公开(公告)号：AU2005313390A1

公开(公告)日：2006-06-15

申请号：AU2005313390

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： KRUSE CORNELIS G ,  VLIET BERNARD J VAN ,  STOIT AXEL ,  SCHARRENBURG GUSTAAF J M VAN ,  PRAS-RAVES MARIA L ,  HESSELINK MAYKE B ,  TERPSTRA JAN-WILLEM ,  MCCREARY ANDREW C ,  FEENSTRA ROELOF W

IPC: A61K31/423 ,  A61P25/00 ,  C07D263/58 ,  C07D413/12

Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

公开(公告)号：AU2005313311A1

公开(公告)日：2006-06-15

申请号：AU2005313311

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： TERPSTRA JAN-WILLEM ,  SCHARRENBURG GUSTAAF J M VAN ,  HESSELINK MAYKE B ,  MCCREARY ANDREW C ,  STOIT AXEL ,  PRAS-RAVES MARIA L ,  VLIET BERNARD J VAN ,  KRUSE CORNELIS G ,  FEENSTRA ROELOF W

IPC: A61K31/423 ,  A61P25/00 ,  C07D263/58

Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

公开(公告)号：DE60203042T2

公开(公告)日：2006-01-19

申请号：DE60203042

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  MCCREARY ANDREW C ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06

Abstract: The invention relates to novel phenylpiperazine derivatives of the formula wherein: -R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.

公开(公告)号：ES2235029T3

公开(公告)日：2005-07-01

申请号：ES02722107

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  MCCREARY ANDREW C ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06

Abstract: Derivados de fenilpiperazina que tienen la fórmula (1) **(Fórmula)** en la que R es un grupo de la fórmula (a) o (b) **(Fórmula)** y sus sales.

公开(公告)号：PL359650A1

公开(公告)日：2004-08-23

申请号：PL35965002

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  MCCREARY ANDREW C ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06 ,  A61K31/423

Abstract: The invention relates to novel phenylpiperazine derivatives of the formula wherein: -R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.

公开(公告)号：AU2003208714A1

公开(公告)日：2003-09-04

申请号：AU2003208714

申请日：2003-02-11

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  GLENNON JEFFREY C ,  MCCREARY ANDREW C ,  RANDEN JAN VAN ,  RONKEN ERIC ,  SCHARRENBURG GUSTAAF J M VAN ,  BRONZOVA JULIANA B

IPC: A61K45/00 ,  A61K31/00 ,  A61K31/138 ,  A61K31/445 ,  A61K31/48 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61K45/06 ,  A61P25/00 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00

Abstract: The invention relates to the use of a compound or a combination of compounds having partial dopamine-D2 receptor agonistic activity and serotonin and/or noradrenaline reuptake inhibitory activity, for the preparation of a pharmaceutical composition for the treatment of psychiatric and/or neurologic disorders caused by disturbances of the major monoaminergic (dopamine, serotonin and/or nordrenaline) systems or that can be treated via manipulation of those systems.

公开(公告)号：CA2462688A1

公开(公告)日：2003-08-21

申请号：CA2462688

申请日：2003-02-11

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  BRONZOVA JULIANA B ,  GLENNON JEFFREY C ,  MCCREARY ANDREW C ,  VAN RANDEN JAN ,  RONKEN ERIC ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K45/00 ,  A61K31/00 ,  A61K31/138 ,  A61K31/445 ,  A61K31/48 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61K45/06 ,  A61P25/00 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00

Abstract: The invention relates to the use of a compound or a combination of compounds having partial dopamine-D2 receptor agonistic activity and serotonin and/or noradrenaline reuptake inhibitory activity, for the preparation of a pharmaceutical composition for the treatment of psychiatric and/or neurologi c disorders caused by disturbances of the major monoaminergic (dopamine, serotonin and/or nordrenaline) systems or that can be treated via manipulati on of those systems.

公开(公告)号：BR0205220A

公开(公告)日：2003-06-24

申请号：BR0205220

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  MCCREARY ANDREW C ,  SCHARRENBURG GUSTAAF J M VAN

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06

Abstract: The invention relates to novel phenylpiperazine derivatives of the formula wherein: -R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.

公开(公告)号：CZ20023721A3

公开(公告)日：2003-02-12

申请号：CZ20023721

申请日：2001-05-10

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  VAN DER HEIJDEN JOHANNES A M ,  KRUSE CORNELIS G ,  LONG STEPHEN K ,  VAN SCHARRENBURG GUSTAAF J M

IPC: C07D413/10 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61P43/00 ,  C07D263/54 ,  C07D263/58 ,  C07D277/62 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

公开(公告)号：CA2405971C

公开(公告)日：2010-03-30

申请号：CA2405971

申请日：2001-05-10

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  VAN DER HEIJDEN JOHANNES A M ,  KRUSE CORNELIS G ,  LONG STEPHEN K ,  VAN SCHARRENBURG GUSTAAF J M

IPC: C07D413/10 ,  C07D413/14 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61P43/00 ,  C07D263/54 ,  C07D263/58 ,  C07D277/62 ,  C07D413/04 ,  C07D413/12

Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents -C, = C or -N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy,and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors.