公开(公告)号：AU2008240727A1

公开(公告)日：2008-10-30

申请号：AU2008240727

申请日：2008-04-18

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: The present invention relates to (1-benzyl-piperidin-4-yl)-(pyridin-2-yl)-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：CA2665924A1

公开(公告)日：2008-06-12

申请号：CA2665924

申请日：2007-12-05

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

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

Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbo nitriles of formula (I) that are fast dissociating dopamine 2 receptor antag onists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find util ity as medicines for treating or preventing central nervous system disorders , for example schizophrenia, by exerting an antipsychotic effect without mot or side effects.

公开(公告)号：AU783292B2

公开(公告)日：2005-10-13

申请号：AU8386401

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：PL358886A1

公开(公告)日：2004-08-23

申请号：PL35888601

申请日：2001-06-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN EMELEN KRISTOF ,  DE BRUYN MARCEL FRANS LEOPOLD ,  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：NO20026219D0

公开(公告)日：2002-12-23

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 ,  C07D

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：CA2448735A1

公开(公告)日：2002-12-19

申请号：CA2448735

申请日：2002-06-11

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K9/10 ,  A61K31/00 ,  A61K31/519 ,  A61K31/55 ,  A61P3/00 ,  A61P7/10 ,  A61P9/10 ,  A61P25/00 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D519/00 ,  C07D239/00 ,  C07D277/00

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 particula r caused by traumatic (TBI) and non-traumatic brain injury, processes for thei r 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-(phenylmethyl)- 1-piperidinyl]ethy l] -2,10-dimethyl pyrimido[1, 2-a]benzimidazol- 4(10H)-one, the pharmaceuticall y acceptable acid or base addition salts thereof, the stereochemically isomeri c forms thereof and the N-oxide form thereof.

公开(公告)号：CA3103910A1

公开(公告)日：2019-12-26

申请号：CA3103910

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  MARTINEZ-VITURRO CARLOS MANUEL

IPC: C07D401/14 ,  A61K31/4375 ,  A61K31/4709 ,  A61P25/28 ,  C07D471/04

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：CA3103047A1

公开(公告)日：2019-12-26

申请号：CA3103047

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  DE LUCAS OLIVARES ANA ISABEL ,  TRESADERN GARY JOHN ,  CONDE-CEIDE SUSANA

IPC: A61K31/437 ,  A61K31/4184 ,  A61P25/28 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

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：CA3102903A1

公开(公告)日：2019-12-26

申请号：CA3102903

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D401/14 ,  A61K31/4427 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61P25/28 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of 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. RB is a radical selected from the group consisting of (b-1) to (b-4).

公开(公告)号：CA3102458A1

公开(公告)日：2019-12-26

申请号：CA3102458

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.