43rd week of 2011 patent applcation highlights part 49 |
Patent application number | Title | Published |
20110263561 | Novel pyrrolidone derivatives for use as MetAP-2 inhibitors - Compounds of the formula (I), in which R, X, Y, Z, R | 2011-10-27 |
20110263562 | BICYCLIC COMPOUND - The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. | 2011-10-27 |
20110263563 | Ansamycin Hydroquinone Compositions - Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use. | 2011-10-27 |
20110263564 | PYRIDINE, BICYCLIC PYRIDINE 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. | 2011-10-27 |
20110263565 | COMPOUNDS - The present invention encompasses compounds of general formula (1), wherein R | 2011-10-27 |
20110263566 | 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives and PBK Inhibitors Containing the Same - 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided. | 2011-10-27 |
20110263567 | COMPOUNDS FOR INHIBITING SEMICARBAZIDE-SENSITIVE AMINE OXIDASE (SSAO) / VASCULAR ADHESION PROTEIN-1 (VAP-1) AND USES THEREOF FOR TREATMENT AND PREVENTION OF DISEASES - The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases. | 2011-10-27 |
20110263568 | TOPICAL PHARMACEUTICAL COMPOSITION COMPRISING A CHOLINERGIC AGENT OR A CALCIUM CHANNEL BLOCKER - A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers. | 2011-10-27 |
20110263569 | RYANODINE CHANNEL BINDERS AND USES THEREOF - Increasing the affinity of calstabin-2 for the cardiac calcium channel RyR2 and thereby stabilizing the channel in the closed state has recently been identified as novel mechanism for treating heart failure, particularly ventricular arrhythmias. JTV-519, a 1,4-benzothiazepine derivative, has been shown to stabilize the calstabin2/RyR2 complex. Novel derivatives of JTV-519 that may be useful in treatment or prevention of heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmias are provided. Synthetic methodology and intermediates in the synthesis of the inventive JTV-519 derivatives are also described. | 2011-10-27 |
20110263570 | PYRIMIDINE DERIVATIVES AS GPCR MODULATORS FOR USE IN THE TREATMENT OF OBESITY AND DIABETES - The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. | 2011-10-27 |
20110263571 | NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE - Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) | 2011-10-27 |
20110263572 | 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5-RECEPTOR ANTAGONISTS - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 2011-10-27 |
20110263573 | HETEROBIARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I | 2011-10-27 |
20110263574 | PIRENZEPINE AS OTOPROTECTIVE AGENT - The present invention generally relates to the otoprotective activity of condensed diazepinones, e.g. condensed benzodiazepines such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as medicaments for the prevention and/or treatment of otic diseases, e.g. diseases associated with loss of hearing. | 2011-10-27 |
20110263575 | 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. | 2011-10-27 |
20110263576 | PHARMACEUTICAL COMPOSITION CONTAINING BENZODIAZEPINE AND/OR BENZODIAZEPINE DERIVATIVES - The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon. | 2011-10-27 |
20110263577 | NOVEL OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 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. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2011-10-27 |
20110263578 | HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES - The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I | 2011-10-27 |
20110263579 | CHLOROTHIAZIDE, CHLOROTHIAZIDE SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to an improved process for the preparation of Chlorothiazide and pharmaceutically acceptable salts thereof. The present invention relates to novel polymorphs of Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium. The present invention further relates to pharmaceutical compositions comprising Chlorothiazide and Chlorothiazide salts, in particular Chlorothiazide sodium and process for preparation thereof. | 2011-10-27 |
20110263580 | METHOD FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS - This invention relates to a method for treating or preventing diseases associated with the deposition of β-amyloid peptide in the brain, such as Alzheimer's disease, said method involving administration of a gamma-secretase inhibitor in an intermittent dosing regime to a patient in need thereof. | 2011-10-27 |
20110263581 | FUSED TRICYCLIC COMPOUNDS AS SERINE-THREONINE PROTEIN KINASE AND PARP MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules. | 2011-10-27 |
20110263582 | CYCLIC UREA INHIBITORS OF 11 B-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell. | 2011-10-27 |
20110263583 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula Il Ik, Im | 2011-10-27 |
20110263584 | Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula I, Ik, Iq | 2011-10-27 |
20110263585 | Screening Assay for Insecticides - The present invention relates to polypeptides, preferably from | 2011-10-27 |
20110263586 | PEST CONTROLLING COMPOSITION AND METHOD OF CONTROLLING PEST - A pest controlling composition comprising tolclofos-methyl and a neonicotinoid compound represented by the formula (1) as active ingredients. | 2011-10-27 |
