15th week of 2012 patent applcation highlights part 39 |
Patent application number | Title | Published |
20120088704 | Lubricant and functional fluid additive package, and lubricants and functional fluids containing same - The present invention is a lubricant or functional fluid additive for a polyolefin oil blend, comprising a mixture of: (a) an anti-wear component consisting essentially of 95% isopropylated triarylphosphate and 5% dodecyl phosphate, the dodecyl phosphate being only partially esterified, the anti-wear component present in the polyolefin oil blend in a range of from about 0.75 percent to about 2.00 percent by weight; (b) an antioxidant component selected from the group consisting of alkylated phenyl-alpha-naphthylamine, phenyl-alpha-naphthylamine and mixtures thereof, and present in the polyolefin oil blend in a range of from about 0.75 percent to about 2.00 percent by weight; (c) an anti-rust component comprising an alkylated succinic acid ester anti-rust agent, and present in the polyolefin oil blend in a range of from about 0.050 percent to about 0.125 percent by weight; and (d) a metal deactivator component comprising a tolytriazole derivative, and present in the polyolefin oil blend in a range of from about 0.050 percent to about 0.125 percent by weight. | 2012-04-12 |
20120088705 | POLYALKYLENE GLYCOL-BASED ETHER PYRROLIDONE CARBOXYLIC ACIDS, AND CONCENTRATES FOR THE PRODUCTION OF SYNTHETIC COOLING LUBRICANTS CONTAINING THE SAME - The subject of the invention is an etherpyrrolidone carboxylic acid of the formula (1) | 2012-04-12 |
20120088706 | WATER-MIXED METAL WORKING FLUIDS CONTAINING ETHER PYRROLIDONE CARBOXYLIC ACIDS - The invention relates to compositions containing a basic oil or base oil, 10 to 50 percent by weight of ether pyrrolidone carboxylic acids of formula (1) or the salts thereof of formula (1), | 2012-04-12 |
20120088707 | ALKYL (METH) ACRYLATES COMPRISING A LONG LINEAR CHAIN BEARING ALKYL RAMIFICATIONS, PREPARATION THEREOF AND USE THEREOF IN THE PRODUCTION OF PETROLEUM ADDITIVES - The invention relates to alkyl(meth)acrylates comprising a long linear chain bearing alkyl ramifications corresponding to general formula (I): | 2012-04-12 |
20120088708 | LUBRICATING COMPOSITION CONTAINING MULTIFUNCTIONAL HYDROXYLATED AMINE SALT OF A HINDERED PHENOLIC ACID - Multi-functional additives which impart improved antioxidancy to lubricating oil compositions and frictional properties resulting in improved fuel economy in an internal combustion engine are disclosed. More particularly disclosed are lubricating oil compositions for internal combustion engines comprising a) a major amount of an oil of lubricating viscosity; and b) a minor amount of an oil soluble hydroxylated amine salt of a hindered phenolic acid, said salt having the general formula I: | 2012-04-12 |
20120088709 | DETERGENT FOR USE IN APPLIANCES - Disclosed are liquid alkaline detergent preparations that are to be dispensed automatically when washing dishes in a dishwasher, comprising: a) 15 to 60 percent by weight of builder; b) 30 to 80 percent by weight of water; and c) less than 5 percent by weight of surfactant. Because of their thermal stability, the detergent preparations are particularly suitable for carrying out automatic dispensing processes when washing dishes in a dishwasher and washing fabrics in a washing machine. Furthermore, the detergent preparations are characterized by significantly improved cleaning power compared with conventional methods. | 2012-04-12 |
20120088710 | MACHINE CLEANING AGENT - A liquid alkaline cleaning agent preparation for automatic dispensing during automatic dishwashing or textile cleaning includes a) 15 to 60% by weight of a builder, b) <5% by weight of silicate and c) 30 to 80% by weight of water. These cleaning agents have a good thermal stability and are therefore suitable for automatic dispensing methods and are furthermore characterized by a substantially improved cleaning performance. | 2012-04-12 |
20120088711 | METAL CLEANER POLISHER AND ANTI-TARNISH SOLUTION - The present invention is directed to a metal cleaner polisher and anti-tarnish solution which comprises the following ingredients per 32 fluid ounces: 5.00 to 10.00 percent mineral spirits by volume; 1.50 to 4.50 percent ethanol by volume; 0.50 to 1.50 percent ammonia by volume; 0.50 to 1.50 percent thiourea by volume; 0.25 to 1.00 percent sulfamic acid by volume; less than 0.20 percent disodium cocoampho-diproprionate by volume; and deionized water. Optionally, the following ingredients may be added individually, in any combination or all together: thickening/suspension agents; abrasive additives; and a modifying/stabilizing agent; and optionally varying amounts of fragrance and colorizing agents. | 2012-04-12 |
