公开(公告)号：PL209953B1

公开(公告)日：2011-11-30

申请号：PL36986402

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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

公开(公告)号：SI1832287T1

公开(公告)日：2009-06-30

申请号：SI200230813

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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

公开(公告)号：DE60231351D1

公开(公告)日：2009-04-09

申请号：DE60231351

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/415 ,  C07D487/04 ,  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 ,  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：HK1101672A1

公开(公告)日：2007-10-26

申请号：HK07106604

申请日：2005-07-15

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K20090101 ,  A61K31/415 ,  A61K31/425 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P20090101 ,  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：AT370149T

公开(公告)日：2007-09-15

申请号：AT02803410

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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：HU0402357A2

公开(公告)日：2005-02-28

申请号：HU0402357

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  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 ,  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：AU2002356715B2

公开(公告)日：2008-05-15

申请号：AU2002356715

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  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 ,  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：DK1451196T3

公开(公告)日：2007-11-12

申请号：DK02803410

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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：PT1451196E

公开(公告)日：2007-10-25

申请号：PT02803410

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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

公开(公告)号：AU2002319232B2

公开(公告)日：2007-09-06

申请号：AU2002319232

申请日：2002-06-11

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： JANSSENS FRANS EDUARD ,  GOMEZ-SANCHEZ ANTONIO ,  ROSSEM KOENRAAD ARTHUR VAN ,  MARTINEZ-JIMENEZ PEDRO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  LEENAERTS JOSEPH ELISABETH ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ALCAZAR-VACA MANUEL JESUS ,  REEMPTS JOS VAN

IPC: C07D471/04 ,  A61K9/10 ,  A61K31/00 ,  A61K31/519 ,  A61K31/55 ,  A61P3/00 ,  A61P7/10 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D519/00

Abstract: The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-alpha]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.