Quinuclidines (including Unsaturation) Patents (Class 514/305)
  • Publication number: 20120277216
    Abstract: 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: Application
    Filed: December 29, 2009
    Publication date: November 1, 2012
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: 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
  • Publication number: 20120276018
    Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 1, 2012
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele AMARI, Mauro Riccaboni, Daniele De Zani
  • Publication number: 20120270857
    Abstract: 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: Application
    Filed: June 30, 2010
    Publication date: October 25, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Patent number: 8288409
    Abstract: 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: Grant
    Filed: February 3, 2009
    Date of Patent: October 16, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
  • Publication number: 20120258964
    Abstract: 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: Application
    Filed: March 6, 2012
    Publication date: October 11, 2012
    Applicant: Bayer Schering Pharma AG
    Inventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
  • Patent number: 8283470
    Abstract: 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: Grant
    Filed: August 31, 2009
    Date of Patent: October 9, 2012
    Assignee: 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
  • Patent number: 8278301
    Abstract: 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: Grant
    Filed: May 15, 2009
    Date of Patent: October 2, 2012
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Zhicai Yang
  • Publication number: 20120244221
    Abstract: 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: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Publication number: 20120237574
    Abstract: 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: Application
    Filed: June 4, 2012
    Publication date: September 20, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Patent number: 8263619
    Abstract: 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: Grant
    Filed: December 4, 2009
    Date of Patent: September 11, 2012
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Truc Minh Nguyen, Jianguo Ma, Carla Maria Gauss, Ashok Tehim
  • Publication number: 20120220557
    Abstract: 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: Application
    Filed: February 10, 2012
    Publication date: August 30, 2012
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Annamaria Soliani RASCHINI, Emilio Lutero
  • Publication number: 20120220599
    Abstract: 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: Application
    Filed: May 2, 2012
    Publication date: August 30, 2012
    Inventors: Dominik FEUERBACH, Konstanze HURTH, Timothy John RITCHIE
  • Publication number: 20120202786
    Abstract: 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: Application
    Filed: April 16, 2012
    Publication date: August 9, 2012
    Applicant: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • Publication number: 20120202819
    Abstract: 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: Application
    Filed: September 27, 2010
    Publication date: August 9, 2012
    Applicant: Merck Sharp & Dohme Corporation
    Inventors: Scott D. Edmondson, Mary Struthers SinhaRroy, Hiroshi Nagabukuro, William S. Denney, Tara F. Frenki
  • Publication number: 20120202842
    Abstract: 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: Application
    Filed: November 4, 2011
    Publication date: August 9, 2012
    Applicant: Bayer Schering Pharma AG
    Inventors: Martin Hendrix, Frank-Gerhard Böß, Christina Erb, Timo Fleßner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
  • Patent number: 8236857
    Abstract: 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: Grant
    Filed: March 19, 2012
    Date of Patent: August 7, 2012
    Assignee: Wellesley Pharmaceuticals, LLC
    Inventor: David A. Dill
  • Patent number: 8236856
    Abstract: 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: Grant
    Filed: March 19, 2012
    Date of Patent: August 7, 2012
    Assignee: Wellesley Pharmaceuticals, LLC
    Inventor: David A. Dill
  • Publication number: 20120190648
    Abstract: 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: Application
    Filed: July 23, 2010
    Publication date: July 26, 2012
    Inventors: Philippe Jubault, Jean-Charles Quirion, Gerald Lemonnier, Cedric Lion
  • Patent number: 8227484
    Abstract: Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: July 24, 2012
    Assignee: Avanir Pharmaceuticals, Inc.
    Inventors: Gerald Yakatan, James Berg, Laura Pope, Richard Alan Smith
  • Publication number: 20120183568
    Abstract: 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: Application
    Filed: December 13, 2011
    Publication date: July 19, 2012
    Inventor: Sarah Hamm-Alvarez
  • Publication number: 20120183605
    Abstract: 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: Application
    Filed: September 14, 2011
    Publication date: July 19, 2012
    Inventors: Kristin Arnold, Matthew W. Davis, Suman Wason, Siva Rama K. Nutalapati
  • Patent number: 8222294
    Abstract: 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: Grant
    Filed: February 14, 2005
    Date of Patent: July 17, 2012
    Assignee: Bioproject
    Inventors: Jean-Charles Schwartz, Jeanne-Marie Lecomte
  • Patent number: 8222274
    Abstract: [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: Grant
    Filed: February 19, 2007
    Date of Patent: July 17, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
  • Publication number: 20120164192
    Abstract: 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: Application
    Filed: March 19, 2012
    Publication date: June 28, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Publication number: 20120164193
    Abstract: 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: Application
    Filed: March 19, 2012
    Publication date: June 28, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Patent number: 8207192
    Abstract: 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: Grant
    Filed: March 9, 2009
    Date of Patent: June 26, 2012
    Inventor: Shuqiang Zhao
  • Patent number: 8207193
    Abstract: 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: Grant
    Filed: November 13, 2007
    Date of Patent: June 26, 2012
    Assignee: Astrazeneca AB
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete
  • Publication number: 20120157464
    Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.
