公开(公告)号：AT347549T

公开(公告)日：2006-12-15

申请号：AT02782881

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS F E ,  LEENAERTS J E ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT THEO FRANS

IPC: A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel 4-phenyl-4-[ 1 H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A=B is C-O or SO 2 , X is a covalent bond, R 1 is alkyloxy, alkyloxyalkyl, Ar or NR 9 R 10 , wherein R 9 and R 10 each independently are hydrogen or Ar; or A=B and R 1 together form a benzoxazolyl radical; p is zero, R 3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R 4 and R 5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide delta-opioid agonists for use in the treatment of various pain conditions.

公开(公告)号：DE60216627T2

公开(公告)日：2007-09-20

申请号：DE60216627

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS F E ,  LEENAERTS J E ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT THEO

IPC: C07D401/04 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel 4-phenyl-4-[ 1 H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A=B is C-O or SO 2 , X is a covalent bond, R 1 is alkyloxy, alkyloxyalkyl, Ar or NR 9 R 10 , wherein R 9 and R 10 each independently are hydrogen or Ar; or A=B and R 1 together form a benzoxazolyl radical; p is zero, R 3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R 4 and R 5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide delta-opioid agonists for use in the treatment of various pain conditions.

公开(公告)号：PT1438304E

公开(公告)日：2007-03-30

申请号：PT02782881

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEERT THEO FRANS ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  GOMEZ-SANCHEZ ANTONIO ,  JANSSENS F E ,  LEENAERTS J E

IPC: C07D401/04 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

公开(公告)号：ES2278065T3

公开(公告)日：2007-08-01

申请号：ES02782881

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS F E ,  LEENAERTS J E ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT THEO FRANS

IPC: C07D401/04 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: Un compuesto según la fórmula (I) (Ver fórmula) sus sales por adición de ácidos o bases farmacéuticamente aceptables, sus formas de isómeros estereoquímicos, sus formas tautómeras y sus formas N-óxidos, en la cual: A=B es un radical divalente de enlaces pi; X es un enlace covalente, -CH2- o CH2CH2-; R1 es hidrógeno, alquiloxi, alquilcarboniloxi, Ar-oxi, Het-oxi, Ar-carboniloxi, Het-carboniloxi, Ar-alquiloxi, Het-alquiloxi, alquilo, polihaloalquilo, alquiloxialquilo, Ar-alquilo, Het-alquilo, Ar, Het, tio, alquiltio, Ar-tio, Het-tio o NR9R10 en que R9 y R10 son cada uno independientemente hidrógeno, alquilo, Ar, Ar-alquilo, Het, Het-alquilo, alquil-carbonilo, Ar-carbonilo, Het-carbonilo o alquiloxicarbonilalquilo; o A=B y R1 forman conjuntamente un radical carbocíclico o heterocíclico, semi-aromático o aromático opcionalmente sustituido Het2 o Het3; R2 es hidroxi, alquiloxi, alquilcarboniloxi, feniloxi, fenilcarboniloxi, halo, ciano, alquilo, polihaloalquilo, alquiloxialquilo, formilo, carboxi, alquilcarbonilo, alquiloxicarbonilo, aminocarbonilo, mono- o di-alquilaminocarbonilo, fenilo, nitro, amino, mono- o di-alquilamino, tio o alquiltio; R3 es alquilo, Ar, Ar-alquilo, Ar-alquenilo, Het, Het-alquilo o Het-alquenilo; R4 y R5 son cada uno independientemente hidrógeno, alquilo, carboxi, aminocarbonilo, alquiloxicarbonilo, halo o hidroxialquilo; p es un número entero igual a cero 1, 2 ó 3.

公开(公告)号：DE60216627D1

公开(公告)日：2007-01-18

申请号：DE60216627

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS F E ,  LEENAERTS J E ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT FRANS

IPC: C07D401/04 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P1/00 ,  A61P1/04 ,  A61P1/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to novel 4-phenyl-4-[ 1 H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A=B is C-O or SO 2 , X is a covalent bond, R 1 is alkyloxy, alkyloxyalkyl, Ar or NR 9 R 10 , wherein R 9 and R 10 each independently are hydrogen or Ar; or A=B and R 1 together form a benzoxazolyl radical; p is zero, R 3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R 4 and R 5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide delta-opioid agonists for use in the treatment of various pain conditions.

公开(公告)号：ZA200502837B

公开(公告)日：2006-06-28

申请号：ZA200502837

申请日：2005-04-07

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRAS E ,  DE BOECK BENOIT C A G ,  VAN ROOSBROECK Y E M ,  SOMMEN F M ,  LEENAERTS J E ,  DIELS G S M

IPC: C07D20060101 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04