50th week of 2009 patent applcation highlights part 54 |
Patent application number | Title | Published |
20090306120 | TERPOLYMERS CONTAINING LACTIDE AND GLYCOLIDE - The present invention provides an amorphous terpolymer for a coating on an implantable device for controlling release of drug and methods of making and using the same. | 2009-12-10 |
20090306121 | AZA-BETA-CARBOLINES AND METHODS OF USING SAME - Provided are compounds having the general structure according to Formula (I): | 2009-12-10 |
20090306122 | SUBSTITUTED TETRAHYDROPYRROLOQUINOLINE DERIVATIVES AS KINASE MODULATORS, ESPECIALLY OF TYROSINE AND RAF KINASES - Compound of the formula (I), in which X, R | 2009-12-10 |
20090306123 | Bicyclononene derivaties - The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. | 2009-12-10 |
20090306124 | 3-(INDOLYL)-4-ARYLMALEIMIDE DERIVATIVES AND THEIR USE AS ANGIOGENESIS INHIBITORS - The present invention relates to a compound of formula (I) wherein R | 2009-12-10 |
20090306125 | Mitochondria-Targeted Antioxidant Prodrugs and Methods of Use - The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation. | 2009-12-10 |
20090306126 | Indole Derivatives - The invention concerns indole derivatives of Formula I | 2009-12-10 |
20090306127 | Certain Chemical Entities, Compositions and Methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. | 2009-12-10 |
20090306128 | PHARMACEUTICAL COMPOSITIONS CONTAINING A FLUOROQUINOLONE ANTIBIOTIC DRUG - Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions. | 2009-12-10 |
20090306129 | SUBSTITUTED PYRAZOLO [3,4-B] PYRIDINES AS PHOSPHODIESTERASE INHIBITORS - The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV Formula (XIV). | 2009-12-10 |
20090306130 | NOVEL TETRAHYDRO-ISOQUINOLINES - The present invention provides a compound selected from compounds of formula (A) as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (A) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (A) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections. | 2009-12-10 |
20090306131 | CELL LINES WITH LATENT IMMUNODEFICIENCY VIRUS AND METHODS OF USE THEREOF - The present invention provides isolated cells that comprise, integrated into the genome of the cell, a transcription-competent immunodeficiency virus or a transcription-competent immunodeficiency virus-based retroviral vector. Under basal in vitro culture conditions, the immunodeficiency virus is latent, and the expression of the latent immunodeficiency virus can be reactivated. The invention farther provides methods of making a subject cell. The invention further provides screening methods for identifying agents that activate a latent immunodeficiency virus; and screening method for identifying agents that block reactivation of latent immunodeficiency virus expression in response to T cell activation signals. The invention further provides agents identified in the subject screening assays. The invention further provides methods of treating an immunodeficiency virus infection. | 2009-12-10 |
20090306132 | USE OF DERIVATIVES OF NAPHTHALENESULPHONIC OR QUINOLINESULPHONIC ACID IN THE TREATMENT OF VASOPROLIFERATIVE OCULAR DISEASES - The invention relates to the use of derivatives of sulphonic acid (I) or one of the pharmaceutically-acceptable prodrugs or salts thereof in the preparation of a medicament for the treatment of vasoproliferative ocular diseases, said sulphonic acid having formula (I). | 2009-12-10 |
20090306133 | New Acetyl Coenzyme A Carboxylase (ACC) Inhibitors And Uses In Treatments Of Obesity And Diabetes Mellitus - 087 - The present invention relates to Acetyl Coenzyme A Carboxylase (ACC) inhibitors according to formula (I), | 2009-12-10 |
20090306134 | Muscarinic receptor antagonists - Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like. | 2009-12-10 |
20090306135 | STABLE AMORPHOUS FEXOFENADINE HYDROCHLORIDE - The present invention relates to stable amorphous form of fexofenadine hydrochloride, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of allergic reactions. | 2009-12-10 |
20090306136 | Benzenesulfonamide Compounds and the Use Thereof - The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R | 2009-12-10 |
20090306137 | TREATMENT FOR DEPRESSIVE DISORDERS - A method of treating depression comprising administering a melatonin agonist. | 2009-12-10 |
20090306138 | PYRROLIDINE DERIVATIVES ACTING AS CCR3-RECEPTOR ANTAGONISTS - Compounds of formula I | 2009-12-10 |
20090306139 | HETEROARYL-SUBSTITUTED PIPERIDINES - The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases. | 2009-12-10 |
20090306140 | 3 or 4-Substituted Piperidine Compounds - There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I) | 2009-12-10 |