    Type: Application
    Filed: July 21, 2010
    Publication date: June 21, 2012
    Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
  • Publication number: 20120157491
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Application
    Filed: February 22, 2012
    Publication date: June 21, 2012
    Applicant: Glaxo Group Limited
    Inventors: Dramane I. Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Publication number: 20120157490
    Abstract: 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: Application
    Filed: September 19, 2011
    Publication date: June 21, 2012
    Applicant: Bayer HealthCare AG
    Inventors: Timo FLEßNER, Frank-Gerhard BÖß, Frank-Thorsten HAFNER, Joachim LUITHLE, Christoph METHFESSEL, Leila TELAN
  • Publication number: 20120141554
    Abstract: 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: Application
    Filed: January 4, 2012
    Publication date: June 7, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Publication number: 20120142725
    Abstract: 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: Application
    Filed: November 4, 2009
    Publication date: June 7, 2012
    Applicant: ASTELLAS IRELAND CO., LTD.
    Inventors: Karin Juliette Van Charldorp, Brigitte Johanna Fanny Bosman, Monique Maria Alida Klaver, Alberto Garcia Hernandez, Tennis Edwin Drogendijk
  • Publication number: 20120134934
    Abstract: Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 31, 2012
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Gabriele AMARI, Mauro Riccaboni, Marco Farina
  • Publication number: 20120135050
    Abstract: 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: Application
    Filed: January 4, 2012
    Publication date: May 31, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. DILL
  • Publication number: 20120129885
    Abstract: 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: Application
    Filed: May 26, 2011
    Publication date: May 24, 2012
    Applicant: TARGACEPT, INC.
    Inventors: Anatoly A. Mazurov, Teresa Y. Phillips
  • Publication number: 20120128805
    Abstract: 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: Application
    Filed: January 30, 2012
    Publication date: May 24, 2012
    Applicant: Vet Planet, LLC
    Inventors: Richard J. Clement, Kati Clement-Frazier
  • Patent number: 8183230
    Abstract: 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: Grant
    Filed: January 17, 2005
    Date of Patent: May 22, 2012
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Roger C. Adami, Frederick David, Julia Ann Wood
  • Patent number: 8183257
    Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: May 22, 2012
    Assignee: Glaxo Group Limited
    Inventors: Dramane I. Laine, Michael R. Palovich, Brent W. McCleland, Christopher E. Neipp, Sonia M. Thomas
  • Patent number: 8173667
    Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.
    Type: Grant
    Filed: October 19, 2006
    Date of Patent: May 8, 2012
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Martin Marzi, Bernard Lucien Roy
  • Patent number: 8173120
    Abstract: 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: Grant
    Filed: December 15, 2006
    Date of Patent: May 8, 2012
    Assignee: Precision Nutrition Pty Ltd
    Inventors: James Baber Rowe, Christopher William Rowe
  • Patent number: 8173671
    Abstract: Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: May 8, 2012
    Assignee: Alcon Research, Ltd.
    Inventors: Onkar N. Singh, Suresh C. Dixit, Michael Wall
  • Publication number: 20120108545
    Abstract: 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: Application
    Filed: May 19, 2010
    Publication date: May 3, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
  • Patent number: 8168654
    Abstract: 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: Grant
    Filed: October 20, 2009
    Date of Patent: May 1, 2012
    Assignee: Novartis AG
    Inventors: Stephen P Collingwood, Brian Cox, Urs Baettig, Gurdip Bhalay, Nicholas J Devereux
  • Publication number: 20120101094
    Abstract: 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: Application
    Filed: December 28, 2011
    Publication date: April 26, 2012
    Inventors: Wenge XIE, Brian HERBERT, Truc NGUYEN, Carla GAUSS, Ashok TEHIM
  • Publication number: 20120101076
    Abstract: 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: Application
    Filed: October 11, 2011
    Publication date: April 26, 2012
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Riccardo Patacchini, Pierangelo Geppetti
  • Patent number: 8163731
    Abstract: 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 the
    Type: Grant
    Filed: August 20, 2008
    Date of Patent: April 24, 2012
    Assignee: Rhodes Technologies
    Inventors: Kenneth C. Slater, Brenda E. Richardson, Scott M. Connors, Wei-wei Chang
  • Publication number: 20120094942
    Abstract: 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: Application
    Filed: October 18, 2011
    Publication date: April 19, 2012
    Applicant: Elcelyx Therapeutics, Inc.
    Inventors: Alain D. BARON, Martin R. Brown, Christopher R.G. Jones, Mark S. Fineman
  • Publication number: 20120095039
    Abstract: 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: Application
    Filed: November 21, 2011
    Publication date: April 19, 2012
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
  • Patent number: 8158649
    Abstract: 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: Grant
    Filed: January 8, 2010
    Date of Patent: April 17, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Lan Miao
  • Patent number: RE43390
    Abstract: 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: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt