Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Publication number: 20120277216Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.Type: ApplicationFiled: December 29, 2009Publication date: November 1, 2012Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
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Publication number: 20120276018Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.Type: ApplicationFiled: April 27, 2012Publication date: November 1, 2012Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele AMARI, Mauro Riccaboni, Daniele De Zani
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Publication number: 20120270857Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: June 30, 2010Publication date: October 25, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Patent number: 8288409Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: February 3, 2009Date of Patent: October 16, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Publication number: 20120258964Abstract: 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: March 6, 2012Publication date: October 11, 2012Applicant: Bayer Schering Pharma AGInventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
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Patent number: 8283470Abstract: A method for the preparation of solifenacin by reacting quinuclidin-3-ol and bis (aryl) carbonate to form (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa); and treating (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa) with (1S)-1-phenyl- 1,2,3,4-tetrahydroisoquinoline of formula (V) in an inert atmosphere to form a Solifenacin base, which is converted into its pharmaceutically acceptable salts. The invention also provides a compound, (3R)-1-azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa), which is used as an intermediate for the preparation of Solifenacin base and a process for the preparation thereof.Type: GrantFiled: August 31, 2009Date of Patent: October 9, 2012Assignee: Megafine Pharma(P) Ltd.Inventors: Vijayvitthal Thippannachar Mathad, Navnath Chintaman Niphade, Anil Chaturlal Mali, Kunal Madhav Jagtap, Bhushan Sudhakar Pandit, P. Raghvendra Kumar, Shashikant Baburao Landge
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Patent number: 8278301Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.Type: GrantFiled: May 15, 2009Date of Patent: October 2, 2012Assignee: Albany Molecular Research, Inc.Inventors: David D. Manning, Zhicai Yang
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Publication number: 20120244221Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. Dill
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Publication number: 20120237574Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: ApplicationFiled: June 4, 2012Publication date: September 20, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. Dill
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Patent number: 8263619Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: December 4, 2009Date of Patent: September 11, 2012Assignee: Memory Pharmaceuticals CorporationInventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Truc Minh Nguyen, Jianguo Ma, Carla Maria Gauss, Ashok Tehim
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Publication number: 20120220557Abstract: Liquid, propellant-free pharmaceutical formulation for administration by nebulization which comprising an antimuscarinic drug as active ingredient are useful for the prevention and/or treatment of a wide range of conditions including respiratory disorders.Type: ApplicationFiled: February 10, 2012Publication date: August 30, 2012Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Annamaria Soliani RASCHINI, Emilio Lutero
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Publication number: 20120220599Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: May 2, 2012Publication date: August 30, 2012Inventors: Dominik FEUERBACH, Konstanze HURTH, Timothy John RITCHIE
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Publication number: 20120202786Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: April 16, 2012Publication date: August 9, 2012Applicant: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120202819Abstract: Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.Type: ApplicationFiled: September 27, 2010Publication date: August 9, 2012Applicant: Merck Sharp & Dohme CorporationInventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
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Publication number: 20120202842Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: ApplicationFiled: November 4, 2011Publication date: August 9, 2012Applicant: Bayer Schering Pharma AGInventors: Martin Hendrix, Frank-Gerhard Böß, Christina Erb, Timo Fleßner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
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Patent number: 8236857Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: GrantFiled: March 19, 2012Date of Patent: August 7, 2012Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Patent number: 8236856Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: GrantFiled: March 19, 2012Date of Patent: August 7, 2012Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Publication number: 20120190648Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH—C(?NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a —CO—(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.Type: ApplicationFiled: July 23, 2010Publication date: July 26, 2012Inventors: Philippe Jubault, Jean-Charles Quirion, Gerald Lemonnier, Cedric Lion
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Patent number: 8227484Abstract: Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.Type: GrantFiled: March 8, 2012Date of Patent: July 24, 2012Assignee: Avanir Pharmaceuticals, Inc.Inventors: Gerald Yakatan, James Berg, Laura Pope, Richard Alan Smith
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Publication number: 20120183568Abstract: Provided are methods for aiding in diagnosing autoimmune diseases in a mammal, comprising contacting a biological sample that is not a tear sample from the mammal with an antibody that specifically binds to a first polypeptide selected from the group Ctss, Ctsh, Ctsr, Ctsw, Ctsz, Ifng, IL-6ra, IL-10, IL-10ra, IL-15, Tnfa, Apo-F, or Lcn-2 or a second polypeptide selected from the group lactoperoxidase, lactoferrin or lysozyme under conditions favoring the formation of an antibody-polypeptide complex, and determining the amount of complex formed, wherein an increased formation of antibody-first-polypeptide complex or a decreased formation of antibody-second-polypeptide complex as compared to a suitable control, indicates a likely positive diagnosis of an autoimmune disease for the mammal, thereby aiding in the diagnosis. Methods of treating the autoimmune diseases are also provided.Type: ApplicationFiled: December 13, 2011Publication date: July 19, 2012Inventor: Sarah Hamm-Alvarez
