16th week of 2010 patent applcation highlights part 12 |
Patent application number | Title | Published |
20100099657 | Diphenylazetidinone Derivatives Possessing Cholesterol Absorption Inhibitory Activity - Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described. | 2010-04-22 |
20100099658 | DI(ARYLAMINO)ARYL COMPOUND - The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. | 2010-04-22 |
20100099659 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: | 2010-04-22 |
20100099660 | METHOD FOR TREATING THROMBOSIS OR EMBOLISM AND RELATED DISEASES - A method for treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing is provided. The method includes administration of an effective amount of a compound represented by formula (1): | 2010-04-22 |
20100099661 | ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS - Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): | 2010-04-22 |
20100099662 | HYDRAZONE DERIVATIVE - A hydrazone derivative of formula [I]: | 2010-04-22 |
20100099663 | 4-TRIFLUOROMETHOXYPHENOXYBENZOL-4'-SULFONIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF IN MEDICAMENTS - The present invention is directed to a compound of formula I, | 2010-04-22 |
20100099664 | SUBSTITUTED PYRROLIDINE AMIDES, THE PRODUCTION THEREOF, AND THE USE THEREOF AS MEDICATIONS - The object of the present invention is novel substituted pyrrolidine amides of the general formula (I) in which D, L. E, G, J, M, L | 2010-04-22 |
20100099665 | ISOQUINOLINONE DERIVATIVES - The present invention relates to isoquinolinone derivatives of formula (I): | 2010-04-22 |
20100099666 | PHENOTHIAZINE MODULATORS OF H1 RECEPTOR AND D2 RECEPTOR - The present invention relates to new phenothiazine modulators of H1 receptors and/or D2 receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-04-22 |
20100099667 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 2010-04-22 |
20100099668 | LOCAL TOPICAL ADMINISTRATION FORMULATIONS CONTAINING INDOXACARB - The present invention provides formulations and methods useful in the control of ectoparasites on a domestic animal, using a formulation comprising Indoxacarb and a veterinarily acceptable carrier that is applied topically to 10% or less of the total surface area of a domestic animal. Other embodiments include these formulations also including one or more additional pesticides such as fipronil. | 2010-04-22 |
20100099669 | Dopamine 3 receptor agonist and antagonist treatment of gastrointestinal motility disorders - Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. | 2010-04-22 |
20100099670 | Benzoquinazoline derivatives - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: | 2010-04-22 |
20100099671 | GLUCOKINASE ACTIVATOR - A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), | 2010-04-22 |
20100099672 | METHODS FOR TREATING HEPATITIS C - In accordance with the present invention, compounds that can inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment or prevention of a viral infection are provided. In another aspect of the invention, compounds useful in the treatment or prevention of HCV infection are provided. | 2010-04-22 |
20100099673 | DECAHYDROQUINOLINE ANALOGS AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES - The present invention relates to compounds represented by Formula (I): and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases. | 2010-04-22 |
20100099674 | METHOD AND MEANS FOR PREVENTING AND INHIBITING TYPE III SECRETION IN INFECTIONS CAUSED BY GRAM-NEGATIVE BACTERIA - A means for decreasing bacterial virulence in a mammal including man or in a plant by inhibition of the Type III secretion system at concentrations that do not prevent or substantially reduce bacterial growth comprises an N-substituted 7-quinolylmethyl amine, in particular one that is further substituted in 5- and 8-position on the quinoline ring. A corresponding therapeutic method and a pharmaceutical composition are also disclosed. | 2010-04-22 |
20100099675 | NOVEL PYRROLE DERIVATIVE HAVING UREIDO GROUP AND AMINOCARBONYL GROUP AS SUBSTITUENTS - Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R | 2010-04-22 |
20100099676 | SULFONYLUREA DERIVATIVE CAPABLE OF SELECTIVELY INHIBITING MMP-13 - A compound represented by the general formula (I): | 2010-04-22 |
20100099677 | Compounds, Compositions and Methods Comprising Thiazole Derivatives - The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2010-04-22 |
20100099678 | DIALKYLAMINO ALKYL ESTERS OF PIVAGABINE AS MEDICAMENTS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine. | 2010-04-22 |
