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：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.

公开(公告)号：US20190284266A1

公开(公告)日：2019-09-19

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 ,  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：US10034861B2

公开(公告)日：2018-07-31

申请号：US15637920

申请日：2017-06-29

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 ,  A61K31/437 ,  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：US09669029B2

公开(公告)日：2017-06-06

申请号：US14749754

申请日：2015-06-25

Applicant: H. Lundbeck A/S

Inventor： Ask Püschl ,  Jacob Nielsen ,  Jan Kehler ,  John Paul Kilburn ,  Mauro Marigo ,  Morten Langgård

IPC: A61K31/4985 ,  C07D487/04 ,  C07D471/04 ,  A61K45/06 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28 ,  A61P25/22

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

公开(公告)号：US20170066741A1

公开(公告)日：2017-03-09

申请号：US15119639

申请日：2015-02-17

Applicant: H. Lundbeck A/S

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

IPC: C07D401/12 ,  C07D211/72 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D401/12 ,  C07D211/72 ,  C07D227/10 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention is directed to novel 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.

Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗Aβ沉积物减少的疾病如阿尔茨海默病的用途。

公开(公告)号：US20170044151A1

公开(公告)日：2017-02-16

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 ,  C07D413/12 ,  C07B59/00 ,  C07D211/72 ,  C07D401/12

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.

Abstract translation: 用于治疗神经变性或认知疾病。 该方法还提供式I化合物的哌啶-2-酮和哌啶-2-硫酮中间体。