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40th week of 2009 patent applcation highlights part 64
Patent application numberTitlePublished
20090247535USE OF RANOLAZINE FOR NON-CARDIOVASCULAR DISORDERS - Disclosed is a method of treating a non-cardiovascular disorder characterized by an abnormal persistent sodium current in a subject in need of treatment thereof, said method comprising administering to the subject an effective amount of a compound of Formula (I):2009-10-01
20090247536Bissulfonamide Compounds As Agonists Of GalR1, Compositions, And Methods Of Use - Embodiments of the present invention provide bissulfonamide compounds that are agonists of GalR1. The present invention further provides compositions comprising bissulfonamide compounds that are agonists of GalR1, and methods of use of such compounds and compositions.2009-10-01
20090247537METHODS FOR PREVENTING OR TREATING BRUXISM USING DOPAMINERGIC AGENTS - Methods for preventing or treating bruxism, including alleviating or eliminating one or more symptoms, diseases or conditions associated with or resulting from bruxism, using dopaminergic agents such as monoamine oxidase inhibitors that increase dopaminergic activity and dopamine agonists, are disclosed.2009-10-01
20090247538Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR2009-10-01
20090247539Novel Pharmaceuticals - This invention relates to compounds of formula (I)2009-10-01
20090247540PEPTIDE AND SMALL MOLECULE AGONISTS OF EPHA AND THEIR USES - Methods and compositions for activating an EphA receptor can be used for identifying therapeutic agents for cancer.2009-10-01
20090247541Novel compounds - Compounds of formula (I)2009-10-01
20090247542SYNTHESES AND PREPARATIONS OF POLYMORPHS OF CRYSTALLINE ARIPIPRAZOLE - The invention relates to polymorphic crystalline forms of aripiprazole, synthetic processes for their preparation and pharmaceutical compositions containing the same. These crystalline forms of aripiprazole can be readily milled and can be easily combined with various pharmaceutical adjuvants without effecting changes to their crystalline structure when, for example, pressed into tablet or capsule form.2009-10-01
20090247543GATIFLOXACIN-CONTAINING AQUEOUS LIQUID PREPARATION - There is provided an aqueous liquid preparation comprising Gatifloxacin or a pharmacologically acceptable salt thereof or a hydrate thereof, phosphoric acid or a salt thereof, and xanthan gum, wherein a pH thereof is 5.5 or more and less than 7.0. The aqueous liquid preparation has improved intraocular penetration of Gatifloxacin. Further, the formation of a precipitate during storage at a lower temperature and at the time of freezing and thawing of the aqueous liquid preparation is suppressed by incorporating at least one of the ingredient selected from the group consisting of nicotinamide, caffeine, methylglucamine, methyl parahydroxybenzoate and a salt thereof into the aqueous liquid preparation.2009-10-01
20090247544Certain Chemical Entities, Compositions and Methods - Certain substituted urea derivatives modulate diskeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and are useful in the treatment of obesity, sarcopenia, wasting syndrome, frailty, muscle spasm, cachexia, neuromuscular diseases (e.g., amyotrophic lateral sclerosis, spinal muscular atrophy, familial or acquired myopathies or muscular dystrophies), post-surgical and post-traumatic muscle weakness, and other conditions.2009-10-01
20090247545SUBSTITUTED OXAZOLIDINONE DERIVATIVES - The present invention provides substituted oxazolidinone derivatives, which can be used as antimicrobial agents. Compounds disclosed can be used for the treatment or prevention of a condition caused by or contributed to by bacteria, such as, inter alia, multiply-resistant 2009-10-01
20090247546Treatment of Prevention of Valvular Heart Disease with Flibanserin - The invention relates to a method for the treatment or prevention of Valvular Heart Disease comprising the administration of a therapeutically effective amount of flibanserin.2009-10-01
20090247547HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES B - The present teachings relate to compounds of Formula I:2009-10-01
20090247548PYRROLOPYRIMIDINE DERIVATIVES FOR TREATING PROLIFERATIVE DISEASES - The present invention relates to a compound of formula I2009-10-01
20090247549Methods of using saha and bortezomib for treating cancer - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.2009-10-01
200902475503-TRIFLUOROMETHYL-PYRAZINE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS - The present invention relates to pyrazine derivatives of the formula2009-10-01