20100099679 | FUSED BICYCLIC mTOR INHIBITORS - Compounds represented by Formula (I) | 2010-04-22 |
20100099680 | PTERIDINONE DERIVATIVES AS P13-KINASES INHIBITORS - New compounds of Formula (1) are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney. | 2010-04-22 |
20100099681 | SUBSTITUTED 5-AMINOPYRAZOLES AND USE THEREOF - The present application relates to novel substituted 5-aminopyrazoles, methods of production thereof, use thereof alone or in combinations for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases. | 2010-04-22 |
20100099682 | ACETYLENE DERIVATIVES - The invention provides compounds of formula (I) | 2010-04-22 |
20100099683 | COMPOUNDS THAT INHIBIT HUMAN DNA LIGASES AND METHODS OF TREATING CANCER - Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases. | 2010-04-22 |
20100099684 | Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 2010-04-22 |
20100099685 | 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. | 2010-04-22 |
20100099686 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 2010-04-22 |
20100099687 | TADALAFIL SOLID COMPOSITES - This invention relates to oral pharmaceutical compositions suitable for making pharmaceutical formulations for oral administration that provide for the rapid dissolution of the phosphodiesterase 5 inhibitor tadalafil. In particular, the pharmaceutical compositions comprise solid composites of tadalafil exhibiting high solubility and rate of dissolution. The invention further relates to methods of preparing these pharmaceutical formulations and the use of such pharmaceutical formulations for treating diseases associated with PDE5 inhibitors. | 2010-04-22 |
20100099688 | NOVEL PHOSPHODIESTERASE INHIBITORS - The present invention relates to a compound according to formula I, | 2010-04-22 |
20100099689 | METHODS OF MODULATING PPAR GAMMA-TYPE RECEPTORS - Novel compounds having the general formula (I) below: | 2010-04-22 |
20100099690 | XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS - The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial. | 2010-04-22 |
20100099691 | PYRIMIDINYL PYRIDONE INHIBITORS OF JNK - This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, | 2010-04-22 |
20100099692 | HARMFUL ORGANISM CONTROL COMPOSITION - This invention provides a harmful organism control composition having an excellent harmful organism control effect and comprising as an effective ingredient the following 4-(2-butynyloxy)-5-fluoro-6-(3,5-dimethylpiperidino)-pyrimidine (X): | 2010-04-22 |
20100099693 | NEW COMBINATION FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS - There is provided combination products comprising (a) ramatroban, or a pharmaceutically-acceptable salt or solvate thereof and (b) a statin, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in the treatment of atherosclerosis and related conditions. | 2010-04-22 |
20100099694 | 2-ANILINO-4-HETEROARYL PYRIMIDINE DERIVATIVES, AND PREPARATION THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS, AND IN PARTICULAR IKK INHIBITORS - The disclosure relates to a compound of formula (I): | 2010-04-22 |
20100099695 | HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. | 2010-04-22 |
20100099696 | Tamper resistant oral dosage forms containing an embolizing agent - Oral dosage form containing a therapeutically effective amount of a drug susceptible to abuse and an effective amount of an embolizing agent which causes the production of a solid or semi-solid embolus or blockage after tampering. | 2010-04-22 |
20100099697 | Method of Treatment Using Inhibitors of Mitosis - Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose. | 2010-04-22 |
20100099698 | Compositions for Improving Skin Conditions Comprising Matrine or Its Oxidized Derivatives - The present invention relates to a composition for improving skin conditions comprising matrine and oxymatrine as an active ingredient. Matrine and oxymatrine have lower cytotoxicity than retinol used as anti-wrinkle agents and exhibit the inhibition effect on collagenase activity and promotion effect on collagen biosynthesis at a molecular level, contributing to excellent efficacy in improvement of skin wrinkles. In addition, both matrine and oxymatrine exhibit the inhibition effect on melanin production by inhibiting intracellular tyrosinase activity, the improving effects of UV-induced skin damage and the skin growth promotion or hair loss prevention. Therefore, matrine and oxymatrine have the excellent improvement effects on skin conditions. Furthermore, matrine and oxymatrine have the excellent anti-obesity and anti-oxidation effects. The composition of this invention can be applied to cosmetic, pharmaceutical and food composition having no cytotoxicities and side effects. | 2010-04-22 |