20120088712 | Particulate fabric softening composition and method of making it - A particulate fabric softening composition, comprising one or more ethylenediamine fatty acid diamides and one or more quaternary ammonium salt fabric softeners, the composition having an exothermal transition at a temperature between 60 and 90° C. with an exothermal transition enthalpy of more than 5 J/g measured by DSC with a heating rate of 2° C./min, can be press shaped to multiple use, dryer added fabric softening articles having high initial surface hardness. | 2012-04-12 |
20120088713 | TNF INHIBITOR FORMULATION FOR USE IN IMPLANTABLE INFUSION DEVICES - A formulation for use in an implantable infusion device includes between about 5 mg/ml and about 500 mg/ml (e.g., about 10-25 mg/ml) of a TNF inhibitor polypeptide, 10 mM-25 mM of a phosphate or citrate buffer, has an ionic strength of the combined buffer and an optional salt of the equivalent of about 0.1-0.2 NaCl (e.g., about 0.15 M), 5% to 10% of a carbohydrate (e.g., trehalose or sucrose), has a pH of between 6 and 7, is fluid at room temperature and at 37° C., and has a viscosity of less than about 10 centipoise (e.g., between about 1 centipoise and 9 centipoise, between about 1 cp and about 5 cp, between about 1 cp and about 3 cp, or between about 1 cp and about 2.5 cp) at room temperature. | 2012-04-12 |
20120088714 | SYSTEM FOR STORAGE AND SUBSEQUENT HANDLING OF BOTULINUM TOXIN - A system and method for storage of botulinum toxin containing pharmaceutical compositions is herein disclosed. Particular aspects of the instant disclosure relate to vials having preferred internal geometries that provide optimized lyophilization, vacuum drying, storage, reconstitution and extraction of a botulinum toxin-containing pharmaceutical composition. | 2012-04-12 |
20120088715 | MUTATED ANTITHROMBINS, A PROCESS FOR PREPARING THE SAME AND THEIR USE AS DRUGS - The present invention relates to the use of a composition including of at least a mutated antithrombin
| 2012-04-12 |
20120088716 | Polypeptide Protracting Tags - Method for increasing half-life of compounds in plasma and novel derivatives of such compounds. | 2012-04-12 |
20120088717 | METHOD FOR TREATING FUNGAL INFECTION WITH ANTIFUNGAL BIFUNCTIONAL MOLECULES - The present invention is directed to a method of treating a fungal infection with a fusion peptide that includes a fungal targeting agent and a channel-forming domain consisting essentially of amino acids 451-626 of colicin Ia. The fungal targeting agent can be a pheromone, such as an alpha-mating pheromone. The fusion peptides of the peptides of the present invention are particularly useful for the treatment of fungal infections in a wide variety of organisms. The fusion peptides can be prepared from the nucleic acids, such as when a vector having the nucleic acid is included in a host cell. | 2012-04-12 |
20120088718 | HCV-DERIVED POLYPEPTIDES AND USES THEREOF - The present invention relates to Hepatitis C virus (HCV)-derived polypeptides and nucleic acid molecules encoding same which advantageously comprises a cd81-binding region. In this connection, the present invention specifically relates to the use of the polypeptides or nucleic acid molecules in compositions and methods for the prevention, the treatment and the diagnosis of HCV infections. | 2012-04-12 |
20120088719 | Mosquitocidal Xenorhabdus, Lipopeptide And Methods - Provided is a bacterial strain which produces a family of mosquitocidal toxins, | 2012-04-12 |
20120088720 | INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES - Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals. | 2012-04-12 |
20120088721 | Cartilage Repair - This invention relates to compositions, methods of preparation thereof, and use thereof for cartilage repair. | 2012-04-12 |
