42nd week of 2011 patent applcation highlights part 47 |
Patent application number | Title | Published |
20110257139 | TREATMENT OF DIARRHOEA - A method for the treatment or prevention of diarrhoea (or diarrhoeal disease) in an individual comprises a step of administering a therapeutically effective amount of a potent and or selective FXR agonist to the individual. A method for the treatment or prevention of dysregulated fluid transport into the intestine in an individual is also described, and comprises a step of administering a therapeutically effective amount of a potent and or selective FXR agonist to the individual. | 2011-10-20 |
20110257140 | Biomarkers of Mineralocorticoid Receptor Activation - The present invention relates to the use of Neutrophil Gelatinase-Associated Lipocalin (NGAL) and/or SERPINA3 as biomarkers of the Mineralocorticoid Receptor (MR) activation in a patient. More particularly, the present invention relates to a method for predicting the responsiveness of a patient to a treatment with a MR antagonist or an aldosterone synthase inhibitor, said method comprising determining in a biological sample obtained from said patient the expression level of the NGAL gene and/or of the SERPINA3 gene. | 2011-10-20 |
20110257141 | TRANSDERMAL PHARMACEUTICAL FORMULATION FOR MINIMIZING SKIN RESIDUES - This invention relates to novel transdermal or transmucosal pharmaceutical formulation having an active agent of testosterone which reduces the occurrences of contamination of other individuals and the transference to clothing of the user. The solvent system of the formulation includes a monoalkylether of diethylene glycol and a glycol present in specified ratios, and a mixture of water and alcohol. The invention also relates to a method for inhibiting or delaying crystallization of the active agent in a pharmaceutical formulation. | 2011-10-20 |
20110257142 | METHOD FOR PREPARING 4-[17BETA-METHOXY-17ALPHA-METHOXYMETHYL-3-OXOESTRA-4,9-DIEN-11-BETA-YL]BE- NZALDEHYDE (E)-OXIME (ASOPRISNIL) - The present invention relates to a method for the reliable and reproducible preparation of 4-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-11β-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.). | 2011-10-20 |
20110257143 | Compositions and Method for the Treatment of Multiple Myeloma - The disclosure provides compositions and methods for treating multiple myeloma. In some embodiments, the compositions comprise (E)-3-hydroxy-21-[2′-(N,N-dimethylamino)ethoxy]-19-norpregna-1,3,5(10),17(20)-tetraene or a pharmaceutically acceptable salt or prodrug thereof and a pharmaceutical carrier. | 2011-10-20 |
20110257144 | NOVEL DERMACEUTICAL CREAM MADE USING SODIUM FUSIDATE - The present invention relates to primary and secondary bacterial skin infections and in particular it relates to the treatment of these infections using a Fusidic acid cream that has been made using Sodium fusidate as the starting Active Pharmaceutical Ingredient (API). The invention discloses a dermaceutical cream containing Fusidic acid which is formed in situ from Sodium Fusidate as the starting raw material, wherein Sodium Fusidate is converted into Fusidic acid under oxygen-free environment. The cream of the present invention has greater shelf-life stability and the finer particle size of the API than the conventional creams containing Fusidic acid. | 2011-10-20 |
20110257145 | METHOD OF TREATING NEUROLOGICAL DISEASES - A method of treating neurological diseases, like Alzheimer's Disease by administering a compound that activates protein kinase C and inhibits histone deacetylases to an individual suffering from the neurological disease. The method utilizes benzolactam compounds that reduce Aβ production and blocks oxidative stress in the treatment of Alzheimer's disease. The benzolactam compounds and compositions containing the benzolactam compounds also are disclosed. | 2011-10-20 |
20110257146 | Method of Treating Kcnq Related Disorders Using Organozinc Compounds - The instant invention describes methods of treating KCNQ related diseases and disorders using organozinc compounds. In certain embodiments, pain is treated using Zinc Pyrithione. | 2011-10-20 |
20110257148 | NOVEL 1-ALKYL-3-HYDROXY-3-PHENYLAZETIDINE DERIVATIVES USEFUL AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION - The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating dopamine neurotransmission and extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications. X is OH; R | 2011-10-20 |