20090247551SUBSTITUTED ENAMINOCARBONYL COMPOUNDS - The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.2009-10-01
20090247552AQUEOUS LIQUID PREPARATION CONTAINING AMIDE COMPOUND - An object of the present invention is to promote penetration of a compound having a Rho kinase inhibitory activity to a topical moiety, and provide an aqueous liquid preparation capable of maintaining a given drug concentration even when administration frequency is reduced. The present invention solves the aforementioned problem by an aqueous liquid preparation containing a compound represented by the following formula (I)2009-10-01
20090247553Highly Pure Paliperidone or a Pharmaceutically Acceptable Salt Thereof Substantially Free of Keto Impurity - Provided herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[1,2-a]pyrimidin-4,9-dione, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of keto impurity.2009-10-01
20090247554KINASE INHIBITORS - Compounds are provided for use with kinases that comprise (I), (II), (III), (IV): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.2009-10-01
200902475555,7-Disubstituted[1,3]Thiazolo[4,5-D]Pyrimidin-2(3H)-One Derivatives 258 - There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I)2009-10-01
20090247556Azolopyrimidines as Inhibitors of Cannabinoid 1 Activity - The invention provides compounds of formula (Ia), (Ic), (Ig) and (Ik), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).2009-10-01
20090247557PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS - Disclosed are novel compounds a compound of Formula I2009-10-01
20090247558USE OF THE CRH (CORTICOTROPIN RELEASING HORMONE) - UCN (UROCORTIN) SYSTEM IN THE TREATMENT OF INFLAMMATORY DISEASES - The invention relates to the use of corticotropin-releasing hormone (CRH) receptor-1 (R1) antagonists and/or CRH-R2 receptor agonists for the treatment of inflammatory diseases via regulation of monocyte/macrophage cell activation, proliferation, differentiation, apoptosis, and inflammatory cytokine production. As CRH system we define natural and synthetic CRH and urocortin (UCN) agonists and antagonists for the CRH-R1 and CRH-R2 receptors and their subtypes as well as the CRH-binding protein (BP), a CRH pseudo-receptor. The invention is directed towards pharmacological intervention for the amelioration or treatment of inflammatory diseases using the CRH system-mediated control of monocyte/macrophage cells which play a key role in initiating and maintaining the inflammatory response via production of pro-inflammatory cytokines such as is the interleukin (IL)-1, IL-6 and tumor necrosis factor (TNF)-alpha. By the term inflammation we define the response of an organism to noxious endogenous or exogenous stimuli causing tissue injury. Inflammation is a host defence mechanism, which might harm the defending organism. The invention also provides methods for the in vitro and in vivo evaluation of natural and synthetic CRH system modulators for the control of the monocyte/macrophage system.2009-10-01
20090247559Benzofuropyrimidinones - A compound according to formula I:2009-10-01
20090247560Diaryl ketimine derivative - Provided is a compound of a formula (I):2009-10-01
20090247561SUBSTITUTED SPIROCYCLIC CYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.2009-10-01
20090247562LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF - 8-Substituted-2,6-methano-3-benzazocines of general structure2009-10-01
20090247563Novel Processes for the Production of Useful Intermediates - The present application relates to a new process for the asymmetric production of 3-(pyridin-4-yl)-3-hydroxy-pentanoic acid derivatives, which are useful intermediates in the manufacture of compounds that are known to show antiproliferative activity. 2009-10-01
20090247564Crystalline Form of Vinflunine Ditartrate - The present invention relates to a novel crystalline form of vinflunine, to a process for preparing it, and to its uses in the therapeutic field, in particular for treating cancer.2009-10-01
20090247565Tyrosine Kinase Inhibitors - The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.2009-10-01
20090247566Pyrano [3,2-C] Pyridones and Related Heterocyclic Compounds as Pharmaceutical Agents for Treating Disorders Responsive to Apoptosis, Antiproliferation or Vascular Disruption, and the Use Thereof - A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I:2009-10-01
20090247567BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, 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 Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.2009-10-01
20090247568AMINOPIPERIDINYL DERIVATIVES AND USES THEREOF - This application discloses aminopiperidinyl compounds of generic Formulae I-II:2009-10-01
20090247569Process for Preparing Clopidogrel Bisulphate - Provided are processes for the preparation of clopidogrel bisulphate Form I.2009-10-01
20090247570PHARMACEUTICALS - The present invention relates to the use of a CCR5 antagonist in an HIV infected patient to enhance their immune reconstitution and so treat to HIV related opportunistic conditions resulting from the immunocompromised state of the HIV patient. The invention also allows treatment with a CCR5 antagonist of patients having a CXCR4 using viral population since such patients will also benefit from an increase in their CD4 and/or CD8 cell count.2009-10-01
20090247571Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.2009-10-01
20090247572AGENT FOR TREATING ATRIAL FIBRILLATION - It is intended to provide an agent for treating atrial fibrillation, comprising an I2009-10-01
20090247573(HETERO)ARYL CYCLOHEXANE DERIVATIVES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.2009-10-01
200902475743-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention provides novel compounds represented by the general formula (I):2009-10-01
20090247575STABILIZING LIPID COMPOSITIONS FOR ORAL PHARMACEUTICAL AGENTS - The present invention relates to a pharmaceutical composition for oral administration comprising an exceptionally labile active agent, a stabilizing vehicle comprising liquid triglycerides and a desiccant, wherein the composition is storage stable for an extended period without substantial degradation of the active agent.2009-10-01
20090247576ANTI-TUMOR AGENT FOR MULTIPLE MYELOMA - The object of the invention is to provide a pharmaceutical composition and a therapeutic method which can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3. The compound represented by General Formula (I), a pharmacologically acceptable salt thereof or a solvate thereof can exert their effects with higher efficiency on a living organism having at least one cell selected from the group consisting of a cell overexpressing FGFR3, a cell that has a t(4;14) translocation and a cell expressing mutant FGFR3.2009-10-01
20090247577PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS - Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula I,2009-10-01
200902475785-HYDROXYMETHYL-OXAZOLIDIN-2-ONE-DERIVATIVES AND THEIR USES AS ANTIBACTERIALS - The invention relates to novel chimeric antibiotics of formula I2009-10-01
200902475792-[3H-THIAZOL-2-YLIDINEMETHYL]PYRIDINES AND RELATED COMPOUNDS AND THEIR USE - The present invention pertains to certain 2-[3H-thiazol-2-ylidinemethyl]pyridine compounds and analogs thereof, which, inter alia, inhibit cell proliferation, treat cancer, etc., and more specifically to compounds of the following formula, wherein R2009-10-01
20090247580NITROXIDE RADIOPROTECTOR FORMULATIONS AND METHODS OF USE - Pharmaceutical compositions useful in preventing and treating negative side effects accompanying radiotherapy are disclosed. More particularly, new formulations that can be applied to the skin and mucous membranes of patients undergoing radiotherapy and methods of using these formulations are disclosed.2009-10-01
20090247581Organic Compounds - The present invention relates to a process for the synthesis of (S)-2′[2-1-(methyl-2-piperidyl) ethyl] cinnamanilide (I) or salts or pharmaceutically acceptable prodrugs thereof:2009-10-01
20090247582METHODS OF TREATING ATHEROSCLEROSIS - The present invention relates to a method for the prevention, delay the onset and treatment of atherosclerosis which method comprises administering to a warm-blooded animal, in need thereof, a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with at least one therapeutic agent selected from the group consisting of: 2009-10-01
20090247583PHARMACEUTICAL COMPOSITION COMPRISING, IN COMBINATION, SAREDUTANT AND PAROXETINE - A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(−)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts thereof and at least one second active ingredient chosen from trans-(−)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine and pharmaceutically acceptable salts thereof.2009-10-01
20090247584PHENOXY-PIPERIDINES FOR THE TREATMENT OF DISEASES SUCH AS SCHIZOPHRENIA AND DEPRESSION - Compounds of the formula (I), in which R2009-10-01
20090247585PHARMACEUTICAL COMPOSITION COMPRISING, IN COMBINATION, SAREDUTANT AND ESCITALOPRAM - A subject-matter of the present invention is pharmaceutical compositions comprising, in combination, at least one active ingredient chosen from (S)-(−)-N-[4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl]-N-methylbenzamide and pharmaceutically acceptable salts thereof and at least one second active ingredient chosen from (S)-(+)-1-[4-(3-(dimethylamino)propyl)]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile and pharmaceutically acceptable salts thereof.2009-10-01
20090247586CARBOXAMIDES FOR CONTROLLING MICRO-ORGANISMS IN PLANT AND MATERIAL PROTECTION - Novel carboxamides of the formula (I)2009-10-01
200902475871,3-DIHYDROISOBENZOFURAN DERIVATIVES - The object is to provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.2009-10-01
200902475882-TRIFLUOROMETHYLNICOTINAMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS - The present invention relates to compounds formula I:2009-10-01
20090247589Monocarboxylates for modifying macrophage function - The present invention is directed to methods of inhibiting the production of proinflammatory agents by macrophages by contacting the cells with a monocarboxylate such as nicotinic acid. The invention also includes methods of treating diseases that are associated with macrophage activation such as atherosclerosis; systemic lupus erythematosus; rheumatoid arthritis; inflammatory bowel disease; and diabetes mellitus.2009-10-01
20090247590Indane amides - The invention relates to novel compounds and processes for their preparation and their use for preparing medicaments for the treatment of disorders, especially hyper-proliferative disorders.2009-10-01
20090247591SUBSTITUTED CYCLOHEXYLDIAMINES - The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.2009-10-01
20090247592Epothilones C, D, E, and F, Preparation and Compositions - The present invention relates to epothilones C, D, E, and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection.2009-10-01
20090247593N-THIAZOL-2-YL-BENZAMIDE DERIVATIVES - The invention relates to compounds of the formula I2009-10-01
20090247594THERAPEUTIC COMPOUNDS - Disclosed herein is a compound having a structure2009-10-01
20090247595Process for the preparation of tetrazolyl compounds - The invention provides a method for preparing candesartan cilexetil and related tetrazolyl compounds. More particularly, the invention relates to the preparation of candesartan cilexetil and related tetrazolyl compounds and includes a method of removing a protective group (e.g., triphenylmethane (trityl) protecting group) from an N-protected tetrazolyl compound using a Lewis acid in an inert solvent and in the presence of an alcohol (e.g., reacting an N-protected tetrazolyl compound with ZnCl2009-10-01
20090247596THIOPHENECARBOXAMIDE DERIVATIVES AS EP4 RECEPTOR LIGANDS - The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included. (Formulas I and II).2009-10-01
20090247597AGROCHEMICAL FORMULATIONS THAT CAN BE DISPERSED IN WATER CONTAINING POLYALKOXYTRIGLYCERIDED AS PENETRATION ENHANCES - The present invention relates to novel water-dispersible agrochemical formulations such as, for example, water-based suspension concentrates and water-dispersible granules of agrochemically active compounds comprising a penetrant from the class of the polyalkoxytriglycerides, to a process for preparing these formulations and to their use for applying the active compounds comprised therein.2009-10-01
20090247598TREATMENT METHODS - There are disclosed methods for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing regimen and/or schedules based on the patient's MGMT level. Additional improved methods for treating patients with temozolomide are also disclosed.2009-10-01
20090247599METHODS OF TREATING CELL PROLIFERATIVE DISORDERS USING A COMPRESSED TEMOZOLOMIDE DOSING SCHEDULE - There are disclosed methods and kits for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing schedules.2009-10-01
20090247600REMEDY FOR CORNEAL DISEASES - A therapeutic agent for a corneal disease comprising ozagrel or a salt thereof as an active ingredient is provided. The purpose is to find a substance capable of effectively treating/ameliorating a corneal disease which has been increased in the number of cases thereof in recent years and to provide a therapeutic agent for a corneal disease comprising the substance as an active ingredient.2009-10-01
