公开(公告)号：US20200369705A1

公开(公告)日：2020-11-26

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：US12226428B2

公开(公告)日：2025-02-18

申请号：US18330293

申请日：2023-06-06

Applicant: H. Lundbeck A/S

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

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

Abstract: The present invention provides compounds of formula (I) 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.
Accordingly, the present invention relates to compounds of formula (Id) wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i); wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

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：US20220257623A1

公开(公告)日：2022-08-18

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

Abstract: The present invention provides compounds of formula (I) 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.
Accordingly, the present invention relates to compounds of formula (Id) wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i); wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10729710B2

公开(公告)日：2020-08-04

申请号：US16198917

申请日：2018-11-23

Applicant: H. Lundbeck A/S

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

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

Abstract: The present invention provides compounds of formula (I) 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.Accordingly, the present invention relates to compounds of formula (Id) wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i); wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11110110B2

公开(公告)日：2021-09-07

申请号：US16872802

申请日：2020-05-12

Applicant: H. Lundbeck A/S

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

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

Abstract: The present invention provides compounds of formula (I) 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.
Accordingly, the present invention relates to compounds of formula (Id) wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i); wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

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：US20200338102A1

公开(公告)日：2020-10-29

申请号：US16872802

申请日：2020-05-12

Applicant: H. Lundbeck A/S

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

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

Abstract: The present invention provides compounds of formula (I) 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.Accordingly, the present invention relates to compounds of formula (Id) wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i); wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

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：US20220024962A1

公开(公告)日：2022-01-27

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 Fogh 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.