公开(公告)号：US11707476B2

公开(公告)日：2023-07-25

申请号：US17386686

申请日：2021-07-28

Applicant: H. Lundbeck A/S

Inventor： Klaus Gjervig Jensen ,  Lisbet Kværnø ,  Morten Jørgensen ,  Martin Juhl

IPC: C07D405/12 ,  A61K31/706 ,  A61P25/00 ,  C07D405/14 ,  A61K31/473

CPC classification number: A61K31/706 ,  A61K31/473 ,  A61P25/00 ,  C07D405/12 ,  C07D405/14

Abstract: The present invention provides compounds of formula (Id) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.

公开(公告)号：US11111263B2

公开(公告)日：2021-09-07

申请号：US16876878

申请日：2020-05-18

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed

IPC: C07H15/26 ,  C07H1/00

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 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 new intermediates 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：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：US11851456B2

公开(公告)日：2023-12-26

申请号：US17391439

申请日：2021-08-02

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed

IPC: C07H15/26 ,  C07H1/00

CPC classification number: C07H15/26 ,  C07H1/00

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 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 new intermediates of said process.

公开(公告)号：US20220213071A1

公开(公告)日：2022-07-07

申请号：US17606319

申请日：2020-05-19

Applicant: H. Lundbeck A/S

Inventor： Morten Jørgensen ,  Martin Juhl ,  Klaus Gjervig Jensen ,  Lisbet Kvænø

IPC: C07D405/12

Abstract: The present invention provides compounds of formula (Id) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.

公开(公告)号：US20220194978A1

公开(公告)日：2022-06-23

申请号：US17391439

申请日：2021-08-02

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed

IPC: C07H15/26 ,  C07H1/00

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 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 new intermediates of said process.

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.

公开(公告)号：US11168056B2

公开(公告)日：2021-11-09

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：US20200369706A1

公开(公告)日：2020-11-26

申请号：US16876878

申请日：2020-05-18

Applicant: H. Lundbeck A/S

Inventor： Martin Juhl ,  Frans Dennis Therkelsen ,  Tobias Gylling Frihed

IPC: C07H15/26 ,  C07H1/00

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 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 new intermediates of said process.