公开(公告)号：NO20044775L

公开(公告)日：2004-12-16

申请号：NO20044775

申请日：2004-11-03

Applicant: SOLVAY PHARM BV

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

IPC: A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D471/04 ,  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：MXPA04004812A

公开(公告)日：2004-08-11

申请号：MXPA04004812

申请日：2003-04-02

Applicant: SOLVAY PHARM BV

Inventor： MCCREARY ANDREW C

IPC: 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 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10 ,  C07D519/00

Abstract: La presente invencion describe un grupo de derivados unicos de diazabiciclo alcano, que tienen una interesante actividad antagonistica del receptor de neurocinina-NK1 que se representa por la formula general (I), ver formula I, en donde: -R1 representa fenilo, 2-indolilo, 3-indolilo, 3-indazolilo o benzo(b(tiofeno-3-ilo, donde los grupos pueden estar substituidos con halogeno o alquilo (1-3C), -R2 y R3 independientemente representan H, OCH3, CH y CF3, R4, R5 y R6 independientemente representan H, OH, O-alquilo (1-4C), CH2OH, NH2, dialquilo (1-3C)N, pirrolidin-1-ilo, piperidin-1-ilo, morfolin-4-ilo substituido con uno o dos grupos metilo o metoximetilo, morfolin-4-ilamino, morfolin-4-ilmetilo, imidazol-1-ilo, tiomorfolin-4-ilo, 1.-dioxo-tiomorfolin-4-ilo o 3-oxa-8-azabiciclo(3.2.1(oct-8-ilo; R4 y R5 juntos representan un grupo ceto, un grupo 1,3-dioxan-2-ilo o 1,3-dioxolan-2-ilo, X representa O o S, n tiene un valor de 1, 2 o 3 respectivamente; la invencion tambien describe un metodo para la preparacion de compuestos novedosos y composiciones farmaceuticas que contienen por lo menos uno de estos como un ingrediente activo.

公开(公告)号：NO20040065L

公开(公告)日：2004-03-09

申请号：NO20040065

申请日：2004-01-08

Applicant: SOLVAY PHARM BV

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

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 ,  C07D241/04 ,  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：AR032711A1

公开(公告)日：2003-11-19

申请号：ARP020100547

申请日：2002-02-18

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 ,  C07D413/04 ,  C07D209/00 ,  A61K31/423 ,  A61P25/18 ,  C07D263/00

Abstract: Derivados de fenilpiperazina de formula (1) en donde R representa el grupo (a) o (b). Los compuestos son agonistas (parciales) del receptor D2 y son utiles para tratar trastornos del CNS, en particular la enfermedad de Parkinson. La presente también se refiere a un método para la preparacion de los nuevos derivados y a una composicion farmacéutica que los contiene.

公开(公告)号：CZ20023933A3

公开(公告)日：2003-03-12

申请号：CZ20023933

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 ,  C07D413/14 ,  A61P25/18

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：NO20025902L

公开(公告)日：2002-12-09

申请号：NO20025902

申请日：2002-12-09

Applicant: SOLVAY PHARM BV

Inventor： SCHARRENBURG GUSTAAF JOHAN MAR ,  FEENSTRA ROELOF W ,  KRUSE CORNELIS GERRIT ,  RONKEN ERIC ,  MCCREARY ANDREW C

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：NO20025902D0

公开(公告)日：2002-12-09

申请号：NO20025902

申请日：2002-12-09

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  RONKEN ERIC ,  KRUSE CORNELIS GERRIT ,  MCCREARY ANDREW C ,  SCHARRENBURG GUSTAAF JOHAN MAR

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：NO20025902A

公开(公告)日：2002-12-09

申请号：NO20025902

申请日：2002-12-09

Applicant: SOLVAY PHARM BV

Inventor： SCHARRENBURG GUSTAAF JOHAN MAR ,  FEENSTRA ROELOF W ,  KRUSE CORNELIS GERRIT ,  RONKEN ERIC ,  MCCREARY ANDREW C

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

CPC classification number: C07D413/12 ,  C07D471/06

公开(公告)号：BRPI0713695A2

公开(公告)日：2012-10-30

申请号：BRPI0713695

申请日：2007-06-15

Applicant: SOLVAY PHARM BV

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

IPC: A61K31/496 ,  A61K31/198

公开(公告)号：BRPI0713691A2

公开(公告)日：2012-10-30

申请号：BRPI0713691

申请日：2007-06-15

Applicant: SOLVAY PHARM BV

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

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