公开(公告)号：AU2012277912B2

公开(公告)日：2017-03-23

申请号：AU2012277912

申请日：2012-06-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ROMBOUTS FREDERIK JAN RITA ,  TRABANCO-SUAREZ ANDRES AVELINO ,  VANHOOF GRETA CONSTANTIA PETER ,  DE ANGELIS MERI ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  GUILLEMONT JEROME EMILE GEORGES ,  BORMANS GUY MAURITS R ,  CELEN SOFIE JEANNE LEOPOLDINE ,  VLIEGEN MAARTEN

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

Abstract: The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. 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 PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.

公开(公告)号：AU2015295298A1

公开(公告)日：2017-01-12

申请号：AU2015295298

申请日：2015-07-30

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ALONSO-DE DIEGO SERGIO-ALVAR ,  VAN GOOL MICHIEL LUC MARIA ,  DELGADO-GONZALEZ OSCAR ,  ANDRES-GIL JOSE IGNACIO ,  TRABANCO-SUAREZ ANDRES AVELINO

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

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

公开(公告)号：CA2967542A1

公开(公告)日：2016-06-09

申请号：CA2967542

申请日：2015-12-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN GOOL MICHIEL LUC MARIA ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  BORMANS GUY MAURITS R ,  CELEN SOFIE JEANNE LEOPOLDINE ,  VERBEEK JOOST

IPC: A61K51/04 ,  A61P25/18 ,  A61P25/24

Abstract: The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

公开(公告)号：CA2910507A1

公开(公告)日：2014-12-11

申请号：CA2910507

申请日：2014-06-03

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN GOOL MICHIEL LUC MARIA ,  ALONSO-DE DIEGO SERGIO-ALVAR ,  CID-NUNEZ JOSE MARIA ,  DELGADO-GONZALEZ OSCAR ,  DECORTE ANNELIES MARIE ANTONIUS ,  MACDONALD GREGOR JAMES ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  TRABANCO-SUAREZ ANDRES AVELINO ,  GARCIA-MOLINA ARANZAZU ,  ANDRES-GIL JOSE IGNACIO

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

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). 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 or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders.

公开(公告)号：AU2010311493B2

公开(公告)日：2014-06-05

申请号：AU2010311493

申请日：2010-10-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  DE ANGELIS MERI ,  BORMANS GUY MAURITS R ,  CELEN SOFIE JEANNE LEOPOLDINE

IPC: C07D401/14 ,  A61K51/04

Abstract: The present invention relates to novel, selective, radio labelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.

公开(公告)号：AU2007328897B2

公开(公告)日：2013-01-10

申请号：AU2007328897

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  ANDRES-GIL JOSE IGNACIO ,  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：CA2838645A1

公开(公告)日：2013-01-03

申请号：CA2838645

申请日：2012-06-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ROMBOUTS FREDERIK JAN RITA ,  TRABANCO-SUAREZ ANDRES AVELINO ,  VANHOOF GRETA CONSTANTIA PETER ,  DE ANGELIS MERI ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  GUILLEMONT JEROME EMILE GEORGES ,  BORMANS GUY MAURITS R ,  CELEN SOFIE JEANNE LEOPOLDINE ,  VLIEGEN MAARTEN

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

Abstract: The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. 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 PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.

公开(公告)号：BRPI0711574A2

公开(公告)日：2011-11-16

申请号：BRPI0711574

申请日：2007-04-19

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  LINARES DE LA MORENA MARIA LOURDES ,  MARTINEZ GONZALEZ SONIA ,  SANTAMARINA JULEN OYARZABAL ,  PASTOR-FERNANDEZ JOAQUIM ,  VEGA-RAMIRO JUAN ANTONIO ,  DELGADO-JIMENEZ FRANCISCA ,  DRINKENBURG WILHELMUS HELENA IGNATIUS MARIA

IPC: C07D413/14 ,  C07D239/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (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 are defined in Claim 1, having selective alpha2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

公开(公告)号：CA2494557C

公开(公告)日：2011-10-18

申请号：CA2494557

申请日：2003-08-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  BARTOLOME-NEBREDA JOSE MANUEL ,  FERNANDEZ-GADEA FRANCISCO JAVIER ,  BAKKER MARGARETHA HENRICA MARIA ,  MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS

IPC: C07D498/12 ,  A61K31/42 ,  A61K31/424 ,  A61K31/437 ,  A61P1/14 ,  A61P3/04 ,  A61P15/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/36 ,  A61P43/00 ,  C07D498/14

Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of 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, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety 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, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity 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.

公开(公告)号：HRP20020988B1

公开(公告)日：2011-06-30

申请号：HRP20020988

申请日：2002-12-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： EMELEN KRISTOF 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.