Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Patent number: 9000008Abstract: The invention relates to novel amides of acetic and propionic acids, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.Type: GrantFiled: August 16, 2013Date of Patent: April 7, 2015Assignee: Bayer Intellectual Property GmbHInventors: Joachim Luithle, Frank-Gerhard Bob, Christina Erb, Katrin Schnizler, Timo Flessner, Marja V. Kampen, Christoph Methfessel
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Publication number: 20150093374Abstract: The invention provides methods of inhalation treatment of a respiratory disease or condition in a patient in need to such treatment without producing in said patient systemic antimuscarinic effects, comprising administering to said patient an effective amount of aclidinium.Type: ApplicationFiled: December 5, 2014Publication date: April 2, 2015Applicant: ALMIRALL S.A.Inventor: Jorge Beleta SUPERVIA
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Patent number: 8993556Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 16, 2010Date of Patent: March 31, 2015Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
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Publication number: 20150087656Abstract: Prolongation compositions for prolonging the presence of drugs in blood.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Aida Salatinjants, Robert Salatinjants
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Publication number: 20150083127Abstract: The present invention relates to aggregate particles comprising nanoparticulate drug particles. In particular, the present invention is directed to aggregate particles comprising nanoparticulate drug particles of umeclidinium bromide and optionally vilanterol trifenatate and/or fluticasone furoate. Aggregate particles of the present invention may further comprise nanoparticulate excipient particles and one or more binders. The invention also relates to powder compositions suitable for inhalation that comprise said aggregate particles, processes of producing said aggregate particles, and use of said powder compositions in the treatment of respiratory diseases, such as asthma and COPD.Type: ApplicationFiled: April 11, 2013Publication date: March 26, 2015Inventors: Michiel Mary Van Oort, John N. Hong
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Publication number: 20150087626Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.Type: ApplicationFiled: July 4, 2011Publication date: March 26, 2015Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Patent number: 8987299Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 6, 2013Date of Patent: March 24, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Ian Linney
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Publication number: 20150080324Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Publication number: 20150080359Abstract: Combinations comprising (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases.Type: ApplicationFiled: November 20, 2014Publication date: March 19, 2015Inventors: Jordi Gras Escardo, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
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Patent number: 8980913Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 6, 2013Date of Patent: March 17, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Ian Linney, Chris Knight, Wolfgang Schmidt
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Publication number: 20150065537Abstract: The invention relates to novel benzothiophene-, benzofuran-, and indole ureas 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.Type: ApplicationFiled: June 9, 2014Publication date: March 5, 2015Inventors: Timo Flessner, Frank-Gerhard Boss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Dieter Lang, Joachim Luithle, Marja Van Kampen, Franz-Josef Van Der Staay
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Publication number: 20150065443Abstract: A composition having a structure of: X-L-Y wherein X comprises at least one embelin moiety; L comprises a linker; and Y comprises a hydrophilic moiety. Also disclosed is a micelle that includes: a core that includes at least one hydrophobic active agent and at least one embelin moiety; and a hydrophilic zone surrounding the core and comprising at least one hydrophilic moiety.Type: ApplicationFiled: April 4, 2013Publication date: March 5, 2015Applicant: University of Pittsburgh - of the Commonwealth System of Higher EducatioonInventors: Song Li, Xiang Gao, Yixian Huang, Jianqin Lu
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Publication number: 20150065511Abstract: The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably use aceclidine separate or together with a cycloplegic agent and/or with a nonionic surfactant and viscosity enhancer, and or with low concentrations of a selective ?-2 adrenergic receptor agonist.Type: ApplicationFiled: March 24, 2014Publication date: March 5, 2015Applicant: Presbyopia Therapies, LLCInventors: Gerald Horn, Lee Nordan
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Publication number: 20150059746Abstract: A method is disclosed for making a pharmaceutical composition for pulmonary administration, the method comprising a step in which an inhalable pharmaceutically active material is acoustically blended in a resonant acoustic blender. The invention also relates to compositions for inhalation prepared by the method.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventor: Matthew Green
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150057272Abstract: 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.Type: ApplicationFiled: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8962574Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 10, 2009Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventor: Paul Anthony Reilly
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Publication number: 20150045386Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.Type: ApplicationFiled: August 25, 2014Publication date: February 12, 2015Inventors: Merouane Bencherif, Lisa Benson, Gary Maurice Dull, Nikolai Federov, Gregory J. Gatto, Kristen G. Jordan, Anatoly A. Mazurov, Lan Miao, Julio A. Munoz, Inigo Pfeffier, Sondra Pfeiffer, Teresa Phillips