20100099700 | HYDROGENATED PYRIDO (4,3-B) INDOLES FOR TREATING AMYOTROPHIC LATERAL SCLEROSIS (ALS) - The invention provides methods for treating and/or preventing and/or slowing the onset and/or development of ALS using hydrogenated pyrido(4,3-b)indoles, such as dimebon. | 2010-04-22 |
20100099701 | ISOQUINOLINONE MODULATORS OF 5-HT3 RECEPTORS - The present invention relates to new isoquinolinone modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-04-22 |
20100099702 | Therapeutic agent for neuropathic pain - Disclosed is a therapeutic agent for neuropathic pain having an excellent therapeutic effect on neuropathic pain which is a intractable disease. More specifically, disclosed are a therapeutic agent for neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist (particularly PK 11195) as the active ingredient; a pharmaceutical composition for the treatment of neuropathic pain which comprises a peripheral benzodiazepine receptor antagonist as the active ingredient; a method for the treatment of neuropathic pain using a peripheral benzodiazepine receptor antagonist; and others. | 2010-04-22 |
20100099703 | PHENYLAMINO-SUBSTITUTED PIPERIDINE COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to phenylamino-substituted piperidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals. | 2010-04-22 |
20100099704 | Lotion Preparation Containing Pyridonecarboxylic Acid Derivative - It is intended to provide a lotion preparation which exerts an excellent antibacterial effect, is excellent in the stability of active ingredient and does not contain an additive having a safety problem. The lotion preparation contains (a) 1-cyclo-propyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and/or a pharmaceutically acceptable salt thereof, (b) a lower alcohol, (c) a water-soluble polymer and (d) a polyhydric alcohol and the pH of the preparation is in the range of 9 to 12. | 2010-04-22 |
20100099705 | ARGATROBAN FORMULATION - An aqueous, stable, sterile pharmaceutical composition of the thrombin inhibitor argatroban in a solution containing an acid to solubilize the argatroban, substantially free from dehydrated alcohol is described, as well as a method for its preparation. | 2010-04-22 |
20100099706 | ARGATROBAN FORMULATION - An aqueous, stable, sterile pharmaceutical composition of the thrombin inhibitor argatroban in a solution containing an acid to solubilize the argatroban, substantially free from dehydrated alcohol is described, as well as a method for its preparation. | 2010-04-22 |
20100099707 | METHOD FOR TREATING PULMONARY ARTERIAL HYPERTENSION - Pulmonary arterial hypertension in a mammal can be prevented or treated using combined 5-HT2A and 5-HT2B receptor antagonist. The antagonists can be present in a single compound or in two separate compounds | 2010-04-22 |
20100099708 | Piperidine Derivative Used for Treating Chemokine Receptor 5 Mediated Diseases - The present invention relates to 4-[3-(1,1-difluoroethyl)-5-methyl-4H-1,2,4-triazol-4-yl]-1-{(1R,3R)-3-(3,5-difluorophenyl)-1-methyl-3-[1-(methylsulfonyl)ρiperidin-4-yl]propyl}piperidine formula (I): or a pharmaceutically acceptable salt thereof, as well as processes for the preparation of this compound and its use in the treatment of CCR5 disease states. | 2010-04-22 |
20100099709 | PYRIDIN-2-YL-METHYLAMINE DERIVATIVES FOR TREATING OPIATE DEPENDENCE - The invention concerns the use pf compounds of general formula (I) | 2010-04-22 |
20100099710 | SRC FAMILY KINASE INHIBITORS - The invention relates to compounds of general formula (I) wherein X, A, R | 2010-04-22 |
20100099711 | Methods and Compositions Using Immunomodulatory Compounds for The Treatment and Management of Cancers and Other Diseases - Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed. | 2010-04-22 |
20100099712 | SUBSTITUTED PYRAZOLINE COMPOUNDS WITH ACAT INHIBITION ACTIVITY - The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia. | 2010-04-22 |
20100099713 | 2-AMINOPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS - Provided are compounds having the Formula I | 2010-04-22 |
