公开(公告)号：US11026924B2

公开(公告)日：2021-06-08

申请号：US17060796

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: C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A61K31/26 ,  A61K31/11 ,  A61K31/522 ,  A61K31/4365 ,  A61K31/4162 ,  A61K31/4745 ,  C07D413/04 ,  C07D305/06 ,  C07D401/04

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (1) 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：US20200375950A1

公开(公告)日：2020-12-03

申请号：US16999247

申请日：2020-08-21

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 ,  C07D471/04 ,  C07D413/04

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：US20200129480A1

公开(公告)日：2020-04-30

申请号：US16670408

申请日：2019-10-31

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 ,  C07D471/04 ,  A61K31/4745 ,  C07D413/04

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：US10603310B2

公开(公告)日：2020-03-31

申请号：US16059715

申请日：2018-08-09

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: A61K31/4439 ,  C07D401/12 ,  A61K31/444 ,  C07D417/12 ,  C07D413/12 ,  A61K31/497 ,  A61P25/28

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：US10512632B2

公开(公告)日：2019-12-24

申请号：US16033395

申请日：2018-07-12

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: A61K31/437 ,  C07D401/14 ,  A61K31/4162 ,  A61K31/4745 ,  C07D413/04 ,  C07D471/04 ,  C07D305/06 ,  C07D401/04

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：US10472415B2

公开(公告)日：2019-11-12

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 ,  A61K39/395 ,  A61K49/00 ,  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：US20190284265A1

公开(公告)日：2019-09-19

申请号：US16371867

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 ,  A61K39/395 ,  A61K49/00 ,  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：US10059669B2

公开(公告)日：2018-08-28

申请号：US15524479

申请日：2015-11-09

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: C07D211/72 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4427 ,  C07D417/12 ,  C07B59/00

CPC classification number: C07D211/72 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to compounds according to Formula (I) which compounds 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 5 which the reduction of Aβ deposits is beneficial such as Alzheimer's disease.

公开(公告)号：US10011596B2

公开(公告)日：2018-07-03

申请号：US15233463

申请日：2016-08-10

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: C07D417/12 ,  C07B59/00 ,  C07D211/72 ,  C07D401/12 ,  C07D413/12 ,  C07D211/76

CPC classification number: C07D401/12 ,  C07B59/002 ,  C07B2200/05 ,  C07D211/72 ,  C07D211/76 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention provides compounds of Formula I for the treatment of neurodegenerative or cognitive diseases. The method further provides for piperidine-2-one and piperidine-2-thione intermediates to compounds of formula I.

公开(公告)号：US20170291901A1

公开(公告)日：2017-10-12

申请号：US15481083

申请日：2017-04-06

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

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  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.