38th week of 2010 patent applcation highlights part 48 |
Patent application number | Title | Published |
20100240663 | HETEROCYCLES AS POTASSIUM CHANNEL MODULATORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions. | 2010-09-23 |
20100240664 | SOLUBILIZED TOPOISOMERASE POISON AGENTS - The invention provides compounds of formula I: | 2010-09-23 |
20100240665 | BIOLOGICAL MARKERS PREDICTIVE OF ANTI-CANCER RESPONSE TO INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR KINASE INHIBITORS - The present invention provides diagnostic methods for predicting the effectiveness of treatment of a cancer patient with an IGF-1R kinase inhibitor. Methods are provided for predicting the sensitivity of tumor cell growth to inhibition by an IGF-1R kinase inhibitor, comprising assessing whether the tumor cell expresses certain sensitivity or resistance biomarkers, or genomic classifiers. Improved methods for treating cancer patients with IGF-1R kinase inhibitors that incorporate this methodology are also provided. | 2010-09-23 |
20100240666 | FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel fused pyrazine compounds are disclosed that have a formula represented by the following: | 2010-09-23 |
20100240667 | CRYSTALLINE FORMS OF (6R)-L-ERYTHRO-TETRAHYDROBIOPTERIN DIHYDROCHLORIDE - Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations. | 2010-09-23 |
20100240668 | Myosin Light Chain Kinase Inhibitor Compounds, Compositions and Related Methods of Use - Pyridazinyl compounds, compositions and related methods of use. | 2010-09-23 |
20100240669 | NEW COMPOUNDS - The present invention relates to the compounds of general formula I | 2010-09-23 |
20100240670 | 4-[(ARYLMETHYL)AMINOMETHYL]PIPERIDINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The invention relates to 4-[(arylmethyl)aminomethyl]piperidine derivatives of general formula (I) | 2010-09-23 |
20100240671 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to substituted heterocyclic compounds of Formula I or XI: | 2010-09-23 |
20100240672 | MELT-PROCESSED IMATINIB DOSAGE FORM - The invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms. | 2010-09-23 |
20100240673 | EML4-ALK Fusion Gene - The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene. | 2010-09-23 |
20100240674 | USE OF COMPOUNDS DERIVED FROM BENZAMIDINE METHANESULPHONATE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, FOR EXAMPLE IMATINIB MESYLATE, FOR THE PREPARATION O F A DRUG FOR THE TREATMENT OF NEURODEGENERATIVE NIEMANN-PICK C DISEASE (NPC) - This invention relates to the use of imatinib mesylate for the treatment of metabolism disorders characterized by neurodegeneration, in particular a metabolism disorder characterized by an inability to metabolize lipids such as in persons with Niemann-Pick Type C disease. More specifically, this invention relates to a method of treating neurodegenerative disease, comprising administering a therapeutically effective amount of a compound derived from imatinib mesylate or a pharmaceutically acceptable salt thereof. | 2010-09-23 |
20100240675 | THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN - Compounds of formulae: | 2010-09-23 |
20100240676 | THIAZOLE DERIVATIVES - Compounds of the formula (I), in which R | 2010-09-23 |
20100240677 | Compounds as PDE IV and TNF Inhibitors - This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). | 2010-09-23 |
20100240678 | LEUKOTRIENE B4 INHIBITORS - Provided herein are compounds of the formula (I): | 2010-09-23 |
20100240679 | 4-Phenylpiperidine Derivatives as Renin Inhibitors - Compounds of the present invention having the formula | 2010-09-23 |
20100240680 | Purine derivatives as a2a agonists - Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R | 2010-09-23 |
20100240681 | VALOMACICLOVIR POLYMORPHS - The present invention relates to crystalline forms of valomaciclovir, processes for preparing crystalline forms of valomaciclovir, pharmaceutical compositions thereof and methods of using thereof. | 2010-09-23 |
20100240682 | PHOPHYLACTIC OR THERAPEUTIC AGENT FOR INFLAMATORY DISEASE COMPRISING THYMIDINE PHOSPHORYLASE INHIBITOR AS ACTIVE INGREDIENT - To provide an excellent agent for prevention or treatment of an inflammatory disease. | 2010-09-23 |
