公开(公告)号：DE60216310D1

公开(公告)日：2007-01-04

申请号：DE60216310

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS EDUARD ,  LEENAERTS ELISABETH ,  FLAMENG WILLEM ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT FRANS ,  BORGERS J ,  HERIJGERS PAUL JOANNES LUDOVIC

IPC: A61K31/454 ,  C07D401/04 ,  A61K31/4545 ,  A61K31/506 ,  A61K45/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：AU2002363369B2

公开(公告)日：2008-08-21

申请号：AU2002363369

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： HERIJGERS PAUL JOANNES LUDOVICUS ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  LEENAERTS JOSEPH ELISABETH ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  BORGERS MARCEL J M ,  JANSSENS FRANS EDUARD ,  MEERT THEO FRANS

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：NO20041681L

公开(公告)日：2004-04-23

申请号：NO20041681

申请日：2004-04-23

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BORGERS MARCEL JAN MARIA ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MEERTS THEO FRANS ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：NO20041681A

公开(公告)日：2004-04-23

申请号：NO20041681

申请日：2004-04-23

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BORGERS MARCEL JAN MARIA ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MEERTS THEO FRANS ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: A61K31/454

公开(公告)号：CA2462374A1

公开(公告)日：2003-05-15

申请号：CA2462374

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LEENAERTS JOSEPH ELISABETH ,  FLAMENG WILLEM ,  MEERT THEO FRANS ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  BORGERS MARCEL J M ,  JANSSENS FRANS EDUARD ,  GOMEZ-SANCHEZ ANTONIO ,  HERIJGERS PAUL JOANNES LUDOVIC

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to a n organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaem ic diseases to the heart and the brain. The agent comprises a substituted 4- phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) t he pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N - oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C=O or SO2, X is a covale nt bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar ; or A=B and R1 together form a benzoxazoly l radical ; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaem ic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：NZ531733A

公开(公告)日：2006-04-28

申请号：NZ53173302

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4523

Abstract: A substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperdine compound according to Formula (I) which is used for the manufacture of a medicament for reducing ischaemic damage to an organ, in particular to a heart and a brain.

公开(公告)号：BR0213325A

公开(公告)日：2004-10-13

申请号：BR0213325

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：HRP20040325A2

公开(公告)日：2005-04-30

申请号：HRP20040325

申请日：2004-04-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO J ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：HU0402332A2

公开(公告)日：2005-02-28

申请号：HU0402332

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVIC ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

IPC: C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the 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 use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

公开(公告)号：CA2462374C

公开(公告)日：2011-01-18

申请号：CA2462374

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  GOMEZ-SANCHEZ ANTONIO ,  FLAMENG WILLEM ,  HERIJGERS PAUL JOANNES LUDOVICUS ,  MEERT THEO FRANS ,  BORGERS MARCEL J M

IPC: A61K31/454 ,  C07D401/04 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C=O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar ; or A=B and R1 together form a benzoxazolyl radical ; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.