Abstract: The present invention is directed to compounds of formula IIa These compounds are considered useful for the treatment of diseases associated with leucine-rich repeat kinase 2 (LRRK2) such as Parkinson's disease. Furthermore, the invention relates to pharmaceutical compositions comprising said compounds.
Type:
Grant
Filed:
September 14, 2023
Date of Patent:
April 16, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Thomas Andersen, Mikkel Jessing, Jacob Nielsen, Henrik Daver, Christopher Richard Jones
Abstract: The present invention is directed to antibodies and antigen binding fragments thereof having binding specificity for PACAP. The antibodies and antigen binding fragments thereof comprise the sequences of the VH, VL, and CDR polypeptides described herein, and the polynucleotides encoding them. Antibodies and antigen binding fragments described herein bind to and/or compete for binding to the same linear or conformational epitope(s) on human PACAP as an anti-PACAP antibody. The invention contemplates conjugates of anti-PACAP antibodies and binding fragments thereof conjugated to one or more functional or detectable moieties. Methods of making said anti-PACAP antibodies and antigen binding fragments thereof are also contemplated.
Type:
Grant
Filed:
December 15, 2020
Date of Patent:
March 26, 2024
Assignee:
H. LUNDBECK A/S
Inventors:
Maria-Cristina Loomis, Leon F. Garcia-Martinez, Benjamin H. Dutzar, Daniel S. Allison, Katherine Lee Hendrix, Ethan W. Ojala, Pei Fan, Jeffrey T. L. Smith, John A. Latham, Charlie Karasek, Jenny Mulligan, Michelle Scalley-Kim, Erica Stewart, Vanessa Lisbeth Rubin, Jens J. Billgren
Abstract: The present invention provides sulfamate derivative prodrugs of the dopamine agonist (4aR,10aR)-1-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline-6,7-diol, their use in the treatment of conditions for which treatment with a dopamine agonist is therapeutically beneficial and pharmaceutical compositions comprising compounds of the invention. Compounds according to the invention are of formula (Id), wherein R1 and R2 are each independently selected from H, and substituent (iii) below, wherein * indicates the attachment point to oxygen, wherein R3 is selected from H and COR4, and wherein R4 is selected from H and C1-C6 alkyl, with the proviso that R1 and R2 cannot both be H,15 or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
November 15, 2021
Publication date:
January 25, 2024
Applicant:
H. Lundbeck A/S
Inventors:
Morten Jørgensen, Klaus Gjervig Jensen, Jarkko Tapani Rautio, Christoffer Gerner, Bavnhøj Hansen, Jette Bisgaard Boll, Lena Gustavsson, Anja Nørgaard Kjeldsen
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.
Type:
Application
Filed:
July 26, 2023
Publication date:
January 18, 2024
Applicant:
H. Lundbeck A/S
Inventors:
Mikkel Fog Jacobsen, Martin Juhl, Frans Dennis Therkelsen, Kåre Søndergaard, Tobias Gylling Frihed
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.
Type:
Grant
Filed:
October 7, 2021
Date of Patent:
January 9, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Mikkel Fog Jacobsen, Martin Juhl, Kåre Søndergaard
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.
Type:
Grant
Filed:
August 3, 2021
Date of Patent:
January 2, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Klaus Gjervig Jensen, Lisbet Kværnø, Morten Jørgensen, Martin Juhl, Heidi Lopez de Diego, Karin Fredholt, Frans Dennis Therkelsen, Tobias Gylling Frihed, Mikkel Fog Jacobsen
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.
Type:
Application
Filed:
June 8, 2023
Publication date:
December 28, 2023
Applicant:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Mikkel Jessing, Wanwan Yu, David Rodriguez Diaz, Jacob Nielsen, Christopher Richard Jones, Thomas Andersen, Mikkel Fog Jacobsen
Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
Type:
Grant
Filed:
December 12, 2018
Date of Patent:
December 26, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
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.
Type:
Grant
Filed:
August 2, 2021
Date of Patent:
December 26, 2023
Assignee:
H. Lundbeck A/S
Inventors:
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 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.
Type:
Grant
Filed:
July 26, 2021
Date of Patent:
November 28, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Martin Juhl, Lisbet Kværnø, Mikkel Fog Jacobsen
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.
Type:
Grant
Filed:
October 26, 2022
Date of Patent:
October 10, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Mikkel Jessing, Wanwan Yu, David Rodriguez Diaz, Jacob Nielsen, Christopher Richard Jones, Thomas Andersen, Mikkel Fog Jacobsen
Abstract: The present invention relates to a novel class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396), as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and tauopathies.
Type:
Grant
Filed:
January 8, 2021
Date of Patent:
August 29, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Jan Torleif Pedersen, Lars Østergaard Pedersen, Justus Claus Alfred Daechsel, Ayodeji Abdur-rasheed Asuni, Nina Helen Rosenqvist, Christiane Volbracht, Lone Helboe, Anders Brandt Elvang, Florence Sotty, Søren Christensen, Jeffrey B. Stavenhagen
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.
Type:
Grant
Filed:
July 26, 2021
Date of Patent:
August 22, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Martin Juhl, Lisbet Kværnø, Mikkel Fog Jacobsen
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.
Type:
Grant
Filed:
July 28, 2021
Date of Patent:
July 25, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Klaus Gjervig Jensen, Lisbet Kværnø, Morten Jørgensen, Martin Juhl
Abstract: Described herein is the manufacture of MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate including salts thereof.
Abstract: The present invention relates to monoclonal anti-Sortilin antibodies which have been found useful in correcting a deficient level of progranulin (PGRN). In particular, these antibodies can be used in the treatment of frontotemporal dementia (FTD) and amyotrophic lateral sclerosis (ALS).
Type:
Application
Filed:
November 18, 2022
Publication date:
May 25, 2023
Applicant:
H. Lundbeck A/S
Inventors:
Lars Christian Biilmann Rønn, Ibrahim John Malik, Jeffrey B. Stavenhagen, Soren Christensen, Jan Egebjerg, Amout Gerritsen, Edward van den Brink, Paul Parren, Rob de Jong
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.
Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising the same. The compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the compounds and compositions are useful for the treatment of pain.
Type:
Grant
Filed:
May 22, 2018
Date of Patent:
May 23, 2023
Assignee:
H. LUNDBECK A/S
Inventors:
Cheryl A. Grice, John J. M. Wiener, Olivia D. Weber, Katharine K. Duncan
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.
Type:
Application
Filed:
October 26, 2022
Publication date:
May 11, 2023
Applicant:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Mikkel Jessing, Wanwan YU, David Rodriguez Diaz, Jacob Nielsen, Christopher Richard Jones, Thomas Andersen, Mikkel Fog Jacobsen