20100240683 | COMBINATION THERAPY, COMPOSITION AND METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS - The present invention relates to a combination therapy for the treatment of cardiovascular disorders. More particularly, the invention relates to compositions combining long-chain optionally substituted amphipatic carboxylates (known as MEDICA drugs) and particularly, M16αα, M16ββ and M18γγ, with HMG-CoA reductase inhibitors (known as statins). The compositions of the invention may particularly be used for the treatment of cardiovascular disorders, for elevating HDL-cholesterol levels, decreasing non-HDL-cholesterol and particularly triglycerides, and decreasing insulin resistance in a subject suffering from Metabolic Syndrome or cardiovascular disorders. The invention further provides methods of treatment of such disorders using these combined compositions. | 2010-09-23 |
20100240684 | MINOXIDIL AQUEOUS COMPOSITION CONTAINING BILE ACID - An object of the present invention is to provide a liquid composition wherein minoxidil can be dissolved at a relatively high concentration (the saturating amount or above), stimulation of skin and stickiness is suppressed without containing an organic solvent, and excellent effects of percutaneous absorption is achieved. The present invention provides a liquid composition comprising (i) minoxidil, (ii) bile acid or a salt thereof, and (iii) an aqueous medium in an amount of 30% by weight or more of the weight of the composition. | 2010-09-23 |
20100240685 | 2-S-Benzyl Substituted Pyrimidines As CRTH2 Antagonists - Provided herein are 2-S-benzyl pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the prophylaxis and treatment of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases. | 2010-09-23 |
20100240686 | CHEMICAL COMPOUNDS - Compounds of formula (I): | 2010-09-23 |
20100240687 | METHOD FOR CHECKING AND CONTROLLING THE MAMMALIAN LACTIC ACID FERMENTATION PROCESS/AEROBIC GLUCOSE FERMENTATION METABOLIC PATHWAY IN MAMMALIAN ORGANISM - The method for qualitative and quantitative detecting of the extend of use and the correct process flow of the mammalian aerobic glucose fermentation metabolic pathway (mam-aGF) in a mammalian individual is characterized in that the enzyme TKTL1 is used as indicator and target molecule and the structural and/or functional parameter of said TKTL1 in a biological sample of said individual (patient) are taken as indication for the qualitative and quantitative run of the mam-aGF in the cells and/or tissue of said individual (patient). In combination with the use of inhibitors and activators of the mam-aGF the method is further suitable for checking and controlling the mam-aGF in an individual (patient). | 2010-09-23 |
20100240688 | 1,3-DISUBSTITUTED-4-PHENYL-3,4,5,6-TETRAHYDRO-2H,1 H-1,4 BIPYRIDINYL-2-ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 2010-09-23 |
20100240689 | N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle). | 2010-09-23 |
20100240691 | MORPHINAN DERIVATIVES WITH HIGH ORAL BIOAVAILABILITY - The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction. | 2010-09-23 |
20100240692 | [1,10]-PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES - The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition, their use as a medicament, especially for treating a treatment neurodegenerative or haematological disease or condition, and a pharmaceutical composition comprising the compounds. | 2010-09-23 |
20100240693 | Oxime and Hydroxylamine Substituted Thiazolo [4,5-C] Ring Compounds and Methods | 2010-09-23 |
20100240694 | SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy. | 2010-09-23 |
20100240695 | STABILIZED ZOLPIDEM PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a carbonate and bicarbonate buffer system in an amount sufficient to raise the pH of saliva to at least 8.5, and wherein the carbonate forms a coating on the bicarbonate wherein the amount of carbonate coating is at least 30% (w/w) of the total buffer amount are described. Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a binary buffer system of carbonate and bicarbonate, wherein the carbonate and bicarbonate are co-located in a single particle, wherein the bicarbonate is coated with the carbonate, and wherein the amount of carbonate coating is at least 30% (w/w) of the binary buffer system are also described. | 2010-09-23 |
20100240696 | 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF - The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C | 2010-09-23 |
20100240697 | PHARMACEUTICAL COMPOSITION FOR TREATING OVERACTIVE BLADDER - [Problems] To provide a pharmaceutical composition which is useful as a therapeutic agent for overactive bladder. | 2010-09-23 |
