52nd week of 2011 patent applcation highlights part 49 |
Patent application number | Title | Published |
20110319384 | Pharmaceutical Compositions - The present invention provides methods of treatment with a pharmaceutical composition, more particularly a sustained release pharmaceutical composition, comprising 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo-[b,f][1,4]thiazepine or a pharmaceutically acceptable salt thereof, as well as new and improved methods for treating a variety of psychological disorders and conditions including, but not limited to, Mood Disorders and Anxiety Disorders and for treating one or more of the symptoms of these disorders. | 2011-12-29 |
20110319385 | QUINOXALINE COMPOUND | 2011-12-29 |
20110319386 | NEUROGENESIS BY MUSCARINIC RECEPTOR MODULATION - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells. | 2011-12-29 |
20110319387 | INDOLE DERIVATIVES FOR TREATING NEURODEGENERATIVE DISEASES - The invention relates to a compound of the following formula (I), | 2011-12-29 |
20110319388 | METHODS OF PREPARING PHARMACEUTICAL COMPOSITIONS COMPRISING ESLICARBAZEPINE ACETATE AND METHODS OF USE - The present disclosure relates to the treatment of various diseases and conditions with eslicarbazepine acetate. The present disclosure also relates to the use of eslicarbazepine acetate in a method for reducing or decreasing epileptic seizures in a patient. The present disclosure also relates to a method for increasing the exposure to eslicarbazepine in a patient. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate. | 2011-12-29 |
20110319389 | METHODS AND COMPOSITIONS FOR TREATING FATIGUE ASSOCIATED WITH DISORDERED SLEEP USING VERY LOW DOSE CYCLOBENZAPRINE - The present invention relates to methods for the treatment or prevention of fatigue associated with disordered sleep, for example, in multiple sclerosis, fibromyalgia, Fabry's disease, Parkinson's disease, or traumatic brain injury, using cyclobenzaprine The present invention further relates to a biomarker for the therapeutic effects of a cyclobenzaprine treatment. | 2011-12-29 |
20110319390 | 6-Aminoisoquinoline Compounds - 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided. | 2011-12-29 |
20110319391 | METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION - The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells. | 2011-12-29 |
20110319392 | Thiazole Sulfonamide And Oxazole Sulfonamide Kinase Inhibitors - The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 2011-12-29 |
20110319393 | ANTHELMINTIC AGENTS AND THEIR USE - This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments. | 2011-12-29 |
20110319394 | FUSED HETEROCYCLIC COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): | 2011-12-29 |
20110319395 | Pharmaceutical Formulation of Olanzapine - A pharmaceutical formulation comprising a homogeneous mixture of (a) olanzapine or a pharmaceutically acceptable salt thereof as an active ingredient, (b) a monosaccharide and/or oligosaccharide, (c) a polysaccharide and, optionally, further ingredients. | 2011-12-29 |
20110319396 | BENZODIAZEPIN-2-ON DERIVATIVES - The present invention relates to a compound represented by the formula (I): wherein R | 2011-12-29 |
20110319397 | NOVEL N-OXIDES OF FURANYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel N-oxides of certain furanyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 2011-12-29 |
20110319398 | INHIBITION OF YOPS TRANSLOCATION - The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof. | 2011-12-29 |
20110319399 | EXTERNAL PREPARATION CONTAINING ANALGESIC/ANTI-INFLAMMATORY AGENT - An external preparation containing the following components (A) and (B):
| 2011-12-29 |
20110319400 | PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN - Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: | 2011-12-29 |
20110319401 | FIVE CRYSTAL FORMS, METHODS OF PREPARATION, PHARMACEUTICAL COMPOSITIONS AND APPLICATIONS OF XLF-III-43 - This invention discloses that the five crystal forms of XLF-III-43 can be used as crude drugs. The invention also relates to the preparation methods of the five crystal forms of XLF-III-43 as crude drugs, to the applications of the sterling of the five crystal forms of XLF-III-43 and mixed crystals in different proportions as medicinally active components to develop various kinds of medicines and compound medicines. In addition, this invention also relates to applying the crystal samples of XLF-III-43 as crude drugs to treat kidney dysfunction, cardiocerebral vessel diseases, hypertension, type II diabetic mellitus, complications of hypertension and diabetic mellitus, tumor, precancerosis, edema, and achieves therapeutic effects by enhancing blood drug levels resulted from effects of crystal forms in the processes of treating all kinds of diseases. | 2011-12-29 |
