02nd week of 2013 patent applcation highlights part 46 |
Patent application number | Title | Published |
20130012442 | VON WILLEBRAND FACTOR- AND FACTOR VIII-POLYMER CONJUGATES HAVING A RELEASABLE LINKAGE - The present invention provides von Willebrand Factor-polymer conjugates and Factor VIII-polymer conjugates, each having a releasable linkage. Methods of making conjugates, methods for administering conjugates, are also provided. | 2013-01-10 |
20130012443 | METHODS OF TREATMENT OF CENTRAL NERVOUS SYSTEM HEMORRHAGE USING PROTOPORPHYRIN IX-FE COMPOUNDS - Described herein are methods and compositions relating to treatment of tissue damage resulting from a central nervous system (CNS) hemorrhage with a protoporphyrin IX-Fe compound. | 2013-01-10 |
20130012444 | CRYSTALLINE SOLVATES OF 6-(PIPERIDIN-4-YLOXY)-2H-ISOQUINOLIN-1-ONE HYDROCHLORIDE - The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)- | 2013-01-10 |
20130012445 | Compositions for Improving Bone Mass - The present invention provides a therapeutic composition, and method of use thereof, for improving bone mass, rigidity, or strength, or preventing and treating bone loss via modulation of the RANK signaling pathway. The therapeutic composition of the present invention comprises a RYBP peptide, or fragments thereof, that specifically interact with a motif of RANK to regulate osteoclastogenesis. The present invention further provides a composition, and method of use thereof, comprising a modulator that is capable of modulating the RYBP-RANK interaction, or modulating an effector in the RANK signaling pathway through the RYBP-RANK interaction. | 2013-01-10 |
20130012446 | COMPOSITIONS AND MANUFACTURE OF MAMMALIAN STEM CELL-BASED COSMETICS - Methods of manufacturing collagen and other extracellular matrix components from SCCs are disclosed. The extracellular matrix components are useful in cosmetic applications, and can be manufactured free of immunogenic concerns and contaminants while controlling for other factors that commonly impact product quality and usefulness. | 2013-01-10 |
20130012447 | PROTEIN KINASE C-DELTA INHIBITORS THAT PROTECT AGAINST CELLULAR INJURY AND INFLAMMATION AND PROMOTE ASTROCYTE PROLIFERATION - The invention relates to the use of δPKC inhibitor peptides to treat brain injury, particularly traumatic brain injury (TBI). In one embodiment, peptide that specifically inhibit δPKC are used to protect neurological tissue by promoting astrocyte proliferation. | 2013-01-10 |
20130012449 | SOLVENT-FREE PROCESS FOR OBTAINING PHOSPHOLIPIDS AND NEUTRAL ENRICHED KRILL OILS - The invention discloses a new solvent-free process for obtaining phospholipids and neutral lipids enriched krill oils containing DHA and EPA poly-unsaturated fatty acids and astaxanthin. The process includes cooking fresh krill at high temperature-without agitation and or grinding; decanting the cooked krill for obtaining a partial de-fatted and de-watered solid and a liquid; squeezing the obtained solid to obtain a press liquid and a solid fraction; centrifuging the press liquid to obtain the phospholipids enriched krill oil; centrifuging of the decanter liquid obtained to obtain the neutral lipid enriched krill oil and stickwater. | 2013-01-10 |
20130012450 | Virion Derived Protein Nanoparticles For Delivering Diagnostic Or Therapeutic Agents For The Treatment Of Dermatology Related Genetic Diseases - This invention relates to a transdermal delivery system for treating skin related genetic diseases. More specifically, the present invention provides particles and methods for using pseudo-viruses, including those derived from the herpes and papillomaviruses, to deliver drugs to keratinocytes and basal membrane cells for the treatment of skin genetic disorders including Pachyonychia Congenita and Xeroderma Pigmentosum. | 2013-01-10 |
20130012451 | COMPOSITIONS AND METHODS FOR INHIBITING MMP-9-MEDIATED CELL MIGRATION - The invention provides peptides, portions and derivatives thereof, that are useful for reducing cell migration, and for reducing symptoms of pathological diseases that are associated with undersirable cell migration, and in particular MMP-9-induced cell migration. | 2013-01-10 |
20130012452 | METHOD FOR TREATING BRAIN CANCER USING A NOVEL TUMOR SUPPRESSOR GENE AND SECRETED FACTOR - The present invention is directed to methods of using HSS1 (Hematopoietic Signal peptide-containing Secreted 1), HSM1 (Hematopoietic Signal peptide-containing Membrane domain-containing 1), or a combination thereof in the treatment of various cancers, such as brain cancers. | 2013-01-10 |