20090306141 | Novel Compounds - The invention provides compounds of general formula (I) wherein m, n, Q, Z | 2009-12-10 |
20090306142 | METHODS TO CONTROL QoI-RESISTANT FUNGAL PATHOGENS - Processes and compositions have been discovered that are suitable for controlling a pathogen induced disease in a plant that is at risk of being diseased from a pathogen resistant to a Qo inhibitor. Such processes and compositions comprise contacting said plant(s) with a composition comprising an effective amount of a Qi inhibitor. | 2009-12-10 |
20090306143 | Derivatives of N-(heteroaryl)-1-heteroaryl-1H-indole-2-carboxamides, preparation thereof and therapeutic use thereof - The invention relates to compounds of formula (I): | 2009-12-10 |
20090306144 | PYRIDINE DERIVATIVES OF ALKYL OXINDOLES AS 5-HT7 RECEPTOR ACTIVE AGENTS - New 3,3-disubstituted indol-2-one derivatives of the general formula (I) | 2009-12-10 |
20090306145 | Pyridylisoxazole Derivatives - This invention offers isoxazole derivatives represented by the following formula (I) | 2009-12-10 |
20090306146 | Nicotinyls, Pyrethroids, and Ketoenols as a Gel Formation or Foam Formulation for Perennial Cultures - Method of controlling insects with a gel or foam formulation containing at least one insecticidal active substance, characterized in that the agrochemical formulation is applied externally to the trunk of the plant to be protected. | 2009-12-10 |
20090306147 | BIOLOGICAL EFFICACY OF AGROCHEMICAL COMPOSITIONS ON APPLICATION IN THE GROWTH SUBSTRATE SUITABLE FORMULATIONS AND USE THEREOF - In soil applications, the action of crop protection compositions comprising active compounds from the classes of the neonicotinoids, the pyrethroids, the butenolides, the ketoenols, the phenylpyrazoles or the fungicides can be improved by adjuvants. The present invention describes corresponding methods and suitable compositions. | 2009-12-10 |
20090306148 | Use of Thiazolidinediones for the Partial Inhibition of Androgen Binding to Aromatase - A method for the treatment or prophylaxis of a disorder, wherein the disorder is affected by estrogen, comprising partially inhibiting aromatase activity or interfering with the binding of androgen to aromatase by administering a therapeutically effective amount of a thiazolidinedione to the patient. The use of rosiglitazone or pioglitazone to partially inhibit the binding of androgen to aromatase by at least 20% is preferred. | 2009-12-10 |
20090306149 | USE OF BIARYLCARBOXAMIES IN THE TREATMENT OF HEDGEHOG PATHWAY-RELATED DISORDERS - The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway. In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of the invention (e.g., a compound of Formula I). | 2009-12-10 |
20090306150 | CARBOXYLIC ACID SALTS OF 2-AMINO-3-CARBETHOXYAMINO-6-(4-FLUORO-BENZYLAMINO)-PYRIDINE - The preparation of flupirtine carboxylate acid addition salts having the following formula (2), | 2009-12-10 |
20090306151 | Pharmaceutical preparation containing an angiotensin II receptor antagonist and a calcium channel blocker - A pharmaceutical preparation comprising an angiotensin II receptor antagonist, a calcium channel blocker and at least one substance selected from a hydrophilic polymer, an acidic substance and a fluidizing agent. The pharmaceutical preparation demonstrates improved dissolution properties. | 2009-12-10 |
20090306152 | COOLING COSMETIC OR DERMATOLOGICAL PREPARATIONS COMPRISING (1R,2S,5R)-2-ISOPROPYL-5-METHYL-N-(2-(PYRIDIN-2-YL)ETHYL)-CYCLOHEXANE CARBOXAMIDE AND/OR (1R,2S,5R)-N-(4-CYANOMETHYL-PHENYL)-2-ISOPROPYL-5-METHYLCYCLOHEXANE CARBOXAMIDE IN COMBINATION WITH MENTHOXYPROPANEDIOL - A cooling topical cosmetic or dermatological preparation which comprises (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethyl)cyclohexane carboxamide and/or (1R,2S,5R)-N-(4-cyanomethyl-phenyl)-2-isopropyl-5-methylcyclohexane carboxamide, in combination with menthoxypropanediol. | 2009-12-10 |
20090306153 | SYNTHESIS AND USE OF NOVEL INHIBITORS AND INACTIVATORS OF PROTEIN ARGININE DEIMINASES - In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F; Cl, and H, y includes OH and NH | 2009-12-10 |
20090306154 | SYNERGISTIC ANTI-MICROBIAL MIXTURES OF TROPOLONE (DERIVATIVES) AND SELECTED COMPOUNDS - The present invention relates to the antimicrobial mixture comprising or consisting of:
| 2009-12-10 |
20090306155 | THIAZOLES, IMIDAZOLES, AND PYRAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions. | 2009-12-10 |
20090306156 | PHOSPHODIESTERASE 4 INHIBITORS - Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: | 2009-12-10 |