20110263587 | REVERSIBLY HEAT-GELABLE AQUEOUS COMPOSITION - The present invention relates to a reversibly heat-gelable aqueous composition comprising a reversibly heat-gelable aqueous composition according to conventional technique, to which a thixotropic property-increasing substance is added. The thixotropic property-increasing substance is preferably at least one member selected from the group consisting of sugar alcohol, lactose, carmellose or pharmaceutically acceptable salts thereof and cyclodextrin. This composition can be stored at room temperature and accordingly, it is quite convenient for users to carry about the same. | 2011-10-27 |
20110263588 | TRICYCLIC COMPOUNDS AS GLUTAMATE RECEPTOR MODULATORS - The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same. | 2011-10-27 |
20110263589 | Method for preventing or treating a glucocorticoid receptor-related disease - A method of preventing or treating a glucocorticoid receptor-related disease involving administering a therapeutically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof. | 2011-10-27 |
20110263590 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: | 2011-10-27 |
20110263591 | 2-HETEROARYL CARBOXAMIDES - The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 2011-10-27 |
20110263592 | IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Imidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 2011-10-27 |
20110263593 | NOVEL IMIDAZO[1,2-a]PYRIMIDINE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed. | 2011-10-27 |
20110263594 | NOVEL TRIAZOLO(4,3-A)PYRIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, USE THEREOF AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE, IN PARTICULAR AS MET INHIBITORS - The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors. | 2011-10-27 |
20110263595 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, global ischemia, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, and giant cell tumors. | 2011-10-27 |
20110263596 | 2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS - Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds. | 2011-10-27 |
20110263597 | SUBSTITUTED PYRIDINES AND PYRIDAZINES WITH ANGIOGENESIS INHIBITING ACTIVITY - Methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula | 2011-10-27 |
20110263598 | KINASE INHIBITORS AND METHOD OF TREATING CANCER - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: | 2011-10-27 |
20110263599 | 7-NONSUBSTITUTED INDOLE MCL-1 INHIBITORS - Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed. | 2011-10-27 |
20110263600 | Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof. | 2011-10-27 |
20110263601 | METHODS OF TREATING ULCERATIVE COLITIS - Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof. | 2011-10-27 |
20110263602 | TETRASUBSTITUTED PYRIDAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R | 2011-10-27 |
20110263603 | Imine Compounds for Combating Invertebrate Pests - The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds. | 2011-10-27 |
20110263604 | Oxidase inhibitors and their use - The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases. | 2011-10-27 |
20110263605 | Azabicyclo[2.2.1]Heptane Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands - The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, 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. | 2011-10-27 |
20110263606 | SOLID ORAL DOSAGE FORMS COMPRISING TADALAFIL - Improved pharmaceutical solid oral dosage forms for the buccal and/or sublingual delivery of Tadalafil. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced methods of preparation by the use improved solubilization systems which can maintain the Tadalafil in a buccal and/or sublingual oral dosage form or a polymeric film matrix that provides improved bioavailability and/or absorption of Tadalafil. | 2011-10-27 |
20110263607 | ALPHA HELIX MIMETICS IN THE TREATMENT OF CANCER - 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 compound 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. | 2011-10-27 |
20110263608 | 16-KETO ASPERGILLIMIDES AND HARMFUL ORGANISM CONTROL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT - Disclosed is a composition for use in controlling ectoparasites, comprising as an active ingredient at least one of compounds represented by formula (I) or (III) or salts thereof. The present invention provides a composition for use in controlling ectoparasites that has excellent ectoparasite control effect and is highly safe. | 2011-10-27 |
20110263609 | Methods of Identifying and Treating Individuals Exhibiting NUP214-ABL1 Positive T-Cell Malignancies with Protein Tyrosine Kinase Inhibitors and Combinations Thereof - The invention described herein relates to diagnostic and treatment methods and compositions useful in the management of disorders, for example cancers, involving NUP214-ABL1 positive T-cell malignancies and methods for treating an individual suffering from a NUP214-ABL1 positive T cell malignancy. | 2011-10-27 |
20110263610 | COMPOUNDS AND COMPOSITIONS AS ITPKB INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb). | 2011-10-27 |
20110263611 | Kinase Inhibitors - The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed. | 2011-10-27 |
20110263612 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | 2011-10-27 |
20110263613 | COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING - Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function. | 2011-10-27 |
20110263614 | Novel compounds - The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders. | 2011-10-27 |
20110263615 | PYRIDINE AND PYRIMIDINE DERIVATIVES AS MGLUR2 ANTAGONISTS - The present invention relates to compounds of formula (I) | 2011-10-27 |