20110257149 | FORMULATION FOR ORAL TRANSMUCOSAL ADMINISTRATION OF LIPID-LOWERING DRUGS - The invention relates to a formulation for delivering by oral transmucosal administration at least one lipid-lowering active principle, preferably from the statin family, said formulation including said active principle in the base or salt form, an aqueous alcohol solution titrating at least 30° alcohol, and optionally a pH correcting agent and/or an antioxidant, said active principle being in a stable and completely dissolved state in the aqueous alcohol solution. The invention also relates to a method of preparing said formulation and to the use thereof, preferably in single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular conditions. | 2011-10-20 |
20110257150 | NEW SALTS - This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment. | 2011-10-20 |
20110257151 | NOVEL 3,3-DIMETHYL TETRAHYDROQUINOLINE DERIVATIVES - A compound of formula (I) | 2011-10-20 |
20110257152 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2011-10-20 |
20110257153 | 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 | 2011-10-20 |
20110257154 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 2011-10-20 |
20110257155 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 2011-10-20 |
20110257156 | GAMMA SECRETASE MODULATORS - In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions. | 2011-10-20 |
20110257157 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 2011-10-20 |
20110257158 | PRECOMPACTED FAST-DISINTEGRATING FORMULATIONS OF COMPOUNDS WITH A LOW ORAL BIOAVAILABILITY - This invention relates to the field of pharmaceutical chemistry. Embodiments of the present invention relate to, and provide precompacted fast-disintegrating formulations of compounds with a low oral bioavailability. | 2011-10-20 |
20110257159 | ORALLY DISINTEGRATING TABLET FORMULATIONS OF MIRTAZAPINE AND PROCESS FOR PREPARING THE SAME - Silicon dioxide free orally disintegrating tablet formulations of mirtazapine or a pharmaceutically acceptable salt thereof having crospovidone and sodium stearyl fumarate and one or more pharmaceutically acceptable excipients and a process for preparing such a formulation. | 2011-10-20 |
20110257160 | QUINOLINE DERIVATIVES AND USES THEREOF - This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQ | 2011-10-20 |
20110257161 | NOVEL DIAZA-BICYCLONONYL-PHENYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel diazabicyclononyl-phenyl 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. | 2011-10-20 |
20110257162 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 2011-10-20 |
20110257163 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Compounds of formula (I) include compounds of formulas (IA) and (IB). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I). | 2011-10-20 |
20110257164 | DIPEPTIDYL PEPTIDASE IV INHIBITORS - Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors. | 2011-10-20 |
20110257165 | BICYCLIC PYRAZOLES AS PROTEIN KINASE INHIBITORS - 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 2011-10-20 |
20110257166 | NOVEL AGROCHEMICAL SUSPOEMULSIONS - The present invention provides an aqueous suspoemulsion comprising (a) an oil phase comprising (i) at least one triazole active compound as emulsified component, solid at room temperature, (ii) at least one alkyl carboxylic acid amide as a solvent and a crystal growth inhibitor, and (iii) a polymeric stabilizer, and (b) a continuous water phase comprising (i) at least one strobilurin active compound as suspended solid component, solid at room temperature, (ii) at least one dispersant selected from the group consisting of methacrylic acid-methyl methacrylate-polyethyleneglycol graft copolymer, tristyrylphenolethoxylates and/or propylene oxide/ethylene oxide block copolymer with 10% to 50% EO, preferably with 20% to 50% EO and most preferably with 30% to 40% EO, (iii) water, and (iiii) additives, if appropriate. a process for preparing the suspoemulsion and its use for applying the active compounds comprised therein to plants and/or their habitat are also provided. | 2011-10-20 |
20110257167 | IDENTIFICATION OF LKB1 MUTATION AS A PREDICTIVE BIOMARKER FOR SENSITIVITY TO TOR KINASE INHIBITORS - Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation. | 2011-10-20 |
20110257168 | DERIVATIVES OF OXABISPIDINE AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to compounds of formula (I) 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). | 2011-10-20 |
20110257169 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 2011-10-20 |
20110257170 | 4-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES - This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers. | 2011-10-20 |
20110257171 | NOVEL IMIDAZO[1,2-A]PYRIDINE DERIVATIVES, METHOD 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 is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors. | 2011-10-20 |
20110257172 | 3-(3-Pyrimidine-2-yl-benzyl)-[1,2,4] triazolo[4,3-b]pyrimidine derivatives - Compounds of the formula I, in which R | 2011-10-20 |
20110257173 | 3 (3-Pyrimidin-2-ylbenzyl)-1,2,4-triazolo[4,3-b]pyridazine derivatives - Compounds of the formula (I), in which R | 2011-10-20 |