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Patent number: 8952165Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.Type: GrantFiled: January 30, 2012Date of Patent: February 10, 2015Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
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Patent number: 8952004Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: January 5, 2011Date of Patent: February 10, 2015Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20150031681Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).Type: ApplicationFiled: April 9, 2013Publication date: January 29, 2015Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
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Publication number: 20150031677Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: February 28, 2013Publication date: January 29, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
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Publication number: 20150030666Abstract: The present invention provides an adhesive skin patch containing a support and an adhesive layer containing a drug which is formed on the support, wherein the adhesive layer comprises a thermoplastic elastomer, a liquid component in an amount exceeding 300 parts by weight per 100 parts by weight of the thermoplastic elastomer, a therapeutic drug having an anticholinergic activity or a salt thereof for overactive bladder as a drug, (A) a non-volatile hydrocarbon oil as a liquid component, and one or more kinds selected from the group consisting of (B) an amide solvent, (C) an alcohol solvent and (D) a liquid organic acid as a liquid component, or a fatty acid salt, and optionally comprises a tackifier at a content of not more than 10 wt % of the adhesive layer.Type: ApplicationFiled: November 28, 2012Publication date: January 29, 2015Inventors: Hiroyuki Ogino, Masaoki Goto, Atsuyo Hamada, Mitsuji Akazawa
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Patent number: 8940763Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 9, 2012Date of Patent: January 27, 2015Assignee: TheraVida, Inc.Inventors: Mehdi Paborji, Wendy Jade Limayo Hernandez, Kenneth L. Duchin, Roger S. Flugel
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Publication number: 20150017099Abstract: The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and/or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.Type: ApplicationFiled: January 25, 2013Publication date: January 15, 2015Inventors: Noam A. Cohen, Robert J. Lee, Danielle R. Reed
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Publication number: 20140377328Abstract: Provided is an intraoral soluble-type film preparation in which an unpleasant taste of a drug is masked. The intraoral soluble-type film preparation comprises a drug layer containing: a drug having a bitter taste and/or an astringent taste; an alkyl sulfate at a content of ¾ mol or more with respect to 1 mol of the drug; and a water-soluble polymer.Type: ApplicationFiled: December 12, 2012Publication date: December 25, 2014Applicant: KYUKYU PHARMACEUTICAL CO., LTD.Inventors: Akihiro Ishise, Hisanobu Nishikawa
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Publication number: 20140371264Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.Type: ApplicationFiled: September 4, 2014Publication date: December 18, 2014Inventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
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Publication number: 20140364451Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.Type: ApplicationFiled: August 1, 2012Publication date: December 11, 2014Applicant: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 8901151Abstract: 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).Type: GrantFiled: May 14, 2013Date of Patent: December 2, 2014Assignee: Targacept, Inc.Inventors: Merouane Bencherif, Nikolai Fedorov, Terry Hauser, Kristen Jordan, Sharon Rae Letchworth, Anatoly Mazurov, Julio A. Munoz, Jason Speake, Daniel Yohannes
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Publication number: 20140350008Abstract: 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.Type: ApplicationFiled: April 25, 2014Publication date: November 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Joachim Luithle, Frank-Gerhard Boess, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
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Publication number: 20140342048Abstract: Sauces, spreads, cooking oils, and cooking fats are created from a wide range of various ingredients. Sauces, spreads, cooking oils, and cooking fats having at least one ingredient, with at least one flavoring, and at least one texture. At least one ingredient is selected from group including of at least one flavoring ingredient, at least one nutritional ingredient, at least one health ingredient, and at least one other ingredient. At least one ingredient is also created as small spherical balls as mixed in. Sauces can be served as appetizer and snack. And served as baby food, for children with less teeth, for old people, and for sick people. Sauces, spreads, cooking oils, and cooking fats are used for food preparation and food flavoring, including condiment and salad dressing. And used in manner selected from group consisting of room temperature, cold, warm, and hot.Type: ApplicationFiled: November 26, 2013Publication date: November 20, 2014Inventor: Alice Chang
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Patent number: 8877774Abstract: Compounds of formula(I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.Type: GrantFiled: June 8, 2012Date of Patent: November 4, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Andrea Rizzi, Gabriele Amari, Matteo Biagetti, Ian Linney
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Patent number: 8871787Abstract: The present invention refers to a stable crystalline salt of (R)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabicyclo[2.2.2]oct-3-yl ester and its use as medicament, in particular for the treatment of urinary incontinence or other diseases involving genitourinary disorders.Type: GrantFiled: February 8, 2013Date of Patent: October 28, 2014Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, José Hildalgo Rodríguez, María del Carmen Serra Comas, Isabel Masip Masip