20120088722 | COMPOSITIONS AND METHODS FOR INHIBITION OF MMP:MMP-SUBSTRATE INTERACTIONS - The present invention provides compounds for disrupting the binding of a matrix metalloprotease (MMP) protein to a substrate protein at an interaction site other than the protease catalytic site. In particular the inventive compounds inhibit the MMP's ability to cleave a substrate protein. In some cases the compound may prevent activation of transforming growth factor beta (TGFβ). The compounds are preferably polypeptide fragments of the hemopexin-like domain of the MMP, but may be mimetics thereof or peptides or mimetics of the portion of the MMP substrate protein to which the MMP interacts. | 2012-04-12 |
20120088723 | SELECTIVE EP4 RECEPTOR AGONISTIC SUBSTANCE FOR TREATMENT OF CANCER - This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents. | 2012-04-12 |
20120088724 | Human Growth Hormone Formulations - Formulations containing complexed human growth hormone crystals are described. Also described are needleless injection systems for crystalline proteins. | 2012-04-12 |
20120088725 | 5-CNAC AS ORAL DELIVERY AGENT FOR PARATHYROID HORMONE FRAGMENTS - Pharmaceutical compositions for the effective oral delivery of a parathyroid hormone, PTH, as well as methods for administration of the compositions are provided. Additionally, methods for stimulating new bone formation and treating and/or preventing osteoporosis are also provided. | 2012-04-12 |
20120088726 | MUCOADHESIVE XYLOGLUCAN-CONTAINING FORMULATIONS USEFUL IN MEDICAL DEVICES AND IN PHARMACEUTICAL FROMULATIONS - Object of the invention are mucoadhesive and controlled release formulations consisting of aqueous solutions containing 0.05% to 5% by weight of a natural purified polymer having xyloglucan structure and 10% to 70% by weight of glycerol. These formulations are suitable for the application on human mucous membranes, such as nasal, oral and vaginal mucous membranes, as moisturizing and softening agents or as pharmaceutical release system. Further objects of the invention are pharmaceutical formulations and medical devices suitable for the application to human mucous membranes, containing the mucoadhesive and controlled release formulations together with active ingredients and excipients. | 2012-04-12 |
20120088727 | RSPONDINS AS MODULATORS OF ANGIOGENESIS AND VASCULOGENESIS - The present invention relates to the use of Rspondins, particularly Rspondin2 (Rspo2) or Rspondin3 (Rspo3) or Rspondin nucleic acids, or regulators or effectors or modulators of Rspondin e.g. Rspo2 and/or Rspo3 to promote or inhibit angiogenesis and/or vasculogenesis, respectively. The invention is based on the demonstration that Rspo3 and Rspo2 are angiogenesis promoters, and the identification of Rspo2 and 3 as positive regulators of vascular endothelial growth factor (VEGF). These results indicate a major role for Rspondins, particularly Rspo3 and/or Rspo2 in the signalling system during angiogenesis. The invention also relates to the use regulators or effectors or modulators of Rspondin3, including agonists and antagonists, in the treatment of conditions where treatment involves inhibiting or promoting angiogenesis and/or vasculogenesis. | 2012-04-12 |
20120088728 | USE OF C1 INHIBITOR FOR THE PREVENTION OF ISCHEMIA-REPERFUSION INJURY - The present invention relates to the therapeutic and prophylactic use of C1 inhibitor for preventing, reducing and treating ischemia and reperfusion injury. The C1 inhibitor of the present invention is still therapeutically effective when administered after an ischemic period and reperfusion and therefore particularly useful for unforeseen occurrences of ischemic reperfusion such as e.g. a stroke. | 2012-04-12 |
20120088729 | NON-GLYCOSYLATED TRANSFERRIN EXPRESSED IN MONOCOTS - Disclosed are compositions and methods of making non-glycosylated transferrin protein in transgenic monocot plants. | 2012-04-12 |
20120088730 | USE OF ANGIOTENSIN CONVERTING ENZYME (ACE) DOMAIN SPECIFIC INHIBITORS TO INHIBIT OR ENHANCE CYTOKINE PRODUCTION AND ALTER IMMUNE RESPONSE - The present invention relates to the discovery that the two ACE domains can have very different effects on cytokine expression. In one embodiment, the present invention provides a method of regulating and/or treating a condition in a subject by administering a therapeutically effective dosage of site specific ACE inhibitor. In another embodiment, the condition is inflammation and/or immune response. | 2012-04-12 |
