公开(公告)号：WO2011051342A8

公开(公告)日：2011-07-07

申请号：PCT/EP2010066264

申请日：2010-10-27

Applicant: JANSSEN PHARMACEUTICA NV ,  PASTOR-FERNANDEZ JOAQUIN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  MACDONALD GREGOR JAMES ,  CONDE-CEIDE SUSANA ,  DELGADO-GONZALEZ OSCAR ,  VANHOOF GRETA CONSTANTIA PETER ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  ALONSO-DE DIEGO SERGIO-ALVAR ,  SWINNEY KELLY ANN ,  LEYS CARINA ,  WEERTS JOHAN ERWIN EDMOND

Inventor： PASTOR-FERNANDEZ JOAQUIN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  MACDONALD GREGOR JAMES ,  CONDE-CEIDE SUSANA ,  DELGADO-GONZALEZ OSCAR ,  VANHOOF GRETA CONSTANTIA PETER ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  ALONSO-DE DIEGO SERGIO-ALVAR ,  SWINNEY KELLY ANN ,  LEYS CARINA ,  WEERTS JOHAN ERWIN EDMOND

IPC: C07D487/04 ,  A61K31/5025 ,  A61P3/00 ,  A61P25/00

CPC classification number: C07D487/04

Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine 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.

Abstract translation: 本发明涉及作为磷酸二酯酶10酶（PDE10）抑制剂的新型咪唑并[1,2-b]哒嗪衍生物，其可用于治疗或预防其中涉及PDE10酶的神经病学，精神病学和代谢病症 。 本发明还涉及包含此类化合物的药物组合物，涉及制备此类化合物和组合物的方法，涉及此类化合物或药物组合物用于预防或治疗神经病学，精神病学和代谢病症和疾病的用途。

公开(公告)号：WO02100862A3

公开(公告)日：2003-02-27

申请号：PCT/EP0206576

申请日：2002-06-11

Applicant: JANSSEN PHARMACEUTICA NV ,  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 JOS

Inventor： 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 JOS

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

CPC classification number: C07D487/04 ,  C07D471/04

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- 6 H - benzimidazo[2,1 -b][3]benzazepin-6-yl) -2-(phenylmethyl)- 1-piperidinyl]ethyl] -2,10-dimethyl pyrimido[1, 2- a ]benzimidazol- 4(10 H )-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof.

Abstract translation: 本发明涉及可用于治疗升高的颅内压（ICP）和/或继发性缺血的新型取代的四环咪唑衍生物，特别是由脑损伤引起的，特别是由创伤性（TBI）和非创伤性脑损伤引起的 其制备方法，包含它们的药物组合物及其作为药物的用途。 新化合物包括根据通式（I）的化合物，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。 特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基）-2-（苯基甲基） - 哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和N-氧化物形式 它们。

公开(公告)号：CA3045745A1

公开(公告)日：2018-08-30

申请号：CA3045745

申请日：2018-02-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  ALCAZAR-VACA MANUEL JESUS

IPC: C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  C07D519/00

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：CA3045816A1

公开(公告)日：2018-08-09

申请号：CA3045816

申请日：2018-02-06

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/10

Abstract: The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors of Formulas (I) and (II). 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：HUE033768T2

公开(公告)日：2017-12-28

申请号：HUE09802514

申请日：2009-07-29

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61P25/00

公开(公告)号：CA2730774C

公开(公告)日：2016-09-13

申请号：CA2730774

申请日：2009-07-29

Applicant: JANSSEN PHARMACEUTICA NV

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

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 com-pounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disor-ders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

公开(公告)号：ZA201206715B

公开(公告)日：2015-04-29

申请号：ZA201206715

申请日：2012-09-07

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

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.

公开(公告)号：ZA201204433B

公开(公告)日：2014-11-26

申请号：ZA201204433

申请日：2012-06-15

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. 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 mGluR5 is involved.

公开(公告)号：CA2665924C

公开(公告)日：2014-08-12

申请号：CA2665924

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  ANDRES-GIL JOSE IGNACIO ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  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-carbonitriles of formula (I) 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：BRPI0807492A2

公开(公告)日：2014-05-27

申请号：BRPI0807492

申请日：2008-02-11

Applicant: JANSSEN PHARMACEUTICA NV

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

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