20090306157 | Antiseptic Alginate Preparation - An antiseptic preparation is provided for the production of wound dressings or bandages. The preparation includes at least one alginate and at least one antiseptically active substance selected from the group biguanide derivatives, octenidine and taurolidine. Processes for the production of the antiseptic preparations, and the use thereof, are also provided. | 2009-12-10 |
20090306158 | Metabotropic Glutamate Receptor Isoxazole Ligands and Their Use as Potentiators 286 - Compounds in accord with Formula I: | 2009-12-10 |
20090306159 | Inhibition of Intermediate-Conductance Calcium Activated Potassium Channels in the Treatment and/or Prevention of Atherosclerosis - Methods for treating or preventing atherosclerosis in human or non-human animal subjects by inhibiting or blocking intermediate-conductance calcium activated potassium channels associated with vascular smooth muscle and/or other cells which play a role in the pathogenesis of atherosclerosis (e.g., KCa3.1, KCNN4, IKCa1, IK1, SK4 channels). | 2009-12-10 |
20090306160 | METHODS FOR IMPROVING DRUG DISPOSITION - The invention provides a method for improving the bioavailability, preferably, oral bioavailability and/or drug disposition, e.g. brain penetration, of an iron chelator, which method comprises co-administering to a mammal, especially a human, in need of such treatment, a combination of an iron chelator and an efflux protein inhibitor. | 2009-12-10 |
20090306161 | METHODS OF TREATING ALPHA ADRENERGIC MEDIATED CONDITIONS - Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an α-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic. | 2009-12-10 |
20090306162 | FUNGICIDAL CONTROL OF MOULDS - A composition for treating fungus infection of turfgrass, such as snow mould infection, comprises a mixture of fungicidally effective amounts of formulae 1 and 2: And in particular mixtures of oprodione and trifloxystrobin. A method for treating snow moulds comprises applying the mixture before the onset of continuous snow cover, in at least one application. | 2009-12-10 |
20090306163 | TOPICAL COMPOSITIONS COMPRISING IMIDAZOLIDINEDIONE ANALOGS AND THEIR USE TO TREAT OR PREVENT THE APPEARANCE OF SKIN WRINKLING - The described invention relates to the formulation and delivery of topical compositions comprising a cosmetically effective amount of at least one imidazolidinedione analog reduce the appearance of wrinkles. | 2009-12-10 |
20090306164 | Methods for Treating Papilloma Virus Infection - The present invention relates to polyamide compositions and therapies for treating cells infected with papilloma virus (PV). | 2009-12-10 |
20090306165 | DIPEPTIDE COMPOUNDS CONTAINING D-HISTIDINE - D-Camosine lipophilic derivatives are disclosed, characterized by higher bioavailability than L-camosine and intended for the pulmonary distribution where they can exert detoxifying activity on the cytotoxic carbonyl compounds induced by cigarette smoke. | 2009-12-10 |
20090306166 | Method of Controlling Phytopathogenic Diseases on Turfgrass - A method of controlling phytopathogenic diseases on turfgrass or on seeds thereof, which comprises applying to the turfgrass, the locus thereof or seeds thereof a composition, that, in addition to formulation adjuvants, comprises a fungicidally effective amount of at least one compound of formula I | 2009-12-10 |
20090306167 | Pharmaceutical Compositions for Intranasal Administration Comprising a Melatonin Receptor Agonist, Uses Thereof - The present invention relates to intranasally deliverable compositions comprising melatonin receptor agonists and to methods of using such compositions in the treatment of various diseases and disorders. | 2009-12-10 |
20090306168 | SirT Inhibitors That Bind to NAD - Compound of formula (I) | 2009-12-10 |
20090306169 | Use of Fused Pyrrole Carboxylic Acids for the Treatment of Neurodegenerative and Psychiatric Diseases and D-Amino Acid Oxidase Inhibitors - The present invention provides the use of fused pyrrole carboxylic acids of formula (I) for the manufacture of a medicament to inhibit D-amino acid oxidase, particularly for the treatment of neurodegenerative and psychiatric disorders or diseases; certain compounds of formula I being novel, pharmaceutical compositions containing them, their use in medicine and methods of treatment using them are also disclosed. | 2009-12-10 |
20090306170 | SYNTHESIS OF TEGASEROD OR A SALT THEREOF - The present invention relates to a novel process for the synthesis of 1-((5-methoxy-1H-indol-3-yl)methyleneamino)-3-pentyl-guanidine, commonly known as tegaserod, which is used as a gastroprokinetic, and salts thereof. The present invention also relates to tegaserod and salts thereof having an HPLC purity of about 95% or more. The present invention further relates to pharmaceutical compositions comprising tegaserod or a salt thereof, second medical uses of tegaserod or a salt thereof, and methods of treating or preventing irritable bowel syndrome using tegaserod or a salt thereof. | 2009-12-10 |
