公开(公告)号：MY113325A

公开(公告)日：2002-01-31

申请号：MYPI19953312

申请日：1995-11-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JOSE IGNACIO ANDRES-GIL ,  THEO FRANS MEERT ,  FRANCISCO JAVIER FERNANDEZ-GADEA ,  PILAR GIL-LOPETEGUI ,  VICTOR KAREL SIPIDO

IPC: C07D223/20 ,  A61K31/535 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  C07D223/30 ,  C07D261/00 ,  C07D498/00 ,  C07D498/04

Abstract: THIS INVENTION CONCERNS THE COMPOUNDS OF FONNULA (1), THE PHARMACEUTICALLY ACCEPTABLE SALTS AND STEREOISOMERIC FONNS THEREOF, AND ALSO THE N-OXIDE FONNS THEREOF. WHEREIN : RL AND R2 EACH INDEPENDENTLY ARE HYDROGEN; CL-6ALKYL; CL-6ALKYLCARBONYL; TRIHALOMETHYLCARBONYL; CL-6 ALKYL SUBSTITUTED WITH HYDROXY, CL-6 ALKYLOXY, CARBOXYL, CL-6 ALKYLCARBONYLOXY, CL-6 ALKYLOXYCARBONYL OR ARYL; OR R 1 AND R2 TAKEN TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED MAY FONN A MORPHOLINYL RING OR AN OPTIONALLY SUBSTITUTED HETEROCYCLE; R3, R4, R5, R6, R9, RL0, RLL OR RL2 EACH INDEPENDENTLY ARE HYDROGEN, HALO, CYANO, HYDROXY, TRIFLUOROMETHYL, TRIFLUOROMETHOXY, CARBOXYL, NITTO, AMINO, MONO- OR DI(CI-6ALKYL)-AMINO, CL-6ALKYLCARBONYLAMINO, AMINOSULFONYL, MONO- OR DI(CL-6ALKYL)-AMINOSULFONYL, CL-6ALKYL, CL-6ALKYLOXY, CL-6 )ALKYLCARBONYL, CL-6ALKYLOXY-CARBONYL; R7 AND R8 ARE EACH INDEPENDENTLY HYDROGEN, HYDROXY, CL-6ALKYL, CL-6ALKYLOXY OR R7 AND R8 TAKEN TOGETHER MAY FORM MONO- OR DI(CYANO)METHYLENE, OR TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED FONN A CARBONYL OR A SPIRO SUBSTITUENT; OR R7 AND R8 TAKEN TOGETHER MAY FORM METHYLENE; RL3 IS HYDROGEN, CL-6ALKYL, OR TRIFLUOROMETHYL; RL4 IS HYDROGEN, CL-6ALKYL, CYANO, OR TRIFLUOROMETHYL; N IS ZERO TO 6. THESE COMPOUNDS WERE TESTED AS MCPP-ANTAGONISTS IN RATS. THE COMPOUNDS OF FONNULA (I) MAY BE USED AS THERAPEUTIC AGENTS IN THE TREATMENT OR THE PREVENTION OF CNS DISORDERS, CARDIOVASCULAR DISORDERS OR GASTROINTESTINAL DISORDERS.

公开(公告)号：HRP20040427B1

公开(公告)日：2012-09-30

申请号：HRP20040427

申请日：2004-05-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TEGTMEIER FRANK ,  FRANS EDUARD JANSSENS ,  JOSEPH ELISABETH LEENAERTS ,  KOENRAAD ARTHUR VAN ROSSEM ,  MANUEL JESUS ALCAZAR-VACA ,  PEDRO MARTINEZ-JIMENEZ ,  JOSE MANUEL BARTOLOME-NEBREDA ,  ANTONIO GOMEZ-SANCHEZ ,  FRANCISCO JAVIER FERNANDEZ-GADEA ,  JOZEF LEO

