公开(公告)号：US10905688B2

公开(公告)日：2021-02-02

申请号：US16345136

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 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  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 psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric 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 psychiatric and/or cognitive disorders.

公开(公告)号：US10806718B2

公开(公告)日：2020-10-20

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: C07D401/14 ,  A61K31/437 ,  A61K31/4162 ,  C07D471/04 ,  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：US20190308968A1

公开(公告)日：2019-10-10

申请号：US16340429

申请日：2017-10-17

Applicant: H. Lundbeck A/S

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

IPC: C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds according to formula (I) below that are PDE1 enzyme inhibitors and their use as medicaments, 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：US20190194204A1

公开(公告)日：2019-06-27

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 ,  A61K31/519 ,  C07D471/04 ,  A61K31/437

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：US20190194189A1

公开(公告)日：2019-06-27

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 ,  A61P25/22 ,  A61P25/24 ,  A61P25/18

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：US20190185489A1

公开(公告)日：2019-06-20

申请号：US16217754

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: C07D498/22 ,  A61K31/4375

CPC classification number: C07D498/22 ,  A61K31/4375

Abstract: The present invention provides macrocycles 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：US20190105302A1

公开(公告)日：2019-04-11

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 Langgàrd ,  Lars Kyhn Rasmussen ,  Carl Martin Sebastian Clementson

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

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：US20190062335A1

公开(公告)日：2019-02-28

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：US20190000823A1

公开(公告)日：2019-01-03

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 ,  C07D417/12 ,  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：US20180230160A1

公开(公告)日：2018-08-16

申请号：US15751777

申请日：2016-08-10

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo ,  Ask Puschl

IPC: C07D491/04 ,  A61P25/28

CPC classification number: C07D491/04 ,  A61P25/28

Abstract: Compounds of the Formula (I) are provided which compounds inhibitors of BACE1.