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1.发明授权3-PYRIDYL-1-AZABICYCLOALKANE DERIVATIVES FOR PREVENTION AND TREATMENT OF CNS DISORDERS 失效3-吡啶基-1-氮杂双环衍生物对中枢神经系统疾病的治疗
公开(公告)号：EP0994875B1
公开(公告)日：2004-03-10
申请号：EP98918598.8
申请日：1998-04-22
发明人： CALDWELL, William, Scott , BENCHERIF, Merouane , DULL, Gary, Maurice , CROOKS, Peter, Anthony , LIPPIELLO, Patrick, Michael , BHATTI, Balwinder, Singh , DEO, Niranjan, Madhukar , RAVARD, Alain
IPC分类号： C07D453/02 , A61K31/44 , C07D487/08
CPC分类号： C07D487/08 , C07D453/02
摘要： 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 an endo or exo form of a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2] octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane.
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2.发明公开3-PYRIDYL-1-AZA-BICYCLO-ALKANE DERIVATIVES FOR PREVENTION AND TREATMENT OF CNS DISORDERS 失效3-吡啶基-1-氮杂双环衍生物对中枢神经系统疾病的治疗
公开(公告)号：EP0994875A1
公开(公告)日：2000-04-26
申请号：EP98918598.8
申请日：1998-04-22
发明人： CALDWELL, William, Scott , BENCHERIF, Merouane , DULL, Gary, Maurice , CROOKS, Peter, Anthony , LIPPIELLO, Patrick, Michael , BHATTI, Balwinder, Singh , DEO, Niranjan, Madhukar , RAVARD, Alain
IPC分类号： C07D453/02 , A61K31/44 , C07D487/08
CPC分类号： C07D487/08 , C07D453/02
摘要： 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 an endo or exo form of a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2] octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane.
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3.发明公开PHARMACEUTICAL COMPOSITIONS FOR PREVENTION AND TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 失效药物PROPHYZAXE和中枢神经系统疾病的治疗
公开(公告)号：EP0801646A1
公开(公告)日：1997-10-22
申请号：EP95944395.0
申请日：1995-12-27
发明人： CROOKS, Peter, Anthony , CALDWELL, William, Scott , DULL, Gary, Maurice , BHATTI, Baldwinder, Singh
CPC分类号： C07D239/26 , C07D213/38 , C07D213/65
摘要： Patients susceptible to or suffering from central nervous system disorders are treated by administering an effective amount of an aryl substituted olefinic amine compound or an aryl substituted acetylenic compound. Exemplary compounds are (E)-N-methyl-4-[3-(6-methylpyrindin)yl]-3-butene-1-amine and N-methyl-4-(3-pyridinyl)-3-butyne-1-amine.
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4.发明授权ARYLSUBSTITUTED OLEFINIC AMINES AND THEIR USE AS CHOLINERGIC RECEPTORS AGONISTS 有权芳基取代的烯胺和它们的用途AS和胆碱能受体激动剂
公开(公告)号：EP1086082B9
公开(公告)日：2005-03-02
申请号：EP99926152.2
申请日：1999-06-03
申请人： Targacept, Inc.
发明人： CALDWELL, William, Scott , DULL, Gary, Maurice , BHATTI, Balwinder, Singh , HADIMANI, Srishailkumar, B. , PARK, Haeil , WAGNER, Jared, Miller , CROOKS, Peter, Anthony , LIPPIELLO, Patrick, Michael , BENCHERIF, Merouane
IPC分类号： C07D213/38 , C07D213/62 , C07D213/61 , C07D213/64 , C07D239/26 , A61K31/44
CPC分类号： C07D213/73 , A61K31/44 , A61K31/4406 , A61K31/505 , C07D213/38 , C07D213/61 , C07D213/65 , C07D239/26
摘要： 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.
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5.发明公开ARYL OLEFINIC AZACYCLIC, AND ARYL ACETYLENIC AZACYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS INHIBITORS OF NICOTINIC CHOLINERGIC RECEPTORS 审中-公开芳基烯烃氮杂环，和芳基乙炔化合物氮杂含药物制剂及其使用尼古丁胆碱能受体的抑制剂
公开(公告)号：EP1225955A1
公开(公告)日：2002-07-31
申请号：EP00948568.1
申请日：2000-06-30
申请人： Targacept, Inc.
