公开(公告)号：AR050630A1

公开(公告)日：2006-11-08

申请号：ARP050103720

申请日：2005-09-06

Applicant: SOLVAY PHARM BV

Inventor： DEN HARTOG JACOBUS A J ,  KOCH MELLE ,  KOOMEN GERRIT-JAN ,  WANNER MARTINUS J ,  FEENSTRA ROELOF W

IPC: C07D473/00 ,  A61K31/52 ,  A61P25/00 ,  A61P29/00 ,  C07D473/28 ,  C07D473/32 ,  C07H19/167

Abstract: La presente trata sobre derivados de 6-trifluorometil purina 2-sustituida con actividad antagonista de adenosina-A3, procesos de obtencion y composiciones farmacéuticas. Reivindicacion 1: Compuestos de la formula general (1) en donde: R1 represnta - [X-(CH2)n]m-Y, en cuya formula X es NH u O, n es 0, 1, 2 o 3, m es 0 o 1,y Y es un anillo aromático o no aromático de 5 o 6 miembros opcionalmente sustituido, que contiene 0, 1 o 2 heteroátomos seleccionados de N, O y S, o R1 representa un grupo nitro; R2 es H, alquilo C1-3, ribosa, -CH2-O-CO-O-t-butilo o aril-(C1-3)alquilo ; R3 representa H, halogeno, NH2, -NH-(C1-6)alquilo, -N-di(C1-6)alquilo, -NH-ciclo(C3-8)alquilo, C2-4-alquenil (hetero)arilo o C2-4-alquinil (hetero)arilo, de los cuales los heteroátomos son seleccionados de N, O y S, y cuyos grupos (hetero)arilo pueden estar opcionalmente sustituidos, o R3 representa un anillo aromático o no aromático de 5 o 6 miembros, opcionalmente sustituido, que contiene 0, 1 o 2 heteroátomos seleccionados de N, O y S, y tautomeros, estereoisomeros y sales de los mismos.

公开(公告)号：AU2006218012A1

公开(公告)日：2006-08-31

申请号：AU2006218012

申请日：2006-02-17

Applicant: SOLVAY PHARM BV

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

IPC: C07D339/04 ,  A61K31/385

Abstract: The invention relates to dithiolethiones 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 invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the invention 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：AU2005313391A1

公开(公告)日：2006-06-15

申请号：AU2005313391

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

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

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：SI1395583T1

公开(公告)日：2005-08-31

申请号：SI200230087

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：ZA200404741B

公开(公告)日：2005-08-29

申请号：ZA200404741

申请日：2004-06-15

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  PRAS-RAVES MARIA L ,  STUIVENBERG HERMAN H VAN ,  KEIZER HISKIAS G ,  LANGE JOSEPHUS H M ,  KRUSE CORNELIS G ,  TUINSTRA TINKA

IPC: A61K31/415 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D231/04 ,  C07D401/04 ,  C07D ,  A61P ,  A61K

Abstract: The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.

公开(公告)号：PL371440A1

公开(公告)日：2005-06-13

申请号：PL37144003

申请日：2003-03-17

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  LANGE JOSEPHUS H M ,  PRAS-RAVES MARIA L ,  KRUSE CORNELIS G ,  VAN STUIVENBERG HERMAN H ,  TUINSTRA TINKA ,  KEIZER HISKIAS G

IPC: A61K31/415 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D231/04 ,  C07D401/04

Abstract: The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.

公开(公告)号：NO20044405A

公开(公告)日：2004-10-15

申请号：NO20044405

申请日：2004-10-15

Applicant: SOLVAY PHARM BV

Inventor： STUIVENBERG HERMAN HEINRICH VAN ,  FEENSTRA ROELOF W ,  KRUSE CORNELIS GERRIT ,  LANGE JOSEPHUS H M ,  PRAS-RAVES MARIA L

IPC: C07D231/04 ,  A61K31/415 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D401/04

CPC classification number: C07D401/04 ,  C07D231/04

公开(公告)号：PL358201A1

公开(公告)日：2004-08-09

申请号：PL35820101

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：TR200302294T4

公开(公告)日：2004-02-23

申请号：TR200302294

申请日：2001-05-10

Applicant: SOLVAY PHARM BV

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

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：ZA200208537B

公开(公告)日：2004-01-22

申请号：ZA200208537

申请日：2002-10-22

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  KRUSE CORNELIS G ,  SCHARRENBURG GUSTAAF J M VAN ,  HEIJDEN JOHANNES A M VAN DER ,  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 ,  C07D ,  A61K ,  A61P