公开(公告)号：SA05260060A

公开(公告)日：2005-12-03

申请号：SA05260060

申请日：2005-03-22

Applicant: SOLVAY PHARM BV

Inventor： MCCREARY ANDREW ,  SCHARRENBURG GUSTAAF J M VAN ,  GLENNON JEFFREY C ,  THAETE CLAUDIA ,  BAKKERAKKER CORNELIS ,  HESSELINK MAYKE B

IPC: A61K31/00 ,  A61K31/496

Abstract: يتعلقالاختراعباستخدامجديدلمشتقات١- [H2- ١- بنزوبيران -٢- أون-٨- يل ]-بيبرازينالمعروفة،والتيتعتبرمركباتربطمستقبل 5-HT ذاتنطاقواسع،وتتميز،منبينأنشطةمستقبلسيروتونينالوظيفيةالأخرى،بنشاطمساعدفعاللمستقبل 1AHT-5،ونشاطمضادلمستقبل 5-HT1D،ونشاطمساعدلمستقبل 7HT-5. المركباتالخاصةبالاختراعمفيدةفيتحضيرأدويةلعلاجالألم.يتعلقالاختراعبالمركباتالتىلهاالصيغةالعامة (١)حيثتحملالرموزنفسالمعانيالتىتمذكرهافيالمواصفات.

公开(公告)号：ES2335222T3

公开(公告)日：2010-03-23

申请号：ES05717127

申请日：2005-03-23

Applicant: SOLVAY PHARM BV

Inventor： BAKKER CORNELIS ,  GLENNON JEFFREY C ,  HESSELINK MAYKE B ,  THAETE CLAUDIA ,  MCCREARY ANDREW ,  VAN SCHARRENBURG GUSTAAF J

IPC: A61K31/496 ,  A61K31/00 ,  A61P25/14 ,  A61P25/16

Abstract: El uso de 3-amino-8-(1-piperazinil)-2H-1-benzopiran-2-ona, que tiene la fórmula (2): **(Ver fórmula)** y todos los esteroisómeros y sales farmacológicamente aceptables de la misma, para la preparación de una composición farmacéutica para el tratamiento, mejora o prevención de la enfermedad de Parkinson, Corea de Huntington, parálisis supranuclear progresiva, enfermedad de Wilson, síndrome de Tourette, epilepsia sintomática y no sintomática, convulsiones, que incluyen convulsiones refractarias y convulsiones post-ataque y otros trastornos electroconvulsivos, diversos temblores crónicos, que incluyen temblor esencial, tics y distonías.

公开(公告)号：AT435863T

公开(公告)日：2009-07-15

申请号：AT03720571

申请日：2003-04-02

Applicant: SOLVAY PHARM BV

Inventor： DE BOER DIRK ,  COOLEN HEIN ,  HESSELINK MAYKE ,  IWEMA BAKKER WOUTER ,  KUIL GIJSBERT ,  VAN MAARSEVEEN JAN ,  MCCREARY ANDREW ,  VAN SCHARRENBURG GUSTAAF

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：DE602005017372D1

公开(公告)日：2009-12-10

申请号：DE602005017372

申请日：2005-03-23

Applicant: SOLVAY PHARM BV

Inventor： BAKKER CORNELIS ,  GLENNON JEFFREY C ,  HESSELINK MAYKE B ,  THAETE CLAUDIA ,  MCCREARY ANDREW ,  VAN SCHARRENBURG GUSTAAF J

IPC: A61K31/496 ,  A61K31/00 ,  A61P25/14 ,  A61P25/16

公开(公告)号：AT417834T

公开(公告)日：2009-01-15

申请号：AT06778284

申请日：2006-08-21

Applicant: SOLVAY PHARM BV

Inventor： KOOPMAN THEODORUS ,  KOSTER HENDRIK ,  VAN AMSTERDAM PETER ,  FEENSTRA ROELOF ,  VERHAGE MARINUS ,  MCCREARY ANDREW ,  HESSELINK MAYKE ,  VAN SCHARRENBURG GUSTAAF

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

Abstract: The present invention relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The invention also relates to the use of compounds disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

公开(公告)号：AT401883T

公开(公告)日：2008-08-15

申请号：AT05850037

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF ,  STOIT AXEL ,  TERPSTRA JAN-WILLEM ,  PRAS-RAVES MARIA ,  MCCREARY ANDREW ,  VAN VLIET BERNARD ,  HESSELINK MAYKE ,  KRUSE CORNELIS ,  VAN SCHARRENBURG GUSTAAF

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：CA2554073A1

公开(公告)日：2005-10-06

申请号：CA2554073

申请日：2005-03-23

Applicant: SOLVAY PHARM BV

Inventor： GLENNON JEFFREY C ,  HESSELINK MAYKE B ,  VAN SCHARRENBURG GUSTAAF J ,  THAETE CLAUDIA ,  MCCREARY ANDREW ,  BAKKER CORNELIS

IPC: A61K31/496 ,  A61K31/00 ,  A61P25/14 ,  A61P25/16

Abstract: The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8- yl]~piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT1A receptor agonistic activity, 5-HT1D receptor antagonistic activity and 5-HT7 receptor agonistic activity. The compounds of the invention are useful for t he preparation of medicaments for treating, ameliorating or preventing movement disorders. The invention relates to compounds of the general formula (1) (1) wherein the symbols have the meanings as given in the description.

公开(公告)号：CA2554074A1

公开(公告)日：2005-10-06

申请号：CA2554074

申请日：2005-03-23

Applicant: SOLVAY PHARM BV

Inventor： VAN SCHARRENBURG GUSTAAF J M ,  GLENNON JEFFREY ,  BAKKER CORNELIS ,  THAETE CLAUDIA ,  HESSELINK MAYKE B ,  MCCREARY ANDREW

IPC: A61K31/496 ,  A61P25/04 ,  A61P29/00

Abstract: The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl] ~- piperazine derivatives, broad spectrum 5-HT receptor binding compounds, havi ng amongst other functional serotonin receptor activities, potent 5-HT1A- agonistic as well as 5-HT1D-antagonistic activity. The compounds of the invention are useful for the preparation of medicaments for treating pain. T he invention relates to compounds of the general formula (1) wherein the symbol s have the meanings as given in the description.

公开(公告)号：HRP20040273A2

公开(公告)日：2005-02-28

申请号：HRP20040273

申请日：2004-03-19

Applicant: SOLVAY PHARM BV

Inventor： BOER DIRK DE ,  COOLEN HEIN ,  HESSELINK MAYKE ,  BAKKER WOUTER IWEMA ,  KUIL GIJSBERT ,  MAARSEVEEN JAN VAN ,  MCCREARY ANDREW ,  SCHARRENBURG GUSTAAF J M VAN

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: 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：AT446757T

公开(公告)日：2009-11-15

申请号：AT05717127

申请日：2005-03-23

Applicant: SOLVAY PHARM BV

Inventor： BAKKER CORNELIS ,  GLENNON JEFFREY C ,  HESSELINK MAYKE B ,  THAETE CLAUDIA ,  MCCREARY ANDREW ,  VAN SCHARRENBURG GUSTAAF J

IPC: A61K31/496 ,  A61K31/00 ,  A61P25/14 ,  A61P25/16

Abstract: The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT 1A receptor agonistic activity, 5-Ht 1D receptor antagonistic activity and 5-HT 7 receptor agonistic activity. The compounds of the invention are useful for the preparation of medicaments for treating, ameliorating or preventing movement disorders. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.