245207 | NICOTINIC ACID COMPOSITIONS FOR TREATING HYPERLIPIDEMIA AND RELATED METHODS THEREFOR - An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyper lipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day “nocturnally,” that is in the evening or at night. | 2012-09-27 |
20120245208 | 2-Oxo-1-Pyrrolidinyl Imidazothiadiazole Derivatives - The present invention relates to 2-oxo-1-pyrrolidine imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 2012-09-27 |
20120245209 | HETEROCYCLIC SULFONAMIDE DERIVATIVES - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation). | 2012-09-27 |
20120245210 | Novel Thiophene Inhibitors of S-Nitrosoglutathione Reductase - The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 2012-09-27 |
20120245211 | Methods of Treating Cognitive Dysfunction by Modulating Brain Energy Metabolism - Methods for treating cognitive dysfunction by modulating brain energy metabolism are discussed. | 2012-09-27 |