20100240698 | MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV of formula al | 2010-09-23 |
20100240699 | METHOD OF TREATING SENSORIMOTOR DISORDERS WITH ALPHA-2 ADRENERGIC RECEPTOR AGONISTS - Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity. | 2010-09-23 |
20100240700 | PROPHYLACTIC PRETREATMENT WITH ANTIOXIDANTS - Methods, compositions, and uses for pre-treating patients who are susceptible to ischemia, including stroke, with nitroxides, in order to prevent or ameliorate the effects of stroke or other ischemic disease. | 2010-09-23 |
20100240701 | TUBULYSINS AND PROCESSES FOR PREPARING - Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations. | 2010-09-23 |
20100240702 | Benzimidazolone Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. | 2010-09-23 |
20100240703 | OXYIMINO COMPOUNDS AND THE USE THEREOF - The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SO | 2010-09-23 |
20100240704 | METHOD OF MODULATING STRESS-ACTIVATED PROTEIN KINASE SYSTEM - Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system. | 2010-09-23 |
20100240705 | SUBSTITUTED ENAMINOCARBONYL COMPOUNDS USED AS INSECTICIDES - The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects. | 2010-09-23 |
20100240706 | 1,3-DISUBSTITUTED-4-PHENYL-1H-PYRIDIN-2-ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 2010-09-23 |
20100240707 | 1,3,5-TRISUBSTITUTED TRIAZOLE DERIVATIVE - The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. | 2010-09-23 |
20100240708 | Alpha-(N-Benzenesulfonamido)Cycloalkyl Derivatives - Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a γ-secretase enzyme; or (ii) the production of β-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: | 2010-09-23 |
20100240709 | Sulfoximine Derivatives as p38 MAP Kinase Inhibitors - The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts pharmaceutical compositions containing them, and novel intermediates involved in their synthesis. | 2010-09-23 |
20100240710 | Use of Pyridoxamine to Treat and/or Prevent Disease Processes - Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. | 2010-09-23 |
20100240711 | SOLID PREPARATION COMPRISING NPYY5 RECEPTOR ANTAGONIST - A preparation which can improve solubility of a NPYY5 receptor antagonist in water, even when the NPYY5 receptor antagonist is contained in the preparation at a high content is provided. A solid preparation containing a NPYY5 receptor antagonist, an amorphous stabilizer, and optionally an amorphousization inducing agent. Particularly, when the amorphous stabilizer is hydroxypropylmethylcellulose phthalate and/or hydroxypropylmethylcellulose acetate succinate, and the amorphousization inducing agent is urea and/or saccharine sodium at an addition amount of less than 8% by weight, dissolution out property of a water-hardly soluble NPYY5 receptor antagonist could be improved. | 2010-09-23 |
20100240712 | INSECTICIDAL COMPOUNDS - Novel aromatic compounds of formula (I): wherein A | 2010-09-23 |
20100240713 | AROMATIC AND HETEROAROMATIC COMPOUNDS USEFUL IN TREATING IRON DISORDERS - This invention is directed to compounds of formula (I), wherein m, formula (II), R | 2010-09-23 |
20100240714 | ORAL COMPOSITION FOR DENTAL PURPOSES - A dental composition for oral use, containing a phosphorylated saccharide (a), a cationic bactericidal agent (b) and a solvent (c). By using the dental composition for oral use of the present invention, the adhesion of the bacteria in the oral cavity to the surfaces of the teeth can be suppressed for a long period of time; therefore, the dental composition for oral use can be suitably used for, for example, a mouse-wash agent, a dentifrice agent, a gargling agent, a mouse spray, a coating agent or a bonding agent to tooth surface or a dental prosthetic, a hypersensitive inhibitor, a therapeutic agent for periodontal diseases, that is applied to a periodontal pocket, or the like. | 2010-09-23 |
20100240715 | Apoptosis promoters - Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. | 2010-09-23 |
20100240716 | THIADIAZOLINE DERIVATIVE | 2010-09-23 |
20100240717 | NOVEL THIOPHENE DERIVATIVES AS S1P1/EDG1 RECEPTOR AGONISTS - The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH═CH—, *—CO—CH | 2010-09-23 |
20100240718 | NOVEL HETEROARYL-SUBSTITUTED ACETONE DERIVATIVE, SUITABLE FOR INHIBITING PHOSPHOLIPASE A2 - The present invention relates to novel heteroaryl-substituted acetone derivatives inhibiting the enzyme phospholipase A2, and pharmaceutical agents comprising said compounds. | 2010-09-23 |