20100099714 | AMPA and NMDA Receptor Antagonists for Neurodegenerative Diseases - The invention provides methods for treating, preventing, and delaying the onset of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Pick's disease, and the like), dementia, mild cognitive impairments, glaucoma, ocular hypertension, and pain (e.g., neuropathic pain, headaches, and the like) by administering therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists to patents in need thereof. The invention also provides combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists. Exemplary AMPA receptor antagonists include 1,2-dihydropyridine compounds, such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. Exemplary NMDA receptor antagonists include adamantane compounds, such as memantine. | 2010-04-22 |
20100099715 | 1,4-DISUBSTITUTED 3-CYANO-PYRIDONE DERIVATIVES AND THEIR USE AS POSITIVE MGLUR2-RECEPTOR MODULATORS - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. | 2010-04-22 |
20100099716 | CETP INHIBITORS - Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: | 2010-04-22 |
20100099717 | SUSPENSION CONCENTRATES FOR IMPROVING THE ROOT ABSORPTION OF AGROCHEMICAL ACTIVE INGREDIENTS - It is possible to increase the uptake of active compounds from crop protection compositions using suitable adjuvants, and thus to improve the action of crop protection agents. The present invention describes suitable adjuvants, methods and compositions. | 2010-04-22 |
20100099718 | PYRIDINE DERIVATIVE SUBSTITUTED BY HETEROARYL RING, AND ANTIFUNGAL AGENT COMPRISING THE SAME - The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: | 2010-04-22 |
20100099719 | COMPOSITION AND METHOD FOR TREATING PROTEINURIA - The present invention discloses 5-methyl-1-(substituted phenyl)-2(1H)-pyridones having the ability to reduce proteinuria and for treating kidney diseases. The ability to reduce proteinuria has a renoprotective effect for slowing the progression of kidney diseases. A representative example of 5-methyl-(1-substituted phenyl)-2(1H)-pyridones is 1-(3′-fluorophenyl)-5-methyl-2(1H)-pyridone, AKF-PD. Accordingly, the present invention provides compositions comprising one or more compounds selected from the group consisting of 5-methyl-1-(substituted phenyl)-2(1H)-pyridones and methods of using the same to treat proteinuria and kidney diseases. | 2010-04-22 |
20100099720 | Gene Polymorphisms as Sex-Specific Predictors in Cancer Therapy - The invention provides compositions and methods for determining the likelihood of gender-specific successful treatment with 5-FU/oxaliplatin or an equivalent of each thereof. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy. | 2010-04-22 |
20100099721 | NOVEL COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS - Inhibitors of prolyl endopeptidase of formula 1 | 2010-04-22 |
20100099722 | 2-(BENZIMIDAZOL-1-YL)-N-(4-PHENYLTHIAZOL-2-YL) ACETAMIDE DERIVATIVES - The invention relates 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives having the general Formula I | 2010-04-22 |
20100099723 | BIOAVAILABLE COMPOSITIONS OF METAXALONE AND PROCESSES FOR PRODUCING THE SAME - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 2010-04-22 |
20100099724 | Formulations Comprising Triazoles and Alkoxylated Amines - The present invention relates to the use of alkoxylated amines to enhance the activity of fungicidal formulations comprising fungicidal triazoles. It also relates to formulations comprising one or more fungicidal triazoles and alkoxylated amines. These formulations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, biodegradable material and textiles against deterioration due to the action of fungi. | 2010-04-22 |
20100099725 | PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATORS - The present invention is directed to compounds of the structural Formula: wherein: R | 2010-04-22 |
20100099726 | INHIBITORS OF PYRUVATE KINASE AND METHODS OF TREATING DISEASE - The invention provides pharmaceutical compositions, kits, and methods of treating cancer, diabetes, obesity, autoimmune disease, and benign prostatic hyperplasia using compounds that selectively inhibit pyruvate kinase M2 and an assay measuring chemical modulation of pyruvate kinase activity. | 2010-04-22 |
20100099727 | Amino acid and peptide conjugates of arylalkylic acids for cosmetic use - The invention provides novel compounds of general formula I | 2010-04-22 |
20100099728 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. | 2010-04-22 |
20100099729 | NITRIC OXIDE DONOR COMPOUNDS - The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metobolismsdysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one 15 therapeutic agent. | 2010-04-22 |
