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:
March 16, 2023
Date of Patent:
March 25, 2025
Assignee:
H. LUNDBECK A/S
Inventors:
Cheryl A. Grice, John J. M. Wiener, Olivia D. Weber, Katharine K. Duncan
Abstract: The present invention provides novel compounds which activate the Kv7 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders responsive to the activation of Kv7 potassium channels.
Type:
Grant
Filed:
July 20, 2022
Date of Patent:
March 25, 2025
Assignee:
H. Lundbeck A/S
Inventors:
Mario Rottlander, Anette Graven Sams, Xiaofang Wang, Debasis Das, Jian Hong, Shu Hui Chen
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.
Type:
Grant
Filed:
June 6, 2023
Date of Patent:
February 18, 2025
Assignee:
H. Lundbeck A/S
Inventors:
Klaus Gjervig Jensen, Lisbet Kværnø, Morten Jørgensen, Martin Juhl
Abstract: Methods for immediate relief of migraine or headache are provided comprising the administration of an anti-CGRP antagonist antibody to a patient in need thereof.
Type:
Grant
Filed:
March 19, 2024
Date of Patent:
February 4, 2025
Assignee:
H. LUNDBECK A/S
Inventors:
Roger K. Cady, Jeffrey T. L. Smith, Joseph Hirman, Barbara Schaeffler, Lahar Mehta
Abstract: Methods for rapid treatment of chronic migraine are provided. Exemplary methods provide relief from migraine within 24 hours of administration. Also provided are methods for acute treatment of migraine. Exemplary methods comprise administration of an anti-CGRP antagonist antibody to a patient in need thereof.
Type:
Grant
Filed:
March 19, 2024
Date of Patent:
February 4, 2025
Assignee:
H. LUNDBECK A/S
Inventors:
Roger K. Cady, Jeffrey T.L. Smith, Joseph Hirman, Barbara Schaeffler, Lahar Mehta
Abstract: The present invention relates to novel spiro-macrocyclic compounds of general formula (I) which are Orexin 2 receptor agonists.
Type:
Application
Filed:
May 31, 2024
Publication date:
December 26, 2024
Applicant:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Wanwan Yu, Thomas Leegaard Andersen, Erhad Ascic, Michael Baek, Gitte Kobberøe Mikkelsen, Andreas Michael Arnold, Anders Højgaard Hansen, Petra Lindovská, Henrik Juhani Keränen, Ferran Planas Padrós
Abstract: The present invention is directed to antagonistic antibodies and antigen binding fragments thereof having binding specificity for PACAP. These antibodies inhibit, block or neutralize at least one biological effect associated with PACAP, e.g., vasodilation. In exemplary embodiments these antibodies and antigen binding fragments thereof may comprise specific VH, VL, and CDR polypeptides described herein. In some embodiments these antibodies and antigen binding fragments thereof bind to and/or compete for binding to specific epitope(s) on human PACAP. The invention is further directed to using these antagonistic anti-PACAP antibodies, and binding fragments thereof, for the diagnosis, assessment, and treatment of diseases and disorders associated with PACAP and conditions where antagonism of PACAP-related activities, such as vasodilation, mast cell degranulation, and/or neuronal activation, are therapeutically beneficial, e.g., headache and migraine indications.
Type:
Grant
Filed:
March 16, 2021
Date of Patent:
December 10, 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: Described herein are new crystalline forms of the MAGL inhibitor 1-(1-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)-1,8-diazaspiro[4.5]decane-8-carbonyl)-1H-pyrazole-3-carboxylic acid, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 1, 2022
Date of Patent:
November 26, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Vetter, Martin Juhl, Heidi Lopez De Diego, Cheryl A. Grice, John J. M. Wiener, Daniel J. Buzard, Amy Allan, Susana Del Rio Gancedo, Samuel George Andrew, Antonio Cincotti, Adam Ross Patterson, Richard James Edwards
Abstract: The present invention relates to a class of monoclonal antibody that specifically binds the phosphorylated serine 396 residue on pathological hyperphosphorylated (PHF) tau (pS396) with improved affinity, as well as to methods of using these molecules and their tau binding fragments in the treatment of Alzheimer's disease and other tauopathies.