20090247601PEPTIDE DERIVATIVES WITH THERAPEUTIC ACTIVITY - Dipeptide compounds containing a histidine residue proved to have interesting blocking activity on secondary products from lipid oxidative stress, in particular on unsaturated aldehydes such as malondialdehyde and hydroxynonenal, which are known to contribute to the inset of quite a number of chronic pathologies such as neurodegenerative, inflammatory chronic, cardiovascular diseases, diabetes complications and cataract.2009-10-01
20090247602COSMETIC USE OF CONJUGATED COMPOUNDS OF INDOLIC AUXINS - The invention has for object the cosmetic use and as neurotrophic agent of at least an indolic auxin conjugate with general formula (I):2009-10-01
20090247603Stabilized pharmaceutical compositions comprising an HMG-CoA reductase inhibitor - The present invention is a new stable drug composition particularly suitable for use as an antihypercholesterolaemic or antihyperlipidaemic agent. The present invention is specifically a drug composition comprising a pharmaceutical, a complexing agent and a surfactant, and a method for manufacturing same. When applied to unstable drugs with low solubility and poor bioavailability, like HMG-CoA reductase inhibitors and especially atorvastatin calcium amorphous form, the resulting drug composition is more stable and is characterized by an improved dissolution profile.2009-10-01
20090247604RNAi Therapeutics for Treatment of Eye Neovascularization Diseases - Compositions and methods for treating ocular disease are provided. Specifically, siRNA molecules and mixtures of siRNA molecules are provided that inhibit angiogenesis and/or neovascularization. The compositions and methods are suitable for treating ocular diseases associated with angiogenesis and/or neovascularization.2009-10-01
20090247605Treating diseases mediated by metalloprotease-shed proteins - This invention relates to the identification of membrane-associated proteins shed by metalloproteinases and in particular by TNF-alpha converting enzyme (TACE), to the use of such metalloproteinase-shed proteins in assays for TACE agonists and antagonists, and to the use of metalloproteinase agonists and antagonists, and particularly TACE agonists and antagonists, in the treatment of diseases mediated by certain shed proteins.2009-10-01
20090247606RNA Interference Mediated Inhibition of Adenosine A1 Receptor (ADORA1) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The present invention concerns methods and reagents useful in modulating adenosine A1 receptor (ADORA1) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small interfering RNA (siRNA) molecules capable of mediating RNA interference (RNAi) against ADORA1 and related receptors.2009-10-01
20090247607dsRNA COMPOSITIONS AND METHODS FOR TREATING HPV INFECTION - The invention relates to a double-stranded ribonucleic acid (dsRNA) for treating human papilloma virus (HPV) infection. The dsRNA comprises an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of an HPV Target gene selected from among HPV E1, HPV E6 and the human E6AP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by HPV infection and the expression of the E6AP gene using the pharmaceutical composition; and methods for inhibiting the expression of the HPV Target genes in a cell.2009-10-01
20090247608Targeting Lipids - The present invention provides targeting lipids of structure2009-10-01
20090247609SM-PROTEIN BASED SECRETION ENGINEERING - The present invention concerns the field of cell culture technology. It describes a novel method for enhancing the secretory transport of proteins in eukaryotic cells by heterologous expression of Munc18c, Sly1 or other members of the SM protein family. This method is particularly useful for the generation of optimized host cell systems with enhanced production capacity for the expression and manufacture of recombinant protein products.2009-10-01
20090247610INTEGRASE COFACTOR - The present invention provides nucleic acid molecules which include a region specifically interacting with the nucleic acid encoding the LEDGF/P75 protein or the nucleic acid encoding a fragment of a LEDGF/P75 protein and methods and uses of such nucleic acid molecules.2009-10-01
20090247611METHOD OF TREATING A CANCER WITH A SURVIVIN ANTISENSE OLIGONUCLEOTIDE AND PACLITAXEL - Provided is a method of treating cancer of the stomach, comprising administering to a patient a therapeutically effective combination of a Survivin antisense oligonucleotide and paclitaxel.2009-10-01