20100240719 | NOVEL ALPHA-(N-SULFONAMIDO)ACETAMIDE COMPOUNDS INCORPORATING DEUTERIUM AS INHIBITORS OF BETA AMYLOID PEPTIDE PRODUCTION - The present disclosure provides novel deuterated alpha-(N-sulfonamido)acetamide compounds, their pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease, head trauma, traumatic brain injury, and/or dementia pugilistica and/or other conditions associated with β-amyloid peptide. | 2010-09-23 |
20100240720 | ALLOSTERIC JNK INHIBITORS - The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents. | 2010-09-23 |
20100240721 | SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF - The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. | 2010-09-23 |
20100240722 | FLUORINE-CONTAINING ORGANOSULFUR COMPOUND AND PESTICIDAL COMPOSITION COMPRISING THE SAME - There is provided a fluorine-containing organosulfur compound having an excellent controlling effect m represents 0 or 1; n represents 0, 1 or 2; A represents an optionally substituted 5-membered aromatic heterocyclic group; R | 2010-09-23 |
20100240723 | METHODS 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. | 2010-09-23 |
20100240724 | Edible Film - The present invention relates to an edible film composition comprising a waxy starch hydrolysate, a modified starch and a water-soluble polymer, and an edible film comprising the same. The present edible film may not only have an excellent film forming property, solubility and feeling in the oral cavity, but also be easily prepared at low cost, and thus be usefully used as an oral cleanser or a bad breath remover for oral cleansing, and a soluble formulation on tongue for uptake of drug in the oral cavity. | 2010-09-23 |
20100240725 | NOVEL 1,3-DIHYDRO-5-ISOBENZOFURANCARBONITRILE DERIVATIVES AND PHARMACEUTICAL COMPOSITION THEREOF FOR THE TREATMENT OF PREMATURE EJACULATION - Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation. | 2010-09-23 |
20100240726 | COMPOSITIONS FOR TREATING AMYLOID ASSOCIATED DISEASES - Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided. | 2010-09-23 |
20100240727 | Model for Glutamate Racemase Inhibitors and Glutamate Racemase Antibacterial Agents - The increase in antibacterial resistance has created the demand for new antibiotics. The present invention relates to a more potent antibiotic that targets the enzyme glutamate racemase from known glutamate racemase inhibitors. Glutamate racemase catalyses the interconversion of L-glutamate to D-glutamate, making D-glutamate available, which is required for bacterial peptidoglycan biosynthesis. Knockout mutations have shown glutamate racemase to be necessary for bacterial cell survival and, before the present invention, no antibiotic on the market targeted this enzyme. The present invention relates to new, ligand based glutamate racemase inhibitors, developed using software to extract a pharmacophore model from a group of known glutamate racemase inhibitors. Forty-seven (47) known inhibitors were collected from the literature and several pharmacophore models were extracted therefrom. The functional groups common to all the known inhibitors were included in a pharmacophore model that described the requirements for glutamate racemase inhibition with 82% accuracy. Of these models, one was found to describe the requirements for glutamate racemase inhibition with 82% accuracy. The model was used to search databases of commercially available chemical compounds and 2-(2-(1H-indol-3-yl)ethylamino)-4-oxo-4-p-tolylbutanoic acid and 2-(2-(1H-indol-3-yl)ethylamino)-4-(4-fluorophenyl)-4-oxobutanoic acid were identified as showing antibacterial activity. These compounds were assayed against | 2010-09-23 |
20100240728 | Co-Crystals of Pyrrolidinones - The present invention relates to new co-crystals of pyrrolidinones having the formula (I) wherein R | 2010-09-23 |
20100240729 | ALPHA, BETA-UNSATURATED IMIDATE COMPOUND AND PESTICIDAL COMPOSITION CONTAINING THE SAME - There is provided a compound having an excellent controlling effect on pests, represented by the formula (I): | 2010-09-23 |
