公开(公告)号：ZA200209897B

公开(公告)日：2004-03-05

申请号：ZA200209897

申请日：2002-12-05

Applicant: SOLVAY PHARM BV

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

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06 ,  C07D

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：HU0303329A2

公开(公告)日：2004-01-28

申请号：HU0303329

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  KRUSE CORNELIS G ,  MCCREARY ANDREW C ,  RONKEN ERIC ,  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：HU0302016A2

公开(公告)日：2003-09-29

申请号：HU0302016

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

公开(公告)号：SK15872002A3

公开(公告)日：2003-04-01

申请号：SK15872002

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

公开(公告)号：CA2411973A1

公开(公告)日：2002-08-29

申请号：CA2411973

申请日：2002-02-19

Applicant: SOLVAY PHARM BV

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

IPC: A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D413/12 ,  C07D471/06 ,  C07D413/10 ,  A61P25/18 ,  A61P25/28

Abstract: The invention relates to novel phenylpiperazine derivatives of the formulawherein:- 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：CA2405971A1

公开(公告)日：2001-11-15

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 ,  VAN SCHARRENBURG GUSTAAF J M ,  LONG STEPHEN K

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

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) substitut ed amino or hydroxy, X is O, S, SO or SO2, ---Z represents -C, = C or -N, R1 an d R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- o r 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 foun d 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.

公开(公告)号：ZA200706258B

公开(公告)日：2009-08-26

申请号：ZA200706258

申请日：2007-07-27

Applicant: SOLVAY PHARM BV

Inventor： BENJAMIN DRUKARCH ,  FEENSTRA ROELOF W ,  JEAN-LOUISE BURGOT ,  IWEMA BAKKER WOUTER I ,  TULP MARTINUS TH M ,  SCHOFFELMEER ANTON N M ,  MARIE-ODILE CHRISTEN ,  MARYLENE CHOLLET ,  VAN VLIET BERNARD J

IPC: A61K20090101 ,  C07D20090101

Abstract: The present disclosure relates to dithiolethione derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The present disclosure also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the present disclosure specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

公开(公告)号：MX2009006411A

公开(公告)日：2009-06-23

申请号：MX2009006411

申请日：2007-12-12

Applicant: SOLVAY PHARM BV

Inventor： KRUSE CORNELIS G ,  SMID PIETER ,  FEENSTRA ROELOF W

IPC: A61K38/05 ,  C07K5/06 ,  A61P1/00 ,  A61P9/12 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07F9/30 ,  C07K5/062 ,  C07K5/065 ,  C07K5/078

Abstract: Esta invención se refiere a inhibidores selectivos de las enzimas que degradan la neurotensina, a composiciones farmacéuticas que contienen estos compuestos, a métodos para preparar los compuestos, métodos para preparar intermediarios novedosos útiles para su síntesis, y métodos para preparar composiciones; la invención también se refiere a los usos de dichos compuestos y composiciones, particularmente su uso en la fabricación de medicamentos para regular la presión sanguinea o el vaciado gástrico, o tratar la enfermedad de Parkinsor,, ansiedad, depresión o psicosis; los compuestos tienen la fórmula general (1) en donde los símbolos tienen los significados dados en la especificación. (ver fórmula (1)).

公开(公告)号：SK286778B6

公开(公告)日：2009-05-07

申请号：SK15872002

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

Abstract: Compounds of the formula (I) 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. 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.

公开(公告)号：ES2318783T3

公开(公告)日：2009-05-01

申请号：ES06778284

申请日：2006-08-21

Applicant: SOLVAY PHARM BV

Inventor： KOOPMAN THEODORUS S M ,  KOSTER HENDRIK J ,  VAN AMSTERDAM PETER H ,  FEENSTRA ROELOF W ,  VERHAGE MARINUS ,  MCCREARY ANDREW C

IPC: C07D263/58 ,  A61K31/423 ,  A61P25/00 ,  C07D295/24

Abstract: Derivados de piperazina y piperidina de fórmula general (1): ** ver fórmula** en donde Q es metilo, bencilo, ó (1,1''-bifenil)-3-il-metilo, y tautómeros, estereoisómeros, sales, hidratos y solvatos de los mismos farmacológicamente aceptables.