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.

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.

发明人： CALDWELL, William, Scott ,  DULL, Gary, Maurice ,  DOBSON, Grayland, Page

IPC分类号： C07D213/38 ,  A61K31/44

CPC分类号： C07D213/38

公开(公告)号：EP0900200B1

公开(公告)日：2008-12-03

申请号：EP97921232.1

申请日：1997-04-16

申请人： Targacept, Inc.

发明人： CALDWELL, William, Scott ,  DULL, Gary, Maurice ,  DOBSON, Grayland, Page

IPC分类号： C07D213/38 ,  A61K31/44

CPC分类号： C07D213/38

摘要： Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.