IPC分类号： A61P25/00 , A61K31/4406 , C07D453/02 , C07D213/32 , C07D401/06 , C07D487/04 , C07D209/02
CPC分类号： C07D401/06 , A61K31/44 , A61K31/505 , C07D209/02 , C07D213/32 , C07D401/14 , C07D453/02 , C07D487/04
摘要： 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 aryl olefinic azacyclic compounds and aryl acetylenic azacylic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. Exemplary compounds include (S)-(E)-3-(3-pyrrolidin-2-yl-prop-1-enyl)pyridine, (S)-(E)-3-(2-pyrrolidin-2-ylvinyl)pyridine, 3-(2-pyrrolidin-2-ylethenyl)pyridine, 3-(3-pyrrolidin-2-ylprop-1-enyl)pyridine, 3-(2-(2-azetidinyl)ethenyl)pyridine, 3-(3-(2-azetidinyl) prop-1-enyl)pyridine, 2-(2-(3-pyridyl)ethenyl)-1-azabicyclo[3.3.0]octane, 2-(3-(3-pyridyl)prop-2-enyl)-1-azabicyclo[3.3.0]octane, 3-(2-(3-pyridyl)ethenyl)-2-azabicyclo[2.2.1]heptane, 3-(3-(3-pyridyl)prop-2-enyl)-2-azabicyclo[2.2.1]heptane, 2-(2-(3-pyridyl)ethenyl)-7-azabicyclo[2.2.1]heptane, 2-(3-(3-pyridyl)prop-2-enyl)-7-azabicyclo[2.2.1]heptane, 2-(2-(3-pyridyl)ethenyl)quinuclidine and 2-(3-(3-pyridyl)prop-2-enyl)quinuclidine.
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公开(公告)号：EP1185514A1
公开(公告)日：2002-03-13
申请号：EP00938183.1
申请日：2000-06-06
申请人： Targacept, Inc.
发明人： DULL, Gary, Maurice , MILLER, Craig, Harrison , CALDWELL, William, Scott , LYNM, Dwo , BHATTI, Balwinder, Singh , SCHMITT, Jeffrey, Daniel , BYRD, Gary, Dwight , HADIMANI, Srishailkumar, Basawannappa
IPC分类号： C07D213/74 , C07D213/82 , C07D213/65 , C07D213/70 , C07D213/26 , C07D213/89 , A61K31/44 , A61K31/505
CPC分类号： C07D213/70 , C07D213/38 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/82 , C07D213/89
摘要： Pharmaceutical compositions incorporate aryl substituted olefinic amine compounds. Representative compounds are (2S)-(4E)-N-methyl-5-[3-(5-isopropoxy-1-oxopyridin)yl)]-4-penten-2-amine, (3E)-N-methyl-4-(3-(1-oxopyridin)yl)-3-buten-1-amine, (4E)-N-methyl-5-(3-(1-oxopyridin)yl)-4-penten-2-amine, (4E)-N-methyl-5-(3-(5-((carboxymethyl)oxy)pyridin)yl)-4-penten-2-amine, (3E)-N-methyl-4-[3-(5-nitro-6-aminopyridin)yl]-3-buten-1-amine, (3E)-N-methyl-4-[3-(5-(N-benzylcarboxamido)pyridin)yl]-3-buten-1-amine(4E)-N-methyl-5-[5-(2-aminopyrimidin)yl]-4-penten-2-amine, (4E)-N-methyl-5-(3-(5-aminopyridin)yl)-4-penten-2-amine (3E)-N-methyl-4-(3-(5-isobutoxypyridin)yl)-3-buten-1-amine, (3E)-N-methyl-4-(3-(5-ethylthiopyridin)yl)-3-buten-1-amine, (4E)-N-methyl-5-(3-(5-trifluoromethylpyridin)yl)-4-penten-2-amine, (4E)-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, and (4E)-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine.
