Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
  • Patent number: 8383817
    Abstract: Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m=1 to 5; n=1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: February 26, 2013
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Amy Hauck Newman, Mu-Fa Zou, Jonathan L. Katz
  • Publication number: 20130045951
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: CARDIOXYL PHARMACEUTICALS, INC.
    Inventor: CARDIOXYL PHARMACEUTICALS, INC.
  • Publication number: 20130045988
    Abstract: Described herein is a combination comprising at least one 5-HT4 receptor agonist and at least one phosphodiesterase 4 (PDE4) inhibitor, and methods and uses thereof in the prevention and/or treatment of one or more disorders in which an increased acetylcholine release is desired; for example in the prevention and/or treatment of gastrointestinal disorders, urinary disorders, and/or respiratory disorders.
    Type: Application
    Filed: August 17, 2012
    Publication date: February 21, 2013
    Inventors: Romain Adelin Lefebvre, Joris Herman De Maeyer
  • Publication number: 20130039885
    Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.
    Type: Application
    Filed: June 19, 2012
    Publication date: February 14, 2013
    Applicant: NEW YORK UNIVERSITY
    Inventors: Victor J. TORRES, Derya UNUTMAZ, Francis ALONZO, III
  • Publication number: 20130040985
    Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: January 14, 2011
    Publication date: February 14, 2013
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Gordon Munro, Elsebet Østergaard Nielsen, Karin Sandager Nielsen
  • Publication number: 20130040986
    Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
    Type: Application
    Filed: October 15, 2012
    Publication date: February 14, 2013
    Inventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
  • Patent number: 8367698
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: February 5, 2013
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20130023496
    Abstract: The present invention discloses a novel combination therapy for HIV-1 treatment relying on a combination of at least one CCR5 antagonist, at least one HIV-1 protease inhibitor and at least one pharmacokinetic enhancer of said at least one CCR5 antagonist and/or at least one HIV-1 protease inhibitor. The combination is intended for use in oral treatment of a disorder selected from the group consisting of HIV-1 infection, retroviral infections genetically related to HIV and AIDS, in a treatment-naïve patient infected with CCR5 tropic HIV-1 virus.
    Type: Application
    Filed: March 30, 2011
    Publication date: January 24, 2013
    Inventors: Randy Tressler, Hernan Valdez
  • Patent number: 8357686
    Abstract: The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description as well as to pharmaceutical compositions and medical treatments employing these compounds.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: January 22, 2013
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
  • Publication number: 20130018023
    Abstract: The invention provides a composition comprising benzoyl peroxide or derivative thereof; and at least one antibiotic compound selected from pseudomonic acid, retapamulin, fusidic acid and derivatives thereof; methods and uses of a composition of the invention in the treatment of at least one topical disease or disorder and kits comprising a composition of the invention.
    Type: Application
    Filed: March 24, 2011
    Publication date: January 17, 2013
    Applicant: SOL-GEL TECHNOLOGIES LTD.
    Inventors: Ofer Toledano, Karine Neimann, Braham Shroot
  • Publication number: 20120328704
    Abstract: The present invention relates to newly identified genes that encode proteins that are involved in the synthesis of L-ascorbic acid (hereinafter also referred to as Vitamin C). The invention also features polynucleotides comprising the full-length polynucleotide sequences of the novel genes and fragments thereof, the novel polypeptides encoded by the polynucleotides and fragments thereof, as well as their functional equivalents. The present invention also relates to the use of said polynucleotides and polypeptides as biotechnological tools in the production of Vitamin C from microorganisms, whereby a modification of said polynucleotides and/or encoded polypeptides has a direct or indirect impact on yield, production, and/or efficiency of production of the fermentation product in said microorganism. Also included are methods/processes of using the polynucleotides and modified polynucleotide sequences to transform host microorganisms.
    Type: Application
    Filed: September 5, 2012
    Publication date: December 27, 2012
    Applicant: Jagotec AG
    Inventor: Rudi Mueller-Walz
  • Publication number: 20120329828
    Abstract: The invention provides novel cocaine analogs. The invention also provides a method of preparing cocaine analogs with control over the substituents installed at the C-1, C-2, C-3, C-4 and N-8 positions of the tropane bicyclic scaffold. The invention further provides methods of providing anesthesia, blocking reuptake of a monoamine neurotransmitter, and treating depression, by administering to a subject in need of such treatment a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 27, 2012
    Applicants: New York University, Temple University - Of The Commonwealth System of Higher Education
    Inventors: Franklin A. Davis, Naresh Theddu, Maarten E. A. Reith
  • Patent number: 8338614
    Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: December 25, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
  • Patent number: 8337817
    Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.