20130012453 | Acceleration Of Wound Healing By A Tissue Inhibitor Of Metalloproteinases (TIMP) Linked To Glycosylphosphatidylinositol (GPI)-Anchors - The present invention relates to fusion constructs of glycosylphosphatidylinositol (GPI)-anchored tissue inhibitors of metalloproteinases (TIMPs) and their use for the treatment of cancer and in regenerative medicine. By this approach, the GPI-anchored TIMP proteins are incorporated into the surface membrane of cells. The fusion constructs of the present invention are effective agents in accelarating wound healing. | 2013-01-10 |
20130012454 | Orally Disintegrating Compositions of Linaclotide - The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well to various methods and processes for the preparation and use of the compositions. | 2013-01-10 |
20130012455 | Use of ARC for inhibiting cell death during liver failure - The invention refers to the use of a polynucleotide encoding “apoptosis repressor with caspase recruitment domain” (ARC) or a functional fragment thereof, and/or an ARC polypeptide or a functional fragment thereof for inhibiting cell death of a liver cell, in particular during liver failure. | 2013-01-10 |
20130012456 | COMPOSITIONS AND METHODS FOR TRANSPORT ACROSS THE BLOOD BRAIN BARRIER - Compositions and methods are provided including a peptide derived from the loop2 domain of the lynx1 protein for transport to a target inside the blood brain barrier. | 2013-01-10 |
20130012457 | BETA SHEET TAPES RIBBONS IN TISSUE ENGINEERING - There is described a material comprising tapes, ribbons, fibrils or fibres characterized in that each of the ribbons, fibrils or fibres have an antiparallel arrangement of peptides in a β-sheet tape-like substructure wherein the material comprises a pair of self assembling complementary polypeptides. | 2013-01-10 |
20130012458 | 7-HYDROXY CHROMONES AS POTENT ANTIOXIDANTS - The present disclosure describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. The present disclosure also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes. Included in this disclosure is an improved method to isolate and purify 7-hydroxychromones from plant sources. | 2013-01-10 |
20130012459 | COMPOSITION FOR INHIBITING THE ONSET OF ARTERIOSCLEROSIS AND INHIBITION METHOD - A composition for inhibiting the onset of arteriosclerosis is characterized by comprising D-psicose as an active ingredient for an antiatherogenic action. The antiatherogenic action as described above includes an action of inhibiting or reducing the expression of a chemokine or a cytokine related to arteriosclerosis in vivo and an action of promoting the expression of a receptor involved in the improvement of arteriosclerosis without affecting the expression of an arteriosclerosis inducer. This composition is used in the form of a product selected from the group consisting of sweeteners, seasonings, food additives, food materials, foods and drinks, health foods and drinks, drugs, quasi drugs and feeds blended with D-psicose and/or its derivative and/or a mixture thereof as the active ingredient. The method of inhibiting the onset of arteriosclerosis is a method of using the above composition. | 2013-01-10 |
20130012460 | TOPICAL PHARMACEUTICAL FORMULATIONS CONTAINING A LOW CONCENTRATION OF BENZOYL PEROXIDE IN SUSPENSION IN WATER AND A WATER-MISCIBLE ORGANIC SOLVENT - An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following, application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea. | 2013-01-10 |
20130012461 | COMPOSITION FOR PREVENTION OF INFLUENZA VIRAL INFECTION COMPRISING TANNIC ACID, AIR FILTER COMPRISING THE SAME AND AIR CLEANING DEVICE COMPRISING THE FILTER - Disclosed are a composition for the prophylaxis of influenza viral infection comprising tannic acid, an air filter coated with the same, and an air cleaner comprising the air filter. Having high inhibitory activity against influenza virus, the composition comprising tannic acid can be applied to the prevention of influenza viral infection. Also, the filter coated with the composition can remove influenza virus from the air so that it can be employed in an air cleaner for the prophylaxis of influenza viral infection. | 2013-01-10 |
20130012462 | RECEPTOR MODULATORS EXHIBITING NEUROPROTECTIVE AND MEMORY ENHANCING ACTIVITIES - The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, methods of enhancing the brain's cognitive functions and methods of treating depression, anxiety and cachexia induced by a chronic disease in mammals and humans. | 2013-01-10 |
20130012463 | IDENTIFICATION OF FREE-B-RING FLAVONOIDS AS POTENT COX-2 INHIBITORS - The present invention provides a novel method for inhibiting the cyclooxygenase enzyme COX-2. The method is comprised of administering a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 mediated diseases and conditions. The method for preventing and treating COX-2 mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids and a pharmaceutically acceptable carrier. | 2013-01-10 |
20130012464 | GLYCYRRHIZINATES OF MORPHINAN DERIVATIVES - The present invention provides a pharmaceutically acceptable compound, a pharmaceutical composition comprising the above-mentioned pharmaceutically acceptable compound. The pharmaceutically acceptable compound provided by the present invention is a salt of a basic group-containing morphinan derivative and a carboxyl group-containing glycyrrhizinic acid and has the ability to be used to manufacture medicaments for treating and/or preventing cough, ameliorating pains, treating respiratory system diseases, treating cardiovascular diseases and treating liver diseases. | 2013-01-10 |
20130012465 | BIBW 2992 FOR USE IN THE TREATMENT OF TRIPLE NEGATIVE BREAST CANCER - The present invention relates to a method of treating patients suffering from triple negative breast cancer comprising administration of an effective amount of the irreversible EGFR/HER1 and HER2 inhibitor BIBW 2992 (1) to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent (2), in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery. | 2013-01-10 |
20130012466 | COLCHICINE NEOGLYCOSIDES AND METHODS FOR THEIR SYNTHESIS AND USE - Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation. | 2013-01-10 |
20130012467 | BQC-G, A TUMOR-SELECTIVE ANTI-CANCER PRODRUG - The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC | 2013-01-10 |
20130012468 | CHEMICAL COMPOUNDS - 3-(2′,3′-dideoxy-ribo-β-L-furanosyl)[2,3-d]pyrimidin-2(3H)-one derivatives comprising 6-substitutents on the base moiety are shown to have anti-viral properties, particularly with respect to vaccinia and measles. The compounds have unnatural L ribose stereochemistry. | 2013-01-10 |
20130012469 | LIQUID NUCLEOTIDES/NUCLEOSIDES-CONTAINING PRODUCT - The invention pertains to a liquid composition for preventing and/or treating memory decline and/or cognitive dysfunction, Alzheimer's, Parkinson's and/or dementia, said composition comprising: (i) at least 50 mg nucleoside and/or nucleotide per 100 ml; (ii) between 0.2 and 10 grams protein per 100 ml; (iii) between 0.05 and 3 wt. % of thickener, based on total weight of the composition. The thickener is preferably selected from the group consisting of cellulose, xanthan gum, gellan gum, alginate, guar gum, locust bean gum, gum karaya, gum tragacanth, carrageenan, and mixtures thereof. The composition preferably has a loss factor tan δ between 0.1 and 100, as measured at any strain in the range of 1-100% at 0.1 Hz and 20° C. It is particularly found that a thickener selected from the group consisting of gellan gum, xanthan gum and cellulose greatly reduces sedimentation. | 2013-01-10 |
20130012470 | ANTIVIRAL COMPOSITIONS AND METHODS OF THEIR USE - Novel compositions comprising viral fusion inhibition compounds and viral replication inhibition compounds as well as methods of their use are disclosed. The novel compositions are useful, inter alia, in the prevention, inhibition and/or treatment of Dengue Fever (DF) or Dengue Hemorrhagic Fever (DHF). | 2013-01-10 |
20130012471 | MEANS AND METHODS FOR PRODUCING ARTIFICIAL CAPSULAR POLYSACCHARIDES OF NEISSERIA MENINGITIDIS - The invention provides for an in vitro method for producing capsular polysaccharides of | 2013-01-10 |
20130012472 | COMPOSITION AND METHODS OF INHIBITING GASTROINTESTINAL PATHOGEN INFECTION - Compositions comprising a milk-derived oligosaccharide such as trifucosyl(1,2-1,2-1,3)-lacto-N-octoase (TFiLNO) and uses thereof for inhibiting invasion of gastrointestinal pathogen into intestinal epithelial cells or for treating an infectious disease (e.g., a disease caused by a gastrointestinal pathogen such as an ETEC) or an inflammatory diseases such as inflammatory bowel disease. | 2013-01-10 |
20130012473 | COMBINED USE OF PHOSPHOLIPID AND SULFATE GROUPS-CARRYING POLYSACCHARIDES FOR INHIBITING METASTATIC SPREAD - The invention relates to a medicament comprising a phospholipid component and a polysaccharide component having polysaccharides containing sulfate groups for inhibiting metastatic spread of tumors. The two components may be in same or separate preparation. | 2013-01-10 |
20130012474 | Cellulose Gel Formulations - The invention relates to dispersible cellulose powder compositions comprising non-seed cellulose powder derived from algae, fungi or tunicates, which compositions are useful in a variety of products such as food products, pharmaceuticals, cosmetics, paints, biocompatible materials for artificial tissue engineering and implantable biomaterials and relates to methods for preparing non-seed cellulose powder compositions. | 2013-01-10 |
