公开(公告)号：US20170081333A1

公开(公告)日：2017-03-23

申请号：US15358168

申请日：2016-11-22

Applicant: H. Lundbeck A/S

Inventor： Niels Svenstrup ,  Klaus Baiek Simonsen ,  Lars Kyhn Rasmussen ,  Karsten Juhl ,  Morten Langgård ,  Kate Wen ,  Yazhou Wang

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/53

Abstract: This invention is directed to compounds, which are PDE9 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 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：US09346797B1

公开(公告)日：2016-05-24

申请号：US14933301

申请日：2015-11-05

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/44

CPC classification number: A61K31/4439 ,  C07D401/12 ,  C07D413/12 ,  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A和Bgr的减少的病症的用途; 沉积物是有益的，例如阿尔茨海默氏病。

公开(公告)号：US11634416B2

公开(公告)日：2023-04-25

申请号：US16772561

申请日：2018-12-12

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: C07D471/04 ,  A61K45/06

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.

公开(公告)号：US11472810B2

公开(公告)日：2022-10-18

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：US11026923B2

公开(公告)日：2021-06-08

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: C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A61K31/26 ,  A61K31/11 ,  A61K31/522 ,  A61K31/235 ,  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 (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：US10912773B2

公开(公告)日：2021-02-09

申请号：US16345157

申请日：2017-10-26

Applicant: H. Lundbeck A/S

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

IPC: A61K31/4985 ,  C07D487/04 ,  A61P25/28 ,  A61P25/16 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  A61K31/55

Abstract: The present invention provides combination treatments comprising compounds of Formula (I): that are PDE1 enzyme inhibitors, and other compounds useful in the treatment of neurodegenerative disorders such as for example Alzheimer's Disease, Parkinson's Disease or Huntington's Disease. Separate aspects of the invention are directed to the combined use of said compounds for the treatment of neurodegenerative and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of neurodegenerative disorders.

公开(公告)号：US10858362B2

公开(公告)日：2020-12-08

申请号：US16002116

申请日：2018-06-07

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：US10766893B2

公开(公告)日：2020-09-08

申请号：US16218019

申请日：2018-12-12

Applicant: H. Lundbeck A/S

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

IPC: C07D471/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  C07D519/00

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridines 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：US10689379B2

公开(公告)日：2020-06-23

申请号：US16424585

申请日：2019-05-29

Applicant: H. Lundbeck A/S

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

IPC: A61K31/4162 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/5025 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/4745 ,  A61K31/502 ,  A61K31/506 ,  A61P25/28 ,  A61P25/18 ,  A61P25/00 ,  A61P25/16

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

公开(公告)号：US10351561B2

公开(公告)日：2019-07-16

申请号：US15849798

申请日：2017-12-21

Applicant: H. Lundbeck A/S

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

IPC: A61K31/4162 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/5025 ,  C07D471/04 ,  C07D487/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/00 ,  A61P25/16 ,  C07D519/00

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.