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.

公开(公告)号：EP1066287B1

公开(公告)日：2003-09-03

申请号：EP99908541.8

申请日：1999-02-26

申请人： Targacept, Inc.

发明人： CROOKS, Peter, Anthony ,  DEO, Niranjan, Madhukar

IPC分类号： C07D471/18

CPC分类号： C07D471/18 ,  Y02E50/17

摘要： A compound of formula (I), wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A' and A' are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z' is hydrogen or a substituent other than hydrogen; Y is C=O, C(OH)R' or C-A, where R' is hydrogen or lower alkyl is provided.

公开(公告)号：EP1068208B1

公开(公告)日：2003-05-14

申请号：EP99909806.4

申请日：1999-03-03

申请人： Targacept, Inc.

发明人： BENCHERIF, Merouane ,  LIPPIELLO, Patrick, Michael ,  CROOKS, Peter, Anthony ,  PARK, Haeil ,  BHATTI, Balwinder, Singh ,  CALDWELL, William, Scott ,  DULL, Gary, Maurice

IPC分类号： C07D471/18 ,  A61K31/435

CPC分类号： A61K31/444 ,  A61K31/439

摘要： A pharmaceutical composition incorporating a nicotinic antagonist is provided. The composition is an effective amount of a compound of formula (I), wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C=O, C(OH)R' or C-A, where R' is hydrogen or lower alkyl.

摘要翻译： 提供了掺入烟碱拮抗剂的药物组合物。 该组合物是有效量的式（I）化合物，其中X'是氮或键合到特征为具有大于0，小于0或0的西格玛值的取代基物质的碳; X是键合到取代物上的氮或碳，其特征在于西格玛m值大于0，小于0或0; A，A'和A“分别为特征为具有大于0，小于0或0的σm值，Z'为除氢以外的取代基，j为0至5的整数的单独的取代基物种;以及波浪线 在结构中表示该化合物可以以对映异构体或非对映异构体的形式存在; Z“是氢或除氢以外的取代基; Y是C = O，C（OH）R'或C-A，其中R'是氢或低级烷基。

公开(公告)号：EP1086082B1

公开(公告)日：2004-08-18

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.

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

申请人： Targacept, Inc. ,  The University of Kentucky Research Foundation

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.