20120088731 | METHOD FOR TREATING PARKINSON'S DISEASE THROUGH REGULATING VDAC1 PROTEIN - The present invention provides a method for curing Parkinson's disease through regulating VDAC1 (voltage-dependent anion channel 1) protein. Specifically, the present invention provides a pharmaceutical composition for curing PD comprising a VDAC1 protein regulator. The VDAC1 protein regulators comprise an inhibitor of VDAC1 mRNA production, an inhibitor of mitochondrial permeability transition pore (mPTP) formation, and a mitochondrial calcium uptake inhibitor. In addition, the present invention provides a method for curing Parkinson's disease comprising administering a VDAC1 protein regulator to a subject with Parkinson's disease. The present invention could provide a method for curing Parkinson's disease through preventing and/or restoring mitochondrial dysfunction. | 2012-04-12 |
20120088732 | THERAPEUTIC COMPOSITION COMPRISING A BOTULINUM NEUROTOXIN - A pharmaceutical preparation comprising one of the botulinum neurotoxins from | 2012-04-12 |
20120088733 | NOVEL USE OF ANTIMICROBIAL PEPTIDES IN REGENERATION OF SKIN CELLS - Disclosed are novel antimicrobial peptides which can promote the regeneration of skin cells, thus healing wounds. Pharmaceutical compositions comprising the peptides as active ingredients are also provided for wound healing and skin rejuvenation. | 2012-04-12 |
20120088734 | Cyclosporin Analogs - Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions. | 2012-04-12 |
20120088735 | One-Step Processing of Hydrogels for Mechanically Robust and Chemically Desired Features - The application of a highly controlled, micron-sized, branched, porous architecture to enhance the handling properties and degradation rate of hydrogels is described in the instant invention. A previously described pattern created through one-step nucleated crystallization in a hydrogel film creates tunable mechanical properties and/or chemical stability for use in tissue engineering applications. The bulk mechanical properties and the degradation rate of the material can be tuned easily by the addition or subtraction of crystalline structure or by the addition and subtraction of backfill material, making this useful for a variety of applications. Relevant mechanical properties that can be tuned through the application of this unique porosity are moduli, elasticity, tensile strength, and compression strength. The method of the present invention can be applied to biopolymers and natural materials as well as synthetic materials. | 2012-04-12 |
20120088736 | [4-(6-HALO-7-Substituted-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]- -5-CHLORO-THIOPHEN-2-YL-SULFONYLUREAS and Forms and Methods Related Thereto - The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof. | 2012-04-12 |
20120088737 | NOVEL ACYL GUANIDINE DERIVATIVES - The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na | 2012-04-12 |
20120088738 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z | 2012-04-12 |
20120088739 | METHOD FOR TREATING MEIBOMIAN GLAND DISEASE - A method for treating a patient having meibomian gland disease, ocular irritation associated with delayed tear clearance, or recurrent corneal epithelial erosion, is disclosed. Preferably, the method concerns treatment of a patient with topical tetracycline, a derivative or analogue of tetracycline, or a chemically modified tetracycline (CMT). Oral administration of a CMT is also disclosed as part of the method for treating meibomian gland disease, ocular irritation associated with delayed tear clearance, or recurrent corneal epithelial erosion. | 2012-04-12 |
20120088740 | CO-CRYSTALS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of salicylic acid, 4-amino salicylic acid, and oxalic acid. Also within the scope of this invention are methods of making and using the same. | 2012-04-12 |
20120088741 | ARYL-SUBSTITUTED HETEROCYCLIC UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE - Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). | 2012-04-12 |
20120088742 | ACETYLSALICYLIC ACID SALTS - Novel betaine salts of acetylsalicylic acid, namely 4-trimethylammoniobutanoate acetylsalicylic acid addition salt (gamma-butyrobetaine acetylsalicylate), L-carnitine acetylsalicylic acid addition salt and 3-(trimethylammonioamino)propanoate (meldonium) acetylsalicylic acid addition salt. Use of meldonium acetylsalicylate as antiplatelet agent for treating various pathologies induced by platelet aggregation, anti-inflammatory and antihyperlipidemic agent. | 2012-04-12 |
20120088743 | COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS - Combinations comprising (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniablcyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases. | 2012-04-12 |
20120088744 | COMPOSITIONS FOR TREATING CMT AND RELATED DISORDERS - The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders. | 2012-04-12 |
20120088745 | CHEMICALLY MODIFIED SMALL MOLECULES - Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material. | 2012-04-12 |
20120088746 | AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 2012-04-12 |
20120088747 | SULFONAMIDE CONTAINING COMPOUNDS AND USES THEREOF - Compounds, compositions and methods for treating GHS-R mediated disorders are described herein. | 2012-04-12 |
20120088748 | HETEROCYCLIC COMPOUNDS - Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) | 2012-04-12 |
20120088749 | S1P Receptor Modulating Compounds and Use Thereof - The present invention relates to amides that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions. | 2012-04-12 |
20120088750 | ANTIBACTERIAL COMPOUNDS - The present invention provides a compound of the following formula and salts thereof: | 2012-04-12 |
20120088751 | PHARMACEUTICAL COMPOUNDS - Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: | 2012-04-12 |
20120088752 | HEDGEHOG PATHWAY ANTAGONISTS AND THERAPEUTIC APPLICATIONS THEREOF - Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications. | 2012-04-12 |
20120088753 | PYRROLOPYRIMIDINES AND USED AS KINASE INHIBITORS - The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R | 2012-04-12 |
20120088754 | SULFONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 2012-04-12 |
20120088755 | Novel Compounds - The present invention relates to the new compounds of general formula I | 2012-04-12 |
20120088756 | Methods for Regulating Neurotransmitter Systems by Inducing Counteradaptations - The present invention relates to methods for regulating neurotransmitter systems by inducing a counteradaptation response. According to one embodiment of the invention, a method for regulating a neurotransmitter includes the step of repeatedly administering a ligand for a receptor in the neurotransmitter system, with a ratio of administration half-life to period between administrations of no greater than ½. The methods of the present invention may be used to address a whole host of undesirable mental and neurological conditions. | 2012-04-12 |
20120088757 | NOVEL 1,4-BENZODIAZEPINE-2,5-DIONES WITH THERAPEUTIC PROPERTIES - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like. | 2012-04-12 |
20120088758 | FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS - The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): | 2012-04-12 |
20120088759 | THIAZOLIDIN-4-ONE AND [1,3]-THIAZINAN-4-ONE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS - The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R | 2012-04-12 |
20120088760 | GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Disclosed are new compounds of formula (1) exhibiting excellent activity for glucokinase, pharmaceutical compositions having the same as an active ingredient, and a method of using the same as an active ingredient for lowering blood glucose level: | 2012-04-12 |
20120088761 | AMINOACYL PRODRUG DERIVATIVES AND MEDICAMENTS FOR THE TREATMENT OF THROMBOEMBOLITIC DISORDERS - The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. | 2012-04-12 |
20120088762 | COMPOUNDS FOR ENZYME INHIBITION - One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention. | 2012-04-12 |
20120088763 | TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE - Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R | 2012-04-12 |
20120088764 | PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY - The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase. | 2012-04-12 |
20120088765 | PURINE DERIVATIVE AND ANTITUMOR AGENT USING SAME - Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof. | 2012-04-12 |
20120088766 | FUSED HETEROCYCLIC COMPOUNDS AND THEIR USES - The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof. | 2012-04-12 |
20120088767 | BENZIMIDAZOLE DERIVATIVES AS PI3 KINASE INHIBITORS - This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kβ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer. | 2012-04-12 |