20110319402 | AEROSOL FORMULATION FOR THE INHALATION OF BETA AGONISTS - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula (1) wherein the groups R | 2011-12-29 |
20110319403 | BICYCLIC COMPOUNDS AS INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE - The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I). | 2011-12-29 |
20110319404 | METHOD FOR TREATING NON-HODKIN'S LYMPHOMA - The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof. | 2011-12-29 |
20110319405 | Treatment and prevention of diffuse parenchymal lung disease by selective active-site mTOR inhibitors - Embodiments are related to new uses for selective active-site mTOR inhibitors in treating or preventing pulmonary fibrosis in diffuse parenchymal lung disease (DPLD) patients, such as a DPLD of environmental cause, a collagen vascular disease (e.g., scleroderma and rheumatoid arthritis), an idiopathic interstitial pneumonia (e.g., idiopathic pulmonary fibrosis and nonspecific interstitial pneumonia), and sarcoidosis. | 2011-12-29 |
20110319406 | 2-PYRIDYL SUBSTITUTED IMIDAZOLES AS THERAPEUTIC ALK5 AND/OR ALK4 INHIBITORS - This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors. | 2011-12-29 |
20110319407 | INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USE THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 2011-12-29 |
20110319408 | Methods of Treating Fibrosis, Cancer and Vascular Injuries - This invention relates to use of inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4) in treating, preventing, or reducing fibrosis, cancer, and vascular injuries. | 2011-12-29 |
20110319409 | 7-AZA-QUINAZOLINE PDE10 INHIBITORS - The present invention is directed to 7-aza-quinazoline compounds of general structural formula I | 2011-12-29 |
20110319410 | PYRAZINE DERIVATIVES AND USE AS PI3K INHIBITORS - The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries. | 2011-12-29 |
20110319411 | ISOINDOLINONE AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2011-12-29 |
20110319412 | PIPERIDINE AND PYRROLIDINE DERIVATIVES HAVING NPY Y5 RECEPTOR ANTAGONISM - The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: | 2011-12-29 |
20110319413 | PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE - This invention relates to a piperazine compound represented by Formula (I), | 2011-12-29 |
20110319414 | NOVEL TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a novel P2X | 2011-12-29 |
20110319415 | Susceptibility to HSP90-Inhibitors - The present invention relates to a method of selecting (a) cell(s), (a) tissue(s) or (a) cell culture(s) with susceptibility to an HSP90 inhibitor. Also a method for determining the responsiveness of a mammalian tumor cell or cancer cell to treatment with an HSP90 inhibitor is described herein. In particular, the present invention provides for an in vitro method for the identification of a responder for or a patient sensitive to an HSP90 inhibitor and uses of an oligo- or polynucleotide capable of detecting (an) activating mutation(s) in the KRAS gene are provided. The present invention also relates to a method of monitoring the efficacy of a treatment of a cancer characterized by the presence of at least one activating mutation in the KRAS gene, and. optionally, in the EGFR gene and/or the BRAF gene. In addition, a method of predicting the efficacy of a cancer treatment is described, in particular in a cancer that is characterized by the presence of at least one activating mutation in the KRAS gene. and. optionally, in the EGFR gene and/or the BRAF gene. Also the use of a (transgenic) non-human animal or a (transgenic) cell having at least one activating mutation in the KRAS gene, and, optionally, in the EGFR gene and/or the BRAF gene for screening and/or validation of a medicament for the treatment of said cancer is described and a kit useful for carrying out the methods described herein is provided. | 2011-12-29 |
20110319416 | Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions - Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed. | 2011-12-29 |
