公开(公告)号：AU2009275887A1

公开(公告)日：2010-02-04

申请号：AU2009275887

申请日：2009-07-29

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D213/74 ,  A61K31/496 ,  A61P25/00 ,  C07D213/84

Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines 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：MX2009011416A

公开(公告)日：2009-11-05

申请号：MX2009011416

申请日：2008-04-18

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D417/12 ,  A61K31/454 ,  A61P25/18

Abstract: La presente invención se refiere a [1-(bencil)-piperidin-4-iI]-([1 ,3,4]tiadiazol-2-iI)-amina y derivados de [1-(bencil)-piperidin-4- il]-(tiazol-2-il)-amina de fórmula (I) que son antagonistas del receptor de dopamina 2 de disociación rápida, los procesos para preparar estos compuestos, las composiciones farmacéuticas que comprenden estos compuestos como un ingrediente activo; los compuestos se usan como medicamentos para tratar o prevenir trastornos del sistema nervioso central, por ejemplo esquizofrenia, al ejercer un efecto antipsicótico sin efectos secundarios motores.

公开(公告)号：MX2009011414A

公开(公告)日：2009-11-05

申请号：MX2009011414

申请日：2008-04-18

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/44 ,  C07D401/12 ,  A61P25/18

Abstract: La presente invención se refiere a (1-bencil-piperidin-4-il)-pirid in-2-il)-aminas que son antagonistas del receptor de dopamina 2 de rápida disociación, procedimientos para preparar estos compuestos, composiciones farmacéuticas que comprenden estos compuestos como un ingrediente activo; los compuestos encuentran utilidad como medicamentos para tratar o prevenir trastornos del sistema nervioso central, por ejemplo esquizofrenia al ejercer un efecto antipsicótico sin efectos secundarios motores.

公开(公告)号：MX2009008616A

公开(公告)日：2009-08-20

申请号：MX2009008616

申请日：2008-02-11

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: La presente invención se refiere a 4-aril-6-piperazin-1-il-3-pirid azinas sustituidas que son antagonistas del receptor de dopamina 2 de rápida disociación, a procedimientos para preparar dichos compuestos, y a composiciones farmacéuticas que comprenden dichos compuestos como principio activo; los compuestos son útiles como medicamentos para el tratamiento o la prevención de trastornos del sistema nervioso central, por ejemplo, la esquizofrenia, ejerciendo un efecto antipsicótico sin producir efectos secundarios motores.

公开(公告)号：PT1832287E

公开(公告)日：2009-05-05

申请号：PT07107669

申请日：2002-11-22

Applicant: JANSSEN PHARMACEUTICA NV

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

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

公开(公告)号：DE60315311T2

公开(公告)日：2008-04-17

申请号：DE60315311

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 ,  MEGENS ANTONIUS ADRIANUS HENDR

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 alpha2-adrenocptor antagonist activity and show a strong antidepressant 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 alpha2-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.

公开(公告)号：SI1451196T1

公开(公告)日：2007-12-31

申请号：SI200230617

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 JANS ,  MARTINEZ-JIMENEZ PEDRO JANSSEN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOMEZ-SANCHEZ ANTONIO JANSSEN- ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  VAN REEMPTS JOZEF LEO HENRI

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

公开(公告)号：JO2352B

公开(公告)日：2006-12-12

申请号：JO200184

申请日：2001-05-29

Applicant: JANSSEN PHARMACEUTICA NV

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

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

CPC classification number: C07D411/04 ,  C07D491/04

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 =a -a =a - is a bivalent radical wherein one or two of a to a are nitrogen and the remaining a to a are -CH-; -Z -Z - is a bivalent radical; -A- is a bivalent radical of formula -N(R )-Alk - or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R , R and R are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk and Alk are optionally substituted C1-6alkanediyl; R is a radical of formula wherein n is 1 or 2; p is 0, and p is 1 or 2; or p is 1 or 2, and p is 0; X is oxygen, sulfur or -NR ; Y is oxygen or sulfur; R is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R is hydrogen or C1-6alkyl; 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：PL369864A1

公开(公告)日：2005-05-02

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 ,  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：CA2525282A1

公开(公告)日：2004-12-09

申请号：CA2525282

申请日：2004-05-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  ANDRES-GIL JOSE IGNACIO

IPC: C07D498/04 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/5383 ,  A61P25/18 ,  C07D221/00 ,  C07D265/00 ,  C07D319/00 ,  C07D491/04

Abstract: The present invention relates to a novel indol derivative according to Formu la (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables R1, R2, R3, R4, R5, p, a1=a2a3=a4, Z1-Z2, X and Y are defined as in claim 1. Said derivative exhibi t a binding affinity towards dopamine receptors, in particular towards dopamin e D2, D3 and D4 receptors, with selective serotonin reuptake inhibition properties and acting as 5-HT1A agonists or partial agonists. The invention also relates to pharmaceutical compositions comprising the compounds accordi ng to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for thei r production.