公开(公告)号：DK1827427T3

公开(公告)日：2008-11-24

申请号：DK05850037

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

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

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：AU2003219164B2

公开(公告)日：2008-07-17

申请号：AU2003219164

申请日：2003-03-17

Applicant: SOLVAY PHARM BV

Inventor： STUIVENBERG HERMAN H VAN ,  LANGE JOSEPHUS H M ,  KRUSE CORNELIS G ,  HERREMANS ARNOLDUS H J ,  MCCREARY ANDREW C ,  DIJKSMAN JESSICA A R

IPC: C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P1/12 ,  A61P1/14 ,  A61P3/04 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  A61P27/06 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D277/56 ,  C07D277/68 ,  C07D417/12

Abstract: The present invention relates to a group of thiazole derivatives which are potent antagonists, agonists or partial agonists of the cannabinoid CB1-receptor. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification

公开(公告)号：AU2003224162B2

公开(公告)日：2008-06-12

申请号：AU2003224162

申请日：2003-04-02

Applicant: SOLVAY PHARM BV

Inventor： MCCREARY ANDREW C ,  BAKKER WOUTER I IWEMA ,  SCHARRENBURG GUSTAAF J M VAN ,  COOLEN HEIN K A C ,  KUIL GIJSBERT D ,  MAARSEVEEN JAN H VAN ,  HESSELINK MAYKE B ,  BOER DIRK DE

IPC: C07D471/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61P1/00 ,  A61P1/08 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P11/08 ,  A61P11/16 ,  A61P13/02 ,  A61P13/10 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/16 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D487/04 ,  C07D491/10 ,  C07D519/00

Abstract: The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK 1 receptor antagonistic activity represented by the general formula (1) wherein: R 1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1-3C), R 2 and R 3 independently represent halogen, H, OCH 3 , CH 3 and CF 3 , R 4 , R 5 and R 6 independently represent H, OH, O-alkyl(1-4C), CH 2 OH, NH 2 , dialkyl(1-3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1,1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; R 4 and R 5 together may represent a keto, a 1,3-dioxan-2-yl or a 1,3-dioxolan-2-yl group, X represents either O or S, n has the value of 1, 2 or 3, a is the asymmetrical carbon atom 8a, 9a or 10a when n equals 1, 2 or 3 respectively The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient.

公开(公告)号：CA2654719A1

公开(公告)日：2007-12-21

申请号：CA2654719

申请日：2007-06-15

Applicant: SOLVAY PHARM BV

Inventor： TULP MARTINUS TH M ,  VAN SCHARRENBURG GUSTAAF J M ,  MCCREARY ANDREW C

IPC: A61K31/496 ,  A61K31/198

Abstract: The invention concerns the use of a combination preparation of SLV308 or its N-oxide, or pharmacologically acceptable salts of those compounds (I), ( II) and L-DOPA, for simultaneous, separate or sequential use in the treatmen t of disorders requiring recovery of dopaminergic function, in particular Pa rkinson's disease and restless leg syndrome.

公开(公告)号：NO20072981L

公开(公告)日：2007-09-05

申请号：NO20072981

申请日：2007-06-11

Applicant: SOLVAY PHARM BV

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

IPC: C07D263/58 ,  A61K31/423 ,  A61P25/00 ,  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：NO20072977A

公开(公告)日：2007-09-05

申请号：NO20072977

申请日：2007-06-11

Applicant: SOLVAY PHARM BV

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

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

CPC classification number: C07D263/58 ,  C07D413/12

公开(公告)号：NO20072969L

公开(公告)日：2007-08-31

申请号：NO20072969

申请日：2007-06-11

Applicant: SOLVAY PHARM BV

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

IPC: 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：NO20072974A

公开(公告)日：2007-08-23

申请号：NO20072974

申请日：2007-06-11

Applicant: SOLVAY PHARM BV

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

IPC: C07D413/12

CPC classification number: C07D263/58 ,  C07D413/12

公开(公告)号：ZA200602435B

公开(公告)日：2007-07-25

申请号：ZA200602435

申请日：2006-03-24

Applicant: SOLVAY PHARM BV

Inventor： IWEMA BAKKER WOUTER I ,  ADRIANUS VAN DEN HOOGENBAND ,  VAN SCHARRENBURG GUSTAAF J M ,  MCCREARY ANDREW C

IPC: A61K20090101 ,  A61P20090101 ,  C07D20090101

公开(公告)号：NO20061836L

公开(公告)日：2006-06-23

申请号：NO20061836

申请日：2006-04-26

Applicant: SOLVAY PHARM BV

Inventor： SCHARRENBURG GUSTAAF JOHAN M VAN ,  MCCREARY ANDREW C ,  BAKKER WOUTER I IWEMA ,  HOOGENBAND ADRIANUS VAN DEN

IPC: C07D471/04 ,  A61P1/08 ,  A61P29/00

Abstract: The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1 receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.