20110257174 | CHROMENONE 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. | 2011-10-20 |
20110257175 | Selected Inhibitors of Protein Tyrosine Kinase Activity - The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions. | 2011-10-20 |
20110257176 | NITROGEN HETEROCYCLE DERIVATIVES AS PROTEASOME MODULATORS - A method for treating and/or ameliorating and/or preventing a disease or a disorder, the method comprising administering to an individual in need thereof at least one nitrogen heterocycle derivative of formula (I): | 2011-10-20 |
20110257177 | BENZYLTHIOTETRAZOLE INHIBITORS OF STORE OPERATED CALCIUM RELEASE - 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, disorders or conditions that would benefit from inhibition of SOC channel activity. | 2011-10-20 |
20110257178 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers. | 2011-10-20 |
20110257179 | NOVEL THIAZOLES DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B) | 2011-10-20 |
20110257180 | Novel Polymorphic Forms of 6-(1-methyl-1H-pyrazol-4-yl)-2--2H-pyridazin-3-one Dihydrogenphosphate and Processes of Manufacturing thereof - The present invention relates to 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer. | 2011-10-20 |
20110257181 | PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which Y, R | 2011-10-20 |
20110257182 | Novel amido derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors - The present invention relates to novel compounds of Formula (I), wherein X | 2011-10-20 |
20110257183 | BIS-ARYL SULFONAMIDES - Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists. | 2011-10-20 |
20110257184 | SHP-2 PHOSPHATASE INHIBITOR - A method of treating SHP-2 phosphatase associated diseases in a subject includes administering a SHP-2 inhibitor to the subject. | 2011-10-20 |
20110257185 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 2011-10-20 |
20110257186 | COMPOSITIONS AND METHODS FOR TREATING VISUAL DISORDERS - Disclosed are methods of treating disorders of the eye by administering to a patient in need of such treatment a compound represented by the formula | 2011-10-20 |
20110257187 | PHTHALAZIN-(2H)-ONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2011-10-20 |
20110257188 | Compositions and methods for the treatment of nasal conditions - The invention provides compositions and methods for treating nasal congestion. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine. | 2011-10-20 |
20110257189 | PYRROLOPYRAZINONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2011-10-20 |
20110257190 | CRYSTALLINE FORMS - The disclosure relates to crystalline forms of 2-[4-(7-ethyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenyl]-propan-2-ol, characterized by physico-chemical data described herein. | 2011-10-20 |
20110257191 | Hydrazine-Substituted Anthranilic Acid Derivatives - The present invention constitutes new hydrazine-substituted anthranilic acid derivatives of the general formula (I), | 2011-10-20 |
20110257192 | COMPOUND FOR TREATMENT OF RESPIRATORY CONDITION OR DISEASE - The present invention relates to the treatment, alleviation, prevention or reduction of symptoms or exacerbations of asthma or chronic obstructive pulmonary disease (COPD), of which reduced lung function is typically symptomatic. | 2011-10-20 |
20110257193 | FUSED IMIDAZOLE DERIVATIVES AS TRPV3 ANTAGONIST - The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. | 2011-10-20 |
20110257194 | SUBSTITUTED OXINDOL DERIVATIVES AND MEDICAMENTS CONTAINING THE SAME - The present invention relates to novel oxindole derivatives of the general formula (I), | 2011-10-20 |
20110257195 | Cosmetic Use of 1-Aroyl-N-(2-oxo-3-piperidinyl)-2-Piperazine Carbomamides and Related Compounds - Cosmetic compositions comprising 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The 1-aroyl-N-(2-oxo-3-piperidinyl)-2-piperazine carboxamides are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging. | 2011-10-20 |
20110257196 | COMPOUNDS FOR TREATMENT OF CANCER - The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. | 2011-10-20 |
20110257197 | Pharmaceutical Formulations Comprising Voriconazole and Processes for Preparation Thereof - The present invention provides a pharmaceutical formulation comprising voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly (D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation of the present invention has been shown to be stable and safe by experiments. | 2011-10-20 |
20110257198 | PIPERIDINE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS - Disclosed are imidazopyridylmethylene substituted piperidine derivatives of Formula (I): | 2011-10-20 |