20110319417 | METHODS AND COMPOSITIONS FOR TREATING ANXIETY - Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described. | 2011-12-29 |
20110319418 | PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN - Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: | 2011-12-29 |
20110319419 | Methotrexate Adjuvants to Reduce Toxicity and Methods for Using the Same - Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2′-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions. | 2011-12-29 |
20110319420 | PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR - The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR. | 2011-12-29 |
20110319421 | BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The invention relates to compounds of the formula R | 2011-12-29 |
20110319422 | PRODRUGS OF NH-ACIDIC COMPOUNDS: ESTER, CARBONATE, CARBAMATE AND PHOSPHONATE DERIVATIVES - The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment. | 2011-12-29 |
20110319423 | NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME - The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction. | 2011-12-29 |
20110319424 | NAPHTHYRIDIN-2(1H) -ONE COMPOUNDS USEFUL AS ANTIBACTERIALS - Compounds of Formula (I), | 2011-12-29 |
20110319425 | HETEROTRICYCLIC COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X | 2011-12-29 |
20110319426 | Substituted Isoindoles - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 2011-12-29 |
20110319427 | USE OF 5AHQ AND BORTEZOMIB FOR THE TREATMENT OF HEMATOLOGICAL DISEASES - The disclosure provides methods and compositions for treating hematological malignancies. In particular, the disclosure provides methods and compositions for treating leukemia, lymphoma and multiple myeloma using bortezomit and 5AHQ (5-ammo-8-hydroxyqumolme) and related compounds that bind non-competitively to an alpha unit of 2OS proteasome and inhibit proteasome activity Kits and commercial packages are also disclosed | 2011-12-29 |
20110319428 | THIAZOLE DERIVATIVES AS PESTICIDES - The present application relates to novel heterocyclic compounds, to their use for controlling animal pests including arthropods and in particular insects, and to processes for preparing the novel compounds. | 2011-12-29 |
20110319429 | SUBSTITUTED 1,1,3,1-TETRAOXIDOBENZO[D][1,3,2]DITHIAZOLES AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION - Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and methods of using the compounds. | 2011-12-29 |
20110319430 | FUNGICIDAL PYRAZOLES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2011-12-29 |
20110319431 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 2011-12-29 |
20110319432 | Fungicidal compositions comprising Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine - Fungicidal compositions comprising as active components Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine in a synergistically effective amount, methods for controlling phytopathogenic harmful fungi using mixtures of Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine, the use of Fluopyram and 5-Ethyl-6-octyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-ylamine for preparing such mixtures, and also compositions and seed comprising such mixtures. | 2011-12-29 |
20110319433 | FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREATMENT OF INFLAMMATION - Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists. | 2011-12-29 |
20110319434 | Bicyclic Heterocyclic Derivatives and Methods of Use Thereof - The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. | 2011-12-29 |
20110319435 | FUNGICIDE MIXTURES - The invention relates to a method for combating fungi and spores and suitable means therefor, and to the use thereof. | 2011-12-29 |
20110319436 | Methods and Compositions for Modulating IRE1, SRC, and ABL Activity - Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl. | 2011-12-29 |
20110319437 | IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition. | 2011-12-29 |
20110319438 | NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I) | 2011-12-29 |
20110319439 | AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - MCHR1 antagonists are provided having the following Formula I: | 2011-12-29 |
20110319440 | Process for Preparing Spirocyclic Cyclohexane Compounds, Compositions Containing Such Compounds and Method of Using Such Compounds - Spirocyclic cyclohexane compounds corresponding to formula I | 2011-12-29 |
