Patents Represented by Attorney Amy H. Fix
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Patent number: 8288420Abstract: 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: GrantFiled: May 10, 2010Date of Patent: October 16, 2012Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishakumar Basawannappa Hadimani, Haeil Park, Jared Miller Wagner, Peter A. Crooks
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Patent number: 8268860Abstract: 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: GrantFiled: March 15, 2010Date of Patent: September 18, 2012Assignee: 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
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Patent number: 8198296Abstract: 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: GrantFiled: March 27, 2008Date of Patent: June 12, 2012Assignee: Targacept, Inc.Inventors: Philip S. Hammond, Anatoly Mazurov, Yun-De Xiao, Srinivasa V. Murthy, Srinivisa Rao Akireddy
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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: 8153821Abstract: 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: GrantFiled: November 30, 2009Date of Patent: April 10, 2012Assignee: Targacept, Inc.Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Craig Harrison Miller, Joseph Pike Mitchener, Jr.
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Patent number: 8143272Abstract: 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: December 11, 2009Date of Patent: March 27, 2012Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Lan Miao
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Patent number: 8124618Abstract: 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: GrantFiled: August 24, 2010Date of Patent: February 28, 2012Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
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Patent number: 8124619Abstract: 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: GrantFiled: August 24, 2010Date of Patent: February 28, 2012Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
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Patent number: 8124620Abstract: 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: GrantFiled: August 24, 2010Date of Patent: February 28, 2012Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao
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Patent number: 8119659Abstract: The present invention relates to (2S,3R)-N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.Type: GrantFiled: May 26, 2011Date of Patent: February 21, 2012Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, John Genus, Jacob Mathew
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Patent number: 8114889Abstract: 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: GrantFiled: November 1, 2007Date of Patent: February 14, 2012Assignee: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Yun-De Xiao
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Patent number: 8084462Abstract: 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: GrantFiled: June 4, 2010Date of Patent: December 27, 2011Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao, Angela S. Seamans, Teresa Youngpeter Phillips, Jeffrey Daniel Schmitt, Craig Harrison Miller
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Patent number: 8063068Abstract: 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: GrantFiled: January 5, 2009Date of Patent: November 22, 2011Assignee: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Craig Harrison Miller, Arielle Genevois-Borella, Marc Capet, Michel Cheve
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Patent number: 8026283Abstract: 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: GrantFiled: January 4, 2010Date of Patent: September 27, 2011Assignee: University of South FloridaInventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
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Patent number: 7981906Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide, novel salt forms thereof, methods for its preparation, novel intermediates, and methods for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central and autonomic nervous systems.Type: GrantFiled: August 1, 2008Date of Patent: July 19, 2011Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, Anatoly A. Mazurov, Teresa Y. Phillips
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Patent number: 7241756Abstract: 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: GrantFiled: June 1, 2006Date of Patent: July 10, 2007Assignee: SmithKline Beecham CorporationInventors: Jonathan Robert Sanders Arch, James Martin Lenhard
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Patent number: 7196201Abstract: 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 utilityType: GrantFiled: June 26, 2002Date of Patent: March 27, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, Amarjit Sab Randhawa, Steven Michael Reister, David N Deaton
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Patent number: 7189851Abstract: 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: GrantFiled: February 24, 2003Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: Ashok Bhandari, Eric Eugene Boros, David John Cowan, Anthony Louis Handlon, Clifton Earl Hyman, Jeffrey Alan Oplinger, Michael Howard Rabinowitz, Philip Stewart Turnbull
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Patent number: 7186717Abstract: 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: GrantFiled: June 6, 2002Date of Patent: March 6, 2007Assignee: SmithKline Beecham CorporationInventors: 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
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Patent number: 7183290Abstract: 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: GrantFiled: June 26, 2002Date of Patent: February 27, 2007Assignee: SmithKline Beecham CorporationInventors: Curt Dale Haffner, Darryl Lynn McDougald, James Martin Lenhard