20110263616 | 11-(2-PYRROLIDIN-1-YL-ETHOXY)-14,19-DIOXA-5,7,26-TRIAZA-TETRACYCLO[19.3.1.- 1(2,6).1(8,12)]HEPTACOSA-1(25),2(26),3,5,8,10,12(27),16,21,23-DECAENE MALEATE SALT - The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26triaza-tetra-cyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the maleate salt of this compound. The invention also relates to pharmaceutical compositions containing this salt and methods of use of the salt in the treatment of certain medical conditions. | 2011-10-27 |
20110263617 | Combination therapy for the treatment of diabetes and related conditions - The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto. | 2011-10-27 |
20110263618 | METHOD OF PROMOTING HAIR GROWTH - The present invention is an invention belonging to the life style improving cosmetic in the field of hair maintenance and enrichment. More particularly, it relates to cosmetic compositions having an improved hair care actions such as to prevent hair loss and/or to promote hair growth on the scalp and skin of a mammal. | 2011-10-27 |
20110263619 | PHARMACEUTICAL FORMULATIONS AND USE THEREOF IN THE PREVENTION OF STROKE, DIABETES AND/OR CONGESTIVE HEART FAILURE - The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF). | 2011-10-27 |
20110263620 | QUINOLINE COMPOUNDS AND THEIR USE FOR TREATING VIRAL INFECTION - Quinoline compounds of formula (I): | 2011-10-27 |
20110263621 | NEW COMBINATION OF ACTIVE INGREDIENTS CONTAINING AN a1-ANTAGONIST AND A PDE 4 INHIBITOR - The subject of the present invention is a new combination of active ingredients consisting of alfuzosin and PDE 4 inhibitor, and pharmaceutical compositions containing them, for ameliorating and/or treating benign prostatic hyperplasia, urinary disorders, disorders related to bladder dysfunction, lower urinary tract symptoms associated or not associated with benign prostatic hyperplasia, urinary incontinence, bladder outlet obstruction associated or not associated with benign prostatic hyperplasia, interstitial cystitis and overactive bladder. | 2011-10-27 |
20110263622 | TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS - The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 2011-10-27 |
20110263623 | PROCESS FOR PREPARATION OF BOSENTAN - The present invention provides improved processes for preparing Bosentan. The present invention provides novel intermediates like 4,6-dihydroxy-5-(2-methoxy phenoxy)[2,2′]bipyrimidine of formula (II) and N-(6-Chloro-5-(2-ethoxyphenoxy)[2,2′-bipyrimidinyl]-4-t-butyl benzenesulfonamide cesium salt and process for preparation thereof. The invention also disclosed novel polymorphic form of the intermediates. | 2011-10-27 |
20110263624 | BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient. | 2011-10-27 |
20110263625 | HIV REPLICATION INHIBITING PYRIMIDINES - This invention concerns the use of compounds of formula | 2011-10-27 |
20110263626 | NOVEL BRADYKININ B1-ANTAGONISTS - The present invention relates to compounds of general formula I | 2011-10-27 |
20110263627 | N3-SUBSTITUTED-N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N3-substituted-N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 2011-10-27 |
20110263628 | N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF - The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis. | 2011-10-27 |
20110263629 | AMIDES OF DIAZABICYCLOOCTANES AND USES THEREOF - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS). | 2011-10-27 |
20110263632 | Solid dispersions comprising tacrolimus - A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability. | 2011-10-27 |
20110263633 | UP TO SIX WEEKS TREATMENT REGIMEN FOR TREATING ACTINIC KERATOSES WITH PHARMACEUTICAL COMPOSITIONS FORMULATED WITH 2.5% IMIQUIMOD - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara° 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2011-10-27 |
20110263634 | LOWER DOSAGE STRENGTH PHARMACEUTICAL COMPOSITIONS FORMULATED WITH 2.5% IMIQUIMOD - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2011-10-27 |
20110263635 | METHOD OF TREATING ACTINIC KERATOSIS WITH 3.75% IMIQUIMOD CREAM - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2011-10-27 |
20110263636 | 3 x 3 x 3 WEEK DOSING REGIMEN FOR TREATING ACTINIC KERATOSIS WITH PHARMACEUTICAL COMPOSITIONS FORMULATED WITH 3.75 % IMIQUIMOD - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara° 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2011-10-27 |
20110263637 | UP TO SIX WEEKS DOSING REGIMEN FOR TREATING ACTINIC KERATOSIS WITH PHARMACEUTICAL COMPOSITIONS FORMULATED WITH 3.75% IMIQUIMOD - Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat actinic keratosis are also disclosed and described. | 2011-10-27 |
20110263638 | Therapeutic agent for glaucoma comprising rho kinase inhibitor and - blocker - A therapeutic agent for glaucoma including a combination of pharmaceutically effective amounts of a Rho kinase inhibitor and a β-blocker, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol. A method of treating glaucoma including administering effective amounts of a Rho kinase inhibitor and a β-blocker to a patient, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol. | 2011-10-27 |
20110263639 | Aryl-substituted bridged or fused diamines as modulators of leukotriene A4 hydrolase - Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A | 2011-10-27 |
20110263640 | 8-AZABICYCLO[3.2.1]OCT-2-ENE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. 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. | 2011-10-27 |