20130012475 | Cosmetic and Pharmaceutical Composition Comprising N-Acetylglucosamine-6-Phosphate - The present invention relates to a cosmetic or pharmaceutical composition comprising N-acetylglucosamine-6-phosphate or a salt thereof and, optionally, a compound of the vitamin A family, and also to a device containing same. | 2013-01-10 |
20130012476 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention relates to compounds of formula (I) | 2013-01-10 |
20130012477 | DERIVATIVES OF DILLAPIOL AND RELATED MONOLIGNANS AND USE THEREOF - Derivatives of dillapiol, sesamol and related monolignans having the following general formula: | 2013-01-10 |
20130012478 | DOSAGE FORMS OF BISPHOSPHONATES - Provided is an oral dosage form comprising a bisphosphonate selected from the group consisting of a risedronate and salts thereof; an ethylenediaminetetraacetic acid (EDTA) or a pharmaceutically acceptable salt thereof; and a delayed release mechanism to deliver the risedronate and the EDTA in the lower gastrointestinal tract, wherein the oral dosage form is administered according to a scheduled dosing interval. The present invention substantially alleviates the interaction between bisphosphonates and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of the bisphosphonate and the chelating agent to the lower GI tract, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies. | 2013-01-10 |
20130012479 | POLYMORPHS OF 6-(PIPERIDIN-4-YLOXY)-2H-ISOQUINOLIN-1-ONE HYDROCHLORIDE - The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments. | 2013-01-10 |
20130012480 | CRYSTALLINE SALTS OF (4S,4AS,5AR,12AS)-4-DIMETHYLAMINO-3,10,12,12A-TETRAHYDROXY-7-[(METHOXY(ME- THYL)AMINO)-METHYL]-1,11-DIOXO-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-NAPHTHACENE-- 2-CARBOXYLIC ACID AMIDE AND METHODS OF USING THE SAME - A crystalline mono hydrochloride salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide is disclosed having improved stability. In addition, a crystalline mono mesylate salt and crystalline mono sulfate salt of (4S,4aS,5aR,12aS)-4-dimethylamino-3,10,12,12a-tetrahydroxy-7-[(methoxy(methyl)amino)-methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-naphthacene-2-carboxylic acid amide are also disclosed having improved stability. A pharmaceutical composition containing the crystalline salts and methods of treating inflammatory skin disorders and bacterial infections comprising administering the crystalline salts are also disclosed. | 2013-01-10 |
20130012481 | CRYSTALLINE FORMS OF TIGECYCLINE HYDROCHLORIDE - The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament. | 2013-01-10 |
20130012482 | INTRAVENOUS FORMULATION WITH WATER-SOLUBLE COCRYSTALS OF ACETYLSALICYLIC ACID AND THEANINE - A water-soluble cocrystal composition contains a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from an alpha variant of theanine or a beta variant of theanine or other form of theanine. | 2013-01-10 |
20130012483 | NOVEL PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF NEURODEGENERATIVE OR NEUROVASCULAR DISEASES - The present invention relates to a pharmaceutical composition comprising an NMDA receptor antagonist and vitamin D as active ingredients for the treatment of neurodegenerative or neurovascular diseases. | 2013-01-10 |
20130012484 | PETROLEUM JELLY-FREE UNGUENT COMPOSITIONS COMPRISING VITAMIN D COMPOUNDS AND OPTIONALLY STEROIDAL ANTI-INFLAMMATORY AGENTS - Novel compositions in petroleum jelly-free unguent form, in particular for topical application, contain a vitamin D compound and optionally an active agent of the family of steroidal anti-inflammatory agents. | 2013-01-10 |
20130012485 | ORGANIC COMPOUNDS - Compounds of the formula (I) are provided: | 2013-01-10 |
20130012486 | COMBINATION STEROID AND GLUCOCORTICOID RECEPTOR ANTAGONIST THERAPY - The present invention provides compositions of an anti-inflammatory glucocorticosteroid and a glucocorticoid receptor (GR) modulator useful for inhibiting glucocorticoid receptor induced transactivation without substantially inhibiting glucocorticoid receptor induced transrepression. Also provided are methods of treating a disorder or condition and reducing the side effects of glucocorticosteroid treatment, using the compositions of the present invention. | 2013-01-10 |
20130012487 | 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS - 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions. | 2013-01-10 |
20130012488 | BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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. | 2013-01-10 |