20090306171 | INDOLE COMPOUNDS HAVING C4-AMIDE SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds according to the formula (I) or (II) optionally having additional heteroatoms, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. Formula (I), formula (II). R | 2009-12-10 |
20090306172 | 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. | 2009-12-10 |
20090306173 | CRYSTALLINE FORMS OF ATORVASTATIN MAGNESIUM - The present invention relates to crystalline forms of Atorvastatin magnesium and processes for their preparation. The crystalline forms of the present invention are designated as form X, form Y, form Z and form P of atorvastatin magnesium. The present invention further relates to pharmaceutical compositions comprising form X, form Y, form Z and form P of atorvastatin magnesium and method of using the crystalline forms. | 2009-12-10 |
20090306174 | Novel Five-Membered Iminocyclitol Derivatives as Selective and Potent Glycosidase Inhibitors: New Structures for Antivirals and Osteoarthritis Therapeutics - Novel 5-membered iminocyclitol derivatives were found to be a potent and selective inhibitors of the glycoprotein processing α- and β-glucosidase which were further found to be active antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (DEN-2), human SARS coronavirus and human β-hexosaminidase, a new target for development of osteoarthritis therapeutics. | 2009-12-10 |
20090306175 | HETEROCYCLIC ARYLSULPHONES SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5HT6 RECEPTOR - The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT | 2009-12-10 |
20090306176 | Use Of Low Doses Of Oligonucleotides Antisense To TGF-Beta, VEGF, Interleukin-10, C-Jun, C-Fos Or Prostaglandin E2 Genes In The Treatment Of Tumors - This invention is related to the use of at least one oligonucleotide with a length of from about 8 to about 30 nucleotide building blocks for manufacturing a pharmaceutical preparation for the prophylaxis and/or the treatment of diseases, that are modulated by TGF-beta2, TGF-beta1, TGF-beta3, VEGF, interleukin-10, c-jun, c-fos, and/or prostaglandin E2 in a mammal, wherein said oligonucleotide hybridizes with a messenger RNA of a TGF-beta2, TGF-beta1, TGF-beta3, VEGF, interleukin-10, c-jun, c-fos and/or prostaglandin E2 gene and wherein said preparation comprises said oligonucleotide in a concentration of about 1 microM to about 25 microM. | 2009-12-10 |
20090306177 | Modulation of Immunostimulatory Properties of Short Interfering Ribonucleic Acid (Sirna) by Nucleotide Modification - Double-stranded short interfering ribonucleic acid (siRNA) are modified to reduce or eliminate their immunostimulatory effect without significantly affecting their gene silencing effect. Modified siRNA include one or more 2′ sugar modifications and, optionally, internucleotide linkages on the sense strand. Compositions containing the modified siRNA and methods of making and using the modified siRNA are disclosed. New and previously characterized siRNA can be synthesized to incorporate modifications according to the invention. | 2009-12-10 |
20090306178 | CONJUGATED DOUBLE STRAND COMPOSITIONS FOR USE IN GENE MODULATION - The present invention provides conjugated double stranded compositions wherein each strand is modified to have a motif defined by positioning of β-D-ribonucleosides and/or sugar modified nucleosides. More particularly, the present compositions comprise a linked conjugate group on one strand and a non hybridizing region of 2′-modified nucleosides on the other strand. Each strand further comprises one or more phosphorothioate internucleoside linkage. The compositions are useful for targeting selected nucleic acid molecules and modulating the expression of one or more genes. In preferred embodiments the compositions of the present invention hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The present invention also provides methods for modulating gene expression. | 2009-12-10 |
20090306179 | COMPOUNDS AND METHODS FOR MODULATING EXPRESSION OF GCGR - The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing. | 2009-12-10 |
20090306180 | COMPOUNDS AND METHODS FOR MODULATING EXPRESSION APOB - The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing. | 2009-12-10 |
20090306181 | Compositions and methods for evaluating and treating heart failure - The invention relates to compositions, formulations, kits, and methods useful for the treatment and evaluation of heart disease in an individual. | 2009-12-10 |