20120088768 | PINANE-SUBSTITUTED PYRIMIDINEDIAMINE DERIVATIVES USEFUL AS AXL INHIBITORS - Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed. | 2012-04-12 |
20120088769 | SALTS OF ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are arylsulfonamide salts, e.g., a salt of a compound of Formula I, which are useful for modulating CCR3 activity, and their pharmaceutical compositions. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 2012-04-12 |
20120088770 | ALPHA HELIX MIMETICS AND METHODS RELATING THERETO - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | 2012-04-12 |
20120088771 | TISSUE-NONSPECIFIC ALKALINE PHOSPHATASE (TNAP): A THERAPEUTIC TARGET FOR ARTERIAL CALCIFICATION - This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity. | 2012-04-12 |
20120088772 | NOVEL PHARMACEUTICAL COMPOSITION FOR PREVENTION AND/OR TREATMENT OF ATTENTION DEFICIT/HYPERACTIVITY DISORDER - The present invention is to provide a therapeutic agent for attention deficit/hyperactivity disorder having a novel mechanism of action which is different from conventional psychostimulants. The present invention is useful for providing an excellent pharmaceutical composition for prevention and/or treatment of attention deficit/hyperactivity disorder, comprising a BEC1 potassium channel inhibitor or a pharmaceutically acceptable salt thereof as an active ingredient, and is particularly useful for providing a pharmaceutical composition for prevention and/or treatment of inattention, impulsivity, and hyperactivity in attention deficit/hyperactivity disorder. | 2012-04-12 |
20120088773 | Circadian rhythm modulation - A method and composition is herein described to modulate the circadian rhythm to effect summer metabolism and the metabolic syndrome. The method entails the once daily, timed ingestion of a dopamine precursor or a dopamine agonist, receptor primed with caffeine, and vitamin D | 2012-04-12 |
20120088774 | ACTIVE PHARMACEUTICAL INGREDIENT ADSORBED ON SOLID SUPPORT - The present invention belongs to the field of pharmaceutical industry and relates to dosage forms comprising active pharmaceutical ingredients (API) such as tadalafil, simvastatin, fenofibrate and lovastatin that are practically insoluble in water, adsorbed on a carrier. Furthermore it relates to an adsorbate comprising API being practically insoluble in water and to a process for the preparation of said adsorbate with non-polar solvent (s) such as chlorinated hydrocarbon, diisopropylethes and hexane. Furthermore the invention relates to a process for the preparation of the dosage form, as well as to the use of the adsorbate for the preparation of the dosage form. Moreover it relates to the dosage form for use in the treatment of erectile dysfunction, human immunodeficiency virus (HIV) infections and/or Acquired Immune Deficiency Syndrome (AIDS). | 2012-04-12 |
20120088775 | Pyrazolo-[1,5-a]-Pyrimidones Derivatives and Pharmaceutical Compositions and Uses Thereof - The present invention provides new pyrazolo-[1,5- | 2012-04-12 |
20120088776 | TREATMENT OF MAMMALIAN DISORDERS MEDIATED BY ALPHA-ANHYDRASE ISOFORMS - The present invention pertains to 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pharmaceutically acceptable salt thereof, or 4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl] benzamide or a pharmaceutically acceptable salt thereof, for the treatment of disorders mediated by alpha-carbonic anhydrase isoforms selected from intraocular hypertension (glaucoma), epilepsy, Lennox-Gastaut syndrome, altitude sickness, headaches, neurological disorders and obesity. | 2012-04-12 |
20120088777 | 5-HT1A RECEPTOR SUBTYPE AGONIST - The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT | 2012-04-12 |
20120088778 | AZOLE DERIVATIVES AND FUSED BICYCLIC AZOLE DERIVATIVES AS THERAPEUTIC AGENTS - This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis. | 2012-04-12 |
20120088779 | HETEROCYCLIC SULFONAMIDES - Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 2012-04-12 |
20120088780 | SUBSTITUTED [1,2,4]TRIAZOLO[1,5-a]PYRIMIDINES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 2012-04-12 |
20120088781 | Famciclovir for the Treatment of Recurrent genital Herpes Labialis with a one day application - A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day. | 2012-04-12 |
20120088782 | LPA RECEPTOR ANTAGONIST - A compound of the general formula (I): | 2012-04-12 |