20090247612PREVENTION OF VIRAL INFECTIVITY - The present invention concerns the inactivation of viral infectivity in a cell-free environment as well as the preparation of a pharmaceutical agent and a method therefore. According to the invention the use of a sequence of oligodeoxynucleotides or oligoribonucleotides or a chimera or a combination thereof capable of binding to conserved regions of viral RNA for the inactivation of viral infectivity outside in a cell-free environment is intended. Furthermore said sequences are used for the preparation of a pharmaceutical agent for the inactivation of viral infectivity.2009-10-01
20090247613RNA INTERFERENCE MEDIATED INHIBITION OF B-CELL CLL/LYMPHOMA-2 (BCL2) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating BCL2 gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of BCL2 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of BCL2 genes (e.g., BCL2, BCL-XL, BCL2-L1, MCL-1 CED-9, BAG-1, E1B-194 and/or BCL-A1). The small nucleic acid molecules are useful in the treatment of cancer, malignant blood disease, polycytemia vera, idiopathic myelofibrosis, essential thrombocythemia, myelodysplastic syndromes, autoimmune disease, viral infection, and proliferative diseases and conditions2009-10-01
20090247614Folate Conjugates - The present invention provides iRNA agent including at least one monomer having the structure shown in formula (I′)2009-10-01
20090247615TRIGGERED RNAi - The present application relates to methods and compositions for triggering RNAi. Triggered RNAi is highly versatile because the silencing targets are independent of the detection targets. In some embodiments, methods of silencing or modulating the expression of a target gene are provided. The methods generally comprise providing an initiator to a cell comprising a detection target and a silencing target gene, wherein the detection target is different from the silencing target gene, wherein binding of the detection target to the initiator initiates formation of an inactivator double-stranded RNA (inactivator dsRNA). The inactivator dsRNA can silence or modulate the expression of the silencing target gene.2009-10-01
20090247616USE OF BENZO-FUSED HETEROCYLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF ANXIETY - The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of anxiety and related disorders, which includes mono-therapy and alternatively, co-therapy with at least one anxiolytic.2009-10-01
20090247617PROCESS FOR THE PREPARATION OF BENZO-FUSED HETEROARYL SULFAMATES - The present invention is directed to a process for the preparation of benzo-fused heteroaryl sulfamates, useful for the treatment of epilepsy and related disorders.2009-10-01
20090247618PROCESS FOR PREPARATION OF BENZO-FUSED HETEROARYL DERIVATIVES - The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.2009-10-01
20090247619Cannabinoid-Containing Compositions and Methods for Their Use - This invention relates to cannabinoid-containing compositions, particularly cannabinoid-containing gel formulations and methods for the treatment of traumatic injury, e.g., strains, sprains and contusions, and disease conditions, e.g., arthritis, particularly osteoarthritis. The methods involve topically applying a cannabinoid or a cannabinoid-containing composition to a subject's skin near, or distant from, the area of the injury or the area affected by the disease condition, e.g., an arthritic joint. The cannabinoid-containing composition is preferably a pharmaceutically acceptable gel containing a therapeutically effective amount of a cannabinoid sufficient to alleviate the symptoms associate with the injury or disease condition.2009-10-01
20090247620Benzochromene Derivatives for Use in Liquid Crystal Media and as Therapeutic Active Substances - The present invention relates to benzochromene derivatives of the formula I2009-10-01
20090247621Diosmetin compounds, a process for their preparation and pharmaceutical composition containing them - Compounds of formula (I):2009-10-01
20090247622Natural topical compositions for the prevention and treatment of diaper rashes and related conditions - The treatment and prevention of skin irritations, including diaper rash, is facilitated with the topical application of cranberry anthocyanins in a cosmetically acceptable vehicle.2009-10-01
20090247623DERIVATIVES OF EPIRUBICIN, THEIR MEDICINAL APPLICATION AND PHARMACEUTICALY ACCEPTABLE FORMS OF DRUGS - The present invention relates to novel derivatives of epirubicin, pharmaceutical composition comprising these derivatives, and uses of epirubicin and its derivative for treating HCV.2009-10-01