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Publication number: 20120183605Abstract: Disclosed herein are quinine formulations and methods of using quinine formulations. Specifically disclosed herein are solid oral dosage forms which can be administered as a capsule or tablet, or alternatively as a sprinkle form with the patient experiencing little or no bitter taste. The dosage forms provide immediate release in vitro and in vivo.Type: ApplicationFiled: September 14, 2011Publication date: July 19, 2012Inventors: Kristin Arnold, Matthew W. Davis, Suman Wason, Siva Rama K. Nutalapati
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Patent number: 8222294Abstract: The present invention concerns combinations of an anti-emetic agent and an enkephalinase inhibitor for use in methods for treating diarrhea and/or gastroenteritis.Type: GrantFiled: February 14, 2005Date of Patent: July 17, 2012Assignee: BioprojectInventors: Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Patent number: 8222274Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: GrantFiled: February 19, 2007Date of Patent: July 17, 2012Assignee: Astellas Pharma Inc.Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
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Publication number: 20120164192Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: ApplicationFiled: March 19, 2012Publication date: June 28, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. Dill
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Publication number: 20120164193Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: ApplicationFiled: March 19, 2012Publication date: June 28, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. Dill
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Patent number: 8207192Abstract: The invention relates to the quinuclidine compounds of formula I having quaternary ammonium group, its preparation, and the pharmaceutical composition comprising an effective amount of the compound of formula I. The compound and the composition are used to prevent and treat the diseases by blocking acetylcholine receptor. Wherein: R1 is selected from C1-12 saturated straight-chain alkyl and cycloalkyl; R2 is selected from C1-12 saturated straight-chain alkyl or straight-chain alkyl; and X is selected from halogen ion, organic and inorganic acid radical.Type: GrantFiled: March 9, 2009Date of Patent: June 26, 2012Inventor: Shuqiang Zhao
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Patent number: 8207193Abstract: The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation (I), (II), (IIIa), (IIIb).Type: GrantFiled: November 13, 2007Date of Patent: June 26, 2012Assignee: Astrazeneca ABInventors: Rhonan Ford, Andrew Mather, Antonio Mete
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Publication number: 20120157464Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.Type: ApplicationFiled: July 21, 2010Publication date: June 21, 2012Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
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Publication number: 20120157491Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: Glaxo Group LimitedInventors: Dramane I. Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
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Publication number: 20120157490Abstract: The invention relates to N-biarylamides useful for the prophylaxis and/or treatment of impairments of perception, concentration, learning and/or memory, and to processes for preparing them, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 19, 2011Publication date: June 21, 2012Applicant: Bayer HealthCare AGInventors: Timo FLEßNER, Frank-Gerhard BÖß, Frank-Thorsten HAFNER, Joachim LUITHLE, Christoph METHFESSEL, Leila TELAN
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Publication number: 20120141554Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: ApplicationFiled: January 4, 2012Publication date: June 7, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. Dill
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Publication number: 20120142725Abstract: The combined use of (R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzene-1-sulfonamide (tamsulosin), or its pharmaceutically acceptable salt, and (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid (3R)-quinuclidin-3-yl ester (solifenacin), or its pharmaceutically acceptable salt, for the preparation Of a medicament for the improvement of lower urinary tract symptoms associated with benign prostatic hyperplasia (LUTS/BPH) with a substantial storage component is provided.Type: ApplicationFiled: November 4, 2009Publication date: June 7, 2012Applicant: ASTELLAS IRELAND CO., LTD.Inventors: Karin Juliette Van Charldorp, Brigitte Johanna Fanny Bosman, Monique Maria Alida Klaver, Alberto Garcia Hernandez, Tennis Edwin Drogendijk
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Publication number: 20120134934Abstract: Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.Type: ApplicationFiled: November 23, 2011Publication date: May 31, 2012Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Gabriele AMARI, Mauro Riccaboni, Marco Farina
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Publication number: 20120135050Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent formulated for extended-release.Type: ApplicationFiled: January 4, 2012Publication date: May 31, 2012Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: David A. DILL
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Publication number: 20120129885Abstract: 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: May 26, 2011Publication date: May 24, 2012Applicant: TARGACEPT, INC.Inventors: Anatoly A. Mazurov, Teresa Y. Phillips
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Publication number: 20120128805Abstract: Disclosed herein are gustatory and/or olfactory aversion compositions comprising one or more bitterants and appropriate adhesives or tackifiers, and the like, which provide a long-lasting effect. The compositions are useful for behavior modification, especially in animals, such as pets or livestock.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Applicant: Vet Planet, LLCInventors: Richard J. Clement, Kati Clement-Frazier