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7.发明授权HETEROARYLDIAZABICYCLOALKANES AS NICOTINIC CHOLINERGIC RECEPTOR LIGANDS 有权HETEROARYLDIAZABICYCLOALKANE AS配体烟碱乙酰胆碱受体
公开(公告)号：EP1289996B1
公开(公告)日：2005-04-06
申请号：EP01941614.8
申请日：2001-05-24
申请人： Targacept, Inc.
发明人： MILLER, Craig, Harrison , DULL, Gary, Maurice , MIAO, Lan , LYNM, Dwo , SCHMITT, Jeffrey, Daniel , CLARK, Thomas, Jeffrey
IPC分类号： C07D487/08 , A61P25/00 , A61K31/40
CPC分类号： C07D487/08
摘要： The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl 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-(3,4-dimethoxyphenoxy)-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.
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8.发明授权PHARMACEUTICAL COMPOSITIONS INCORPORATING ARYL SUBSTITUTED OLEFINIC AMINE COMPOUNDS 失效药物组合物WHAT芳基取代的烯胺化合物
公开(公告)号：EP0973743B1
公开(公告)日：2004-08-25
申请号：EP98905108.1
申请日：1998-02-19
申请人： Targacept, Inc.
发明人： CALDWELL, William, Scott , DULL, Gary, Maurice , DOBSON, Grayland, Page , MILLER, Craig, Harrison , BENCHERIF, Merouane , LIPPIELLO, Patrick, Michael
IPC分类号： C07D213/64 , C07D213/61 , C07D213/38 , A61K31/44
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61
摘要： Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound of Formula (I): wherein X is C-R', C-OR', C-CH2-OR' wherein R' is selected from the group consisting of H, C1-C5 alkyl, an aromatic group containing species and alkyl-, halo-, or amino-substituted aromatic group containing species; E' is hydrogen or C1-C5 alkyl or halo substituted C1-C5 alkyl; E'' is C1-C5 alkyl or halo substituted C1-C5 alkyl; Z' and Z'' are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, aryl rings, and can form a ring structure (a), A, A' and A'' are each individually selected from the group consisting of hydrogen, C1-C7 alkyl, and halo; m is 0 or 1; p is 0 or 1 with the proviso that when m or p is 0 then that E'' is hydrogen; and the wavy line in the structure represents a cis (Z) or trans (E) form of the compound. Exemplary compounds include (E)-N-methyl-4-[3-(benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.
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9.发明公开(R) -3- (E) -2- (PYRR0LIDIN-3-YL) VINYL) -5- (TETRAHYDR0PYRAN-4-YL0XY) PYRIDINE, ITS SALTS, ITS SYNTHESIS AND ITS USE AS LIGAND FOR NICOTINIC ACETYLCHOLINERGIC RECEPTORS 审中-公开（R）-2-（E）-2-（吡咯烷-3-基）乙烯基）-5-（四氢吡喃-4-基氧基）吡啶，其盐，其合成，以及其作为烟碱乙酰胆碱受体的配体的使用
公开(公告)号：EP2358705A1
公开(公告)日：2011-08-24
申请号：EP09775410.5
申请日：2009-11-30
申请人： Targacept Inc.
发明人： AKIREDDY, Srinivisa, Rao , BREINING, Scott, R. , CUTHBERTSON, Timothy, J. , DULL, Gary, Maurice , GATTO, Gregory, J. , GENUS, John , HAMMOND, Philip, S. , MITCHENER, Joseph, Pike, Jr. , MUNOZ, Julio, A. , OTTEN, Pieter, Albert , YOHANNES, Daniel , FEDOROV, Nikolai
IPC分类号： C07D405/14 , A61P25/00 , A61K31/4439
CPC分类号： A61K31/4439 , C07D405/14
摘要： 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. The present invention relates also the use of this compound in the manufacture of a medicament for the treatment of CNS related disorders.
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10.发明授权PHARMACEUTICAL COMPOSITIONS FOR PREVENTION AND TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 失效药物组合物的预防和治疗中枢神经系统疾病
公开(公告)号：EP0900200B9
公开(公告)日：2009-10-21
申请号：EP97921232.1
申请日：1997-04-16
申请人： Targacept, Inc.
IPC分类号： C07D213/38 , A61K31/44
CPC分类号： C07D213/38
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