20110319441 | MANUFACTURE OF VARIABLE DENSITY DOSAGE FORMS UTILIZING RADIOFREQUENCY ENERGY - The present invention features the present invention features a tablet including at least one pharmaceutically active ingredient, wherein the shape of said tablet includes at least one major face wherein: (i) the peak penetration resistance at the perimeter of said major face of the tablet is at least about 10% greater than the peak penetration resistance at the center of said major face; and (ii) the tablet disintegrates in the mouth when placed on the tongue in less than about 30 seconds, and a machine and method for manufacture of such tablet. | 2011-12-29 |
20110319442 | PHARMACEUTICAL COMPOSITIONS COMPRISING IMIDAZOQUINOLIN(AMINES) AND DERIVATIVES THEREOF SUITABLE FOR LOCAL ADMINISTRATION - The present invention relates in general to the field of modulators of the innate immune system, particularly to pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof, preferably suitable for local administration, such as, intravesical administration. In addition, the present invention concerns the use of imidazoquinolin(amines) and derivatives thereof for intravesical treatment of bladder diseases, such as, for example, bladder cancer and cystitis. The present invention furthermore comprises methods of treatment for these diseases as well as methods of administration of the inventive pharmaceutical compositions. | 2011-12-29 |
20110319443 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 2011-12-29 |
20110319444 | QUINUCLIDINE CARBONATE SALTS AND MEDICINAL COMPOSITION THEREOF - Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases. | 2011-12-29 |
20110319445 | HETEROARYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases. | 2011-12-29 |
20110319446 | BICYCLO[2.2.1]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES - Compounds of formula (I) have muscarinic M3 receptor modulating activity; | 2011-12-29 |
20110319447 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 2011-12-29 |
20110319448 | GUANIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula I: | 2011-12-29 |
20110319449 | PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - MCHR1 antagonists are provided having the following Formula I: | 2011-12-29 |
20110319450 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 2011-12-29 |
20110319451 | 5-Ht6 Receptor and Modulators Thereof for the Treatment of Insulin-Related Disorders - The present invention relates to a method for identifying a glycemic stabilizing compound, by: a) contacting a candidate compound with a 5-HT | 2011-12-29 |
20110319452 | CYANO ANTHRANILAMIDE INSECTICIDES - This invention provides compounds of Formula 1, N-oxides and suitable salts thereof | 2011-12-29 |
20110319453 | Methods of Administering Pirfenidone Therapy - The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes. | 2011-12-29 |
20110319454 | DERIVATIVES OF CYCLOALKYL- AND CYCLOALKENYL-1,2-DICARBOXYLIC ACID COMPOUNDS HAVING FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) AGONIST OR ANTAGONIST ACTIVITY - The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders. | 2011-12-29 |
20110319455 | Antifungal Treatment - A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole. | 2011-12-29 |
20110319456 | BENZOARYLUREIDO COMPOUNDS, AND COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEGENERATIVE BRAIN DISEASE CONTAINING THE SAME - Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like. | 2011-12-29 |
20110319457 | DEFERACIROX DISPERSIBLE TABLETS - The invention pertains to dispersible tablets comprising as active ingredient 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or pharmaceutically acceptable salt thereof in an amount of from 5 to 40% in weight by weight of the total tablet. | 2011-12-29 |
20110319458 | COMPOUND WITH AGITATION EFFECT ON PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR. PROCESS FOR ITS PREPARATION AND USE THEREOF - The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype δ (PPARδ), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPARδ thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate. | 2011-12-29 |
20110319459 | Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System - Disclosed are compounds of the general formula (I): | 2011-12-29 |
20110319460 | KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 2011-12-29 |
