Patents Represented by Attorney Amy H. Fix
  • Patent number: 8288420
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: October 16, 2012
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishakumar Basawannappa Hadimani, Haeil Park, Jared Miller Wagner, Peter A. Crooks
  • Patent number: 8268860
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: September 18, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Lan Miao, Yun-De Xiao, Philip S. Hammond, Craig H. Miller, Srinivisa Rao Akireddy, V. Srinivasa Murthy, Regina C. Whitaker, Scott R. Breining, Matt S. Melvin
  • Patent number: 8198296
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide, ketone, and ester compounds prepared from certain azabicycloalkane carboxylic acids. The resulting compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the ?4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, such as those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: June 12, 2012
    Assignee: Targacept, Inc.
    Inventors: Philip S. Hammond, Anatoly Mazurov, Yun-De Xiao, Srinivasa V. Murthy, Srinivisa Rao Akireddy
  • 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: 8153821
    Abstract: The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: April 10, 2012
    Assignee: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Craig Harrison Miller, Joseph Pike Mitchener, Jr.
  • Patent number: 8143272
    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: December 11, 2009
    Date of Patent: March 27, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Lan Miao
  • Patent number: 8124618
    Abstract: The present invention relates to pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the ?7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: February 28, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
  • Patent number: 8124619
    Abstract: The present invention relates to pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the ?7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: February 28, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
  • Patent number: 8124620
    Abstract: The present invention relates to pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the ?7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: February 28, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
  • Patent number: 8119659
    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: Grant
    Filed: May 26, 2011
    Date of Patent: February 21, 2012
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, John Genus, Jacob Mathew
  • Patent number: 8114889
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4?2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: February 14, 2012
    Assignee: Targacept, Inc.
    Inventors: Anatoly Mazurov, Lan Miao, Yun-De Xiao
  • Patent number: 8084462
    Abstract: The present invention relates to the pharmaceutical compositions incorporating compounds capable of affecting nicotinic acetylcholinergic receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the ?7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: December 27, 2011
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao, Angela S. Seamans, Teresa Youngpeter Phillips, Jeffrey Daniel Schmitt, Craig Harrison Miller
  • Patent number: 8063068
    Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: November 22, 2011
    Assignee: Targacept, Inc.
    Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Craig Harrison Miller, Arielle Genevois-Borella, Marc Capet, Michel Cheve
  • Patent number: 8026283
    Abstract: A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition.
    Type: Grant
    Filed: January 4, 2010
    Date of Patent: September 27, 2011
    Assignee: University of South Florida
    Inventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
  • Patent number: 7981906
    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: Grant
    Filed: August 1, 2008
    Date of Patent: July 19, 2011
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, Anatoly A. Mazurov, Teresa Y. Phillips
  • Patent number: 7241756
    Abstract: A method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in need thereof.
    Type: Grant
    Filed: June 1, 2006
    Date of Patent: July 10, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Jonathan Robert Sanders Arch, James Martin Lenhard
  • Patent number: 7196201
    Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility
    Type: Grant
    Filed: June 26, 2002
    Date of Patent: March 27, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, David N Deaton
  • Patent number: 7189851
    Abstract: The present invention relates to novel fused heterocyclic ring system compounds and methods for their use in the treatment and prevention of diseases or conditions.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: March 13, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Ashok Bhandari, Eric Eugene Boros, David John Cowan, Anthony Louis Handlon, Clifton Earl Hyman, Jeffrey Alan Oplinger, Michael Howard Rabinowitz, Philip Stewart Turnbull
  • Patent number: 7186717
    Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: March 6, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
  • Patent number: 7183290
    Abstract: The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.
    Type: Grant
    Filed: June 26, 2002
    Date of Patent: February 27, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Curt Dale Haffner, Darryl Lynn McDougald, James Martin Lenhard