Abstract: The present invention provides quinoline derivatives of formula I that are PDE10A enzyme inhibitors, and as such are useful to treat neurodegenerative and psychiatric disorders. Especially, the invention provides compounds that are highly selective for PDE10A over other PDE subtypes. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
October 31, 2017
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Jacob Nielsen, Ask Püschl, John Paul Kilburn, Morten Langgård
Abstract: The present invention relates to the use of an acetylcholinesterase inhibitor and idalopirdine for reducing falls in patients suffering from a CNS disease, in particular patients with Parkinson's disease, wherein balance, gait or movement is impaired.
Type:
Application
Filed:
April 25, 2017
Publication date:
October 26, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Inge E.M. de Jong, Aaron Kucinski, Martin Sarter
Abstract: The present invention provides triazolopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Application
Filed:
October 9, 2015
Publication date:
October 19, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Mikkel Jessing
Abstract: The present invention describes methods of treating dementia comprising administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.
Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Application
Filed:
April 6, 2017
Publication date:
October 12, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Mauro Marigo, Jan Kehler, Lars Kyhn Rasmussen
Abstract: The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof:
Type:
Application
Filed:
April 6, 2017
Publication date:
October 12, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Mikkel Fog Jacobsen, Florian Anton Martin Huber
Abstract: The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Application
Filed:
June 6, 2017
Publication date:
October 12, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl
Abstract: The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adipate salt, the hydrogen malonate salt, the lactate salt, the hydrogen fumarate salt, the hydrogen succinate salt, the benzene sulfonate salt, the hydrogen maleate salt and the salicylate salt of nalmefene. The present invention also relates to such salts for use in therapy.
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:
July 12, 2016
Publication date:
September 21, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Lars Christian Biilmann Rønn, Ibrahim John Malik, Søren Christensen, Jan Egebjerg, Jeffrey B. Stavenhagen, Arnout Gerritsen, Edward van den Brink, Paul Parren, Rob de Jong
Abstract: The present invention provides Quinazolin-THF-amines as PDE I inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Application
Filed:
June 5, 2017
Publication date:
September 21, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård
Abstract: The present invention relates to methods for modulating the activity of one or more Vps10p-domain receptors selected from the group consisting of Sortilin, SorLA, SorCS1, SorCS2 and SorCS3, in an animal and methods for preparation of a medicament for the treatment of mental and behavioral disorders. The modulation is carried out by inhibiting or promoting the binding of ligands to the Vps10p-domain receptor. In vitro and in vivo methods for screening for agents capable of modulation of said Vps10p-domain receptor activity are also provided. The invention furthermore relates to methods of altering expression of said receptors in vivo.
Type:
Application
Filed:
May 2, 2017
Publication date:
August 24, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Simon Glerup Pedersen, Ulrich Bolcho, Kimmo Jensen, Anders Nykjaer
Abstract: The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motoneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease.
Type:
Application
Filed:
May 2, 2017
Publication date:
August 24, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Phillip James Maltas, Stephen Watson, Morten Langgård, Laurent David
Abstract: The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adipate salt, the hydrogen malonate salt, the lactate salt, the hydrogen fumarate salt, the hydrogen succinate salt, the benzene sulfonate salt, the hydrogen maleate salt and the salicylate salt of nalmefene. The present invention also relates to such salts for use in therapy.
Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
Type:
Application
Filed:
April 18, 2017
Publication date:
August 3, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
Abstract: The present invention provides hexahydrofuropyrroles as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Grant
Filed:
February 6, 2015
Date of Patent:
August 1, 2017
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård
Abstract: The present invention is directed to benzamide-containing compounds of formula I or pharmaceutically acceptable salts thereof which inhibit the P2X7 receptor, and their use in the treatment of epilepsy.
Type:
Application
Filed:
April 5, 2017
Publication date:
July 20, 2017
Applicant:
H. Lundbeck A/S
Inventors:
John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohamed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
Type:
Grant
Filed:
June 19, 2015
Date of Patent:
July 18, 2017
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
Abstract: The present invention provides Quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
July 11, 2017
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård
Abstract: The present invention describes methods of treating dementia comprising administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.