公开(公告)号：NO20090164A

公开(公告)日：2009-01-14

申请号：NO20090164

申请日：2009-01-12

Applicant: SOLVAY PHARM BV

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

IPC: A61K31/496 ,  A61K31/198 ,  A61P25/16

CPC classification number: A61K31/198 ,  A61K31/496 ,  A61K2300/00

公开(公告)号：NO20090165A

公开(公告)日：2009-01-12

申请号：NO20090165

申请日：2009-01-12

Applicant: SOLVAY PHARM BV

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

IPC: A61K45/06 ,  A61K31/195 ,  A61K31/496 ,  A61P25/14 ,  A61P25/16

CPC classification number: A61K31/195 ,  A61K31/496 ,  A61K45/06 ,  A61K2300/00

公开(公告)号：CA2690294A1

公开(公告)日：2008-12-31

申请号：CA2690294

申请日：2008-06-23

Applicant: SOLVAY PHARM BV

Inventor： TURSKI LECHOSLAW A ,  STOIT AXEL ,  KRUSE CORNELIS G ,  VADER SANDER ,  TULP MARTINUS TH M

IPC: C07D487/04 ,  A61K31/519 ,  A61P11/00 ,  A61P15/10

Abstract: The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1A) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.

公开(公告)号：BRPI0518372A2

公开(公告)日：2008-11-18

申请号：BRPI0518372

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： HES ROELOF VAN ,  SMID PIETER ,  KRUSE CORNELIS G ,  TULP MARTINUS TH M

IPC: A61K31/496 ,  A61P25/00 ,  C07D405/12

Abstract: The present invention relates to a group of novel 3 -(2-piperidin-4-yl-ethyl)-1H-indole derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D 2 receptors and to methods for the preparation of these compounds. 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：CA2654557A1

公开(公告)日：2007-12-21

申请号：CA2654557

申请日：2007-06-15

Applicant: SOLVAY PHARM BV

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

IPC: A61K45/06 ,  A61K31/195 ,  A61K31/496 ,  A61P25/14 ,  A61P25/16

Abstract: The invention concerns the use of a combination preparation of bifeprunox or its N-oxide, or pharmacologically acceptable salts of those compounds: a nd L-DOPA, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, in particular Parkins on's disease and restless leg syndrome.

公开(公告)号：MX2007006758A

公开(公告)日：2007-11-09

申请号：MX2007006758

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： HES ROELOF VAN ,  KRUSE CORNELIS G ,  SMID PIETER ,  TULP MARTINUS TH M

IPC: A61K31/00 ,  C07D405/12 ,  A61P25/00

Abstract: La presente invencion se refiere a un grupo de nuevos derivados de 3-(2-piperidin-4-il-etil)-1H-indol con un doble modo de accion: inhibicion de la reabsorcion de la serotonina y afinidad para receptores de dopamina-D2 y a metodos para la preparacion de estos compuestos; la invencion tambien se refiere al uso de un compuesto descrito en la presente para la fabricacion de un medicamento que tiene un efecto beneficioso; los compuestos tienen la formula general (1) donde los simbolos tienen los significados dados en la memoria descriptiva.

公开(公告)号：NO20073389L

公开(公告)日：2007-07-05

申请号：NO20073389

申请日：2007-07-02

Applicant: SOLVAY PHARM BV

Inventor： KRUSE CORNELIS G ,  HES ROELOF VAN ,  SMID PIETER ,  TULP MARTINUS TH M

IPC: C07D401/14 ,  A61K31/505 ,  A61P25/00 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

公开(公告)号：NO20073387A

公开(公告)日：2007-07-02

申请号：NO20073387

申请日：2007-07-02

Applicant: SOLVAY PHARM BV

Inventor： KRUSE CORNELIS G ,  HES ROELOF VAN ,  SMID PIETER ,  TULP MARTINUS TH M

IPC: C07D405/12 ,  A61K31/404 ,  A61P25/00

CPC classification number: C07D405/12

公开(公告)号：AU2002333229B2

公开(公告)日：2006-11-30

申请号：AU2002333229

申请日：2002-07-03

Applicant: SOLVAY PHARM BV

Inventor： HERREMANS ARNOLDUS H J ,  MCCREARY ANDREW C ,  SCHARRENBURG GUSTAAF J M VAN ,  COOLEN HEIN K A C ,  TULP MARTINUS TH M ,  MAARSEVEEN JAN H VAN ,  HOOGENBAND ADRIANUS VAN DEN ,  BAKKER WOUTER I IWEMA

IPC: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P3/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/08 ,  A61P13/02 ,  A61P13/10 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D201/00 ,  C07D241/00 ,  C07D241/04 ,  C07D265/00 ,  C07D401/14 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D413/14 ,  C07D471/04

Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH 3 , CF 3 , OCH 3 , halogen, cyano and 5-CF 3 -tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1-3C); n has the value 0-3; m has the value 0-2; R 1 represents NH 2 , NH-alkyl (1-3C), dialkyl (1-3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH 3 -piperazinyl; R 2 is hydrogen, alkyl (1-4C) or phenyl, or R 2 together with (CH 2 ) m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R 3 and R 4 independently represent hydrogen or methyl, or R 3 and R 4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved

公开(公告)号：CA2594165A1

公开(公告)日：2006-08-31

申请号：CA2594165

申请日：2006-02-17

Applicant: SOLVAY PHARM BV

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

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.