20100099730 | ANNELLATED PYRROLE COMPOUNDS FOR CANCER MANAGEMENT - The present invention relates to the use of annellated pyrrole compounds and in particular ML3000 (licofelone), salts or derivatives thereof, for cancer management, and in general to the use of a compound of Formula (I): wherein the variables have the meanings given in the present description, for the prevention and/or treatment of neoplasia, in particular neoplasia selected from the group consisting of papilloma, carcinoma, adenoma and adenocarcinoma, e.g. human airway or colorectal carcinoma, preferably fast-growing, multidrug resistant and/or COX-2 negative neoplasia. The invention further relates to pharmaceutical compositions for the aforesaid purposes, comprising annellated pyrrole compounds and in particular ML3000 (licofelone), optical isomers, salts or derivatives thereof, as well as to a method of treating and/or preventing neoplasia and/or restoring the ability to undergo apoptosis in a cell having lost the same. This treatment ameliorates, diminishes, actively treats, reverses or prevents any disease related to insufficient apoptosis, in particular neoplasia, and it may be combined with irradiation, heating and treatment with a cytotoxic agent for preventive and/or curative purposes. | 2010-04-22 |
20100099731 | Use of Endothelial Interrupters in the Treatment of Neurodegenerative Diseases - In various embodiments, the present invention relates generally to methods of treating at least one neurodegenerative disease by administering a medicament comprising an endothelial interrupter. | 2010-04-22 |
20100099732 | MEDICAMENTS USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to pharmaceutical compositions comprising phenylcarbamoyl-methyl-indole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. | 2010-04-22 |
20100099733 | Method for obtaining a stable dispersion of benzoyl peroxide - Powder containing benzoyl peroxide is readily wetted by contacting the powder with a liquid containing one or more of a polyol, a polyol ether, and a low-carbon organic alcohol. | 2010-04-22 |
20100099734 | AMINO ACID AND ITS USES - This invention relates to a supplement, the use thereof and method for supplementing the concentration of free cellular L-proline in an organism, for restricting dehydration of such an organism, the supplement comprising an effective amount of free L-proline. The supplement is effective in reducing the levels of free radicals in organisms experiencing water stress. This invention further relates to a method of treating dehydration in humans and animals including the step of administering to an individual in need thereof an effective amount of a supplement according to the third aspect of the invention. An effective amount of free L-proline is typically between 20 and 1000 mg, preferably 100 mg free L-proline per kilogram body mass of the organism, three times a day. | 2010-04-22 |
20100099735 | METHODS AND COMPOSITIONS FOR IMPROVING COGNITIVE FUNCTION - This invention relates to treating age-related cognitive impairment. This invention in particular relates to the use of inhibitors of synaptic vesicle protein 2A (SV2A), such as levetiracetam, seletracetam, and brivaracetam, in improving cognitive function in subjects that exhibit age-related cognitive impairment or are at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-related Cognitive Decline (ARCD) or Age-Associated Memory Impairment (AAMI). | 2010-04-22 |
20100099736 | PHENYL SUBSTITUTED MALEIMIDES AS MEDICAMENTS FOR BLOCKING DEGENERATIVE TISSUE DAMAGES BY INHIBITING MPT - The invention discloses the use of a compound of formula (I), wherein R | 2010-04-22 |
20100099737 | COMPOSITIONS AND METHODS FOR TREATING MYELOSUPPRESSION - The invention provides, in part, compositions and methods for protecting a hemopoietic cell, or for treating myelosuppression, in a subject in need thereof, by administering an effective amount of an inhibitor of a SH2-containing inositol-5′-phosphatase. | 2010-04-22 |
20100099738 | POLYETHYLENE GLYCOL LIPID CONJUGATES AND USES THEREOF - Polyethylene glycol (PEG)-lipid conjugates, polyethylene glycol (PEG)-lipid conjugate based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed. | 2010-04-22 |
20100099739 | Compositions and Methods for Gene Silencing - Compositions and methods for modulating the expression of a protein of interest are provided. | 2010-04-22 |
