公开(公告)号：AT353649T

公开(公告)日：2007-03-15

申请号：AT04726520

申请日：2004-04-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： STECKLER THOMAS HORST WOLFGANG ,  JANSSENS FRANS EDUARD JANSSEN ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO J ,  GOMEZ-SANCHEZ ANTONIO ,  MEERT THEO FRANS

IPC: A61K31/454 ,  A61K31/506 ,  A61P25/22 ,  A61P25/24 ,  A61K31/4545 ,  A61K31/496 ,  A61P3/04

Abstract: The present invention relates to the use of 4-phenyl-4-[1H-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 as selective non-peptide delta-opioid agonists for use in the prevention and/or treatment of various central nervous system disorders, in particular as selective antidepressant and anxiolytic non-peptide delta-opioid agonists. 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 allyloxy, 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.

公开(公告)号：NO20065022A

公开(公告)日：2006-11-03

申请号：NO20065022

申请日：2006-11-03

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LEENAERTS JOSEPH ELISABETH ,  SOMMEN FRANCOIS MARIA ,  BOECK BENOIT CHRISTIAN ALBERT ,  EDUARD FRANS

IPC: C07D401/12 ,  A61K31/495 ,  A61K31/496 ,  A61P25/00 ,  C07D211/16 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D409/14 ,  C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

公开(公告)号：HK1087703A1

公开(公告)日：2006-10-20

申请号：HK06107904

申请日：2006-07-14

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBERT GHISLAIN ,  LEENAERTS JOSEPH ELISABETH

IPC: A61K20060101 ,  A61K31/454 ,  A61P20060101 ,  A61P25/00 ,  C07D20060101 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/14

Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 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 of schizophrenia, anxiety, depression, emesis and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

公开(公告)号：ZA200505070B

公开(公告)日：2006-09-27

申请号：ZA200505070

申请日：2005-06-22

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  BOECK BENOIT CHRISTIAN ALBERT ,  SOMMEN FRANCOIS MARIA ,  LEENAERTS JOSEPH ELISABETH

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

公开(公告)号：HK1084394A1

公开(公告)日：2006-07-28

申请号：HK06104676

申请日：2006-04-19

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBERT GHISLAIN ,  LEENAERTS JOSEPH ELISABETH ,  ROOSBROECK YVES EMIEL MARIA VAN ,  DIELS GASTON STANISLAS MARCELLA

IPC: C07D20100101 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.

公开(公告)号：UA75980C2

公开(公告)日：2006-06-15

申请号：UA20040503666

申请日：2002-10-10

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSEN PAUL ADRIAAN JAN ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  HERIJGERS PAUL JOANNES LUDOVIC ,  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 the agent for reducing ischaemic damage of 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-pheny1-4-[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 R 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 , (I)

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：CA2238816C

公开(公告)日：2006-03-21

申请号：CA2238816

申请日：1996-12-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SURLERAUX DOMINIQUE LOUIS NEST ,  LEENAERTS JOSEPH ELISABETH ,  SOMMEN FRANCOIS MARIA

IPC: C07D413/14 ,  A61K31/00 ,  A61K31/415 ,  A61K31/435 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/498 ,  A61K31/55 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P25/00 ,  A61P25/04 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

Abstract: This invention concerns the compounds of formula (I), (see formula I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2 , provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR3-; =Q is =O or =NR3; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl wherein the C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B); (see formula II) wherein p is 0, 1 or 2; (see formula III)Y~ is a bivalent radical of formula -CH2-, -CH(OH)-, -C(=O) -, -O-, -S-, - S(=O)-, -S(=O)2-, -NR3-, -CH2-NR3- or -C(=O)-NR3-; or a trivalent radical of formula =CH-; -A=B- is a bivalent radical of formula -CH=CH-, -N=CH- or -CH=N-; R3 independently is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl or a radical of formula -Alk-R7 ~(c-1) or -Alk Z-R8 ~(c-2); wherein Alk is C1-6alkanediyl; Z is a bivalent radical of formula -O-, -S- or -NR3-; R7 is phenyl; phenyl substituted with 1 or 2 substituents selected from halo, C1-6alkyl and . C1-6alkyloxy; furanyl; furanyl substituted with 1 or 2 ~~ substituents selected from C1-6alkyl, and hydroxyC1-6alkyl;thienyl; thienyl substituted with 1 or 2 substituents selected from halo and C1-6alkyl; oxazolyl; oxazolyl substituted with 1 or 2 C1-6alkyl substituents; thiazolyl; thiazolyl substituted with 1 or 2 C1-6alkyl substituents; pyridinyl or pyridinyl substituted with 1 or 2 C1-6alkyl substituents; R8 is C1-6alkyl or C1-6alkyl substituted with hydroxy, carboxyl or C1-6alkyloxycarbonyl; R5 is hydrogen, halo, hydroxy or C1-6alkyloxy; R6 is hydrogen, C1-6alkyl or Ar1C1-6alkyl; Ar1 is optionally substituted phenyl; Ar2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bycyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：PL376403A1

公开(公告)日：2005-12-27

申请号：PL37640303

申请日：2003-10-07

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DIELS GASTON STANISLAS MARCELL ,  VAN ROOSBROECK YVES EMIEL MARI ,  LEENAERTS JOSEPH ELISABETH ,  DE BOECK BENOIT CHRISTIAN ALBE

IPC: C07D211/58 ,  C07D409/14 ,  C07D413/14

公开(公告)号：PL376048A1

公开(公告)日：2005-12-12

申请号：PL37604803

申请日：2003-12-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  SOMMEN FRANCOIS MARIA ,  DE BOECK BENOIT CHRISTIAN ALBE ,  LEENAERTS JOSEPH ELISABETH

IPC: A61K31/454 ,  A61P25/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/14

Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 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 of schizophrenia, anxiety, depression, emesis and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.