公开(公告)号：US09974775B2

公开(公告)日：2018-05-22

申请号：US15202600

申请日：2016-07-06

Applicant: Janssen Pharmaceutica NV

Inventor： Ishtiyaque Ahmad ,  Rajagopal Bakthavatchalam ,  Sivaramakrishna Battula ,  Henricus Jacobus Maria Gijsen ,  Saravanan Vadivelu ,  Mark Wall ,  Christopher Flores

IPC: A61K31/4178 ,  C07D405/14 ,  C07D405/04 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506

CPC classification number: A61K31/4178 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  C07D405/04 ,  C07D405/14

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.

公开(公告)号：US09834559B2

公开(公告)日：2017-12-05

申请号：US14897420

申请日：2014-06-12

Applicant: Janssen Pharmaceutica NV

Inventor： Daniel Oehlrich ,  Henricus Jacobus Maria Gijsen

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to novel 5,6-dihydroimidazo[1,5-a]pyrazin-3(2H)-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, in particular BACE1 and/or BACE2 (wherein BACE1, is also known as Asp2, or memapsin2 and BACE2 is also known as Asp1, Memapsin 1 or DRAP). 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, dementia of the Alzheimer's type, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.

公开(公告)号：US11319321B2

公开(公告)日：2022-05-03

申请号：US16346745

申请日：2017-10-31

Applicant: Janssen Pharmaceutica NV

Inventor： Yves Emiel Maria Van Roosbroeck ,  Frans Alfons Maria Van den Keybus ,  Adriana Ingrid Velter ,  Petrus Jacobus Johannes Antonius Buijnsters ,  Gary John Tresadern ,  Henricus Jacobus Maria Gijsen

IPC: C07D487/04

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：US10653673B2

公开(公告)日：2020-05-19

申请号：US15892846

申请日：2018-02-09

Applicant: Janssen Pharmaceutica NV

Inventor： Ishtiyaque Ahmad ,  Rajagopal Bakthavatchalam ,  Sivaramakrishna Battula ,  Henricus Jacobus Maria Gijsen ,  Saravanan Vadivelu ,  Mark Wall ,  Christopher Flores

IPC: A61K31/4178 ,  C07D405/14 ,  C07D405/04 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.

公开(公告)号：US20200048260A1

公开(公告)日：2020-02-13

申请号：US16346766

申请日：2017-10-31

Applicant: Janssen Pharmaceutica NV

Inventor： Yves Emiel Maria Van Roosbroeck ,  Petrus Jacobus Johannes Antonius Buijnsters ,  Gary John Tresadern ,  Edgar Jacoby ,  Daniel Oehlrich ,  Henricus Jacobus Maria Gijsen

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

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：US20190389882A1

公开(公告)日：2019-12-26

申请号：US16489910

申请日：2018-03-06

Applicant: Janssen Pharmaceutica NV

Inventor： Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Ann Marleen Vos ,  Daniel Oehlrich

IPC: C07D513/04 ,  C07D519/00

Abstract: The present invention relates to tricyclic inhibitors of beta-secretase having the structure shown in Formula (I) and (II) wherein the radicals are as defined in the specification. 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, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes and other metabolic disorders.

公开(公告)号：US20190276462A1

公开(公告)日：2019-09-12

申请号：US16346730

申请日：2017-10-31

Applicant: Janssen Pharmaceutica NV

Inventor： Yves Emiel Maria Van Roosbroeck ,  Frans Alfons Maria Van den Keybus ,  Gary John Tresadern ,  Petrus Jacobus Johannes Buijnsters ,  Adriana Ingrid Velter ,  Edgar JACOBY ,  Gregor James Macdonald ,  Henricus Jacobus Maria Gijsen ,  Abdellah Ahnaou ,  Wihelmus Helena lgnatius Drinkenburg

IPC: C07D487/04 ,  C07D513/08 ,  C07D519/00 ,  A61P25/28

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：US10106524B2

公开(公告)日：2018-10-23

申请号：US15536474

申请日：2015-12-16

Applicant: Janssen Pharmaceutica NV

Inventor： Andrés Avelino Trabanco-Suárez ,  Óscar Delgado-González ,  Henricus Jacobus Maria Gijsen ,  Michiel Luc Maria Van Gool ,  Sven Franciscus Anna Van Brandt ,  Michel Anna Jozef De Cleyn ,  Santos Fustero Lardiés ,  Natalia Mateu Sanchís

IPC: A61K31/4965 ,  C07D401/12 ,  C07D401/10 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506

Abstract: The present invention relates to 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase having the structure shown in Formula (I) wherein the radicals are as defined in the specification. 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, dementia associated with beta-amyloid, age-related macular degeneration, type 2 diabetes or metabolic disorders.

公开(公告)号：US11053248B2

公开(公告)日：2021-07-06

申请号：US16346766

申请日：2017-10-31

Applicant: Janssen Pharmaceutica NV

Inventor： Yves Emiel Maria Van Roosbroeck ,  Petrus Jacobus Johannes Antonius Buijnsters ,  Gary John Tresadern ,  Edgar Jacoby ,  Daniel Oehlrich ,  Henricus Jacobus Maria Gijsen

IPC: C07D487/04 ,  A61P25/28 ,  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：US10562897B2

公开(公告)日：2020-02-18

申请号：US16038761

申请日：2018-07-18

Applicant: Janssen Pharmaceutica NV

Inventor： François Paul Bischoff ,  Adriana Ingrid Velter ,  Frederik Jan Rita Rombouts ,  Michel Anna Jozef De Cleyn ,  Sven Franciscus Anna Van Brandt ,  Henricus Jacobus Maria Gijsen ,  Chiara Zavattaro ,  Frans Alfons Maria Van den Keybus

IPC: A61K31/4985 ,  C07D487/04 ,  C07D471/04

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.