    Type: Grant
    Filed: December 25, 2007
    Date of Patent: December 25, 2012
    Assignee: Shin Nippon Biomedical Laboratories, Ltd.
    Inventors: Ryoichi Nagata, Shunji Haruta
  • Publication number: 20120322804
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Application
    Filed: May 3, 2012
    Publication date: December 20, 2012
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20120322719
    Abstract: 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: Application
    Filed: June 14, 2012
    Publication date: December 20, 2012
    Applicant: The Feinstein Institute For Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Patent number: 8334303
    Abstract: Disclosed is a novel polymorphic form of the compound of formula (I) also known as mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate, a process for the preparation of the polymorphic form, pharmaceutical compositions comprising the polymorphic form, and the use of the polymorphic form in medicine, particularly in antibacterial therapy.
    Type: Grant
    Filed: February 28, 2006
    Date of Patent: December 18, 2012
    Assignee: Glazo Group Limited
    Inventors: Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
  • Publication number: 20120309785
    Abstract: The subject invention provides materials and methods for treating neurodegenerative diseases. In one embodiment of the invention, a cysteamine compound is administered to a patient to treat Parkinson's Disease and/or complications associated with Parkinson's Disease. In another embodiment, a cysteamine compound is administered to a patient to prevent the onset of Parkinson's Disease in an at-risk patient and/or treat or prevent the onset of Parkinson's Disease-associated symptoms.
    Type: Application
    Filed: December 5, 2011
    Publication date: December 6, 2012
    Inventor: Bill Piu Chan
  • Publication number: 20120302541
    Abstract: 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: Application
    Filed: October 28, 2010
    Publication date: November 29, 2012
    Inventors: 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
  • Publication number: 20120294943
    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: July 27, 2012
    Publication date: November 22, 2012
    Applicant: Wellesley Pharmaceuticals, LLC
    Inventor: David A. DILL
  • Publication number: 20120295877
    Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
    Type: Application
    Filed: July 23, 2010
    Publication date: November 22, 2012
    Inventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
  • Publication number: 20120288561
    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: July 27, 2012
    Publication date: November 15, 2012
    Applicant: WELLESLEY PHARMACEUTICALS, LLC
    Inventor: David A. Dill
  • Publication number: 20120289543
    Abstract: 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: Application
    Filed: May 9, 2012
    Publication date: November 15, 2012
    Applicant: THERAVIDA, INC.
    Inventors: Mehdi PABORJI, Wendy Jade Limayo HERNANDEZ, Kenneth L. DUCHIN, Roger S. FLUGEL
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Publication number: 20120283240
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: June 26, 2012
    Publication date: November 8, 2012
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • Publication number: 20120276050
    Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.
    Type: Application
    Filed: March 16, 2010
    Publication date: November 1, 2012
    Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
  • Patent number: 8299062
    Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: October 30, 2012
    Inventor: Franklin Volvovitz
  • Publication number: 20120264808
    Abstract: The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions).
    Type: Application
    Filed: June 7, 2012
    Publication date: October 18, 2012
    Inventors: D. James Surmeier, Michelle Day, Jun Ding, Savio Chan, Jamie Guzman, Jeff Mercer, Tatiana Tkatch, Zhongfeng Wang, Ema Ilijic
  • Publication number: 20120264779
    Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 1, 2012
    Publication date: October 18, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Publication number: 20120251632
    Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Inventors: Kazuko MATSUDA, Yuichi Iwaki, Kirk W. Johnson
  • Publication number: 20120252833
    Abstract: Sustained-release oral pharmaceutical compositions and methods of use, wherein the compositions are in a single dosage form and include an amine-containing compound (including salts thereof), a salt of a non-steroidal anti-inflammatory drug (NSAID), and a hydrophilic matrix.
    Type: Application
    Filed: December 31, 2009
    Publication date: October 4, 2012
    Applicant: UPSHER-SMITH LABORATORIES, INC.
    Inventors: Christian F. Wertz, James S. Jensen, Victoria Ann O'Neill, Sean B. Mahoney, Stephen M. Berge
  • 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: 20120238600
    Abstract: The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I): The compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 20, 2012
    Applicant: SANOFI
    Inventors: Yong Mi CHOI-SLEDESKI, Guyan LIANG, Patrick Wai-Kwok SHUM
  • 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: 8268863
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: September 18, 2012
    Assignee: Theravance, Inc.
    Inventors: Daisuke Roland Saito, Daniel D. Long, John R. Jacobsen
  • Publication number: 20120232048
    Abstract: A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.
    Type: Application
    Filed: April 24, 2012
    Publication date: September 13, 2012
    Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
  • Publication number: 20120232109
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 13, 2012
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20120232025
    Abstract: Prolonged administration of subanesthetic dosages of ketamine, which suppresses activity at NMDA receptors, can provide a damaged central nervous system with an opportunity to use its innate healing processes to “reset” NMDA receptors which were pushed into an unwanted hyper-sensitized state by unusually high activity. However, such treatments can cause permanent brain damage, if the ketamine dosage is too heavy or prolonged. Certain types of “safener” drugs have previously been identified, which can block or at least reduce those unwanted side effects. It is disclosed that if two classes of safener drugs are combined, which will simultaneously suppress activity at both (i) muscarinic acetylcholine receptors, and (ii) the kainate and AMPA classes of glutamate receptors, those safener drug combinations can provide exceptionally potent and reliable safening activity, which can enable the safe use of potent NMDA antagonist drugs for a number of highly beneficial purposes.
    Type: Application
    Filed: September 8, 2011
    Publication date: September 13, 2012
    Inventor: John W. Olney
  • Patent number: 8263618
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: September 11, 2012
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, Timothy J. Church, John R. Jacobsen, Lan Jiang, Daisuke Roland Saito, Ioanna Stergiades, Priscilla M. Van Dyke
  • Patent number: 8263617
    Abstract: This invention relates to novel chromen-2-one derivatives of Formula (I) useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: September 11, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, John Paul Redrobe, Gunnar M. Olsen, Elsebet Østergaard Nielsen
  • Publication number: 20120225884
    Abstract: The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: February 27, 2012
    Publication date: September 6, 2012
    Inventors: Karlheinz Baumann, Luke Green, Anja Limberg, Thomas Luebbers, Andrew Thomas
  • Publication number: 20120214817
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • Publication number: 20120214805
    Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Application
    Filed: October 28, 2010
    Publication date: August 23, 2012
    Inventors: Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
  • Publication number: 20120207817
    Abstract: The invention found that overexpression and activation of ?9-nAChR are associated with tumorigenesis of breast cancer and create a number of small interfering RNAs to inhibit the expression of ?9-nAChR so as to inhibit breast cancer. Therefore, the invention provides small interfering RNAs (siRNAs) for inhibiting expression of ?9-nAChR so as to inhibit breast cancer, methods to prevent/inhibit/treat malignant progression of nicotine-derived-compound-induced breast cancer and method of determining malignant level of such breast cancer.
    Type: Application
    Filed: February 14, 2011
    Publication date: August 16, 2012
    Applicant: TAIPEI MEDICAL UNIVERSITY
    Inventors: Chia-Hwa Lee, Ching-Shui Huang, Ching-Shyang Chen, Shih-Hsin Tu, Ying-Jan Wang, Yu-Jia Chang, Ka-Wai Tam, Po-Li Wei, Tzu-Chun Cheng, Jan-Show Chu, Li-Ching Chen, Chih-Hsiung Wu, Yuan-Soon Ho
  • Publication number: 20120208841
    Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
    Type: Application
    Filed: April 4, 2012
    Publication date: August 16, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
  • Publication number: 20120202796
    Abstract: This invention relates to a method for combating adverse effects arising from antipsychotic treatment. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of formula I and an antipsychotic drug.
    Type: Application
    Filed: September 2, 2009
    Publication date: August 9, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Jørgen Scheel-Krüger, Henrik Björk Hansen
  • 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
  • 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
  • Publication number: 20120172354
    Abstract: The present invention relates to N-phenyl-1-(4-pyridinyl)-1H-pyrazol-3-amine derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to formula (I) Wherein R1, R2, R3, R4, R5, R6 have the meaning defined in the claims. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
    Type: Application
    Filed: September 16, 2010
    Publication date: July 5, 2012
    Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Frans Alfons Maria Van den Keybus, Yves Emiel Maria Van Roosbroeck
  • Publication number: 20120172393
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: September 14, 2010
    Publication date: July 5, 2012
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior