Patents Assigned to Targacept, Inc.
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Publication number: 20110059947Abstract: The present invention relates to a synergistic combination of an alpha7 (?7) nicotinic agonist and an antipsychotic agent.Type: ApplicationFiled: February 13, 2009Publication date: March 10, 2011Applicant: Targacept, Inc.Inventors: Merouane Bencherif, Gregory J. Gatto, Terry Hauser, Kristen G. Jordan, Sharon R. Letchworth
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Patent number: 7897611Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.Type: GrantFiled: February 26, 2010Date of Patent: March 1, 2011Assignee: Targacept, Inc.Inventors: Balwinder Singh Bhatti, Scott R. Breining, Gregory D. Hawkins, Anatoly Mazurov, Lan Miao, Craig Harrison Miller, Teresa Y. Phillips
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Publication number: 20100286282Abstract: 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: ApplicationFiled: January 4, 2010Publication date: November 11, 2010Applicant: Targacept, Inc.Inventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
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Publication number: 20100267776Abstract: 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: ApplicationFiled: January 6, 2010Publication date: October 21, 2010Applicant: Targacept, Inc.Inventors: Arielle Genevois-Borella, Craig H. Miller
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Publication number: 20100249196Abstract: Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts 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.Type: ApplicationFiled: May 8, 2007Publication date: September 30, 2010Applicants: ASTRAZENECA AB, TARGACEPT, INC.Inventors: Martin Hans Bohlin, Gary M. Dull, Caroline Eriksson, Craig H. Miller, Julio A. Munoz, Tesfai Sebhatu
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Publication number: 20100247617Abstract: The present invention generally relates to the transdermal administration of (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof. The transdermal administration can be effected using transdermal drug delivery devices, semi-solid dosage forms, or iontophoresis. The drug delivery devices and/or semi-solid dosage forms can provide instantaneous release, sustained release, or combinations thereof, and can include permeation enhancers and other components to assist in drug transport across the dermis, especially the epidermis. The compositions can be used to treat and/or prevent any indication which the active ingredients are capable of treating and preventing, but deliver (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof, in an efficacious manner. Disorders that can be treated and/or prevented include central nervous system disorders, addictions, pain, and inflammation.Type: ApplicationFiled: July 30, 2008Publication date: September 30, 2010Applicants: TARGACEPT, INC., ASTRAZENECA ABInventors: Merouane Bencherif, John W. James, Michael G. Williams, Johannes Antonius Maria Neelissen
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Publication number: 20100240696Abstract: 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.Type: ApplicationFiled: June 4, 2010Publication date: September 23, 2010Applicant: 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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Publication number: 20100240689Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly 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. The compounds and compositions can also be used to alleviate pain.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Applicant: Targacept, Inc.Inventors: Balwinder Bhatti, Scott R. Breining, Phillip S. Hammond, Jozef Klucik, Yun-De Xiao
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Patent number: 7790757Abstract: 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: October 31, 2007Date of Patent: September 7, 2010Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Publication number: 20100222395Abstract: 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: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Publication number: 20100204481Abstract: 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: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Applicant: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Publication number: 20100197720Abstract: The present invention relates to amide and urea derivatives of heteroaryl-substituted diazatricycloalkanes, pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the ?7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the ?7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N-arylcarbamoyl) (urea type derivative) group.Type: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Applicant: Targacept, Inc.Inventors: Anatoly Mazurov, Lan Miao, Jozef Klucik
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Patent number: 7767193Abstract: 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.Type: GrantFiled: June 20, 2005Date of Patent: August 3, 2010Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Lan Miao
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Publication number: 20100179183Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.Type: ApplicationFiled: January 12, 2010Publication date: July 15, 2010Applicant: Targacept, Inc.Inventors: Balwinder S. Bhatti, Gregory D. Hawkins
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Patent number: 7754189Abstract: 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 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: February 6, 2008Date of Patent: July 13, 2010Assignee: 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: 7754708Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly 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. The compounds and compositions can also be used to alleviate pain.Type: GrantFiled: May 9, 2008Date of Patent: July 13, 2010Assignee: Targacept, Inc.Inventors: Balwinder Bhatti, Scott R. Breining, Philip S. Hammond, Jozef Klucik, Yun-De Xiao
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Publication number: 20100173968Abstract: 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: ApplicationFiled: March 27, 2008Publication date: July 8, 2010Applicant: TARGACEPT, INC.Inventors: Philip S. Hammond, Anatoly Mazurov, Yun-De Xiao, Srinivasa V. Murthy, Srinivisa Rao Akireddy
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Publication number: 20100173932Abstract: 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: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: Targacept, Inc.Inventors: Anatoly 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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Publication number: 20100160390Abstract: 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: ApplicationFiled: March 2, 2010Publication date: June 24, 2010Applicant: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Patent number: RE41439Abstract: The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(3-thienyl)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.Type: GrantFiled: February 5, 2007Date of Patent: July 13, 2010Assignee: Targacept, Inc.Inventors: Craig Harrison Miller, Gary Maurice Dull, Lan Miao, Dwo Lynm, Jeffrey Daniel Schmitt, Thomas Jeff Clark