20100240730 | RNA Interference Mediated Inhibition of Gene Expression Using Chemically Modified Short Interfering Nucleic Acid (siNA) - The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, cosmetic, cosmeceutical, prophylactic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified 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 target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of disease (e.g., cancer, proliferative, inflammatory, metabolic, autoimmune, neurologic, ocular diseases), condition, trait (e.g., hair growth and removal), genotype and phenotype that responds to modulation of gene expression or activity in a cell, tissue, or organism. Such small nucleic acid molecules can be administered systemically, locally, or topically. | 2010-09-23 |
20100240731 | LIPOPEPTIDES FOR DELIVERY OF NUCLEIC ACIDS - Lipopeptide compounds comprising a peptide having 2 to 100 amino acid residues, and having a lipophilic group attached to at least one terminus of the peptide or to at least one amino acid residue of the peptide, and salts and uses thereof. The lipophilic group may be attached to the N-terminus, C-terminus or both termini of the peptide. The lipophilic group may be attached to at least one interal amino acid residue (i.e., an amino acid residue that is not the N-terminus or the C-terminus amino acid residue of the peptide). The lipophilic group may be attached to either termini or both and at least one internal amino acid residue. | 2010-09-23 |
20100240732 | APTAMER-TARGETED SIRNA TO PREVENT ATTENUATION OR SUPPRESSION OF A T CELL FUNCTION - Compositions for countering immune attenuating/suppressive pathways comprise targeting agents or aptamer targeted RNAi-mediated gene silencing (siRNA/shRNA). These compositions have broad applicability in the treatment of many diseases. | 2010-09-23 |
20100240733 | Histone Demethylation Mediated by the Nuclear Amine Oxidase Homolog LSD1 - LSD1, a homolog of nuclear amine oxidases, functions as a histone demethylase and transcriptional co-repressor. LSD1 specifically demethylates histone H3 lysine 4, which is linked to active transcription. Lysine demethylation occurs via an oxidation reaction that generates formaldehyde. Importantly, RNAi inhibition of LSD1 causes an increase in H3 lysine 4 methylation and concomitant de-repression of target genes, suggesting that LSD1 represses transcription via histone demethylation. The results thus identify a histone demethylase conserved from | 2010-09-23 |
20100240734 | METHODS AND COMPOSITIONS FOR THE SPECIFIC INHIBITION OF GENE EXPRESSION BY DOUBLE-STRANDED RNA - The invention is directed to compositions and methods for selectively reducing the expression of a gene product from a desired target gene in a cell, as well as for treating diseases caused by the expression of the gene. More particularly, the invention is directed to compositions that contain double stranded RNA (“dsRNA”), and methods for preparing them, that are capable of reducing the expression of target genes in eukaryotic cells. The dsRNA has a first oligonucleotide sequence that is between 25 and about 30 nucleotides in length and a second oligonucleotide sequence that anneals to the first sequence under biological conditions. In addition, a region of one of the sequences of the dsRNA having a sequence length of at least 19 nucleotides is sufficiently complementary to a nucleotide sequence of the RNA produced from the target gene to trigger the destruction of the target RNA by the RNAi machinery. | 2010-09-23 |
20100240735 | Pharmaceutical Compositions for Angiogenic Therapy - The present invention provides: (1) pharmaceutical compositions for angiogenic therapy which contain, as the active ingredients, at least one substance selected from substances having vasodilating effect and/or platelet aggregation inhibitory effect, and substances producing them; and a gene encoding an angiogenesis factor; (2) agents for potentiating the angiogenic effect of a gene encoding an angiogenesis factor that contain, as the active ingredient, at least one substance selected from substances having vasodilating effect and/or platelet aggregation inhibitory effect and substances producing them; (3) an angiogenic agent which contains a prostacyclin synthase gene as the active ingredient; (4) pharmaceutical compositions for angiogenic therapy which contain ets-1 gene and another gene encoding an angiogenesis factor as the active ingredients; (4) an agent which contain ets 1 gene as the active ingredient for potentiating the angiogenic effect of another gene encoding an angiogenesis factor; and (5) an angiogenic agent which contains ets-1 gene as the active ingredient. | 2010-09-23 |
20100240736 | Novel Compounds for the Treatment or Alleviation of Edema, and Methods for their Use - Isolated and substantially purified oligonucleotide compounds have been shown to be effective in reducing swelling and edema. Novel methods and substances are presented for the prevention, alleviation or treatment of edema of various aetiology. | 2010-09-23 |
20100240737 | ENZYME-PRODRUG THERAPY FOR PROSTHETIC JOINT REPAIR - The invention relates to the use of gene therapy in the treatment of aseptic loosening of orthopaedic prostheses and discloses methods of refixing such prostheses without open revision surgery. In particular, it provides adenoviral vectors and prodrugs for simultaneous, separate or sequential use in the destruction of interface tissue allowing subsequent recementing of loose prostheses in a minimally invasive manner. | 2010-09-23 |
20100240738 | ANTISENSE MODULATION OF KINESIN-LIKE 1 EXPRESSION - Antisense compounds, compositions and methods are provided for modulating the expression of kinesin-like 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding kinesin-like 1. Methods of using these compounds for modulation of kinesin-like 1 expression and for treatment of diseases associated with expression of kinesin-like 1 are provided. | 2010-09-23 |
20100240739 | WIDESPREAD GENE DELIVERY TO MOTOR NEURONS USING PERIPHERAL INJECTION OF AAV VECTORS - The present invention relates to compositions and methods, in particular to methods based on systemic injection of rAAV, for delivering genes to cells of the central nervous system in mammals, such as brain neurons or glial cells, and in particular to motor neurons or glial cells of the spinal cord The invention also relates to methods of treating motor neuron disorders in mammals by expression of therapeutic genes. The invention stems from the unexpected discovery that peripheral injection of AAV vectors leads to a bypass of the blood brain barrier and a massive infection of motor neurons. The invention may be used in any mammal, including human subjects. | 2010-09-23 |
20100240740 | EX VIVO AND IN VIVO EXPRESSION OF THE THROMBOMODULIN GENE FOR THE TREATMENT OF CARDIOVASCULAR AND PERIPHERAL VASCULAR DISEASES - The present invention relates to methods and compositions for treatment of cardiovascular and peripheral vascular diseases using ex vivo and in vivo gene delivery technologies. One aspect of the present invention relates to a method for treating a vascular disease by introducing a DNA sequence encoding a TM protein or its variant into a segment of a blood vessel in vivo using a gutless adenovirus vector. Another aspect of the present invention is to provide a method to deliver a gutless adenovirus vector carrying a DNA sequence encoding a TM protein or its variant using a stent. | 2010-09-23 |
20100240741 | PHARMACEUTICAL COMPOSITIONS FOR THE ADMINISTRATION OF APTAMERS - Pharmaceutical compositions comprising an aptamer and an amino acid ester or amide or an aptamer; a divalent metal cation; and a carboxylic acid, a phospholipid, a phosphatidyl choline, or a sphingomyelin. Methods of treating or preventing a condition in an animal comprising administering to the animal the pharmaceutical compositions. | 2010-09-23 |
20100240742 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 2010-09-23 |
20100240743 | CANNABINOID RECEPTOR MODULATOR - A cannabinoid receptor modulator containing a compound represented by Formula (I | 2010-09-23 |
20100240744 | METHODS FOR THE TREATMENT OF DEMENTIA BASED ON APO E GENOTYPE - This invention relates to methods to prevent worsening of and/or to improve cognitive functioning and behavior problems in patients with dementia by means of ApoE genotyping to guide the use of AChEI drugs, including rivastigimine. Also included are kits for determining ApoE4 status and recommended treatment strategy. | 2010-09-23 |
20100240745 | METHOD OF TREATMENT OF INFLAMMATION IN HYPERTENSIVE PATIENTS - The present invention relates to the use of 4-(nitrooxy)-butyl-(S)-2-(6-methoxy-2-naphthyl)-propanoate (naproxcinod) for the treatment of pain and/or inflammation in patients with hypertension treated with renin-angiotensin system blocking agents. | 2010-09-23 |
20100240746 | STEREOISOMERS OF TRICYCLODECAN-9-YL-XANTHOGENATE - Provided herein are optically active stereoisomers of tricylclodecan-9-yl xanthogenate, processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disease caused by a virus. | 2010-09-23 |