20130012489 | Morpholinylquinazolines - The invention relates to compounds of the formulae (I), (II) and (III) | 2013-01-10 |
20130012490 | Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators - A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 2013-01-10 |
20130012491 | PYRIMIDINE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS - Disclosed are pyrimidine derivatives for use as a sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis. | 2013-01-10 |
20130012492 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: | 2013-01-10 |
20130012493 | NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE - The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R | 2013-01-10 |
20130012494 | CYCLOPROPYL-FUSED-1,3-THIAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I | 2013-01-10 |
20130012495 | 5HT2C RECEPTOR MODULATORS - The present invention relates to novel compounds of Formula (I): | 2013-01-10 |
20130012496 | BENZAZEPINE COMPOUND - Provided is a compound which is useful as an agent for treating or preventing 5-HT | 2013-01-10 |
20130012497 | METHODS FOR DETECTING ADHD SUSCEPTIBILITY AND PREDICTING SEVERITY AND LONG TERM OUTCOME OF ADHD SYMPTOMS - The invention provides methods of determining an altered susceptibility to develop ADHD, methods of predicting or determining the severity of symptoms of ADHD and associated disorders, and methods of treatment based on the presence or absence of one or more alleles of single nucleotide polymorphism (SNP) markers. | 2013-01-10 |
20130012498 | 5HT2C RECEPTOR MODULATORS - The present invention relates to novel compounds of Formula (I): | 2013-01-10 |
20130012499 | TRPV4 ANTAGONISTS - The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 2013-01-10 |
20130012500 | ORGANIC COMPOUNDS - A compound of Formula I | 2013-01-10 |
20130012501 | PYRIMIDINEDIAMINE KINASE INHIBITORS - Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders. | 2013-01-10 |
20130012502 | Pharmaceutical or Veterinary Antiviral Compositions - Pharmaceutical or veterinary compositions to prevent or treat viral infections, in particular to prevent or treat influenza A, B and C virus infections. | 2013-01-10 |
20130012503 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 2013-01-10 |
20130012504 | BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I: | 2013-01-10 |
20130012505 | BENZONAPHTHYRIDINAMINES AS AUTOTAXIN INHIBITORS - The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases. | 2013-01-10 |
20130012506 | ANTI-INFECTIVE PYRIDO (1,2-A) PYRIMIDINES - The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis. | 2013-01-10 |
20130012507 | SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - Compounds represented by formula (Ia) or (Ib) and wherein R and R | 2013-01-10 |
20130012508 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 2013-01-10 |
20130012509 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 2013-01-10 |
20130012510 | 1-BENZYL-3-HYDROXYMETHYLINDAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES BASED ON THE EXPRESSION OF MCP-1 AND CX3CR1 - The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1. | 2013-01-10 |
20130012511 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver. | 2013-01-10 |
20130012512 | P38 MAP kinase inhibitors - There are provided inter alia compounds of formula (I) | 2013-01-10 |
20130012513 | HEDGEHOG INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders. | 2013-01-10 |
20130012514 | AMINOALKYLOXAZOLE AND AMINOALKYLTHIAZOLECARBOXYLIC ACID AMIDES AS REGENERATION-PROMOTING SUBSTANCES FOR SENSORY ORGANS AND POST-MITOTIC TISSUE - Aminoalkyloxazole and aminoalkylthiazolecarboxylic acid amides of formulae (1) and (2) | 2013-01-10 |
20130012515 | Fused Bicyclic Pyridine and Pyrazine Derivatives as Kinase Inhibitors - A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 2013-01-10 |
20130012516 | 6-CYCLOAMINO-3-(PYRID-4-YL)IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): | 2013-01-10 |
20130012517 | Quinoline and Quinoxaline Derivatives as Kinase Inhibitors - A series of quinoline and quinoxaline derivatives, substituted by an optionally substituted bicyclic heteroaryl moiety consisting of two fused six-membered aromatic rings attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 2013-01-10 |
20130012518 | BICYCLIC COMPOUNDS AND THEIR USES AS DUAL C-SRC / JAK INHIBITORS - The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3. | 2013-01-10 |
20130012519 | Biomarker Identifying the Reactivation of STAT3 After Src Inhibition - A method of identifying cancer or an associated disorder comprising identifying and quantifying STAT3 occurring in a biological sample taken from a subject after administering a SFK inhibitor to said subject. | 2013-01-10 |