20100099740 | METHODS AND COMPOSITIONS FOR RNAI MEDIATED INHIBITION OF GENE EXPRESSION IN MAMMALS - Methods and compositions are provided for modulating, e.g., reducing, expression of a target sequence in mammals and mammalian cells in vivo. In the subject methods, an effective amount of an RNAi agent, e.g., an interfering ribonucleic acid (such as an siRNA or shRNA) is introduced into a target cell, e.g., by being administered to a mammal that includes the target cell, e.g., via intravascular injection. Also provided are RNAi agent pharmaceutical preparations for use in the subject methods. The subject methods and compositions find use in a variety of different applications, including academic and therapeutic applications. | 2010-04-22 |
20100099741 | Molecular Targets for Treatment of Learning and Memory Dysfunction - Described herein are methods for identification of alternative safe molecular targets and novel regulators in complex molecular networks using a novel fault diagnosis engineering approach. For example, in this invention we claim new molecular targets that could be effectively targeted for changing the activity of CREB, and therefore for treatment of learning and memory related disorders. Learning and memory dysfunction is a major clinical manifestation of a number of human disorders, such as Alzheimer Disease (AD), schizophrenia, dementias, autism, etc. More specifically, we claim that composition and compounds that can target the activity of L AND/OR P/Q-, N-type calcium channels, Gαi, Gβγ, PP2A and CaMKII and IV are effective therapeutics for the treatment of disorders manifested by learning and memory dysfunction. | 2010-04-22 |
20100099742 | Sensitizing Cells for Apoptosis by Selectively Blocking Cytokines - The invention refers to the use of a cytokine antagonist which modulates the expression and/or the function of a cytokine, particularly a Th2 helper cell cytokine, in a cell and causes the down-regulation of anti-apoptotic proteins in said cell through the cytokine modulation for sensitizing cells for apoptosis. In particular, the cells that can be treated with the cytokine antagonists are drug-resistant cancer cells which fail to undergo apoptosis. | 2010-04-22 |
20100099743 | RNA INTERFERENCE MEDIATED INHIBITION OF CHECKPOINT KINASE-1 (CHK-1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating checkpoint kinase (e.g., checkpoint kinase-1 or CHK-1) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of checkpoint kinase gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of checkpoint kinase genes. | 2010-04-22 |
20100099744 | RNA INTERFERENCE MEDIATED INHIBITION OF MATRIX METALLOPROTEINASE 13 (MMP13) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - This invention relates to compounds, compositions, and methods useful for modulating matrix metalloproteinase (e.g., MMP13) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of MMP13 gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of MMP13 genes. | 2010-04-22 |
20100099745 | ENHANCING DISEASE RESISTANCE AGAINST RNA VIRAL INFECTIONS WITH INTRACYTOPLASMIC PATHOGEN SENSORS - The present disclosure provides compositions and methods for enhancing resistance to viral infections. The compositions include adenovirus vectors containing nucleic acid molecules encoding CARD domains from RIG-I and MDA5, recombinant adenoviruses and immunogenic compositions comprising such recombinant adenovirus vectors and adenoviruses. Methods for enhancing resistance to viral infections involving administering such adenovirus vectors or recombinant adenovirus are also provided. | 2010-04-22 |
20100099746 | NOVEL NUCLEIC ACID - The present invention provides a nucleic acid such as a micro-RNA or a micro-RNA precursor, having a novel sequence. The nucleic acid of the present invention is useful for detecting the expression or a mutation of a micro-RNA, separating cells, suppressing the expression of a gene having a target sequence, screening for a substance that promotes or suppresses a function of a micro-RNA, and diagnosing or treating a disease caused by a mast cell abnormality, a disease caused by an abnormality of mesenchymal stem cell proliferation or differentiation, cancers, and a disease caused by abnormal proliferation of cells, tissue hyperplasia or the like. | 2010-04-22 |
20100099747 | REDUCTION OF POLYALANINE-INDUCED PROTEIN AGGREGATES AND TOXICITY BY UBIQUILIN - A method for decreasing cell death in a cell exhibiting aggregation of polyalanine-containing proteins. The method includes introduction of an expression vector to a host cell comprising a nucleotide sequence encoding ubiquilin, followed by maintaining the transformed host cell under biological conditions sufficient for expression and accumulation of the ubiquilin in the host cell, wherein overexpression of ubiquilin reduces sensitivity of cell stress induced by expanded polyalanine proteins. | 2010-04-22 |
