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:
July 22, 2013
Publication date:
January 23, 2014
Applicant:
Targacept,Inc.
Inventors:
Merouane Bencherif, Lisa Benson, Gary Maurice Dull, Nikolai Federov, Gregory J. Gatto, Kristen G. Jordan, Anatoly A. Mazurov, Lan Miao, Julio A. Munoz, Inigo Pfeiffer, Sondra Pfeiffer, Teresa Phillips
Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions, and methods for treating schizophrenia.
Type:
Application
Filed:
January 17, 2012
Publication date:
January 23, 2014
Applicant:
TARGACEPT, INC.
Inventors:
Merouane Bencherif, Geoffrey C. Dunbar, David A. Hosford, Gregory J. Gatto, Terry Hauser, Kristen G. Jordan, Anthony Carl Segreti
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:
February 24, 2011
Date of Patent:
January 21, 2014
Assignee:
Targacept, Inc.
Inventors:
Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve, Craig Harrison Miller
Abstract: The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.
Type:
Grant
Filed:
November 30, 2009
Date of Patent:
January 21, 2014
Assignee:
Targacept, Inc.
Inventors:
Srinivasa Rao Akireddy, Scott R. Breining, Timothy J. Cuthbertson, Gary Maurice Dull, Gregory J. Gatto, John Genus, Philip S. Hammond, Joesph Pike Mitchener, Jr., Julio A. Munoz, Pieter Albert Otten, Daniel Yohannes, Nikolai Fedorov
Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
Type:
Grant
Filed:
November 30, 2009
Date of Patent:
December 10, 2013
Assignee:
Targacept, Inc.
Inventors:
Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Gary Maurice Dull, Craig Harrison Miller, Joseph Pike Mitchener, Jr., Julio A. Munoz, Pieter Albert Otten
Abstract: A method of obtaining chemical or molecular compound information from a document is provided. The method includes applying optical structure recognition to a document and extracting compound structure information from data obtained by applying the optical structure recognition. The method includes applying a text search module to a main body of the document and metadata of the document and extracting one or more chemical names from data obtained by applying the text search module to the main body and to the metadata. The method includes storing, in a database, an identifier, the compound structure information, and the one or more chemical names, wherein at least one method operation is executed through a processor.
Abstract: Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are hydroxybenzoate salts of E-metanicotine-type compounds. The formation of hydroxybenzoate salts of the E-metanicotine compounds is also useful in purifying the E-metanicotine compounds, as the hydroxybenzoate salts tend to crystallize out, leaving impurities such as Z-metanicotine compounds, and compounds where the double bond has migrated, in solution. If desired, the hydroxybenzoate salts can be converted to either the free base (the E-metanicotine) or to another pharmaceutically acceptable salt form.
Type:
Grant
Filed:
October 26, 2011
Date of Patent:
November 12, 2013
Assignee:
Targacept, Inc.
Inventors:
Julio A. Munoz, John Genus, James R. Moore
Abstract: The present invention includes a combination comprising: a) mecamylamine; and b) an ACE inhibitor, an AT2 receptor inhibitor, a renin inhibitor, or a combination thereof.
Abstract: The present invention relates to dexmecamylamine and the use of dexmecamylamine, substantially free of exo-R-mecamylamine, in the treatment of bladder disorders, including overactive bladder.
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 azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. 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.
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:
September 24, 2013
Assignee:
Targacept, Inc.
Inventors:
Merouane Bencherif, Lisa Benson, Gary Maurice Dull, Nikolai Fedorov, Gregory J. Gatto, Kristen G. Jordan, Anatoly A. Mazurov, Lan Miao, Julio A. Munoz, Inigo Pfeiffer, Sondra Pfeiffer, Teresa Phillips
Abstract: The present invention relates to method of treating constipation and enhancing colonic motility by administration of 5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
March 4, 2011
Publication date:
September 12, 2013
Applicant:
TARGACEPT, INC.
Inventors:
Steven M. Toler, David Hosford, Patrick M. Lippiello, Geoffrey Charles Dunbar, William Scott Caldwell, Parviz Hamedani, Merouane Bencherif
Abstract: An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.
Type:
Application
Filed:
May 19, 2011
Publication date:
August 29, 2013
Applicants:
TARGACEPT, INC., ASTRAZENECA AB
Inventors:
Gary Maurice Dull, John Genus, Tommi Ratilainen, Per Olof Ryberg, Janna Hellstrom, Niklas Wahlstrom, Thomas Wannman
Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, 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:
January 25, 2010
Date of Patent:
July 2, 2013
Assignee:
Targacept, Inc.
Inventors:
Merouane Bencherif, Nikolai Fedorov, Terry Hauser, Kristen Jordan, Sharon Rae Letchworth, Anatoly Mazurov, Julio A. Munoz, Jason Speake, Daniel Yohannes
Abstract: Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
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).
Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, 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:
Application
Filed:
December 3, 2010
Publication date:
December 6, 2012
Applicant:
Targacept, Inc.
Inventors:
Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
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).
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