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1.
公开(公告)号:CA2799640A1
公开(公告)日:2011-12-15
申请号:CA2799640
申请日:2011-06-08
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: TRABANCO-SUAREZ ANDRES AVELINO , ROMBOUTS FREDERIK JAN RITA , TRESADERN GARY JOHN , VAN GOOL MICHIEL LUC MARIA , MACDONALD GREGOR JAMES , MARTINEZ LAMENCA CAROLINA , GIJSEN HENRICUS JACOBUS MARIA
IPC: C07D265/30 , A61K31/535 , A61K31/5355 , A61P25/16 , A61P25/28 , C07D413/04
Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. 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 beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta- amyloid.
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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.
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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.
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4.
公开(公告)号:EA021240B1
公开(公告)日:2015-05-29
申请号:EA201291435
申请日:2011-06-08
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: TRABANCO-SUAREZ ANDRES AVELINO , ROMBOUTS FREDERIK JAN RITA , TRESADERN GARY JOHN , VAN GOOL MICHIEL LUC MARIA , MACDONALD GREGOR JAMES , MARTINEZ LAMENCA CAROLINA , GIJSEN HENRICUS JACOBUS MARIA
IPC: C07D265/30 , A61K31/535 , A61K31/5355 , A61P25/16 , A61P25/28 , C07D413/04
Abstract: Настоящееизобретениеотноситсяк новымпроизводным 5,6-дигидро-2Н-[1,4]оксазин-3-иламинав качествеингибиторовбета-секретазы, такжеизвестнойкакфермент, расцепляющийамилоидв бета-участке, ВАСЕ, ВАСЕ1, Asp2 илимемапсин 2. Изобретениетакжеотноситсяк фармацевтическимкомпозициям, содержащимтакиесоединения, кспособамполучениятакихсоединенийи композицийи кприменениютакихсоединенийи композицийдляпредотвращенияи лечениянарушений, вкоторыевовлеченабета-секретаза, такихкакболезньАльцгеймера (AD), умеренноекогнитивноенарушение, старость, деменция, деменцияс тельцамиЛеви, синдромДауна, деменция, ассоциированнаяс инсультом, деменция, ассоциированнаяс болезньюПаркинсона, идеменция, ассоциированнаяс бета-амилоидом.
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公开(公告)号:CL2012003428A1
公开(公告)日:2013-04-01
申请号:CL2012003428
申请日:2012-12-05
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: GIJSEN HENRICUS JACOBUS MARIA , MACDONALD GREGOR JAMES , VAN GOLL MICHIEL LUC MARIA , TRABANCO SUAREZ ANDRES AVELINO , TRESADERN GARY JOHN , ROMBOUTS FREDERIK JAN RITA , MARTINEZ LAMENCA CAROLINA
IPC: C07D265/30 , A61K31/535 , A61K31/5355 , A61P25/16 , A61P25/28 , C07D413/04
Abstract: Compuestos derivados de 5,6-dihidro-2h-[1,4]oxazin-3il-amina; composición farmacéutica; proceso para prepararla y uso en el tratamiento de un trastorno seleccionado de Alzheimer, senilidad, demencia, entre otros.