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Patent number: 8865641Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: GrantFiled: June 14, 2012Date of Patent: October 21, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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Patent number: 8859560Abstract: The present invention relates to a method of treating attention deficit hyperactivity disorder in a subject. This method includes selecting a subject with attention deficit hyperactivity disorder and administering to the selected subject a sodium/hydrogen exchanger inhibitor under conditions effective to treat the subject for attention deficit hyperactivity disorder. Methods of identifying compounds suitable to treat attention deficit hyperactivity disorder are also disclosed.Type: GrantFiled: February 15, 2013Date of Patent: October 14, 2014Assignee: The Research Foundation of State University of New YorkInventor: Stephen V. Faraone
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Patent number: 8859535Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: GrantFiled: June 19, 2012Date of Patent: October 14, 2014Assignee: Novartis AGInventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
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Publication number: 20140303126Abstract: A compound according to formula (I) wherein z© is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH?CR6, —CR6?CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; in is an integer from 0 to 8; proType: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventors: Maria Dolors FERNANDEZ FORNER, Maria PRAT QUINONES, Maria Antonia BUIL ALBERO
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Publication number: 20140303231Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.Type: ApplicationFiled: January 24, 2014Publication date: October 9, 2014Applicant: The Johns Hopkins UniversityInventors: Xinzhong Dong, Qin Liu, David J. Anderson
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Patent number: 8853404Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.Type: GrantFiled: October 14, 2013Date of Patent: October 7, 2014Assignee: Glaxo Group LimitedInventors: Dramane Ibrahim Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
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Publication number: 20140296197Abstract: Combinations comprising (a) a ?2 agonist and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: June 16, 2014Publication date: October 2, 2014Inventors: Jordi GRAS ESCARDO, Jesus LLENAS CALVO, Hamish RYDER, Pio ORVIZ DIAZ
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Patent number: 8846715Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.Type: GrantFiled: July 22, 2013Date of Patent: September 30, 2014Assignee: Targacept, Inc.Inventors: Merouane Bencherif, Lisa Benson, Gary Maurice Dull, Nikolai Federov, Gregory J. Gatto, Kristen G. Jordan, Anatoly A. Mazurov, Lan Miao, Julio A. Munoz, Inigo Pfeiffer, Sondra Pfeiffer, Teresa Phillips
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Patent number: 8846655Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: September 30, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
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Publication number: 20140288118Abstract: The invention relates to N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improvement in cognition, concentration power, learning power and/or memory.Type: ApplicationFiled: February 21, 2014Publication date: September 25, 2014Inventors: Timo Flebner, Frank-Gerhard Boss, Frank-Thorsten Hafner, Joachim Luithle, Christoph Methfessel, Leila Telan
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140286945Abstract: Disclosed herein is a new and improved therapy for the treatment of diseases including cancer, which comprises the step of altering cell membrane lipid composition by treating a cancer cell with an enzyme inhibitor which inhibits enzymes regulating the cholesterol biosynthetic pathway. The method may also be employed in combination with existing chemotherapeutic agents to combat the drug resistance and enhance the therapeutic efficacy of conventional therapy.Type: ApplicationFiled: October 22, 2012Publication date: September 25, 2014Applicant: The Curators of the University of MissouriInventors: Carl Freter, Indira Benakanakere
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Publication number: 20140275011Abstract: Disclosed are compound of Formula (Ia), wherein R2, R12, R16, J, Q, X, Y and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (Ia).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: AbbVie Inc.Inventors: Anthony Mastracchio, Milan Bruncko, Chunqiu Lai, Julie M. Miyashiro, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers
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Publication number: 20140256730Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.Type: ApplicationFiled: January 13, 2014Publication date: September 11, 2014Applicant: Corsair Pharma, Inc.Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
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Publication number: 20140255381Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.Type: ApplicationFiled: September 18, 2013Publication date: September 11, 2014Applicant: GENZYME CORPORATIONInventors: Elyse BOURQUE, Cassandra CELATKA, Bradford HIRTH, Markus METZ, Zhong ZHAO, Renato SKLERJ, Yibin XIANG, Katherine JANCSICS, John MARSHALL, Seng CHENG, Ronald SCHEULE, Mario CABRERA-SALAZAR, Andrew GOOD
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Publication number: 20140248357Abstract: A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.Type: ApplicationFiled: April 7, 2014Publication date: September 4, 2014Applicant: PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITEDInventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
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Publication number: 20140249179Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.Type: ApplicationFiled: February 19, 2014Publication date: September 4, 2014Applicant: ENVIVO PHARMACEUTICALS, INC.Inventors: Patricia Oliver-Shaffer, Gideon Shapiro, Richard Chesworth, Muneki Kishida, Takayuki Ishige