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Patent number: 8183230Abstract: The present invention is directed to pharmaceutical compositions containing a therapeutically effective amount of an Active Pharmaceutical Ingredient (“API”), a pharmaceutically acceptable cyclodextrin and a pharmaceutically acceptable preservative. The invention is also directed to pharmaceutical compositions of the compounds of Formula (I) wherein R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl and a pharmaceutically acceptable cyclodextrin and preservative. Formula (I): In particular, the invention is directed to pharmaceutical compositions of the compound of Formula 1a, and a pharmaceutically acceptable cyclodextrin and a preservative.Type: GrantFiled: January 17, 2005Date of Patent: May 22, 2012Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Roger C. Adami, Frederick David, Julia Ann Wood
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Patent number: 8183257Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.Type: GrantFiled: January 14, 2009Date of Patent: May 22, 2012Assignee: Glaxo Group LimitedInventors: Dramane I. Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
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Patent number: 8173667Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.Type: GrantFiled: October 19, 2006Date of Patent: May 8, 2012Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Martin Marzi, Bernard Lucien Roy
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Patent number: 8173120Abstract: The present invention relates to a method for substantially preventing a reduction in feed intake in an animal which occurs when said animal is administered an antibiotic, the method comprising administering to an animal in need of prevention of a reduction in feed intake, increasing doses of a composition comprising one or more antibiotics. The present invention also relates to a method for treating laminitis and fermentative acidosis in an animal in need of said treatment, the method comprising administering increasing doses of a composition comprising one or more antibiotics. The present invention further relates to a method for treating equine grass sickness and pulpy kidney in an animal in need of said treatment, the method comprising administering increasing doses of a composition comprising one or more antibiotics.Type: GrantFiled: December 15, 2006Date of Patent: May 8, 2012Assignee: Precision Nutrition Pty LtdInventors: James Baber Rowe, Christopher William Rowe
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Patent number: 8173671Abstract: Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.Type: GrantFiled: December 14, 2010Date of Patent: May 8, 2012Assignee: Alcon Research, Ltd.Inventors: Onkar N. Singh, Suresh C. Dixit, Michael Wall
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Publication number: 20120108545Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters 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: May 19, 2010Publication date: May 3, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Patent number: 8168654Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 20, 2009Date of Patent: May 1, 2012Assignee: Novartis AGInventors: Stephen P Collingwood, Brian Cox, Urs Baettig, Gurdip Bhalay, Nicholas J Devereux
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Publication number: 20120101094Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: December 28, 2011Publication date: April 26, 2012Inventors: Wenge XIE, Brian HERBERT, Truc NGUYEN, Carla GAUSS, Ashok TEHIM
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Publication number: 20120101076Abstract: The invention relates to use of certain quinuclidine carbonate derivatives as cough suppressants, particularly for treating patients with upper respiratory tract infections or asthma.Type: ApplicationFiled: October 11, 2011Publication date: April 26, 2012Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Riccardo Patacchini, Pierangelo Geppetti
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Patent number: 8163731Abstract: A method of reducing the concentration of a chemical or drug substance in the blood plasma that targets the same or similar receptors as the normal neurotransmitters in the central or peripheral nervous system includes titrating an initial peak concentration of the chemical or drug substance in the blood for a predefined dosing period, titrating a lowest concentration level of the chemical or drug substance in the blood immediately before the end of the dosing period, and providing a plurality of subsequent dosing periods where each subsequent dosing period requires administration of a dosing amount of the chemical or drug substance and titrating of the peak concentration and the lowest concentration level to ensure that the lowest concentration level of the chemical or drug substance in the blood plasma for the subsequent dosing period is decreased by not more than five percent of the lowest concentration level of the previous dosing period and where the plurality of dosing periods added together extends theType: GrantFiled: August 20, 2008Date of Patent: April 24, 2012Assignee: Rhodes TechnologiesInventors: Kenneth C. Slater, Brenda E. Richardson, Scott M. Connors, Wei-wei Chang
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Publication number: 20120094942Abstract: Provided herein are methods of modulating hormone concentrations in a subject comprising the administration of a composition comprising a chemosensory receptor ligand, wherein the composition is adapted to deliver the ligand to one or more regions of the intestine of said subject. Also provided are methods directed to the modulation of circulating concentrations of one or more of GLP-1 (total), GLP-1 (active), GLP-2, oxyntomodulin, PYY (total), PYY 3-36, CCK, GIP, insulin, C-peptide, glycentin, uroguanylin amylin, and ghrelin (total), ghrelin (active) and glucagon.Type: ApplicationFiled: October 18, 2011Publication date: April 19, 2012Applicant: Elcelyx Therapeutics, Inc.Inventors: Alain D. BARON, Martin R. Brown, Christopher R.G. Jones, Mark S. Fineman
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Publication number: 20120095039Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.Type: ApplicationFiled: November 21, 2011Publication date: April 19, 2012Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
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Patent number: 8158649Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.Type: GrantFiled: January 8, 2010Date of Patent: April 17, 2012Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Lan Miao
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Patent number: RE43390Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: May 15, 2012Assignees: GlaxoSmithKline LLC, SmithKline Beecham LimitedInventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt