公开(公告)号：CA2561975C

公开(公告)日：2012-12-11

申请号：CA2561975

申请日：2005-04-04

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D471/10 ,  A61K31/438 ,  A61P29/00

Abstract: This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonist ic activity, a combined NK1/NK3 antagonist ic 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：CA2561944C

公开(公告)日：2012-11-27

申请号：CA2561944

申请日：2005-04-04

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D471/10 ,  A61K31/438 ,  A61P29/00

Abstract: This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 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, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) (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：AU2006221984B2

公开(公告)日：2011-04-21

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：MX2010011767A

公开(公告)日：2010-11-30

申请号：MX2010011767

申请日：2009-04-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEERPOEL LIEVEN ,  LINDERS JOANNES THEODORUS MARIA ,  VER DONCK LUC AUGUST LAURENTIUS ,  DOYON JULIEN GEORGES PIERRE-OLIVIER ,  SCHOENTJES BRUNO ,  PONCELET ALAIN PHILIPPE

IPC: C07C215/44 ,  A61K31/135 ,  A61K31/335 ,  C07C213/02 ,  C07C213/08 ,  C07C217/52 ,  C07C313/08

Abstract: La presente invención se refiere a un compuesto de la fórmula (I), (ver fórmula I) incluyendo cualquier forma estereoquímicamente isomérica del mismo, en donde los sustituyentes son como se define en la especificación y las reivindicaciones; un N-óxido del mismo, una sal farmacéuticamente aceptable del mismo o un solvato del mismo; siempre que el compuesto sea distinto de la fórmula (B) (ver fórmula B) o una sal farmacéuticamente aceptable del mismo; los compuestos reivindicados son útiles para el tratamiento de una enfermedad, el tratamiento de la cual es afectado, mediado o facilitado por activación del receptor de GHS1A-r; la invención también se refiere a composiciones farmacéuticas del mismo y procedimientos para la preparación del mismo.

公开(公告)号：ES2346985T3

公开(公告)日：2010-10-22

申请号：ES05729796

申请日：2005-04-04

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D471/10 ,  A61K31/438 ,  A61P29/00

Abstract: Un compuesto de acuerdo con la Fórmula general (I), **(Ver fórmula)** sus sales de adición de ácido o base farmacéuticamente aceptables, sus formas estereoquímicamente isoméricas y su forma de N-óxido, donde: R2 es Ar2; X es un enlace covalente; Q es O; R1 es alquil-Ar1; n es un número entero, igual a 1; m es un número entero, igual a 1; Z es un enlace covalente; j, k, p, q son números enteros, independientemente unos de otros, iguales a 1 ó 2; siempre que (j+k) y(p+q) sean cada uno igual a 3 ó 4 y siempre que cuando (j+k) sea igual a 3, entonces (p+q) sea igual a 4; o cuando (j+k) sea igual a 4, entonces (p+q) sea igual a 3; dos radicales T adyacentes se pueden juntar para formar un radical de fórmula =CH-CH=CH-CH=; y t es un número entero, igual a 0 ó 2; cada Alk representa, independientemente uno de otro, un enlace covalente; un radical hidrocarburo lineal bivalente saturado que contiene de 1 a 6 átomos de carbono; Y es un radical bivalente de fórmula -C(=O)-, -SO2-; L se selecciona del grupo conformado por alquilo, alquiloxi, Ar3 y Het2; Ar1 es fenilo; Ar2 es fenilo sustituido con 2 radicales alquilo; Ar3 es fenilo, opcionalmente sustituido con 1 sustituyente seleccionado del grupo conformado por alquilo y halo; Het2 es un radical heterocíclico monocíclico seleccionado del grupo conformado por tetrahidrofuranilo, furanilo y tienilo; Alquilo es un radical hidrocarburo lineal saturado que contiene de 1 a 6 átomos de carbono o un radical hidrocarburo cíclico saturado que contiene de 3 a 6 átomos de carbono; estando cada radical hidrocarburo opcionalmente sustituido en uno o más átomos de carbono con uno o más radicales seleccionados del grupo conformado por halo.

公开(公告)号：BRPI0608847A2

公开(公告)日：2010-02-02

申请号：BRPI0608847

申请日：2006-03-03

Applicant: JANSSEN PHARMACEUTICA NV

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

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：EA012421B1

公开(公告)日：2009-10-30

申请号：EA200701879

申请日：2006-03-03

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: Данноеизобретениекасаетсязамещенныхпроизводныхоксадиазаспиро[5.5]ундеканона, имеющихантагонистическуюактивностьв отношениинейрокинина, вчастности NK-антагонистическуюактивность, NK-антагонистическуюактивность, объединенную NK/NK-антагонистическуюактивностьи объединенную NK/NK/NK-антагонистическуюактивность, ихполучения, композиций, ихсодержащих, иихпримененияв качествелекарственногосредства, вчастности, длялеченияи/илипрофилактикишизофрении, рвоты, тревожностии депрессии, синдромараздраженногокишечника (IBS), нарушенийциркадногоритма, преэклампсии, ноцицепции, боли, вчастностивисцеральнойи невропатическойболи, панкреатита, нейрогенноговоспаления, астмы, хроническогообструктивногозаболеваниялегких (ХОЗЛ) ирасстройствмочеиспускания, такихкакнедержаниемочи. Соединенияв соответствиис даннымизобретениеммогутбытьпредставленыобщейформулой (I)ивключаюттакжеихфармацевтическиприемлемыекислотно-аддитивныесоли, ихстереохимическиизомерныеформыи форму N-оксида, гдевсезаместителиявляютсятакими, какопределенов п.1 формулыизобретения.

公开(公告)号：EE05195B1

公开(公告)日：2009-08-17

申请号：EEP200300126

申请日：2001-09-25

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/047 ,  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

Abstract: The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z4-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula -CH2-CH2-CH2-CH2-; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

公开(公告)号：HK1103073A1

公开(公告)日：2007-12-14

申请号：HK07107482

申请日：2007-07-12

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20100101 ,  A61K31/438 ,  A61P20100101 ,  A61P29/00 ,  C07D20100101 ,  C07D471/10

Abstract: This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 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, 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：MX2007011079A

公开(公告)日：2007-10-08

申请号：MX2007011079

申请日：2006-03-03

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: Esta invencion se relaciona con derivados sustituidos de diaza-espiro-[4.4]-nonano que tienen actividad antagonista de la neurocinina, en particular una actividad antagonista de NK1, su preparacion, composiciones que los comprenden y su uso como una medicina, en particular para el tratamiento y/o profilaxis de la esquizofrenia, emesis, ansiedad y depresion, sindrome del intestino irritable (IBS), perturbaciones del ritmo circadiano, preeclampsia, nocicepcion, dolor, en particular dolor visceral y 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 por la Formula (I) general y comprenden tambien las sales de adicion de acido o base farmaceuticamente aceptables de los mismos, las formas estereoquimicamente isomericas de los mismos, la forma de N oxido de los mismos y profarmacos de los mismos, en donde todos los sustituyentes se definen como en la Reivindicacion 1. (ver formula (I)).