公开(公告)号：NO20042618L

公开(公告)日：2004-06-22

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 JAVI ,  JANSSENS FRANS EDUARD ,  LEENAERTS JOSEPH ELISABETH ,  TEGTMEIER FRANK ,  ROSSEM KOENRAAD ARTHUR VAN ,  REEMPTS JOZEF LEO HENRI VAN

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：EE200200694A

公开(公告)日：2004-06-15

申请号：EEP200200694

申请日：2001-06-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EMELEN KRISTOF VAN ,  BRUYN MARCEL FRANS LEOPOLD DE ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MATESANZ-BALLESTEROS MARIA ENC ,  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

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：BR0111859A

公开(公告)日：2003-05-13

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 JAVI ,  MATESANZ-BALLESTEROS MARIA ENC ,  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

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：NO20026219A

公开(公告)日：2003-02-17

申请号：NO20026219

申请日：2002-12-23

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EMELEN KRISTOF VAN ,  BRUYN MARCEL FRANS LEOPOLD DE ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  MATESANZ-BALLESTEROS MARIA ENC ,  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

公开(公告)号：CA3103758A1

公开(公告)日：2019-12-26

申请号：CA3103758

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  DE LUCAS OLIVARES ANA ISABEL ,  DELGADO-JIMENEZ FRANCISCA ,  CONDE-CEIDE SUSANA ,  VEGA RAMIRO JUAN ANTONIO

IPC: C07D491/056 ,  A61K31/445 ,  A61P25/28 ,  C07D417/14 ,  C07D513/04

Abstract: The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).

公开(公告)号：CA3102462A1

公开(公告)日：2019-12-26

申请号：CA3102462

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  MARTINEZ-VITURRO CARLOS MANUEL ,  DELGADO-JIMENEZ FRANCISCA ,  CONDE-CEIDE SUSANA ,  VEGA RAMIRO JUAN

IPC: C07D401/14 ,  A61K31/436 ,  A61K31/536 ,  A61K31/5365 ,  A61K31/538 ,  A61K31/5383 ,  A61P25/28 ,  C07D405/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D498/04

Abstract: The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.

公开(公告)号：CA2674752C

公开(公告)日：2015-03-31

申请号：CA2674752

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 ,  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：JO2849B1

公开(公告)日：2015-03-15

申请号：JOP20080032

申请日：2008-02-02

Applicant: JANSSEN PHARMACEUTICA NV

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

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, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：JO2849B

公开(公告)日：2015-03-15

申请号：JO200832

申请日：2008-02-02

Applicant: JANSSEN PHARMACEUTICA NV

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

CPC classification number: C07D487/04 ,  C07D237/20 ,  C07D237/24 ,  C07D401/14 ,  C07D403/04 ,  C07D409/04 ,  C07D409/14

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, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：AU2011226174B2

公开(公告)日：2015-01-22

申请号：AU2011226174

申请日：2011-03-08

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  CONDE-CEIDE SUSANA ,  MACDONALD GREGOR JAMES ,  PASTOR-FERNANDEZ JOAQUIN ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  VANHOOF GRETA CONSTANTIA PETER

IPC: C07D487/04 ,  A61K31/4985 ,  A61P3/00 ,  A61P25/00

Abstract: The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.