20110319461 | NOVEL SALTS, POLYMORPHS, AND SYNTHETIC PROCESSES REGARDING IMIDAZOLE DERIVATIVE - The present invention relates to a process for producing 2-[1-(S)-carboxy-2(S)-[3-(3,5-dichloro-benzyl)-3H-imidazol-4-yl]-ethylamino]-4-methyl-pentanoic acid, as well as novel salts, including hydrates and solvates thereof, and novel crystalline and amorphous forms thereof. | 2011-12-29 |
20110319462 | Use of Dithiine-tetracarboximides for Controlling Phytopathogenic Fungi - The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides. | 2011-12-29 |
20110319463 | PREVENTIVE OR THERAPEUTIC AGENTS FOR OPTIC NERVE DISORDERS COMPRISING 4,6-DICHLORO-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF AS ACTIVE INGREDIENTS - A method for preventing or treating an optic nerve disorder, inhibiting retinal nerve cell death or recovering a neurofilament light chain expression level by administering to a patient a pharmacologically effective amount of at least one of the compound represented by the following formula (1): | 2011-12-29 |
20110319464 | METHODS FOR TREATING BENIGN PROSTATIC HYPERPLASIA - Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof. | 2011-12-29 |
20110319465 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR | 2011-12-29 |
20110319466 | Method and composition for treating heart failure - A method and composition for treating, preventing or ameliorating heart failure, cardiac hypertrophy, and/or myocardial dysfunction includes administering a therapeutically effective amount of a HDAC inhibitor, such as phenylbutyrate, in combination with an ACE inhibitor, such as captopril. | 2011-12-29 |
20110319467 | Absorption Enhancement of Statins and Omega Fatty Acids - A composition and method to enhance absorption and bioavailability of Statin and Omega fatty acids consumed by humans and in an anhydrous base is presented. | 2011-12-29 |
20110319468 | CYCLIC AMINE COMPOUNDS - Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof | 2011-12-29 |
20110319469 | SNPs of Apolipoprotein B and Modulation of Their Expression - Compounds, compositions and methods are provided for modulating the expression of apolipoprotein B. The compositions comprise oligonucleotides, targeted to nucleic acid encoding apolipoprotein B. Methods of using these compounds for modulation of apolipoprotein B expression and for diagnosis and treatment of diseases and conditions associated with expression of apolipoprotein B are provided. | 2011-12-29 |
20110319470 | Diagnosis, prognosis and identification of potential therapeutic targets of multiple myeloma based on gene expression profiling - Provided herein is a method for gene expression profiling multiple myeloma patients into distinct subgroups via DNA hybridization and hierarchical clustering analysis of the hybridization data where the results may further be used to identify therapeutic gene targets. Also provided is a method for controlling bone loss in an individual via pharmacological inhibitors of DKK1 protein. In addition provided herein is a method for diagnosing multiple myeloma using a 15-gene model that classifies myeloma into subtypes 1-7. | 2011-12-29 |
20110319471 | LNA ANTAGONISTS TARGETING THE ANDROGEN RECEPTOR - The invention relates to oligonucleotide compounds (oligomers), which target androgen receptor mRNA in a cell, leading to reduced expression of the androgen receptor. Reduction of the androgen receptor expression is beneficial for the treatment of certain disorders, such as a hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of androgen receptor using said oligomers, including methods of treatment. | 2011-12-29 |
20110319472 | METHODS OF PROGNOSTICATING AND TREATING EWING SARCOMA/PNET AND OTHER NEOPLASMS - A method of distinguishing between Ewing sarcoma patients having a good prognosis relative to those having a poor prognosis by screening for specific genomic copy number alterations (CNA) isolated and/or measuring denticleless homolog (Drosophila) (DTL) protein levels from the tumors of patients diagnosed with Ewing Sarcoma. | 2011-12-29 |
20110319473 | COMPOSITIONS AND METHODS FOR ENHANCEMENT OF NUCLEIC ACID DELIVERY - Embodiments of the invention include devices and methods for delivery of nucleic acids as active agents. Embodiments of the invention include devices and methods for delivery of nucleic acids as active agents. In an embodiment, an article for delivering an active agent is included. The article can include a dehydrated complex including a nucleic acid, a transfection agent, and a saccharide protectant. The nucleic acid and transfection agent can form a liposome or a lipoplex. The dehydrated complex can be disposed within a polymeric matrix. The dehydrated complex can be disposed within a microparticle. Other embodiments are also included herein. | 2011-12-29 |