20100240747 | Motuporamine Mimic Agents - Disclosed herein are motuporamine mimic agents and methods of making and using same. Particularly exemplified are motuporamine mimic agents comprising cytotoxic activity and/or anti-metaplastic activity. | 2010-09-23 |
20100240748 | TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES - The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms, benign prostate hyperplasia, prostate cancer, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer. | 2010-09-23 |
20100240749 | ANESTHETIC SPRAY COMPOSITION - An anesthetic spray composition suitable for application to the back of the throat comprising a topical anesthetic and a mucoadhesive polymer. | 2010-09-23 |
20100240750 | CATHETER LOCK SOLUTION COMPRISING CITRATE AND A PARABEN - This invention relates to compositions, methods, devices and kits relating to the infusion of a catheter lock solution into an indwelling catheter. Inventive compositions, methods, devices and kits aid in diminishing the effects of microbial infection in catheters and occlusion of the catheters. A lock solution provided by the invention includes citrate and a paraben. The solution preferably has a density suitable for retention of the solution in a catheter during the lock period. Another lock solution provided by the invention includes citrate, a paraben and a photo-oxidant, such as, for example, methylene blue. | 2010-09-23 |
20100240751 | Methods - A perfluoroctanoic acid or a salt or an ester thereof; perfluorosuberic acid, perfluoroheptanoic acid, perfluorohexanoic acid, perfluoropentanoic acid, perfluorobutanoic acid or perfluoropropionic acid or a salt or an ester any thereof; or perfluoroctane are useful in treating diabetes, obesity, hypercholesterolaemia, hyperlipidaemia, cancer, inflammation or other conditions in which modulation of lipid or eicosanoid status or function may be desirable. | 2010-09-23 |
20100240752 | Aqueous Acidic Hard Surface Cleaning and Disinfecting Compositions - A highly aqueous liquid acidic hard surface treatment composition having a pH of about 3.5 or less which necessarily comprises:
| 2010-09-23 |
20100240753 | EFFECTIVE PHARMACEUTICAL CARRIER FOR POORLY BIOAVAILABLE DRUGS - The present invention is directed to an improved effectiveness pharmaceutical carrier comprising anyone or a combination of edible or pharmaceutical acceptable fatty acids and anyone or a combination of non-ionic surfactants, which is capable of improving the bio-absorption of drugs with intermediate log P ranging from 2 to 4 (having poor solubility in both water and triglycerides) as well as those with high log P of more than 4. | 2010-09-23 |
20100240754 | UNSATURATED FATTY AMINO ACID DERIVATIVES AND USE THEREOF IN DERMAL COSMETOLOGY - The present invention relates to drugs consisting of unsaturated fatty amino-acid derivatives of the general formula (I), and to their pharmaceutically acceptable acid addition salts, in which: X is oxygen or NH, Rn are independently hydrogen or a (C | 2010-09-23 |
20100240755 | THERAPEUTIC AND COSMETIC COMPOSITIONS FOR TREATMENT OF SKIN - The present invention is directed to a skin cream containing L-glutathione and methyl sulfone in combination with perfluorodecalin and various vitamins such as Vitamin D and C. The cream can be used to treat cancerous and precancerous diseases found in or on the skin. | 2010-09-23 |
20100240756 | COMPOUNDS FOR TREATING INFLAMMATION AND PAIN - The present invention is directed to a compound of 2-N halo-4-methylsulfonyl-butyric acid, such as 2-N chloro-4-methylsulfonyl-butyric acid, or a pharmaceutically acceptable salt or solvate thereof. The present invention is also directed to a pharmaceutical composition comprises the compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation or inflammatory-related disorders, bacterial infection, pain, or skin conditions, by administering 2-N halo-4-methylsulfonyl-butyric acid to a subject in need thereof. | 2010-09-23 |
20100240757 | SYSTEMS AND METHODS FOR DELIVERING A FLUID DRUG - Devices and methods for distributing a fluid, e.g., a fluid drug, are disclosed. Fluid-drug distribution can be advantageously utilized to help patients suffering from a disorder that affect fine motor skill usage, e.g., Parkinson's Disease. Some aspects are directed to dosing containers that are adapted to distribute one or more selected dosages of fluid from the container. In some instances, the containers are adapted to be operable by patients with hindered fingertip motor control to help dispense a fluid-drug, such as a fluid including carbidopa and levodopa. Other aspects are directed to a kit for distributing a fluid drug that can be stored with a longer shelf life in solid form. Also discussed herein are methods for distributing a fluid drug for treating a disorder such as Parkinson's Disease. | 2010-09-23 |