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00

Abstract: The invention concerns the use of an H1- and/or H2-histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. In particular, the histamine antagonist is selected from the group of acrivastine, alimemazine, antazoline, astemizole, azatadine, azelastine, brompheniramine, buclizine, carbinoxamine, carebastine, cetirizine, chlorcyclizine, chlorpheniramine, cinnarizine, clemastine, clemizole, clocinizine, clonidine, cyclizine, cyproheptadine, descarboethoxyloratidine, dexchlorpheniramine, dimenhydrinate, dimethindene, dimethothiazine, diphenhydramine, diphenylpyraline, doxylamine, ebastine, efletirizine, epinastine, fexofenadine, hydroxyzine, ketotifen, levocabastine, loratidine, meclizine, mequitazine, methdilazine, mianserin, mizolastine, niaprazine, noberastine, norastemizole, oxatomide, oxomemazine, phenbenzamine, pheniramine, picumast, promethazine, pyrilamine, temelastine, terfenadine, trimeprazine, tripelennamine, triprolidine, ranitidine, cimetidine, famotidine, nizatidine, tiotidine, zolantidine, ritanserine, and derivatives thereof and mixtures of any two or more of the foregoing.

公开(公告)号：ZA200403923B

公开(公告)日：2005-10-26

申请号：ZA200403923

申请日：2004-05-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JOSEPH ELISABETH LEENAERTS ,  FRANS EDUARD JANSSENS ,  MANUEL JESUS ALCAZAR-VACA ,  FRANCISCO JAVIER FERNANDEZ-GADEA ,  JOSE MANUEL BARTOLOME-NEBREDA ,  ANTONIO GOMEZ-SANCHEZ ,  FRANK TEGTMEIER ,  KOENRAAD ARTHUR VAN ROSSEM ,  PEDRO MARTINEZ-JIMENEZ ,  JOZEF LEO HENRI VAN REEMPTS

IPC: C07D20060101 ,  A61K20060101 ,  C07D487/04 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P20060101 ,  A61P1/04 ,  A61P9/10 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00 ,  C07D519/00

Abstract: The invention concerns the use of an H1- and/or H2-histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. In particular, the histamine antagonist is selected from the group of acrivastine, alimemazine, antazoline, astemizole, azatadine, azelastine, brompheniramine, buclizine, carbinoxamine, carebastine, cetirizine, chlorcyclizine, chlorpheniramine, cinnarizine, clemastine, clemizole, clocinizine, clonidine, cyclizine, cyproheptadine, descarboethoxyloratidine, dexchlorpheniramine, dimenhydrinate, dimethindene, dimethothiazine, diphenhydramine, diphenylpyraline, doxylamine, ebastine, efletirizine, epinastine, fexofenadine, hydroxyzine, ketotifen, levocabastine, loratidine, meclizine, mequitazine, methdilazine, mianserin, mizolastine, niaprazine, noberastine, norastemizole, oxatomide, oxomemazine, phenbenzamine, pheniramine, picumast, promethazine, pyrilamine, temelastine, terfenadine, trimeprazine, tripelennamine, triprolidine, ranitidine, cimetidine, famotidine, nizatidine, tiotidine, zolantidine, ritanserine, and derivatives thereof and mixtures of any two or more of the foregoing.

公开(公告)号：ZA200402818B

公开(公告)日：2005-06-29

申请号：ZA200402818

申请日：2004-04-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： THEO FRANS MEERT ,  FRANS EDUARD JANSSENS ,  JOSEPH ELISABETH LEENAERTS ,  FRANCISCO JAVIER FERNANDEZ-GADEA ,  ANTONIO GOMEZ-SANCHEZ

IPC: C07D20060101 ,  A61K20060101 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61P20060101 ,  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：ZA200402816B

公开(公告)日：2005-06-29

申请号：ZA200402816

申请日：2004-04-13

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20060101 ,  C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P20060101 ,  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.