20090306182 | RNA INTERFERENCE MEDIATED INHIBITION OF MAP KINASE GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating mitogen activated protein kinase (MAP kinase) 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 MAP kinase 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 MAP kinase genes, such as Jun amino-terminal kinase (e.g., JNK-1, JNK-2), p38 (MAPK 14), ERK (e.g., ERK-1, ERK-2) and/or c-Jun. | 2009-12-10 |
20090306183 | Compositions and Methods for the Treatment of Diseases Associated with Aberrant Cilia Assembly and Regulation - Compositions and methods are provided for identifying agents which have efficacy for the treatment of disorders related to aberrant cilial structure and function, including polycystic kidney disease. | 2009-12-10 |
20090306184 | RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS C VIRUS (HCV) EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions. Specifically, the invention relates to double stranded nucleic acid molecules including 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 capable of mediating RNA interference (RNAi) against gene expression, including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. The present invention also relates to small nucleic acid molecules, such as siNA, siRNA, and others that can inhibit the function of endogenous RNA molecules, such as endogenous micro-RNA (miRNA) (e.g, miRNA inhibitors) or endogenous short interfering RNA (siRNA), (e.g., siRNA inhibitors) or that can inhibit the function of RISC (e.g., RISC inhibitors), to modulate gene expression by interfering with the regulatory function of such endogenous RNAs or proteins associated with such endogenous RNAs (e.g., RISC), including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. Such small nucleic acid molecules and are useful, for example, in providing compositions to prevent, inhibit, or reduce diseases, traits and conditions that are associated with gene expression or activity in a subject or organism. | 2009-12-10 |
20090306185 | Nanogenomics for medicine: siRNA engineering - Described herein are materials and methods for the delivery of siRNA and the production of nanoparticles useful for the delivery of siRNA. Methods of treating a disease or disorder using the nanoparticles described herein also are disclosed. | 2009-12-10 |
20090306186 | NOVEL TISSUE PROTECTIVE ERYTHROPOIETIN RECEPTOR (NEPOR) AND METHODS OF USE - There is disclosed a molecular composition(s) of a novel tissue protective erythropoietin (EPO) binding receptor protein complex, termed NEPOR. Presence of NEPOR components on a tumour allows EPO to impinge on the survival of associated cells thereby enhancing tumour progression and negatively effecting patient survival. Presence of NEPOR represents a prognostic biomarker for poorer patient outcome. Thus, methods are provided for stratifying patients having a tumour as suitable (i.e. NEPOR not present) or non-suitable (i.e., NEPOR present) for EPO treatment, comprising: (a) isolating a tissue sample from an individual who is receiving or is a candidate for receiving erythropoietin, (b) determining the level of expression of the NEPOR gene(s) (mRNA) and/or the presence of the NEPOR gene product (protein) from the isolated tissue, and (c) correlating the presence of an NEPOR gene expression product or the presence of NEPOR protein to a physiological response to the treatment with erythropoietin. Furthermore, by disclosing the molecular compositions of NEPOR species, there are disclosed methods for rationally identifying/designing NEPOR modulating therapeutics. Methods also are provided for treating neurological insults such as stroke (via enhancement of NEPOR activity) and cancer (via down-regulation of cyto-protective signaling from NEPOR). | 2009-12-10 |
20090306187 | Modulators of Itch Ubiquitinase Activity - The present invention relates to the identification of new drug targets for therapy of disorders including cancer. In particular, the present invention relates to inhibition of the E3 ubiquitin ligase, Itch, as a means for treating disorders. Furthermore, the present invention relates to the regulation of p63 and p73 stability in cells. In particular, the invention relates to the modulation of the regulation of p63 and p73 stability in cells through modulation of the expression or activity of Itch. Moreover, the invention relates to the use of Itch as a target for the development of agents capable of modulating p63 or p73 stability and especially agents capable of modulating the interaction of Itch and p63 or p73. Such agents may be useful in therapeutic applications including cancer treatment and modulation of skin differentiation. | 2009-12-10 |
