公开(公告)号：AU2019291099A1

公开(公告)日：2021-01-07

申请号：AU2019291099

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOMÉ-NEBREDA JOSÉ MANUEL ,  TRABANCO-SUÁREZ ANDRÉS AVELINO ,  LEENAERTS JOSEPH ELISABETH ,  OEHLRICH DANIEL ,  BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS ,  MARTINEZ LAMENCA CAROLINA ,  VELTER ADRIANA INGRID ,  VAN ROOSBROECK YVES EMIEL MARIA

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/501 ,  A61P25/28

Abstract: The present invention relates to O-GIcNAc 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：CA3103048A1

公开(公告)日：2019-12-26

申请号：CA3103048

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  LEENAERTS JOSEPH ELISABETH ,  OEHLRICH DANIEL ,  BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS ,  MARTINEZ LAMENCA CAROLINA ,  VELTER ADRIANA INGRID ,  VAN ROOSBROECK YVES EMIEL MARIA

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/501 ,  A61P25/28

Abstract: The present invention relates to O-GIcNAc 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：CA3041412A1

公开(公告)日：2018-05-11

申请号：CA3041412

申请日：2017-10-31

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN ROOSBROECK YVES EMIEL MARIA ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  TRESADERN GARY JOHN ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  VELTER ADRIANA INGRID ,  JACOBY EDGAR ,  MACDONALD GREGOR JAMES ,  GIJSEN HENRICUS JACOBUS MARIA ,  AHNAOU ABDELLAH ,  DRINKENBURG WILHELMUS HELENA IGNATIUS MARIA

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

Abstract: The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the 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, such as neurological and psychiatric disorders.

公开(公告)号：CA2891755A1

公开(公告)日：2014-07-24

申请号：CA2891755

申请日：2014-01-16

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BISCHOFF FRANCOIS PAUL ,  VELTER ADRIANA INGRID ,  ROMBOUTS FREDERIK JAN RITA ,  DE CLEYN MICHEL ANNA JOZEF ,  VAN BRANDT SVEN FRANCISCUS ANNA ,  GIJSEN HENRICUS JACOBUS MARIA ,  ZAVATTARO CHIARA ,  VAN DEN KEYBUS FRANS ALFONS MARIA

IPC: C07D471/04 ,  A61K31/498 ,  A61P25/28

Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：EA039788B1

公开(公告)日：2022-03-14

申请号：EA201991109

申请日：2017-10-31

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN ROOSBROECK YVES EMIEL MARIA ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  TRESADERN GARY JOHN ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  VELTER ADRIANA INGRID ,  JACOBY EDGAR ,  MACDONALD GREGOR JAMES ,  GIJSEN HENRICUS JACOBUS MARIA ,  AHNAOU ABDELLAH ,  DRINKENBURG WILHELMUS HELENA IGNATIUS MARIA

Abstract: Настоящееизобретениеотноситсяк новымпроизводным [1,2,4]триазоло[1,5-a]пиримидинила, характеризующимсяформулой (I), вкачествеингибиторовфосфодиэстеразы 2 (PDE2). Настоящееизобретениетакженаправленонафармацевтическиекомпозиции, содержащиесоединения, наспособыполучениятакихсоединенийи композицийи наприменениетакихсоединенийи композицийдляпредупрежденияи лечениярасстройств, вкоторыевовлечена PDE2, такихкакневрологическиеи психическиерасстройства.

公开(公告)号：AU2019291101A1

公开(公告)日：2021-01-07

申请号：AU2019291101

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOMÉ-NEBREDA JOSÉ MANUEL ,  TRABANCO-SUÁREZ ANDRÉS AVELINO ,  TRESADERN GARY JOHN ,  MARTINEZ LAMENCA CAROLINA ,  LEENAERTS JOSEPH ELISABETH ,  OEHLRICH DANIEL ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  VELTER ADRIANA INGRID ,  VAN ROOSBROECK YVES EMIEL MARIA

IPC: C07D401/04 ,  A61K31/437 ,  A61K31/44 ,  A61K31/501 ,  A61K31/5377 ,  A61P25/16 ,  A61P25/28 ,  C07D519/00

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.

公开(公告)号：CA3103049A1

公开(公告)日：2019-12-26

申请号：CA3103049

申请日：2019-06-20

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BARTOLOME-NEBREDA JOSE MANUEL ,  TRABANCO-SUAREZ ANDRES AVELINO ,  TRESADERN GARY JOHN ,  MARTINEZ LAMENCA CAROLINA ,  LEENAERTS JOSEPH ELISABETH ,  OEHLRICH DANIEL ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  VELTER ADRIANA INGRID ,  VAN ROOSBROECK YVES EMIEL MARIA

IPC: C07D401/04 ,  A61K31/437 ,  A61K31/44 ,  A61K31/501 ,  A61K31/5377 ,  A61P25/16 ,  A61P25/28 ,  C07D519/00

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.

公开(公告)号：AU2014206834B2

公开(公告)日：2017-06-22

申请号：AU2014206834

申请日：2014-01-16

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BISCHOFF FRANCOIS PAUL ,  VELTER ADRIANA INGRID ,  ROMBOUTS FREDERIK JAN RITA ,  DE CLEYN MICHEL ANNA JOZEF ,  VAN BRANDT SVEN FRANCISCUS ANNA ,  GIJSEN HENRICUS JACOBUS MARIA ,  ZAVATTARO CHIARA ,  VAN DEN KEYBUS FRANS ALFONS MARIA

IPC: C07D471/04 ,  A61K31/498 ,  A61P25/28

Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R

公开(公告)号：HK1212346A1

公开(公告)日：2016-06-10

申请号：HK16100319

申请日：2016-01-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BISCHOFF FRANOIS PAUL ,  VELTER ADRIANA INGRID ,  ROMBOUTS FREDERIK JAN RITA ,  DE CLEYN MICHEL ANNA JOZEF ,  BRANDT SVEN FRANCISCUS ANNA VAN ,  GIJSEN HENRICUS JACOBUS MARIA ,  ZAVATTARO CHIARA ,  DEN KEYBUS FRANS ALFONS MARIA VAN

IPC: C07D20060101 ,  A61K20060101 ,  A61P20060101

Abstract: The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R1, R2, R3, R4, R5, L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：MX390505B

公开(公告)日：2025-03-20

申请号：MX2019005123

申请日：2019-04-30

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VELTER ADRIANA INGRID ,  VAN DEN KEYBUS FRANS ALFONS MARIA ,  TRESADERN GARY JOHN ,  GIJSEN HENRICUS JACOBUS MARIA ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  VAN ROOSBROECK YVES EMIEL MARIA

IPC: C07D487/04 ,  A61K31/519 ,  A61P25/00 ,  C07D451/02

Abstract: La presente invencion se relaciona con nuevos derivados de [1,2,4]triazol[1,5- a]pirimidin-ilo como inhibidores de la fosfodiesterasa 2 (PDE2); la invencion tambien esta dirigida a composiciones farmaceuticas que comprenden los compuestos, a procesos para preparar dichos compuestos y composiciones, y al uso de dichos compuestos y composiciones en la prevencion y el tratamiento de trastornos en los cuales esta involucrada la PDE2, tales como trastornos neurológicos y psiquiatricos.