公开(公告)号：US11858954B2

公开(公告)日：2024-01-02

申请号：US17392970

申请日：2021-08-03

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：US11827665B2

公开(公告)日：2023-11-28

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

CPC classification number: 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：US11731999B2

公开(公告)日：2023-08-22

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

CPC classification number: 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：US20200369615A1

公开(公告)日：2020-11-26

申请号：US16876966

申请日：2020-05-18

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Martin Juhl ,  Frans Dennis Therkelsen ,  Kåre Søndergaard ,  Tobias Gylling Frihed

IPC: C07D215/06 ,  C07D317/60

Abstract: The present invention relates to a new process for manufacturing (6aR,10aR)-7-propyl-6,6a,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.

公开(公告)号：US12071416B2

公开(公告)日：2024-08-27

申请号：US18058587

申请日：2022-11-23

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Morten Jørgensen

IPC: C07D295/037

CPC classification number: C07D295/037

Abstract: The present invention relates to prodrugs of 4-((1R,3S)-6-cloro-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 composition comprising prodrugs, or pharmaceutically acceptable salts thereof, of the invention.

公开(公告)号：US20240018107A1

公开(公告)日：2024-01-18

申请号：US18359136

申请日：2023-07-26

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Martin Juhl ,  Frans Dennis Therkelsen ,  Kåre Søndergaard ,  Tobias Gylling Frihed

IPC: C07D215/06 ,  C07D317/60

CPC classification number: C07D215/06 ,  C07D317/60

Abstract: The present invention relates to a new process for manufacturing (6aR,10aR)-7-propyl-6,6a,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.

公开(公告)号：US20230416272A1

公开(公告)日：2023-12-28

申请号：US18331289

申请日：2023-06-08

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：US11780851B2

公开(公告)日：2023-10-10

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：US20230159478A1

公开(公告)日：2023-05-25

申请号：US18058587

申请日：2022-11-23

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Morten Jørgensen

IPC: C07D295/037

CPC classification number: C07D295/037

Abstract: The present invention relates to prodrugs of 4-((1R,3S)-6-cloro-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 composition comprising prodrugs, or pharmaceutically acceptable salts thereof, of the invention.

公开(公告)号：US20220024875A1

公开(公告)日：2022-01-27

申请号：US17495997

申请日：2021-10-07

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Martin Juhl ,  Frans Dennis Therkelsen ,  Kåre Søndergaard ,  Tobias Gylling Frihed

IPC: 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.