20120088783 | CHROMAN DERIVATIVES - The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I | 2012-04-12 |
20120088784 | Substituted Aromatic Compounds and Pharmaceutical Uses thereof - The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders. | 2012-04-12 |
20120088785 | NEW USES FOR QUATERNARY AMMONIUM ANTICHOLINERGIC MUSCARINIC RECEPTOR ANTAGONISTS IN PATIENTS BEING TREATED FOR COGNITIVE IMPAIRMENT OR ACUTE DELIRIUM - A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and/or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence. Further, the combination of rivastigmine and glycopyrrolate has been effective in significantly improving cognitive function in patients suffering from acute dementia or cognitive impairment. | 2012-04-12 |
20120088786 | IMMEDIATE RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING OXYCODONE AND NALOXONE - The present invention pertains to oral immediate release pharmaceutical compositions suitable for treating patients suffering from pain comprising oxycodone and naloxone or their pharmaceutically acceptable salts. | 2012-04-12 |
20120088788 | SUBSTITUTED IMIDAZOLES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS - Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes. | 2012-04-12 |
20120088789 | CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 2012-04-12 |
20120088790 | PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to phenalkylamine derivatives of the formula (I) or (II) | 2012-04-12 |
20120088791 | AMIDOBIPIPERIDINECARBOXYLATE M1 ALLOSTERIC AGONISTS, ANALOGS AND DERIVATIVES THEREOF, AND METHODS OF MAKING AND USING SAME - In one aspect, the invention relates to compounds having a general structure: Formula (I) which are useful as allosteric agonists of the M | 2012-04-12 |
20120088792 | Pyridin-2-YL Methylamine Derivatives for Treating Opiate Dependence - The invention concerns the use of compounds of general formula (I) | 2012-04-12 |
20120088793 | Bicyclic Compounds and Methods of Making and Using Same - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same. | 2012-04-12 |
20120088795 | FACTOR XA INHIBITORS - The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 2012-04-12 |
20120088796 | COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND USE THEREOF - The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals. | 2012-04-12 |
20120088797 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 2012-04-12 |
20120088798 | Intramolecular Hydrogen-Bonded Nitric Oxide Synthase Inhibitors - Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases. | 2012-04-12 |
20120088799 | SEROTONIN REUPTAKE INHIBITORS - In one aspect, the invention relates to compounds of formula I: | 2012-04-12 |
20120088800 | 2-(SUBSTITUTED) (ARYLMETHYL, ARYLOXY and ARYLTHIO))-N-(SUBSTITUTED PYRIDIN-2-YL)-2-(SUBSTITUTED ARYL) COMPOUNDS AS SUBTYPE-SELECTIVE MODULATORS OF SPHINGOSINE-1-PHOSPHATE-3 (S1P3) RECEPTORS - The invention provides compounds represented by the formula (I), each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: wherein: A, m, n, p, a, X, Y and Z are defined in the specification. These compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis and pulmonary edema. | 2012-04-12 |
20120088801 | Pirfenidone Therapy and Inducers of Cytochrome P450 - The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking. | 2012-04-12 |
20120088802 | TRICYCLIC COMPOUNDS, COMPOSITIONS AND METHODS - The present invention is directed to compounds of Formula I: | 2012-04-12 |
20120088803 | CONTROL AGENT FOR SOFT ROT AND CONTROL METHOD FOR THE SAME - Provided is a novel control agent for soft rot and a novel control method for the same. The control agent for soft rot of a plant contains 3-chloro-N-(3-chloro-5-trifluoromethyl-2-pyridyl)-alpha,alpha,alpha-trifluoro-2,6-dinitro-p-toluidine as an active ingredient, which is applied to plant cultivation soil. | 2012-04-12 |
20120088804 | CLEVIDIPINE EMULSION FORMULATIONS CONTAINING ANTIMICROBIAL AGENTS - Pharmaceutical formulations comprising clevidipine and an antimicrobial agent exhibit a reduced propensity for microbial growth and provide increased convenience to health care workers administering clevidipine-containing formulations to patients. | 2012-04-12 |
20120088805 | COMPOUND HAVING DETRUSOR MUSCLE-CONTRACTING ACTIVITY AND URETHRAL SPHINCTER MUSCLE-RELAXING ACTIVITY - Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder. | 2012-04-12 |