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![PROCESS FOR THE MANUFACTURE OF (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](/abs-image/US/2024/10/24/US20240352055A1/abs.jpg.150x150.jpg)
公开(公告)号：US20240352055A1
公开(公告)日：2024-10-24
申请号：US18507662
申请日：2023-11-13
Applicant: H. LUNDBECK A/S
Inventor： Martin Juhl , Frans Dennis Therkelsen , Tobias Gylling Frihed
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.-
![PROCESS FOR THE MANUFACTURE OF (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](/abs-image/US/2022/06/16/US20220185839A1/abs.jpg.150x150.jpg)
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.-
![SOLID FORMS OF (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](/abs-image/US/2022/01/27/US20220024962A1/abs.jpg.150x150.jpg)
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.
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![Solid forms of (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](/abs-image/US/2021/09/28/US11130775B2/abs.jpg.150x150.jpg)
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.
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公开(公告)号：US20190160083A1
公开(公告)日：2019-05-30
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
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.
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Patent Agency Ranking
公开(公告)号：US20240156851A1
公开(公告)日：2024-05-16
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
CPC classification number: 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.-
![Process for the manufacturing of (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 and (4AR, 10AR)-1-propyl-1,2,3,4,4A,5,10,10A-octahydro-benzo[G]quinoline-6,7-diol](/abs-image/US/2024/01/09/US11866410B2/abs.jpg.150x150.jpg)
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.-
![Solid forms of (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](/abs-image/US/2024/01/02/US11858954B2/abs.jpg.150x150.jpg)
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.-
![Process for the manufacture of (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](/abs-image/US/2023/11/28/US11827665B2/abs.jpg.150x150.jpg)
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.-
![Process for the manufacture of (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](/abs-image/US/2023/08/22/US11731999B2/abs.jpg.150x150.jpg)
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.
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