Type:
Grant
Filed:
August 11, 2021
Date of Patent:
October 29, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Jan Torleif Pedersen, Kristian Kjaergaard, Lars Østergaard Pedersen, Ayodeji Abdur-Rasheed Asuni, Nina Helen Rosenqvist, Justus Claus Alfred Daechsel, Karsten Juhl, Lena Tagmose, Mauro Marigo, Thomas Jensen, Søren Christensen, Laurent David, Christiane Volbracht, Lone Helboe
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:
Application
Filed:
November 13, 2023
Publication date:
October 24, 2024
Applicant:
H. LUNDBECK A/S
Inventors:
Martin Juhl, Frans Dennis Therkelsen, Tobias Gylling Frihed
Abstract: The present disclosure provides methods for the prevention or treatment of metabolic disorders. In exemplary embodiments, methods of administering an anti-CGRP antibody are provided, optionally in combination with a second agent, wherein peripheral and/or hepatic glucose utilization is increased, thereby preventing or treating diseases and disorders associated with insulin resistance. Compositions comprising an anti-CGRP antibody are also provided, optionally in combination with a second agent, which are suitable for administration to increase peripheral and/or hepatic glucose utilization and thereby prevent or treat diseases and disorders associated with insulin resistance.
Type:
Grant
Filed:
July 12, 2019
Date of Patent:
October 22, 2024
Assignee:
H. LUNDBECK A/S
Inventors:
Brian Baker, Jeffrey T.L. Smith, John Latham
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:
Application
Filed:
February 21, 2024
Publication date:
October 17, 2024
Applicant:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Thomas Andersen, Mikkel Jessing, Jacob Nielsen, Henrik Daver, Christopher Richard Jones
Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.
Type:
Grant
Filed:
June 7, 2021
Date of Patent:
October 15, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Morten Jorgensen, Peter Hongaard Andersen, Klaus Gjervig Jensen
Abstract: The present invention provides novel compounds which activate the Kv7 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders responsive to the activation of Kv7 potassium channels.
Type:
Application
Filed:
December 6, 2022
Publication date:
October 3, 2024
Applicant:
H. Lundbeck A/S
Inventors:
Mario Rottlander, Xiaofang Wang, Debasis Das, Jian Hong, Shu Hui Chen, Anette Graven Sams, Krestian Larsen
Abstract: The present invention is directed to antagonistic antibodies and antigen binding fragments thereof having binding specificity for PACAP. These antibodies inhibit, block or neutralize at least one biological effect associated with PACAP, e.g., vasodilation. In exemplary embodiments these antibodies and antigen binding fragments thereof may comprise specific VH, VL, and CDR polypeptides described herein. In some embodiments these antibodies and antigen binding fragments thereof bind to and/or compete for binding to specific epitope(s) on human PACAP. The invention is further directed to using these antagonistic anti-PACAP antibodies, and binding fragments thereof, for the diagnosis, assessment, and treatment of diseases and disorders associated with PACAP and conditions where antagonism of PACAP-related activities, such as vasodilation, mast cell degranulation, and/or neuronal activation, are therapeutically beneficial, e.g., headache and migraine indications.
Type:
Grant
Filed:
December 16, 2021
Date of Patent:
September 3, 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: Methods for producing heterologous proteins are disclosed. In particular, the present disclosure provides improved methods of producing desired proteins, including multi-subunit proteins such as antibodies, with a higher yield and improved purity. In exemplary embodiments, the transformed cells are a yeast, e.g., methylotrophic yeast such as Pichia pastoris.
Abstract: The present invention relates to stable and low viscosity liquid pharmaceutical compositions comprising antibodies binding to human alpha synuclein and to methods for use of antibodies binding to human alpha synuclein for treating synucleinopathies or prodromal synucleinopathy, incl. suitable doses and/or dosing regimens. These antibodies for use in treatment of synucleinopathies or prodromal synucleinopathy may be formulated in the stable and low viscosity liquid pharmaceutical compositions of the invention.
Type:
Grant
Filed:
June 26, 2023
Date of Patent:
September 3, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Josefine Nielsen Søderberg, Pekka Kallunki, Louise Buur, Frank Larsen
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: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.
Type:
Grant
Filed:
November 8, 2022
Date of Patent:
June 25, 2024
Assignees:
H. LUNDBECK A/S, THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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:
Application
Filed:
November 16, 2023
Publication date:
June 13, 2024
Applicant:
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