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02nd week of 2013 patent applcation highlights part 46
Patent application numberTitlePublished
20130012435MULTIVALENT FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS - The present invention relates to multivalent polypeptides comprising at least two fibronectin scaffold domains connected via a polypeptide linker. The invention also relates to multivalent polypeptides for use in diagnostic, research and therapeutic applications. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins.2013-01-10
20130012436FIBRONECTIN BASED SCAFFOLD DOMAIN PROTEINS THAT BIND IL-23 - The present invention relates to fibronectin based scaffold domain protein that bind interleukin 23 (IL-23), specifically the p19 subunit of IL-23. The invention also relates to the use of the innovative proteins in therapeutic applications to treat autoimmune diseases. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins.2013-01-10
20130012437LYTIC PEPTIDES HAVING ANTI-PROLIFERATIVE ACTIVITY AGAINST PROSTATE CANCER CELLS - Lytic peptides, including fusion peptides of lytic peptides conjugated with luteinizing hormone-releasing hormone or modified versions thereof to target luteinizing hormone-releasing hormone receptors, are disclosed. The lytic peptides show anti-proliferative activity against human prostate cancer cell lines, but are nontoxic to normal primary human prostate epithelial cells or to bone marrow stromal cells in co-culture. The lytic peptides have specificity for and anti-proliferative activity against prostate cancer tumor cells, and low toxicity for normal prostate cells, making the peptides useful in therapies for prostate cancer.2013-01-10
20130012438KALLIKREIN INHIBITORS AND ANTI-THROMBOLYTIC AGENTS AND USES THEREOF - Methods, kits and compositions are described that include a non-naturally occurring kallikrein inhibitor and an anti-thrombolytic agent, e.g., an anti-fibrinolytic agent, for preventing or reducing blood loss and/or ischemia, e.g., ischemia associated with perioperative blood loss and cerebral ischemia, the onset of systemic inflammatory response, and/or reperfusion injury, e.g., reperfusion injury associated with cerebral ischemia or a focal brain ischemia, e.g., in patients subjected to invasive surgical procedures, especially procedures requiring cardiopulmonary bypass.2013-01-10
20130012439COMPOSITION FOR NASAL ADMINISTRATION AND METHOD FOR PREPARING SAME - The invention provides a powdered composition for nasal administration, comprising a physiologically active peptide and cellulose acetate as the base, and having excellent nasal absorption for physiologically active peptides.2013-01-10
20130012440PREVENTIVE AND/OR THERAPEUTIC AND/OR AGGRAVATION SUPPRESSING AGENT FOR HUMAN ARTHRITIS DEFORMANS - A medicine that is extremely useful for preventing and/or treating osteoarthritis, which includes a parathyroid hormone (PTH), and methods of use of such medicine.2013-01-10
20130012441PREDICTION AND PREVENTION OF PREECLAMPSIA - The present disclosure relates to methods for assessing increased risk of preeclampsia in a pregnant woman. The methods described herein employ measuring relaxin levels, and optionally measuring C-reactive protein levels in a biological sample of a pregnant woman. The disclosure further encompasses methods of reducing the risk of preeclampsia and treating it, once it has occurred by administering a pharmaceutical formulation of relaxin to a pregnant woman.2013-01-10
20130012442VON 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
20130012443METHODS 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
20130012444CRYSTALLINE 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
20130012445Compositions 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
20130012446COMPOSITIONS 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
20130012447PROTEIN 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
20130012448SYNTHETIC PEPTIDE AMIDES - The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P2013-01-10
20130012449SOLVENT-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
20130012450Virion 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
20130012451COMPOSITIONS 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
20130012452METHOD 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
20130012453Acceleration 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
20130012454Orally 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
20130012455Use 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
20130012456COMPOSITIONS 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
20130012457BETA 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
201300124587-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
20130012459COMPOSITION 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
20130012460TOPICAL 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
20130012461COMPOSITION 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
20130012462RECEPTOR 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
20130012463IDENTIFICATION 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
20130012464GLYCYRRHIZINATES 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
20130012465BIBW 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
20130012466COLCHICINE 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
20130012467BQC-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 (IC2013-01-10
20130012468CHEMICAL 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
20130012469LIQUID 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