20110257199 | NOVEL TERARYL COMPOUNDS AS ANTIPARASITIC AGENTS - Novel dicationic terphenyl compounds and their aza analogues. Methods for combating microbial infections with novel dicationic terphenyl compounds and their aza analogues. Processes for synthesizing novel dicationic terphenyl compounds and their aza analogues. | 2011-10-20 |
20110257200 | Treatment of Acne and Other Diseases - The invention relates to compounds for the treatment of dermatological diseases where inflammation, matrix metalloproteinases (MMPs) and peroxisome proliferator-activated receptors (PPARs) play a role in mediating the disease, such as the treatment of acne with Pemirolast or a closely related compound thereof. | 2011-10-20 |
20110257201 | AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT - An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance. | 2011-10-20 |
20110257202 | Therapeutic Compositions and Methods for Treating Chronic Kidney Disease Associated with a Metabolic Imbalance - Disclosed herein are compositions and methods for treating chronic kidney disease and/or a metabolic imbalance. Specifically exemplified herein are methods involving the coadministration of a RAS inhibitor with a conjunctive agent that improves endothelial NO or endothelial function. Also disclosed are methods of treating a patient exhibiting symptoms of a stage of chronic kidney disease and at least one symptom of a metabolic imbalance, such as one or more diagnostic criteria of the metabolic syndrome. | 2011-10-20 |
20110257203 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2011-10-20 |
20110257204 | Penciclovir or Famciclovir for Treatment of Recurrent Genital Herpes with a One-Day Application - A method for the treatment of recurrent genital herpes, in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a treatment period of one day. | 2011-10-20 |
20110257205 | 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 these 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. | 2011-10-20 |
20110257206 | Combinations of Therapeutic Agents for Treating Cancer - The invention relates to a combination comprising a microtubule active agent; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination. | 2011-10-20 |
20110257207 | RAF INHIBITORS - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 2011-10-20 |
20110257208 | COMPOUNDS USEFUL AS FAAH MODULATORS AND USES THEREOF - Compounds are disclosed that have formula I: where A, B, L | 2011-10-20 |
20110257209 | 6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW POTENT ANALGESICS AND ANTI-INFLAMMATORY AGENTS - The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases. | 2011-10-20 |
20110257210 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - The present application discloses novel benzimidazole derivatives of general formula (I) or an N-oxide thereof, any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein R represents a pyridyl or pyrimidyl group; which pyridyl or pyrimidyl group is optionally substituted with one or more substituents independently selected from the group consisting of: halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, alkyl, hydroxy, hydroxyalkyl and alkoxy, and their use as modulators of the GABA | 2011-10-20 |
20110257211 | Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics - Small molecule choline kinase inhibitors having the following formula: | 2011-10-20 |
20110257212 | NEW AZACYCLIC DERIVATIVES - The invention provides novel compounds having the general formula (I) | 2011-10-20 |
20110257213 | SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). | 2011-10-20 |
20110257214 | MORPHINAN COMPOUNDS - This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity. | 2011-10-20 |
20110257216 | 2 x 2 x 2 WEEK TREATMENT REGIMEN FOR TREATING ACTINIC KERATOSIS 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. | 2011-10-20 |
20110257217 | 3 x 3 x 3 WEEK TREATMENT REGIMEN FOR TREATING ACTINIC KERATOSIS 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. | 2011-10-20 |
20110257218 | 2 x 2 x 2 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. | 2011-10-20 |
20110257219 | LOWER DOSAGE STRENGTH PHARMACEUTICAL COMPOSITIONS FORUMLATED 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. | 2011-10-20 |
20110257220 | 3,11 b-cis-Dihydrotetrabenazine for the Treatment of Schizophrenia and Other Psychoses - The invention provides the use of 3,11b-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the prophylaxis or treatment of schizophrenia and other psychoses. | 2011-10-20 |
20110257221 | NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS - Compounds of the formula Ia***** | 2011-10-20 |
20110257222 | COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES - The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound. | 2011-10-20 |