20090247624FORMULATIONS OF RADIOPROTECTIVE ALPHA BETA UNSATURATED ARYL SULFONES - Solution and suspension formulations are provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject which comprises an effective amount of at least one radioprotective α,β unsaturated aryl sulfone wherein the composition has a pH within the range of about 8 to about 9.2009-10-01
20090247625COMPOSITIONS CONTAINING LIGNAN-CLASS COMPOUNDS - An object of the invention is to provide compositions containing lignan-class compounds as dissolved at high concentrations. The compositions having lignan-class compounds such as sesamin and episesamin dissolved in solvent oils or fats that contain triglycerides of middle-chain fatty acids having 8-12 carbon atoms, preferably triglycerides of caprylic acid and/or capric acid and/or lauric acid can contain the lignan-class compounds stably at higher concentrations than when other solvents are used and, hence, have high enough value as foods and pharmaceuticals.2009-10-01
20090247626Method of Treating Dyslipidemia Using Naturally Occurring Diterpene - A method for treatment and or/prevention of dyslipidemia is provided. The invention relates to reducing low density lipoprotein cholesterol concentration by using naturally occurring diterpene (16α-hydroxycleroda-3,13(14)Z-dien-15,16-olide, a compound having formula (1)) isolated from leaves of 2009-10-01
20090247627AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS - The invention provides amino- and amido-aminotetralin compounds of formula (I):2009-10-01
20090247628SUBSTITUTED PHENYLCYCLOHEXYLGLYCOLATES - Disclosed herein are substituted phenylcyclohexylglycolate-based muscarinic acetylcholine receptor modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.2009-10-01
20090247629Dimer poly-quaternary ester compounds - The present invention relates to a novel class of polymeric compounds having specific quaternized amine based upon a dimer acid reacted with an alkanolamine to make an ester quaternary compound. Dimer acid is a C-36 diacid having a cyclic structure and two amine groups that allow for the synthesis of a high molecular weight cationic compound which is extremely substantitive to human skin and are well tolerated by human tissue making them suitable for use preparation of barrier products for personal care applications. These materials are dimethylaminopropyl amine free, which is highly desirable in personal care applications.2009-10-01
20090247630DERMATOLOGICAL COMPOSITIONS COMPRISING AT LEAST ONE NAPHTHOIC ACID COMPOUND AND AT LEAST ONE FILM-FORMING AGENT AND TREATMENT OF KERATINIZATION DISORDERS THEREWITH - Topically applicable, reduced-irritant dermatological/cosmetic compositions useful for the prevention/treatment of a variety of keratinization disorders, for example acne vulgaris, contain at least one naphthoic acid compound essentially uniformly distributed therethrough and an amount of at least one hydrophilic film-forming agent, formulated into topically applicable, physiologically acceptable media therefor.2009-10-01
20090247631Enzymatic Production Of Peracids Using Perhydrolytic Enzymes - A process is provided to produce a concentrated aqueous peracid solution in situ using at least one enzyme having perhydrolase activity in the presence of hydrogen peroxide (at a concentration of at least 500 mM) under neutral to acidic reaction conditions from suitable carboxylic acid esters (including glycerides) and/or amides substrates. The concentrated peracid solution produced is sufficient for use in a variety of disinfection and/or bleaching applications.2009-10-01
20090247632DERMATOLOGICAL COMPOSITIONS AND METHODS - Dermatological compositions (methods of making and using) that include one or more anesthetic agents and/or one or more anti-inflammatory agents and/or a combination of ammonium, sodium, and potassium salts, preferably of an alpha-hydroxy acid.2009-10-01
20090247633NUTRIENT EXTRACTS DERIVED FROM GREEN PLANT MATERIALS - An extract from green plant materials includes controlled concentrations of nutritional components. In one embodiment, the nutritional components include at least one xanthophyll, at least one hydrocarbon carotene, and at least one fatty acid wherein the xanthophyll, hydrocarbon carotene, and fatty acid each have about equal weight percentages. In a one embodiment, the green plant is alfalfa, the xanthophyll is lutein, the hydrocarbon carotene is β-carotene, and the fatty acids include an omega-3 essential fatty acid, an omega-6 essential fatty acid, or a combination of the acids thereof.2009-10-01
20090247634Methods for identifying modulators of eoxin formation - A method for identifying a compound for modulating the formation of 14,15-LTC2009-10-01