20130012470ANTIVIRAL 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
20130012471MEANS 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
20130012472COMPOSITION 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
20130012473COMBINED 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
20130012474Cellulose 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
20130012475Cosmetic 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
20130012476COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention relates to compounds of formula (I)2013-01-10
20130012477DERIVATIVES OF DILLAPIOL AND RELATED MONOLIGNANS AND USE THEREOF - Derivatives of dillapiol, sesamol and related monolignans having the following general formula:2013-01-10
20130012478DOSAGE 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
20130012479POLYMORPHS 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
20130012480CRYSTALLINE 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
20130012481CRYSTALLINE 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
20130012482INTRAVENOUS 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
20130012483NOVEL 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
20130012484PETROLEUM 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
20130012485ORGANIC COMPOUNDS - Compounds of the formula (I) are provided:2013-01-10
20130012486COMBINATION 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
201300124871-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
20130012488BENZOXEPIN 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
20130012489Morpholinylquinazolines - The invention relates to compounds of the formulae (I), (II) and (III)2013-01-10
20130012490Pyrimidine 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
20130012491PYRIMIDINE 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
20130012492FUSED 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
20130012493NOVEL 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, R2013-01-10
20130012494CYCLOPROPYL-FUSED-1,3-THIAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I2013-01-10
201300124955HT2C RECEPTOR MODULATORS - The present invention relates to novel compounds of Formula (I):2013-01-10
20130012496BENZAZEPINE COMPOUND - Provided is a compound which is useful as an agent for treating or preventing 5-HT2013-01-10
20130012497METHODS 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
201300124985HT2C RECEPTOR MODULATORS - The present invention relates to novel compounds of Formula (I):2013-01-10
20130012499TRPV4 ANTAGONISTS - The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.2013-01-10
20130012500ORGANIC COMPOUNDS - A compound of Formula I2013-01-10
20130012501PYRIMIDINEDIAMINE 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
20130012502Pharmaceutical 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
20130012503METALLOENZYME 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
20130012504BI-FUNCTIONAL QUINOLINE ANALOGS - Provided are compounds of Formula I:2013-01-10
20130012505BENZONAPHTHYRIDINAMINES 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
20130012506ANTI-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
20130012507SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS - Compounds represented by formula (Ia) or (Ib) and wherein R and R2013-01-10
20130012508NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I)2013-01-10
20130012509NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I)2013-01-10
201300125101-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
20130012511SOLUBLE 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
20130012512P38 MAP kinase inhibitors - There are provided inter alia compounds of formula (I)2013-01-10
20130012513HEDGEHOG 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
20130012514AMINOALKYLOXAZOLE 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
20130012515Fused 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
201300125166-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
20130012517Quinoline 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
20130012518BICYCLIC 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
20130012519Biomarker 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
20130012520TRAZODONE 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
20130012521APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I):2013-01-10
20130012522NEW 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: R2013-01-10
20130012523PYRAZINONE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND THEIR USES - The present invention relates to pyrazinone derivatives of formula (I):2013-01-10
20130012524STABILIZED 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
20130012525INHIBITORS 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
20130012526OXAZOLE 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
20130012527PREQ1 RIBOSWITCHES AND METHODS AND COMPOSITIONS FOR USE OF AND WITH PREQ1 RIBOSWITCHES2013-01-10
20130012528NOVEL 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
20130012529HETEROBICYCLIC CARBOXAMIDES AS INHIBITORS FOR KINASES - The invention relates to novel organic compounds of formula (I)2013-01-10
20130012530New 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
20130012531TREATMENT 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
20130012532CYCLOPROPANECARBOXYLIC ACID DERIVATIVE - A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R2013-01-10
20130012533CONTROLLED 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
20130012534Pharmaceutical 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