20110257223 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to pharmaceutical compositions comprising a compound of Formula I with one or both of a Compound of Formula II and/or a Compound of Formula III. Further, the present invention relates to methods of treating CFTR mediated diseases, particularly cystic fibrosis, using modulators of CFTR, and compositions and combinations thereof. | 2011-10-20 |
20110257224 | PREPARATION AND THERAPEUTIC APPLICATIONS OF (2S,3R)-N-2-((3-PYRIDINYL)METHYL)-1-AZABICYCLO[2.2.2]OCT-3-YL)-3,5-DIFLUO- ROBENZAMIDE - The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetyl-choline 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). | 2011-10-20 |
20110257225 | CYCLOHEXYLAMINE DERIVATIVE CONTAINING PHENYL GROUP, AND THERAPEUTIC AGENT FOR DISEASES ACCOMPANIED BY CENTRAL NERVOUS SYSTEM DISORDERS - Disclosed is a novel cyclohexylamine derivative containing a phenyl group, which is useful as a novel sigma receptor ligand. Also disclosed is a therapeutic agent for diseases accompanied by a central nervous system disorder, which comprises the compound as an active ingredient. The therapeutic agent comprises a compound represented by general formula [1] or a pharmacologically acceptable salt thereof as an active ingredient: | 2011-10-20 |
20110257226 | HALOGEN-CONTAINING ORGANOSULFUR COMPOUND AND USE THEREOF - There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R | 2011-10-20 |
20110257227 | Methods For Treatment Of Cognitive And Menopausal Disorders With D-Threo Methylphenidate - In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including executive function defects. The methods involve the administration of a composition comprising D-threo methylphenidate that is substantially free of L-threo methylphenidate and of erythro forms of methylphenidate. | 2011-10-20 |
20110257228 | LIQUID PHARMACEUTICAL COMPOSITIONS COMPRISING A TRIPTAN COMPOUND AND XYLITOL - The present disclosure relates to aqueous liquid pharmaceutical compositions comprising a) at least one triptan compound, pharmaceutically acceptable salts or hydrates thereof, and b) xylitol. | 2011-10-20 |
20110257229 | SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES - Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis. | 2011-10-20 |
20110257230 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - The present application discloses novel benzimidazole derivatives and their use as modulators of the GABA | 2011-10-20 |
20110257231 | ANTHRANILAMIDE COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND PESTICIDES CONTAINING THEM - Anthranilamide compounds, a process for their production, and pesticides containing these compounds as active ingredients. This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way. | 2011-10-20 |
20110257232 | BIPHENYL OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE RECEPTORS MODULATORS - The present invention relates to novel biphenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 2011-10-20 |
20110257233 | BENZOISOTHIAZOLONES AS INHIBITORS OF PHOSPHOMANNOSE ISOMERASE - The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia. | 2011-10-20 |
20110257234 | Agrochemical Auxiliary Compositions - Suggested are agrochemical auxiliary compositions, comprising (a) alkoxylated polyol esters, (b) optionally alkoxylated alk(en)yl oligoglycosides, and (c) fatty acids or their salts. | 2011-10-20 |
20110257235 | TRIAZOLIUM AND IMIDAZOLIUM SALTS AND USES THEREOF - The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a | 2011-10-20 |
20110257236 | SOLID SOLUTION OF VALINE, ISOLEUCINE, LEUCINE AND ITS MANUFACTURING METHOD - [Problem] A valine, isoleucine, leucine mixture which is excellent in the reduction of bitter taste and improved dissolution speed is provided. | 2011-10-20 |
20110257237 | PROCESS FOR THE PREPARATION OF CRYSTALLINE FORMS OF SUNITINIB MALATE - The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer. | 2011-10-20 |
20110257238 | Heteroaryl Dihydroindolones as Kinase Inhibitors - The present invention provides a compound represented by the formula: | 2011-10-20 |
20110257239 | SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION AND METHOD OF RELEASING PHARMACEUTICALLY ACTIVE AGENT - The present invention is directed to solid, sustained-release, oral dosage form pharmaceutical compositions which contain therapeutic amounts of a pharmaceutically active agent, hydroxypropyl methyl cellulose and a non-ionic, hydrophilic polymer selected froth the group consisting of hydroxyethyl cellulose having a number average molecular weight ranging from 90,000 to 1,300,000, hydroxypropyl cellulose having a number average molecular weight of 370,000 to 1,500,000, and poly(ethylene oxide) having a number average molecular weight ranging from 100,000 to 500,000. | 2011-10-20 |
20110257240 | STABILIZED STATIN FORMULATIONS - The present invention is directed to statin formulations having improved solubility and/or stability and methods for the same. | 2011-10-20 |