20090306188 | IMPORTATION OF MITOCHONDRIAL PROTEIN BY AN ENHANCED ALLOTOPIC APPROACH - The inventors demonstrate that mRNA sorting to the mitochondrial surface is an efficient way to proceed to such an allotopic expression, and that this mRNA sorting can be controlled by selecting appropriate mitochondrion-targeting sequence (MTS) and appropriate 3′UTR sequences. The CDS sequence which codes for the protein to be delivered into the mitochondrion is guided by these appropriate MTS and 3′UTR sequences from the nuclear compartment to the mitochondrion-bound polysomes (where the CDS is translated), and aids in an efficient translocation of a mature functional protein into the mitochondria. Appropriate MTS and 3′UTR sequences correspond to those of nuclearly-transcribed mitochondrially-targeted mRNAs. The inventors demonstrate that, to obtain a stable therapeutically-effective importation, both an appropriate MTS and an appropriate 3′UTR should preferably be used. | 2009-12-10 |
20090306189 | Methods for Controlling Pests Using Rnai - The present invention relates to methods for controlling pest infestation using double stranded RNA molecules. The invention provides methods for producing transgenic cells expressing the double stranded RNA molecules, as well as compositions and commodity products containing or treated with such molecules. | 2009-12-10 |
20090306190 | NEUROPROTECTANTS - Methods of protecting cells against cytotoxic insults are provided. The methods involve administering a composition including a CpG oligonucleotide to a subject. The methods are applicable to the protection of neural and non-neural cells. For example, methods of protecting a neural cell against excitotoxic brain injury are provided. Methods for preparing medicaments for the prophylactic treatment of excitotoxic injury, ischemia and/or hypoxia are also provided. Also provided are compositions for use in the described methods. | 2009-12-10 |
20090306191 | TREATMENT OF A DISEASE OR A CONDITION ASSOCIATED WITH ABERRANT GENE HYPOMETHYLATION BY A METHOD INVOLVING TAILORED EPIGENOMIC MODIFICATION - Disclosed herein is a method for treating a subject having or suspected of having a disease or condition associated with aberrant hypomethylation of one or more genes in the subject, the method involving a tailored epigenomic modification of the subject using methylated polynucleotides directed to hypomethylated genes in the subject. | 2009-12-10 |
20090306192 | BAG3 nucleotide and protein sequences to be used in research, diagnostics and therapy for cell death-involving diseases, and for modulation of cell survival and/or death - The present invention provides BAG3 nucleotide and protein sequences to be used in research, diagnostics and therapy for modulation of cell survival and/or death, in particular in leukemias, other neoplasias and apoptosis-involving diseases. More particularly the invention refers to the use of specific antisense-based constructs and peptide-specific polyclonal and monoclonal antibodies in leukemias, other neoplasias and cell death-involving diseases. | 2009-12-10 |
20090306193 | NUCLEIC ACID AND CORRESPONDING PROTEIN ENTITLED 121P1F1 USEFUL IN TREATMENT AND DETECTION OF CANCER - A novel gene (designated 121P1F1) and its encoded protein, and variants thereof, are described wherein 121P1F1 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, 121P1F1 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 121P1F1 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with 121P1F1 can be used in active or passive immunization. | 2009-12-10 |
20090306194 | NOVEL COMPOSITIONS FOR THE IN VIVO DELIVERY OF RNAI AGENTS - This application describes emulsion formulations containing neutral phospholipids for delivering RNAi, anti-miRNA, or aptamer agents in vivo. The application also relates to methods of making the formulations, and uses of the formulations as delivery agents. | 2009-12-10 |
20090306195 | Fusion Proteins of Mycobacterium Tuberculosis - The present invention relates to fusion proteins containing at least two | 2009-12-10 |
20090306196 | IMINE BASED LIQUID CRYSTALS FOR THE CONTROLLED RELEASE OF BIOACTIVE MATERIALS - The present invention relates to a delivery system based on a film of an imine forming liquid crystalline phase, mixed with at least with one biologically active substance, to which a constant or variable electric field can be applied. The delivery system can be used as a delivery system for biologically active substances such as flavors, fragrances, bactericides, fungicides, insecticides, insect attractants or repellents, agrochemicals or pharmaceuticals. | 2009-12-10 |
20090306197 | Substituted Chromanol Derivatives and Their Use - The present invention relates to substituted chromanol derivatives, to processes for their preparation, to their use on their own or in combination for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 2009-12-10 |