20100099748 | MICRORNA MOLECULES | 2010-04-22 |
20100099749 | Nucleic Acid Inhibitors Of Glutamate Receptors - The present invention relates to novel nucleic acid ligands or aptamers that bind to and inhibit the activation of the α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) subtype of ionotropic glutamate receptors. Also disclosed is a novel combination of technologies, i.e., SELEX and laser pulse photolysis for the selection and screening of aptamers that inhibit receptor function and are useful therefore, in the treatment of diseases associated with excessive activation of ionotropic glutamate receptors. | 2010-04-22 |
20100099750 | RNA INTERFERENCE MEDIATED INHIBITION OF MUSCARINIC COLINERGIC RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - The present invention relates to compounds, compositions, and methods useful for modulating the expression of genes associated with respiratory and pulmonary disease, such as cholinergic muscarinic receptor genes, using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of cholinergic muscarinic receptor genes, or other genes involved in pathways of cholinergic muscarinic receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3). | 2010-04-22 |
20100099751 | Method of treating diabetes-related vascular complications - A method of treating diabetes-related vascular complications is provided. It has been found that a heightened state of oxidative stress, either acting alone or in concert with augmented apoptotic and inflammatory processes, contributes to diabetes-related vascular dysfunction. The method of treating diabetes-related vascular complications includes the treatment of diabetic patients with alpha-lipoic acid (LA) in order to mitigate the negative impact of diabetes-related vascular dysfunctions upon vascular homeostasis. The treatment method includes the step of administering to the patient a therapeutically effective dosage of alpha-lipoic acid. | 2010-04-22 |
20100099752 | PHARMACEUTICAL COMPOSITION CONTAINING BICYCLIC TYPE COMPOUNDS - The present invention relates to pharmaceutical compositions containing bicyclic type compounds and to methods of using same, for example, in the treatment or prevention of anxiety, mania, depression, disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse, Parkinson's Disease, psychosis, migraine and/or cerebral ischaemia. | 2010-04-22 |
20100099753 | Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivates and their uses - The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R | 2010-04-22 |
20100099754 | 5,6-DIMETHYL XANTHONE-4-ACETIC ACID DERIVATIVES AND METHOD OF PREPARING THE SAME - A method of preparation of 5,6-dimethylxanthone-4-acetic acid (DMXAA) and derivatives thereof. The derivatives are represented by formula (I), wherein R represents totally 1 to 2 substitutes at 1, 2, 3, 7, and 8 position selected from a lower alkyl, halogen, CF | 2010-04-22 |
20100099755 | CHEMOTHERAPEUTIC FLAVONOIDS, AND SYNTHESES THEREOF - Substituted flavonoid compounds, and pharmaceutical formulations of flavonoid compounds are described. Also described are processes for preparing flavonid compounds, as are methods for treating cancer in mammals using the described flavonoid compounds or pharmaceutical formulations thereof. | 2010-04-22 |
20100099756 | USES OF INCENSOLE, INCENSOLE ACETATE AND DERIVATIVES THEREOF - The described subject matter relates to the use of incensole, incensole acetate, and derivatives thereof, for the treatment, prevention or amelioration of diseases or conditions, including inflammatory-associated conditions; a disease or condition where neuroprotection is required; and a disease or condition selected from depression, anxiety, obsessive compulsive behaviors, deterioration in cognitive function, and deterioration in neurobehavioral function. Pharmaceutical compositions and method of treatment, prevention or amelioration of the above-mentioned diseases or conditions are also provided. | 2010-04-22 |
20100099757 | DISULFIRAM DOSES AND TREATMENT REGIMEN SUITABLE FOR TREATMENT OF ANGIOGENESIS-DEPENDENT DISORDERS - A pharmaceutical composition is provided. The pharmaceutical composition includes an amount of disulfuram in unit dosage form which results in a peak serum concentration level which is therapeutically effective in treating an angiogenesis-dependent disorder and can also exhibit minimal or no disulfuram related side effects. | 2010-04-22 |