公开(公告)号：AU2014276963C1

公开(公告)日：2018-11-08

申请号：AU2014276963

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：SI3004107T1

公开(公告)日：2017-09-29

申请号：SI201430322

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: C07D487/00 ,  A61K31/00 ,  A61P25/00

公开(公告)号：PH12017500170A1

公开(公告)日：2017-07-10

申请号：PH12017500170

申请日：2017-01-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ALONSO-DE DIEGO SERGIO-ALVAR ,  VAN GOOL MICHIEL LUC MARIA ,  MARTIN-MARTIN MARIA LUZ ,  CONDE-CEIDE SUSANA ,  ANDRES-GIL JOSE IGNACIO ,  DELGADO-GONZALEZ OSCAR ,  TRESADERN GARY JOHN ,  TRABANCO-SUAREZ ANDRES

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

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：CA2954218A1

公开(公告)日：2016-02-04

申请号：CA2954218

申请日：2015-07-30

Applicant: JANSSEN PHARMACEUTICA NV

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

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：AU2013283426A1

公开(公告)日：2014-11-20

申请号：AU2013283426

申请日：2013-06-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  LANGLOIS XAVIER JEAN MICHEL ,  VANHOOF GRETA CONSTANTIA PETER ,  ANDRES-GIL JOSE IGNACIO ,  DE ANGELIS MERI ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  TRABANCO-SUAREZ ANDRES AVELINO ,  ROMBOUTS FREDERIK JAN RITA

IPC: A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  A61P21/00

Abstract: The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE 10). In particular, the invention relates to combinations of 1-aryl-4- methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051342 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1- aryl-4-methyl- [1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

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：CA2872216A1

公开(公告)日：2014-01-03

申请号：CA2872216

申请日：2013-06-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEGENS ANTONIUS ADRIANUS HENDRIKUS PETRUS ,  LANGLOIS XAVIER JEAN MICHEL ,  VANHOOF GRETA CONSTANTIA PETER ,  ANDRES-GIL JOSE IGNACIO ,  DE ANGELIS MERI ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  TRABANCO-SUAREZ ANDRES AVELINO ,  ROMBOUTS FREDERIK JAN RITA

IPC: A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  A61P21/00

Abstract: The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE 10). In particular, the invention relates to combinations of 1-aryl-4- methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051342 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1- aryl-4-methyl- [1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

公开(公告)号：UA98940C2

公开(公告)日：2012-07-10

申请号：UAA200903503

申请日：2007-12-05

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  ANDRES-GIL JOSE IGNACIO ,  VAN DEN KEYBUS FRANS ALFONS MA ,  BARTOLOME-NEBREDA JOSE MANUEL ,  VAN GOOL MICHIEL LUC MARIA

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

Abstract: Представленноеизобретениекасается 6-(пиперидин-4-иламино)пиридазин-3-карбонитриловформулы (I)(I),которыеявляютсябыстродиссоциирующимиантагонистамирецепторовдопамина 2, способовполученияэтихсоединений, фармацевтическихкомпозиций, которыесодержатэтисоединениякакактивныйкомпонент; атакжепримененияихв качествелекарственныхсредствдлялеченияилипредупреждениярасстройствцентральнойнервнойсистемы, напримершизофрении, демонстрируяантипсихотическоедействиебезмоторныхпобочныхэффектов.

公开(公告)号：CA2480113C

公开(公告)日：2012-04-24

申请号：CA2480113

申请日：2003-03-27

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  BAKKER MARGARETHA HENRICA MARIA ,  DE LUCAS OLIVARES ANA ISABEL

IPC: C07D498/04 ,  A61K31/424 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D261/00 ,  C07D261/20 ,  C07D311/00 ,  C07D498/14

Abstract: The invention concerns substituted amino isoxazoline derivatives according to Formula (I) wherein X = CH2, N-R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N-R10 R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted. piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system ; pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional .prop.2-adrenoceptor antagonist activity

公开(公告)号：HK1137434A1

公开(公告)日：2010-07-30

申请号：HK10101123

申请日：2010-02-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MACDONALD GREGOR JAMES ,  ANDRES-GIL JOSE IGNACIO ,  DEN KEYBUS FRANS ALFONS MARIA VAN ,  BARTOLOME-NEBREDA JOSE MANUEL ,  GOOL MICHIEL LUC MARIA VAN

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

Abstract: The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as 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.