20090306198 | Anti-Oxidant Synergy Formulation Nanoemulsions to Treat Caner - A uniform microfluidized nanoemulsion is disclosed containing a synergistic combination of two antioxidants and a cell membrane stabilizer phospholipid (i.e., an anti-oxidant synergy formulation; ASF). The microfluidized nanoemulsion improves the combination's cell membrane permeability by at least four-fold over conventional nanoemulsion compositions, which significantly increases the intracellular concentration of typically cell-impermeant antioxidants (i.e., for example, tocopherol) and/or systemic bioavailability. As a nanoemulsion, synergistic combination has greater anticancer efficacy than the same combination applied as a free solution. | 2009-12-10 |
20090306199 | Method for inhibiting activation of macrophages, inhibiting formation of osteoclasts, inhibiting function of osteoclasts, and/or activating osteoblasts - A method for inhibiting the activation of macrophages, inhibiting the formation of osteoclasts, inhibiting the function of osteoclasts, and/or activating osteoblasts in a mammal is provided. The method comprises the administration of an effective amount of kinsenoside of formula (I) or a pharmaceutically acceptable salt or ester thereof to the mammal: | 2009-12-10 |
20090306200 | Prophylactic or Therapeutic Agent for Nocturnal Conduct Disorder Associated With Dementia - The present invention provides a prophylactic or therapeutic agent for nocturnal conduct disorders associated with dementia, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide. | 2009-12-10 |
20090306201 | SELECTIVE INHIBITORS FOR TRANSFERASES - A pharmaceutical composition comprising a compound of formula I or II and a pharmaceutically acceptable carrier. Methods for treating a proliferative disorder mediated by a methyl transferase comprising administering an anti-proliferative effective amount of the compound of formula I or II are also presented. | 2009-12-10 |
20090306202 | D-homoandrosta-17-yl carbamate derivatives as selective glucocorticoid receptor ligands - The present invention is directed to D-homoandrosta-17-yl-carbamate derivatives as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. | 2009-12-10 |
20090306203 | PLEUROMUTILIN DERIVATIVES CONTAINING A HYDROXYAMINO- OR ACYLOXYAMINOCYCLOALKYL GROUP - The present invention relates to Compounds of general formula (I), wherein R is hydrogen and R | 2009-12-10 |
20090306204 | Pharmaceutical Composition Comprising Cyclobenzaprine and Aceclofenac in Association - The present invention relates to an association of active ingredients. More specifically: to an association of cyclobenzaprine and aceclofenac. Additionally, the present invention is also related to the use of aceclofenac and cyclobenzaprine, in association for the preparation of a medicine useful in the treatment of painful muscular diseases, as well as to a method of treatment of painful muscular diseases using an association of aceclofenac and cyclobenzaprine. | 2009-12-10 |
20090306205 | METHOXYPOLYETHYLENE GLYCOL THIOESTER CHELATE AND USES THEREOF - The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to donate electrons to free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients. | 2009-12-10 |
20090306206 | SOLID FORM SODIUM LAURYL SULFATE (SLS) PESTICIDE COMPOSITION - A pesticide composition and method of eliminating pests combines water and a solid form of sodium lauryl sulfate to form a pesticide composition effective to cause mortality in pests. The pesticide composition is applied to the indoor structure in an area which the pests inhabit. The sodium lauryl sulfate can be in needle form, pellet form or powder form and constitutes between about 1% and about 10% by weight of the pesticide composition. The pesticide composition may be applied to an area inhabited by cockroaches, including, but not limited to, in crevices, cracks, corners, wall and floor junctures or other enclosed or partially enclosed areas of a structure. | 2009-12-10 |
20090306207 | Treatment of Drug-Resistant Proliferative Disorders - α,β-Unsaturated sulfones, sulfoxides and sulfonamides according to Formula I: | 2009-12-10 |
20090306208 | PROPHYLACTIC OR THERAPEUTIC COMPOSITION FOR HEMOGLOBINURIA OR MYOGLOBINURIA - A prophylactic or therapeutic composition for hemoglobinuria or myoglobinuria which may occur in humans or animals upon loading of exercise or stress or the like is provided. | 2009-12-10 |