20100240758 | EXTERNAL PREPARATION FOR PERCUTANEOUS ADMINISTRATION CONTAINING NONSTEROIDAL ANTI-INFLAMMATORY ANALGESIC - An external preparation for percutaneous administration which contains a light-sensitive nonsteroidal anti-inflammatory analgesic and a UVA-shielding agent which inhibits the analgesic to cause light toxicity and a light allergy. This external preparation for percutaneous administration, which contains a nonsteroidal anti-inflammatory analgesic, can be prevented, with higher certainty, from causing the hypersensitivity to light attributable to light toxicity and a light allergy. | 2010-09-23 |
20100240759 | USE OF AN AGENT THAT CONTAINS CORBAMIDE AND/OR AT LEAST A DERIVATIVE THEREOF AS A CLEANING AGENT - The invention relates to the use of an agent that contains 5 to 99.9% in weight of carbamide and/or at least a derivative thereof, as a cleaning agent for closed systems, in particular as a dishwasher detergent, as a laundry detergent for washing machines, as an agent for cleaning, sanitizing and/or disinfecting for equipment in the food processing industry and for medical equipment, the use as a hand dishwashing detergent or sanitary cleaner or as a hand cleaner. In addition, the invention relates to a method for reducing or avoiding enzymes in cleaning agents for closed systems, in hand dishwashing detergents or in sanitary cleaning agents as well as an enzyme-free dishwashing detergent or enzyme-free sanitary cleaning agent that contain 5 to 99.9% in weight of carbamides or derivates thereof. Finally, the invention relates to the use of percarbamide as a bleaching agent in particular in dishwashing detergents and in sanitary toilet cleaning agents. | 2010-09-23 |
20100240760 | Biomarkers for Efficacy of Aliskiren as a Hypertensive Agent - A retrospective pharmacogenetic analysis was conducted in an attempt to evaluate potential association between genetic variation and outcome of a clinical trial of efficacy of aliskiren as an antihypertensive agent. Forty-eight polymorphisms were examined in twelve genes from the renin-angiotensin-aldosterone system (RAS) or previously implicated in blood pressure regulation. Significant associations were seen between one polymorphism in the angiotensin converting enzyme (ACE) gene, two polymorphisms in the angiotensin II type 2 receptor (AGTR2) gene, and clinical parameters of mean sitting diastolic and systolic blood pressure decrease. These effects were not found with irbesartan and placebo treatment, but instead were specific to aliskiren treatment. | 2010-09-23 |
20100240761 | BRONCHODILATING BETA-AGONIST COMPOSITIONS AND METHODS - Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided. | 2010-09-23 |
20100240762 | SANITIZER FORMULATIONS - The present invention relates to a stable and effective sanitizer formulation for indirect food contact applications. The formulation contains: (a) an antimicrobial active agent selected from the group consisting of biguanides, monoguanides, and combinations thereof; (b) a dialkyldimethyl ammonium salt, and (c) a compound selected from the group consisting of an alkyldimethylbenzyl ammonium salt, an alkyldimethyl(ethylbenzyl) ammonium salt, an alkoxylated alcohol, and combinations thereof. | 2010-09-23 |
20100240763 | Method to Determine and Biomarker for Treatment Efficacy With Ssri, Snri, and Sari Antidepressants - The invention provides a method for determining whether a patient suffering from a condition that is susceptible to treatment with a compound that activates the brain serotonin system is resistant to treatment with the compound. The method comprises observing whether the genome of the patient contains at least one copy of the BDNF allele containing a genetic alteration, and correlating the presence of the allele containing the genetic alteration with patients who are resistant to treatment with the compound. In another embodiment, the method comprises observing whether the patient expresses a BDNF protein containing an amino acid alteration, and correlating the expression of the BDNF protein containing the amino acid alteration with patients who are resistant to treatment with the compound. | 2010-09-23 |