公开(公告)号：US20240190909A1

公开(公告)日：2024-06-13

申请号：US18511231

申请日：2023-11-16

Applicant: H. Lundbeck A/S

Inventor： Klaus Gjervig Jensen ,  Lisbet Kværnø ,  Morten Jørgensen ,  Martin Juhl ,  Heidi Lopez De Diego ,  Karin Fredholt ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed ,  Mikkel Fog Jacobsen

IPC: C07H15/26

CPC classification number: C07H15/26 ,  C07B2200/13

Abstract: The present invention relates to new solid forms of the compound (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below.




The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease.

公开(公告)号：US11993612B2

公开(公告)日：2024-05-28

申请号：US18331289

申请日：2023-06-08

Applicant: H. Lundbeck A/S

Inventor： Thomas Jensen ,  Mikkel Jessing ,  Wanwan Yu ,  David Rodriguez Diaz ,  Jacob Nielsen ,  Christopher Richard Jones ,  Thomas Andersen ,  Mikkel Fog Jacobsen

IPC: C07D498/22

CPC classification number: C07D498/22 ,  C07B2200/05

Abstract: The present invention is directed to compounds of formula I




The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Parkinson's disease.

公开(公告)号：US20230144725A1

公开(公告)日：2023-05-11

申请号：US18049802

申请日：2022-10-26

Applicant: H. Lundbeck A/S ,  Vernalis (R&D) Limited

Inventor： Thomas Jensen ,  Mikkel Jessing ,  Wanwan YU ,  David Rodriguez Diaz ,  Jacob Nielsen ,  Christopher Richard Jones ,  Thomas Andersen ,  Mikkel Fog Jacobsen

IPC: C07D498/22

CPC classification number: C07D498/22 ,  C07B2200/05

Abstract: The present invention is directed to compounds of formula I




The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Parkinson's disease.

公开(公告)号：US11104697B2

公开(公告)日：2021-08-31

申请号：US16876843

申请日：2020-05-18

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Lisbet Kværnø ,  Mikkel Fog Jacobsen

IPC: C07H15/26

Abstract: The present invention relates to a process for manufacturing (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]guinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below and pharmaceutically acceptable salts thereof The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease. The invention also relates to a new intermediate of said process.

公开(公告)号：US20170291874A1

公开(公告)日：2017-10-12

申请号：US15480647

申请日：2017-04-06

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Florian Anton Martin Huber

IPC: C07D209/14

CPC classification number: C07D209/14 ,  B01D3/36 ,  C07D209/16

Abstract: The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof:

公开(公告)号：US11535600B2

公开(公告)日：2022-12-27

申请号：US17297717

申请日：2019-11-27

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Morten Jørgensen

IPC: C07D295/03 ,  C07D295/037

Abstract: The present invention relates to prodrugs of 4-((1R,3S)-6-chloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)-1,2,2-trimethylpiperazine in the form of 1a and 1b; and 4-((1R,3S)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1H-inden-1-yl)-2,2-dimethyl-1-(methyl-d3)piperazine in the form of 2a and 2b, wherein X—is a counter ion, or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising prodrugs, or pharmaceutically acceptable salts thereof, of the invention.

公开(公告)号：US20220185839A1

公开(公告)日：2022-06-16

申请号：US17385166

申请日：2021-07-26

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Lisbet Kværnø ,  Mikkel Fog Jacobsen

IPC: C07H15/26

Abstract: The present invention relates to a process for manufacturing (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below and pharmaceutically acceptable salts thereof The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease.
The invention also relates to a new intermediate of said process.

公开(公告)号：US11130775B2

公开(公告)日：2021-09-28

申请号：US16876908

申请日：2020-05-18

Applicant: H. Lundbeck A/S

Inventor： Klaus Gjervig Jensen ,  Lisbet Kværnø ,  Morten Jørgensen ,  Martin Juhl ,  Heidi Lopez de Diego ,  Karin Fredholt ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed ,  Mikkel Fog Jacobsen

IPC: C07H15/26

Abstract: The present invention relates to new solid forms of the compound (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below. The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease.

公开(公告)号：US09309165B2

公开(公告)日：2016-04-12

申请号：US14653318

申请日：2013-12-19

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Sebastian Brandes

IPC: C07C49/00 ,  C07D295/00 ,  C07D209/00 ,  C07B59/00 ,  C07C49/697 ,  C07D295/073

CPC classification number: C07B59/001 ,  C07B2200/05 ,  C07C49/697 ,  C07D295/073

Abstract: The present invention discloses the compound 6-chloro-3-(phenyl-d5)-inden-1-one (I) and routes of synthesis to obtain (I). In a further aspect the present invention discloses the use of (I) for the synthesis of (S)-6-chloro-3-(phenyl-d5)-indan-1-one.

公开(公告)号：US11866410B2

公开(公告)日：2024-01-09

申请号：US17495997

申请日：2021-10-07

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Martin Juhl ,  Kåre Søndergaard

IPC: C07D317/60 ,  C07D215/06

CPC classification number: C07D215/06 ,  C07D317/60

Abstract: The present invention relates to a new process for manufacturing (6aR,10aR)-7-propyl-6,6 a,7,8,9,10,10a,11-octahydro-[1,3]dioxolo[4′,5′:5,6]benzo[1,2-g]quinoline with formula (Ib) below, (4aR,10aR)-1-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline-6,7-diol with formula (I) below and salts thereof.




Both compounds are for use in the treatment of neurodegenerative diseases and disorders such as Parkinson's Disease. The invention also relates to new intermediate compounds of said process.