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：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：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：US09649308B2

公开(公告)日：2017-05-16

申请号：US14744103

申请日：2015-06-19

Applicant: H. Lundbeck A/S

Inventor： John Paul Kilburn ,  Lars Kyhn Rasmussen ,  Mikkel Jessing ,  Eman Mohamed Eldemenky ,  Bin Chen ,  Yu Jiang ,  Allen T. Hopper

IPC: A61K31/505 ,  C07C233/66 ,  C07C233/73 ,  C07C233/75 ,  C07C233/78 ,  C07D211/26 ,  C07D213/40 ,  C07D213/61 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D309/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D403/04

CPC classification number: A61K31/505 ,  C07C233/66 ,  C07C233/73 ,  C07C233/75 ,  C07C233/78 ,  C07C2601/08 ,  C07D211/26 ,  C07D213/40 ,  C07D213/61 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D309/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06

Abstract: The present invention is directed to benzamide-containing compounds of formula I or pharmaceutically acceptable salts thereof which inhibit the P2X7 receptor, and their use in the treatment of pain.

公开(公告)号：US20170128460A1

公开(公告)日：2017-05-11

申请号：US15415073

申请日：2017-01-25

Applicant: H. Lundbeck A/S

Inventor： John Paul Kilburn ,  Lars Kyhn Rasmussen ,  Mikkel Jessing ,  Eman Mohamed Eldemenky ,  Bin Chen ,  Yu Jiang

IPC: A61K31/553 ,  A61K31/5375 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/40 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/445

CPC classification number: A61K31/553 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/625 ,  C07D209/52 ,  C07D211/38 ,  C07D213/40 ,  C07D239/26 ,  C07D267/10 ,  C07D295/13 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.

公开(公告)号：US09434733B2

公开(公告)日：2016-09-06

申请号：US14374278

申请日：2013-01-25

Applicant: H. Lundbeck A/S

Inventor： Niels Svenstrup ,  Klaus Bæk 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：US20150274736A1

公开(公告)日：2015-10-01

申请号：US14434308

申请日：2012-10-09

Applicant: H. LUNDBECK A/S

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

IPC: C07D487/04

CPC classification number: A61K31/506 ,  C07D487/04

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).

Abstract translation: 本发明涉及PDE9酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供制备式（I）化合物的方法。 本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括给予受试者治疗有效量的式（I）化合物。 本发明还提供了治疗患有精神障碍的受试者的方法，其包括向受试者施用治疗有效量的式（I）化合物。

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.