20110263641 | Isoxazolines For Controlling Invertebrate Pests - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2011-10-27 |
20110263642 | METHODS FOR TREATMENT OF MULTIPLE SCLEROSIS - The present invention relates to methods and compounds useful for treating multiple sclerosis. | 2011-10-27 |
20110263643 | 2,3-Disubstituted Piperidine Orexin Receptor Antagonists - The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 2011-10-27 |
20110263644 | Compounds and Methods for Treatment of Stroke - The present invention relates to methods and agents useful for the treatment of stroke, including ischemic stroke and hemorrhagic stroke. In particular, methods and agents for treating stroke in a subject are provided, wherein the agent is administered prior to diagnosis of the stroke as an ischemic stroke or a hemorrhagic stroke. | 2011-10-27 |
20110263645 | Compositions and Methods of Treating Retinal Disease - Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed | 2011-10-27 |
20110263646 | PHARMACEUTICAL TOPICAL COMPOSITIONS - The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream. | 2011-10-27 |
20110263647 | FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE - The invention relates to thiazole compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. | 2011-10-27 |
20110263648 | BRIDGED TETRAHYDRONAPHTHALENE DERIVATIVES - The invention relates to compounds of formula (I) wherein R | 2011-10-27 |
20110263649 | CRYSTALLINE FORM OF LENALIDOMIDE AND A PROCESS FOR ITS PREPARATION - The present invention relates to a novel crystalline form of lenalidomide having formula (I) and chemically known as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to a process for the preparation of said novel form and its use in pharmaceutical preparations for the treatment of autoimmune disease, inflammation, inflammatory disease and diseases such as cancer, in particular the management of multiple myeloma. | 2011-10-27 |
20110263650 | Tubulysin D Analogues - The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The essential features for the potent cytotoxicity of tubulysin D have been established for the first time by the synthesis and evaluation of a series of analogues. By identifying functionality that surprisingly is not necessary for activity, highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D. | 2011-10-27 |
20110263651 | NOVEL PIPERIDINE-BUTYRAMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - The present invention relates to novel piperidine-4-butyramide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. 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. | 2011-10-27 |
20110263652 | Treatment and/or Prevention of Inner Ear Conditions by Modulation of a Metabotropic Glutamate Receptor - Described herein are compositions and methods of treating and/or preventing inner ear conditions by administering to a patient in need thereof a modulator of a metabotropic glutamate receptor. | 2011-10-27 |
20110263653 | MIGRASTATIN ANALOG COMPOSITIONS AND USES THEREOF - In one aspect, the present invention provides pharmaceutical compositions comprising a therapeutically effective amount of a compound of general formula (I), | 2011-10-27 |
20110263654 | SOLID FORMS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID - The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 2011-10-27 |
20110263655 | METHOD FOR CONTROLLING INSECTS IN PLANTS - The invention relates to a method for controlling woolly apple aphid insect comprising contacting the insect or a locus, where control of the insect is desired, with a combination of at least one neonicotinoid compound and at least one benzoylphenyl urea compound. | 2011-10-27 |
20110263656 | Pirfenidone Treatment for Patients with Atypical Liver Function - Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone. | 2011-10-27 |
20110263657 | DIARYL UREAS FOR TREATING HEART FAILURE - The present invention relates to pharmaceutical compositions for treating, preventing or managing heart failure and/or connected diseases therewith comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound. | 2011-10-27 |
20110263658 | RENIN INHIBITORS - The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency. | 2011-10-27 |
20110263659 | Analogs of 1-Methylnicotinamide - The present invention is directed to derivatives and analogs of 1-methyl-nicotinamide useful for elevating the blood levels of 1-methylnicotinamide or deuterated species in a subject. | 2011-10-27 |
20110263660 | ANTIHYPERTENSIVE PHARMACEUTICAL COMPOSITION - An antihypertensive pharmaceutical composition is provided, which contains levamlodipine or a pharmaceutically acceptable salt thereof, and indapamide. In the present invention, levamlodipine and indapamide are administrated in combination for treating hypertension, a good synergistic antihypertensive effect is achieved, and the edema side effect due to sodium and water retention caused when levamlodipine is administrated alone and the side effect of glucose metabolism interference caused when indapamide is administrated alone are mitigated. | 2011-10-27 |
20110263661 | 3-(4-((1H-IMIDAZOL-1-YL)METHYL)PHENYL)-5-ARYL-1,2,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS - Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. | 2011-10-27 |
20110263662 | 1,2-DIAMIDO-ETHYLENE DERIVATIVES AS OREXIN ANTAGONISTS - The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R | 2011-10-27 |