公开(公告)号：EP0765320B1

公开(公告)日：2001-10-10

申请号：EP95914492.4

申请日：1995-04-24

申请人： PFIZER INC.

发明人： FLIRI, Anton, F. ,  O'NEILL, Brian, T. ,  FARACI, William, S. ,  SANNER, Mark, A. ,  ZORN, Stevin, H.

IPC分类号： C07D401/12 ,  A61K31/415 ,  C07D403/14

CPC分类号： C07D213/73 ,  C07D235/26 ,  C07D401/12 ,  C07D403/12

摘要： This invention relates to novel, pharmaceutically active benzimidazolone derivatives of formula (I), wherein the dashed line, R0 through R?6 and X1¿ through X3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.

公开(公告)号：EP0783503B1

公开(公告)日：2001-11-28

申请号：EP95927915.9

申请日：1995-08-24

申请人： PFIZER INC.

发明人： DESAI, Kishor, A. ,  FLIRI, Anton, F., J. ,  SANNER, Mark, A.

IPC分类号： C07D471/04 ,  A61K31/505

CPC分类号： C07D471/04

摘要： Substituted pyrido[1,2-a]pyrazines of general formula (I) wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO¿2?, C=O, CHOH, or -(CR?3R4¿) and n is 0-2 as well as precursors thereto are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system.

公开(公告)号：EP0874849A1

公开(公告)日：1998-11-04

申请号：EP96935226.0

申请日：1996-11-06

申请人： PFIZER INC.

发明人： SANNER, Mark, A.

IPC分类号： A61K31 ,  A61P1 ,  A61P9 ,  A61P25 ,  A61P27 ,  A61P39 ,  C07D487 ,  C07D209 ,  C07D241

CPC分类号： C07D487/04

摘要： This invention relates to compounds of formula (I), wherein R1 is phenyl, naphthyl, benzoxazolonyl, indolyl, indolonyl, benzimidazolyl, quinolyl, furyl, benzofuryl, thienyl, benzothienyl, oxazolyl, benzoxazolyl; R2 is H or (C1-C6)alkyl; R3 is phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is O, S, SO, SO2, NR4, C=O, CH(OH), CHR4, (a), (b), (c), or (d); m is 0, 1 or 2; n is 0, 1 or 2. The compounds of this invention are ligands for dopamine receptor subtypes, especially the dopamine D4 receptor, and are therefore useful in the treatment of disorders of the dopamine system.

公开(公告)号：EP0775118B1

公开(公告)日：2003-06-04

申请号：EP95917441.8

申请日：1995-05-18

申请人： PFIZER INC.

发明人： FARACI, William, S. ,  FLIRI, Anton, F., J. ,  O'NEILL, Brian, T. ,  SANNER, Mark, A. ,  ZORN, Stevin, H.

IPC分类号： C07D235/06 ,  C07D235/26 ,  C07D403/12 ,  A61K31/445 ,  A61K31/495

CPC分类号： C07D471/04 ,  C07D235/06 ,  C07D235/26

摘要： This invention relates to novel, pharmaceutically active benzimidazole derivatives of formula (I), wherein the dotted line, X and R1 through R?7, R11 and R15¿ through R17 are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.

公开(公告)号：EP0783503A1

公开(公告)日：1997-07-16

申请号：EP95927915.0

申请日：1995-08-24

申请人： PFIZER INC.

发明人： DESAI, Kishor, A. ,  FLIRI, Anton, F., J. ,  SANNER, Mark, A.

IPC分类号： A61K31 ,  A61P1 ,  A61P9 ,  A61P25 ,  A61P27 ,  A61P43 ,  C07D471 ,  C07D221 ,  C07D241

CPC分类号： C07D471/04

摘要： Substituted pyrido[1,2-a]pyrazines of general formula (I) wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO¿2?, C=O, CHOH, or -(CR?3R4¿) and n is 0-2 as well as precursors thereto are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system.

公开(公告)号：EP0775118A1

公开(公告)日：1997-05-28

申请号：EP95917441.0

申请日：1995-05-18

申请人： PFIZER INC.

发明人： FARACI, William, S. ,  FLIRI, Anton, F., J. ,  O'NEILL, Brian, T. ,  SANNER, Mark, A. ,  ZORN, Stevin, H.

IPC分类号： C07D235 ,  A61K31 ,  A61P1 ,  A61P3 ,  A61P9 ,  A61P13 ,  A61P15 ,  A61P21 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P31 ,  A61P37 ,  A61P43 ,  C07D303 ,  C07D401 ,  C07D403 ,  C07D471

CPC分类号： C07D471/04 ,  C07D235/06 ,  C07D235/26

摘要： This invention relates to novel, pharmaceutically active benzimidazole derivatives of formula (I), wherein the dotted line, X and R1 through R?7, R11 and R15¿ through R17 are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.

公开(公告)号：EP0874849B1

公开(公告)日：2001-09-19

申请号：EP96935226.9

申请日：1996-11-06

申请人： PFIZER INC.

发明人： SANNER, Mark, A.

IPC分类号： C07D487/04 ,  A61K31/495

CPC分类号： C07D487/04

摘要： This invention relates to compounds of formula (I), wherein R1 is phenyl, naphthyl, benzoxazolonyl, indolyl, indolonyl, benzimidazolyl, quinolyl, furyl, benzofuryl, thienyl, benzothienyl, oxazolyl, benzoxazolyl; R2 is H or (C1-C6)alkyl; R3 is phenyl, pyridinyl, pyrimidinyl, pyrazinyl, or pyridazinyl; X is O, S, SO, SO2, NR4, C=O, CH(OH), CHR4, (a), (b), (c), or (d); m is 0, 1 or 2; n is 0, 1 or 2. The compounds of this invention are ligands for dopamine receptor subtypes, especially the dopamine D4 receptor, and are therefore useful in the treatment of disorders of the dopamine system.

公开(公告)号：EP0765320A1

公开(公告)日：1997-04-02

申请号：EP95914492.0

申请日：1995-04-24

申请人： PFIZER INC.

发明人： FLIRI, Anton, F. ,  O'NEILL, Brian, T. ,  FARACI, William, S. ,  SANNER, Mark, A. ,  ZORN, Stevin, H.

IPC分类号： A61K31 ,  A61P1 ,  A61P5 ,  A61P9 ,  A61P25 ,  A61P37 ,  A61P43 ,  C07D213 ,  C07D235 ,  C07D401 ,  C07D403

CPC分类号： C07D213/73 ,  C07D235/26 ,  C07D401/12 ,  C07D403/12

摘要： This invention relates to novel, pharmaceutically active benzimidazolone derivatives of formula (I), wherein the dashed line, R0 through R?6 and X1¿ through X3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.