20090306209 | ENTERIC-COATED FORMULATIONS OF POLYETHYLENE GLYCOL AND ONE OR MORE SOLUBLE AMINO ACIDS FOR ORAL INGESTION AND ENHANCED UPTAKE OF SAME - Oral amino acid formulations comprising polyethylene glycol are enteric coated. Most preferred amino acids are leucine, glutamine, and arginine. The most preferred polyethylene glycols have an average molecular weight of from 3150 to 3685, although for particular formulation formulations and particular uses, the average molecular weight polyethylene glycols may range from 190 to 9000. | 2009-12-10 |
20090306210 | Solubilizates of Preservatives and Method for Producing the Same - Described is a solubilisate of a preservative containing an aliphatic and/or aromatic acid such as sorbic acid and/or benzoic acid that is free of stabilizing agents, as well as one or more emulsifiers with an HLB value between 9 and 18 with a concentration of about 50% and about 95% emulsifier with regard to the total quantity of the solubilisate, and a procedure for the production of such a solubilisate. | 2009-12-10 |
20090306211 | Peritoneal dialysis fluid - The present invention concerns a peritoneal dialysis fluid with enhanced ultrafiltration during the dialysis dwell period. According to the present invention this is achieved by a peritoneal dialysis fluid comprising sodium ions, osmotic agent and a buffer, characterised in that it comprises citrate at a level of 4 to 10 mM in a final solution ready for use. | 2009-12-10 |
20090306212 | Compositions and Methods for Treating Diabetes and Neuropsychological Dysfunction - The present invention relates to compositions and methods for treating diabetes mellitus, neuropsychological and neurological disorders in a particular group of patient. More specifically, the invention relates to methods of treating diabetes mellitus, neuropsychological and neurological disorders in patients having defective potassium channels. The invention may be used in human subjects, particularly adults or children, and is appropriate to treat various neurological disorders. | 2009-12-10 |
20090306213 | Process for Synthesis of Glycomimicking Cationic Amphiphiles - The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells. | 2009-12-10 |
20090306214 | Use of Syk Tyrosine Kinase Inhibitors for the Treatment of Cell Proliferative Disorders - The invention relates to polyalkylene glycol compounds and their use in treating cell proliferative disorders, more specifically Syk tyrosine kinase-mediated disorders. | 2009-12-10 |
20090306215 | DEUTERIUM-ENRICHED ARFORMOTEROL - The present application describes deuterium-enriched arformoterol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 2009-12-10 |
20090306216 | Use of Beta-Aminoalcohols in the Treatment of Inflammatory Disorders and Pain - A compound for therapeutic use, of the formula (I), wherein R | 2009-12-10 |
20090306217 | Method and Compositions - The present invention provides compositions for inhibiting the activity of an insect pest against a subject (or repelling an insect pest from an environment or preventing attraction to an environment) which compositions comprise geranylacetone as an active ingredient plus a carrier plus a further active ingredient selected from the list consisting of: 6-Methyl-hepten-2-one, octanal, plus optional other chemicals. Also provided are related materials and methods of use. | 2009-12-10 |
20090306218 | Antimicrobial formulations - An antimicrobial formulation containing a synergistic combination of a quinone, such as an optionally substituted benzoquinone or hydroquinone, and a bismuth salt. The formulation may in particular be used against propionibacteria, more particularly to treat skin and skin structure conditions such as acne, or against microbial infections within the oral cavity. | 2009-12-10 |
20090306219 | TOPICAL USE OF PLANT EXTRACT FOR SKIN DETOXIFICATION - Specific plant extracts are applied topically to upregulate genes which code for proteins to prevent the build-up of and mitigate the activity of various harmful materials within the skin. These upregulated proteins include glutathione transferases, peroxiredoxins, oxidoreductases, glutaredoxins and glutathione syntheses. These proteins produce additional glutathione, glyoxalase I, maintain cellular redox homeostasis, reduce hydrogen peroxide and alkylhydroperoxides, and conjugate glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Keratinocytes have been induced to significantly upregulate glutathione and glyoxalase I protein expression. Additionally, keratinocytes pre-treated with diallyl trisulfide have increased viability when exposed to ozone, UV radiation or cigarette smoke extract. The active material can be extracted from plants such as garlic, onions, shallots, leeks, chives, scallions, brussel sprouts, broccoli, cabbage, cauliflower, bok choy, kale, mustard, turnip or radish, may include any compound of the allyl sulfide family, and may be of synthetic origin. | 2009-12-10 |