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公开(公告)号:MA52942A
公开(公告)日:2021-04-28
申请号:MA52942
申请日:2019-06-20
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: BARTOLOMÉ-NEBREDA JOSÉ MANUEL , BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS , LEENAERTS JOSEPH ELISABETH , MARTINEZ LAMENCA CAROLINA , OEHLRICH DANIEL , TRABANCO-SUÁREZ ANDRÉS AVELINO , TRESADERN GARY JOHN , VAN ROOSBROECK YVES EMIEL MARIA , VELTER ADRIANA INGRID
IPC: A61K31/437 , A61K31/44 , A61K31/501 , A61K31/5377 , A61P25/16 , A61P25/28 , C07D401/04 , C07D519/00
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公开(公告)号:MX2012014368A
公开(公告)日:2013-01-22
申请号:MX2012014368
申请日:2011-06-08
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: ROMBOUTS FREDERIK JAN RITA , GIJSEN HENRICUS JACOBUS MARIA , TRABANCO-SUAREZ ANDRES AVELINO , MACDONALD GREGOR JAMES , GOOL MICHIEL LUC MARIA VAN , TRESADERN GARY JOHN , MARTINEZ LAMENCA CAROLINA
IPC: C07D265/30 , A61K31/535 , A61K31/5355 , A61P25/16 , A61P25/28 , C07D413/04
Abstract: La presente invención se refiere a derivados novedosos de 5, 6-dihidro-2H-[1, 4]oxazin-3-ilamina como inhibidores de la beta-secretasa, conocida también como enzima de escisión amiloide del sitio beta, BACE, BACE1, Asp2 o memapsina2; la invención se refiere también a composiciones farmacéuticas que comprenden dichos compuestos, a procedimientos para la preparación de dichos compuestos y composiciones, y al uso de dichos compuestos y composiciones para la prevención y el tratamiento de trastornos en los cuales se encuentra involucrada la beta-secretasa, tales como en enfermedad de Alzheimer (EA), deterioro cognitivo leve, senilidad, demencia, demencia con cuerpos de Lewy, síndrome de Down, demencia asociada con el accidente cerebrovascular, demencia asociada con la enfermedad de Parkinson o demencia asociada con beta-amiloide.
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公开(公告)号:ES2927355T3
公开(公告)日:2022-11-04
申请号:ES19732991
申请日:2019-06-20
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: BARTOLOME-NEBREDA JOSÉ MANUEL , TRABANCO-SUAREZ ANDRÉS , LEENAERTS JOSEPH , OEHLRICH DANIEL , BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS , MARTINEZ LAMENCA CAROLINA , VELTER ADRIANA , VAN ROOSBROECK YVES
IPC: C07D471/04 , A61K31/437 , A61K31/444 , A61K31/501 , A61P25/28
Abstract: La presente invención se refiere a inhibidores de O-GIcNAc hidrolasa (OGA). La invención también está dirigida a composiciones farmacéuticas que comprenden tales compuestos, a procesos para preparar tales compuestos y composiciones, y al uso de tales compuestos y composiciones para la prevención y tratamiento de trastornos en los que la inhibición de OGA es beneficiosa, como tauopatías, en particular enfermedad de Alzheimer o parálisis supranuclear progresiva; y enfermedades neurodegenerativas acompañadas de una patología tau, en particular esclerosis lateral amiotrófica o demencia del lóbulo frontotemporal causada por mutaciones C90RF72. (Traducción automática con Google Translate, sin valor legal)
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公开(公告)号:AU2020409728A1
公开(公告)日:2022-08-11
申请号:AU2020409728
申请日:2020-12-18
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: BARTOLOMÉ-NEBREDA JOSÉ MANUEL , BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS , DE LUCAS OLIVARES ANA ISABEL , LEENAERTS JOSEPH ELISABETH , MARTINEZ LAMENCA CAROLINA , OEHLRICH DANIEL , TRABANCO-SUÁREZ ANDRÉS AVELINO , VAN ROOSBROECK YVES EMIEL M , VELTER ADRIANA INGRID
IPC: C07D471/04 , A61K31/437 , A61P25/28
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 C9ORF72 mutations.
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公开(公告)号:MA52939A
公开(公告)日:2021-04-28
申请号:MA52939
申请日:2019-06-20
Applicant: JANSSEN PHARMACEUTICA NV
Inventor: BARTOLOMÉ-NEBREDA JOSÉ MANUEL , BUIJNSTERS PETRUS JACOBUS JOHANNES ANTONIUS , LEENAERTS JOSEPH ELISABETH , MARTINEZ LAMENCA CAROLINA , OEHLRICH DANIEL , TRABANCO-SUÁREZ ANDRÉS AVELINO , VAN ROOSBROECK YVES EMIEL MARIA , VELTER ADRIANA INGRID
IPC: A61K31/437 , A61K31/444 , A61K31/501 , A61P25/28 , C07D471/04
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