20130012520 | TRAZODONE AND TRAZODONE HYDROCHLORIDE IN PURIFIED FORM - A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride. | 2013-01-10 |
20130012521 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 2013-01-10 |
20130012522 | NEW DERIVATIVES OF PROPARGYLAMINE HAVING NEUROPROTECTIVE CAPACITY FOR THE TREATMENT OF ALZHEIMER'S AND PARKINSON'S DISEASES - The present invention relates to a compound of formula (I) wherein: R | 2013-01-10 |
20130012523 | PYRAZINONE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND THEIR USES - The present invention relates to pyrazinone derivatives of formula (I): | 2013-01-10 |
20130012524 | STABILIZED PROLONGED RELEASE PHARMACEUTICAL COMPOSITION COMPRISING ATYPICAL ANTIPSYCHOTIC - The present invention provides stabilized prolonged release pharmaceutical compositions comprising atypical antipsychotic drug like paliperidone or pharmaceutically acceptable salts thereof without incorporating surfactant and/or water penetration enhancer. Such compositions are preferably in the form of a matrix wherein one or more release controlling agents are present in and/or on the matrix. Further, such compositions comprise one or more release controlling agent and exhibits desired in vitro release of drug with or without lag period. The invention also provides a process for the preparation of such compositions. | 2013-01-10 |
20130012525 | INHIBITORS OF BRUTON'S TYROSINE KINASE FOR THE TREATMENT OF SOLID TUMORS - Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors. | 2013-01-10 |
20130012526 | OXAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. | 2013-01-10 |
20130012527 | PREQ1 RIBOSWITCHES AND METHODS AND COMPOSITIONS FOR USE OF AND WITH PREQ1 RIBOSWITCHES | 2013-01-10 |
20130012528 | NOVEL DERIVATIVES OF ERLOTINIB - This invention relates to novel compounds and hydrochloric acid salts thereof. More specifically, this invention relates to novel compounds and hydrochloric acid salts thereof derived from erlotinib. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor, such as erlotinib. | 2013-01-10 |
20130012529 | HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I) | 2013-01-10 |
20130012530 | New Positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. | 2013-01-10 |
20130012531 | TREATMENT METHOD - The present invention is directed to methods of treating disorders of ocular angiogenesis or vascular leakage in a patient by administration of suitable inhibitors, including pazopanib or pharmaceutically acceptable salts or hydrates thereof. | 2013-01-10 |
20130012532 | CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R | 2013-01-10 |
20130012533 | CONTROLLED RELEASE OXYCODONE COMPOSITIONS - A method for preparing a solid oral dosage form comprising up to about 160 mg of oxycodone or a salt thereof to control pain in substantially all patients is disclosed. The method comprises wet granulating at least one hydrophilic or hydrophobic polymer, preferably a hydroxyalkyl cellulose or an alkyl cellulose, with oxycodone or a salt thereof to form a controlled-release matrix. Repeated “q12h” (i.e., every 12 hour) administration of the dosage form through steady-state conditions results in a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after administration. | 2013-01-10 |
20130012534 | Pharmaceutical Compositions Comprising Prasugrel and Cyclodextrin Derivatives and Methods of Making and Using the Same - The present invention is directed to pharmaceutical compositions comprising prasugrel and a cyclodextrin derivative, and methods of making and using the same. | 2013-01-10 |
20130012535 | SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation. | 2013-01-10 |
20130012536 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, | 2013-01-10 |
20130012537 | 3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE - A method for treatment of a systemic wasting disease, by administering, to a subject in need thereof, an effective amount of a 3,8-diaminotetrahydroquinoline derivative represented by formula (Ia) (wherein X represents CH | 2013-01-10 |
20130012538 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example. | 2013-01-10 |
20130012539 | Compositions and Methods for Treating Lysosomal Disorders - The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds. | 2013-01-10 |
20130012540 | Hepatitis C Virus Inhibitors - This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds. | 2013-01-10 |
20130012541 | Therapeutic Agents Useful for Treating Pain - A compound of formula: | 2013-01-10 |
20130012542 | INJECTABLE DEPOT FORMULATION COMPRISING CRYSTALS OF ILOPERIDONE - An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation. | 2013-01-10 |