公开(公告)号：BR0111859B1

公开(公告)日：2015-01-06

申请号：BR0111859

申请日：2001-06-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EMELEN KRISTOPH VAN ,  BRUYN MARCEL FRANS LEOPOLD DE ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  MATESANZ-BALLESTEROS MARIA ENCARNACION ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D491/056 ,  C07D491/06 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4545 ,  A61K31/513 ,  A61K31/5383 ,  A61P1/00 ,  A61P1/14 ,  C07D411/04 ,  C07D491/04 ,  C07D491/052 ,  C07D497/04 ,  C07D498/04

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a 1 -a 2 -a 3 -a 4 - is a bivalent radical wherein one or two of a 1 to a 4 are nitrogen and the remaining a 1 to a 4 are -CH-; -Z 1 -Z 2 - is a bivalent radical; -A- is a bivalent radical of formula -N(R 6 )-Alk 2 - or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; Alk 1 and Alk 2 are optionally substituted C 1-6 alkanediyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y 2 is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

公开(公告)号：AU2009266001B2

公开(公告)日：2014-03-27

申请号：AU2009266001

申请日：2009-07-01

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN GOOL MICHIEL LUC MARIA ,  BARTOLOME-NEBREDA JOSE MANUEL ,  CONDE-CEIDE SUSANA ,  MACDONALD GREGOR JAMES ,  DELGADO-JIMENEZ FRANCISCA

IPC: C07D237/20 ,  A61K31/501 ,  A61P3/04 ,  C07D237/22 ,  C07D401/12

Abstract: The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) wherein R

公开(公告)号：NO333656B1

公开(公告)日：2013-08-05

申请号：NO20042618

申请日：2004-06-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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：AU2008214716B2

公开(公告)日：2013-05-09

申请号：AU2008214716

申请日：2008-02-11

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LANGLOIS XAVIER JEAN MICHEL ,  VAN GOOL MICHIEL LUC MARIA ,  BARTOLOME-NEBREDA JOSE MANUEL ,  MACDONALD GREGOR JAMES

IPC: C07D237/20 ,  A61K31/495 ,  A61P25/18 ,  C07D237/24 ,  C07D409/04 ,  C07D487/04

Abstract: The present invention relates to 4-aryl-6-piperazin-1-yl-3-substituted-pyridazines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, forexample schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：RS52518B

公开(公告)日：2013-04-30

申请号：RSP20120481

申请日：2008-04-18

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  BARTOLOME-NEBREDA JOSE MANUEL

IPC: C07D401/12 ,  A61K31/501 ,  A61P25/18

Abstract: The present invention relates to (1-benzyl-piperidin-4-yl)-(4-alkoxy-pyridazin-3-y1)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：EA017508B1

公开(公告)日：2013-01-30

申请号：EA200970760

申请日：2008-02-11

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  LANGLOIS XAVIER JEAN MICHEL ,  BARTOLOME-NEBREDA JOSE MANUEL ,  VAN GOOL MICHIEL LUC MARIA

IPC: C07D237/20 ,  A61K31/495 ,  C07D237/24 ,  C07D409/04 ,  C07D487/04

Abstract: Изобретениеотноситсяк 4-арил-6-пиперазин-1-ил-3-замещеннымпиридазинам, которыеявляютсябыстродиссоциирующимиантагонистамирецептора 2 дофамина. Описываемыесоединениянаходятприменениев качествелекарственныхсредств, предназначенныхдлялеченияилипредотвращениярасстройствцентральнойнервнойсистемы, напримершизофрении, благодарятому, чтоонипроявляютантипсихотическоедействиебезпобочныхмоторныхэффектов.

公开(公告)号：CA2690483C

公开(公告)日：2012-07-24

申请号：CA2690483

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: A61K31/4402 ,  C07D487/04 ,  A61K31/138 ,  A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61K31/445 ,  A61K31/4535 ,  A61K31/495 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5415 ,  A61K31/55 ,  A61P1/04 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  C07D471/00 ,  C07D471/04 ,  C07D487/00 ,  C07D519/00

Abstract: Disclosed is use of a histamine receptor antagonist for the manufacture of a medicament for reduction of intracranial pressure (ICP). Histamine receptor antagonists useful for this purpose include: histamine H1-receptor antagonists, histamine H2-receptor antagonists and histamine receptor antagonists with a combined H1/H2 antagonistic activity. Also disclosed are uses of the same histamine receptor antagonists for the reduction and prevention of elevated ICP or secondary ischaemia in a mammal, and medicaments for the same.

公开(公告)号：MX2012007006A

公开(公告)日：2012-07-03

申请号：MX2012007006

申请日：2010-12-16

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  MACDONALD GREGOR JAMES ,  BARTOLOME-NEBREDA JOSE MANUEL ,  CONDE-CEIDE SUSANA ,  TRESADERN GARY JOHN ,  PASTOR-FERNANDEZ JOAQUIN

IPC: C07D513/04 ,  A61K31/428 ,  A61K31/429 ,  A61P25/18

Abstract: La presente invención se refiere a novedosos tiazoles bicíclicos los cuales son moduladores alostéricos positivos del subtipo 5 receptor de glutamato metabotrópico ("mGluR5") y los cuales son útiles para el tratamiento o prevención de trastornos asociados con la disfunción de glutamato y enfermedades en las cuales el subtipo mGluR5 de receptores está involucrado; la invención se refiere además a composiciones farmacéuticas que comprenden dichos compuestos, a procesos para preparar dichos compuestos y composiciones, y al uso de dichos compuestos y composiciones para la prevención y tratamiento de trastornos en los cuales mGluR5 está involucrado.

公开(公告)号：JO2642B1

公开(公告)日：2012-06-17

申请号：JOP20070479

申请日：2007-11-19

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  MACDONALD GREGOR JAMES ,  BARTOLOME-NEBREDA JOSE MANUEL ,  VAN GOOL MICHIEL LUC MARIA

Abstract: The precent invention relates to 6-(piperidine -4-ylamino)pyridazin-3-carbonitriles that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The Compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effect.

公开(公告)号：CA2494235C

公开(公告)日：2011-10-11

申请号：CA2494235

申请日：2003-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  BARTOLOME-NEBREDA JOSE MANUEL ,  ALVAREZ-ESCOBAR ROSA MARIA ,  BAKKER MARGARETHA HENRICA MARIA ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS

IPC: C07D498/04 ,  A61K31/424 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/04 ,  A61P25/02 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D261/00 ,  C07D311/00

Abstract: The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline , dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in Claim 1. (I) The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity in combination with additional .alpha.2-adrenoceptor antagonist activity and show a strong anti-depressant and/or anxiolytic activity and/or antipsychotic and/or a body weight control activity without being sedative. Also, in view of their selective serotonine (5-HT) reuptake inhibitor as well as .alpha.2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.