公开(公告)号：US10058540B2

公开(公告)日：2018-08-28

申请号：US15524565

申请日：2015-11-09

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: A61K31/455 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/42 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  C07D211/68 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4439

CPC classification number: A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/506 ,  C07D401/12 ,  C07D413/12

Abstract: The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.

公开(公告)号：US10004738B2

公开(公告)日：2018-06-26

申请号：US15231182

申请日：2016-08-08

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mauro Marigo ,  Lena Tagmose ,  Thomas Jensen

IPC: A61K31/506 ,  A61K45/06 ,  A61K31/13 ,  A61K31/27 ,  A61K31/343 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/445 ,  A61K31/497 ,  A61K31/5415 ,  A61K31/55

CPC classification number: A61K31/506 ,  A61K31/13 ,  A61K31/27 ,  A61K31/343 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/445 ,  A61K31/497 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention is directed to the combined use of BACE1 inhibitor of Formula I and a compound useful in active or passive Tau immunotherapy, a compound useful in active or passive Aβ peptide immunotherapy, an NMDA receptor antagonists, an acetylcholine esterase inhibitor, an antiepileptic, an anti-inflammatory drug, a Tau aggregation inhibitor or an SSRI for the treatment of neurodegenerative or cognitive disorders.

公开(公告)号：US20180016330A1

公开(公告)日：2018-01-18

申请号：US15645442

申请日：2017-07-10

Applicant: H. Lundbeck A/S

Inventor： Jan Torleif Pedersen ,  Kristian Kjærgaard ,  Lars Østergaard Pedersen ,  Abdur-Rasheed Asuni ,  Nina Helen Rosenqvist ,  Justus Claus Alfred Daechsel ,  Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo ,  Thomas Jensen ,  Søren Christensen ,  Laurent David ,  Christiane Volbracht ,  Lone Helboe

IPC: C07K16/18 ,  A61K39/00

Abstract: The present invention relates to a class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396) with improved affinity, as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and other tauopathies.

公开(公告)号：US20170291903A1

公开(公告)日：2017-10-12

申请号：US15615380

申请日：2017-06-06

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård ,  Mikkel Jessing ,  Paulo Jorge Vieira Vital ,  Karsten Juhl

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US12129289B2

公开(公告)日：2024-10-29

申请号：US17399205

申请日：2021-08-11

Applicant: H. Lundbeck A/S

Inventor： Jan Torleif Pedersen ,  Kristian Kjaergaard ,  Lars Østergaard Pedersen ,  Ayodeji Abdur-Rasheed Asuni ,  Nina Helen Rosenqvist ,  Justus Claus Alfred Daechsel ,  Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo ,  Thomas Jensen ,  Søren Christensen ,  Laurent David ,  Christiane Volbracht ,  Lone Helboe

IPC: C07K16/18 ,  A61K39/395 ,  A61K49/00 ,  G01N33/68 ,  A61K39/00

CPC classification number: C07K16/18 ,  A61K39/395 ,  A61K49/00 ,  G01N33/6896 ,  A61K2039/505 ,  C07K2317/24 ,  C07K2317/30 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/51 ,  C07K2317/515 ,  C07K2317/565 ,  C07K2317/75 ,  C07K2317/76 ,  C07K2317/92 ,  C07K2317/94 ,  G01N2800/2814 ,  G01N2800/2821

Abstract: The present invention relates to a class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396) with improved affinity, as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and other tauopathies.

公开(公告)号：US11104680B2

公开(公告)日：2021-08-31

申请号：US16701269

申请日：2019-12-03

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mikkel Jessing ,  Morten Langgård ,  Paulo Jorge Vieira Vital ,  Mauro Marigo ,  Jan Kehler ,  Lars Kyhn Rasmussen

IPC: A61K31/437 ,  A61K31/519 ,  C07D487/04 ,  C07D471/04

Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US20210238182A1

公开(公告)日：2021-08-05

申请号：US17079951

申请日：2020-10-26

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård ,  Mikkel Jessing ,  Karsten Juhl ,  Paulo Jorge Vieira Vital

IPC: C07D487/04 ,  C07D519/00

Abstract: The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US20210023056A1

公开(公告)日：2021-01-28

申请号：US17060742

申请日：2020-10-01

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Karsten Juhl ,  Mauro Marigo ,  Paulo Jorge Vieira Vital ,  Mikkel Jessing ,  Morten Langgård ,  Lars Kyhn Rasmussen ,  Carl Martin Sebastian Clementson

IPC: A61K31/4162 ,  A61K31/4745 ,  C07D413/04 ,  C07D471/04

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US10647762B2

公开(公告)日：2020-05-12

申请号：US16371902

申请日：2019-04-01

Applicant: H. Lundbeck A/S

Inventor： Jan Torleif Pedersen ,  Kristian Kjaergaard ,  Lars Østergaard Pedersen ,  Abdur-Rasheed Asuni ,  Nina Helen Rosenqvist ,  Justus Claus Daechsel ,  Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo ,  Thomas Jensen ,  Søren Christensen ,  Laurent David ,  Christiane Volbracht ,  Lone Helboe

IPC: C07K16/18 ,  A61K49/00 ,  A61K39/395 ,  A61K39/00 ,  G01N33/68

Abstract: The present invention relates to a class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396) with improved affinity, as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and other tauopathies.

公开(公告)号：US10538525B2

公开(公告)日：2020-01-21

申请号：US16051612

申请日：2018-08-01

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mikkel Jessing ,  Morten Langgård ,  Paulo Jorge Vieira Vital ,  Mauro Marigo ,  Jan Kehler ,  Lars Kyhn Rasmussen

IPC: C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/519

Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.