20110319474 | siRNA targeting cyclin-dependent kinase 4 (CDK4) - Efficient sequence specific gene silencing for cyclin-dependent kinase 4 is possible through the use of siRNA technology. By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed. | 2011-12-29 |
20110319475 | TREATMENT OF BRAIN DERIVED NEUROTROPHIC FACTOR (BDNF) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO BDNF - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Brain derived neurotrophic factor (BDNF), in particular, by targeting natural antisense polynucleotides of Brain derived neurotrophic factor (BDNF). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of BDNF. | 2011-12-29 |
20110319476 | TREATMENT OF GLIAL CELL DERIVED NEUROTROPHIC FACTOR (GDNF) RELATED DISEASES BY INHIBITION OF NATURAL ANTISENSE TRANSCRIPT TO GDNF - The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Glial cell derived neurotrophic factor (GDNF), in particular, by targeting natural antisense polynucleotides of Glial cell derived neurotrophic factor (GDNF). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of GDNF. | 2011-12-29 |
20110319477 | MUTATIONS OF THE PIK3CA GENE IN HUMAN CANCERS - Phosphatidylinositol 3-kinases (PI3Ks) are known to be important regulators of signaling pathways. To determine whether PI3Ks are genetically altered in cancers, we analyzed the sequences of the PI3K gene family and discovered that one family member, PIK3CA, is frequently mutated in cancers of the colon and other organs. The majority of mutations clustered near two positions within the PI3K helical or kinase domains. PIK3CA represents one of the most highly mutated oncogenes yet identified in human cancers and is useful as a diagnostic and therapeutic target. | 2011-12-29 |
20110319478 | Compositions to Treat Cardiac Pacing Conditions - The HCN polynucleotide includes a nucleotide sequence encoding an HCN polypeptide having channel activity. The amino acid sequence of the HCN polypeptide and the amino acid sequence of a reference polypeptide have at least 80% identity, where the reference polypeptide begins with an amino acid selected from amino acids 92-214 and ends with an amino acid selected from amino acids 723-1188 of SEQ ID NO:8. An example of a reference polypeptide is amino acids 214-723 of SEQ ID NO:8. The HCN polynucleotide may be DNA or RNA. The HCN polynucleotide may be present in a vector, such as a viral vector (including, for instance, a single strand adeno-associated virus or a self complementary adeno-associated virus), a transposon vector, or a plasmid vector. | 2011-12-29 |
20110319479 | POLYPEPTIDES AND POLYNUCLEOTIDES ENCODING SAME AND USE THEREOF IN THE TREATMENT OF MEDICAL CONDITIONS ASSOCIATED WITH ISCHEMIA - An isolated polynucleotide is disclosed comprising a nucleic acid sequence encoding a polypeptide having an amino acid sequence of HIF-1 alpha, the polypeptide being stably expressed and constitutively active. Isolated polypeptides encoded by same are also disclosed and uses thereof. | 2011-12-29 |
20110319480 | Method of Inducing and/or Enhancing an Immune Response to Tumor Antigens - An improved method of inducing and/or enhancing an immune response to a tumor antigen is disclosed. The method involves administering the tumor antigen. nucleic acid coding therefor, vectors and/or cells comprising said nucleic acid or vaccines comprising the aforementioned to a lymphatic site. | 2011-12-29 |
20110319481 | SCHWEINFURTHIN ANALOGUES - Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs. | 2011-12-29 |
20110319482 | NOVEL TREATMENTS - The present invention relates to the treatment of the premonitory symptoms of migraine, to the treatment of aura associated with or without migraine, epilepsy, non-epileptic seizures, stroke or other cardiovascular disorders, to the pre-emptive treatment of aura, migraine, epilepsy, stroke or other cardiovascular disorders, to the treatment of migraine recurrence or aura recurrence, and to tonabersat, co-crystals thereof, and compositions comprising tonabersat for use in said treatments. | 2011-12-29 |
20110319483 | 1-ADAMANTYL CHALCONES FOR THE TREATMENT OF PROLIFERATIVE DISORDERS - The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], | 2011-12-29 |