公开(公告)号：CA2598530A1

公开(公告)日：2006-09-14

申请号：CA2598530

申请日：2006-03-03

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： SCHOENTJES BRUNO ,  PONCELET ALAIN PHILIPPE ,  JANSSENS FRANS EDUARD ,  COUPA SOPHIE

IPC: C07D498/10 ,  A61K31/537 ,  A61P25/18 ,  A61P25/24

Abstract: This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

公开(公告)号：AU2006221984A1

公开(公告)日：2006-09-14

申请号：AU2006221984

申请日：2006-03-03

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  PONCELET ALAIN PHILIPPE ,  SCHOENTJES BRUNO ,  COUPA SOPHIE ,  SIMONNET YVAN RENE FERDINAND

IPC: C07D487/08 ,  A61K31/435 ,  A61P25/00

Abstract: This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

公开(公告)号：PA8628201A1

公开(公告)日：2005-11-25

申请号：PA8628201

申请日：2005-04-01

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SCHOENTJES BRUNO ,  COUPA SOPHIE ,  PONCELET ALAIN PHILIPPE ,  SIMONNET YVAN RENE FERDINAND

IPC: C07D471/10

Abstract: LA PRESENTE INVENCION SE REFIERE A DERIVADOS SUSTITUIDOS DE DIAZA- ESPIRO-[5.5]-UNDECANO QUE TIENEN ACTIVIDAD ANTAGONISTA DE NEUROQUININAS, EN PARTICULAR ACTIVIDAD ANTAGONISTA DE NK1, UNA ACTIVIDAD ANTAGONISTA COMBINADA DE NK1/NK2, UNA ACTIVIDAD ANTAGONISTA COMBINADA DE NK1/NK3 Y UNA ACTIVIDAD ANTAGONISTA COMBINADA DE NK1/NK2/NK3, A SU PREPARACION, A COMPOSICIONES QUE LOS CONTIENEN Y A SU USO COMO MEDICAMENTO, EN PARTICULAR PARA TRATAMIENTO Y/O PROFILAXIS DE LA ESQUIZOFRENIA, EMESIS, ANSIEDAD Y DEPRESION, SINDROME DEL INTESTINO IRRITABLE (IBS), TRASTORNOS DEL RITMO CIRCADIANO, PRE-ECLAMSIA, NOCICEPCION, DOLOR, EN PARTICULAR, DOLOR VISCERAL Y DOLOR NEUROPATICO, PANCREATITIS, INFLAMACION NEUROGENICA, ASMA, ENFERMEDAD PULMONAR OBSTRUCTIVA CRONICA (COPD) Y TRASTORNOS DE LA MICCION TALES COMO INCONTINENCIA URINARIA. LOS COMPUESTOS DE ACUERDO CON LA INVENCION PUEDEN REPRESENTARSE MEDIANTE LA FORMULA (l). Y COMPRENDE ADEMAS SUS SALES DE ADICION CON BASES O CON ACIDOS ACEPTABLES PARA USO FARMACEUTICO, SUS FORMAS ESTEREOQUIMICAMENTE ISOMERICAS, SUS FORMAS N-OXIDO Y SUS PROFARMACOS, DONDE TODOS LOS SUSTITUYENTES SE DEFINEN SEGUN LA REIVINDICACION 1.

公开(公告)号：NO20031474A

公开(公告)日：2003-05-05

申请号：NO20031474

申请日：2003-04-01

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MABIRE DOMINIQUE JEAN-PIERRE ,  VENET MARC GASTON ,  COUPA SOPHIE ,  PONCELET ALAIN PHILIPPE ,  LESAGE ANNE SIMONE JOSEPHINE

IPC: A61K31/47 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/08 ,  A61P5/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P43/00 ,  C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/22 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D215/60 ,  C07D219/02 ,  C07D221/10 ,  C07D221/12 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D453/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07F7/08 ,  C07F7/10

CPC classification number: C07D215/04 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D215/50 ,  C07D215/54 ,  C07D221/10 ,  C07D221/12 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D417/04 ,  C07D453/06 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07F7/0812