Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I) The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
Type:
Grant
Filed:
March 8, 2017
Date of Patent:
June 12, 2018
Assignee:
H. LUNDBECK A/S
Inventors:
Niels Svenstrup, Klaus Bæk Simonsen, Lars Kyhn Rasmussen, Karsten Juhl, Morten Langgård, Kate Wen, Yazhou Wang
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:
Grant
Filed:
April 6, 2017
Date of Patent:
May 22, 2018
Assignee:
H. LUNDBECK A/S
Inventors:
Mikkel Fog Jacobsen, Florian Anton Martin Huber
Abstract: The present invention relates to specific dosages of an A2A antagonist for use as a medicament and in particular useful for the treatment of Parkinson Disease and Attention Deficit/Hyperactivity Disorder.
Type:
Application
Filed:
November 10, 2017
Publication date:
May 10, 2018
Applicant:
H. Lundbeck A/S
Inventors:
Lone Frydelund Larsen, Johan Areberg, Nathalie Breysse, Gamini Chandrasena
Abstract: The invention relates to novel monoclonal anti-alpha-synuclein antibodies. The antibodies can be used for treating a synucleinopathy such as Parkinson's disease (including idiopathic and inherited forms of Parkinson's disease), Diffuse Lewy Body Disease (DLBD), Lewy body variant of Alzheimer's disease (LBV), Combined Alzheimer's and Parkinson disease, pure autonomic failure and multiple system atrophy.
Type:
Application
Filed:
November 14, 2017
Publication date:
May 10, 2018
Applicant:
H. Lundbeck A/S
Inventors:
Pekka Kallunki, Karina Fog, Louise Buur Vesterager, Ann-Louise Bergstrôm, Florence Sotty, David Satijn, Edward van den Brink, Paul Parren, Rik Rademaker, Tom Vink, Ibrahim John Malik, Liliana Christina Pereira Montezinho
Abstract: The invention relates to novel monoclonal anti-alpha-synuclein antibodies. The antibodies can be used for treating a synucleinopathy such as Parkinson's disease (including idiopathic and inherited forms of Parkinson's disease), Diffuse Lewy Body Disease (DLBD), Lewy body variant of Alzheimer's disease (LBV), Combined Alzheimer's and Parkinson disease, pure autonomic failure and multiple system atrophy.
Type:
Application
Filed:
November 14, 2017
Publication date:
May 10, 2018
Applicant:
H. Lundbeck A/S
Inventors:
Pekka Kallunki, Karina Fog, Louise Buur Vesterager, Ann-Louise Bergstrôm, Florence Sotty, David Satijn, Edward van den Brink, Paul Parren, Rik Rademaker, Tom Vink, Ibrahim John Malik, Liliana Christina Pereira Montezinho
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: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.
Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.
Type:
Application
Filed:
March 22, 2016
Publication date:
March 8, 2018
Applicant:
H. Lundbeck A/S
Inventors:
Carla De Faveri, Florian Anton Martin Huber
Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
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:
Application
Filed:
July 10, 2017
Publication date:
January 18, 2018
Applicant:
H. Lundbeck A/S
Inventors:
Jan Torleif Pedersen, Kristian Kjærgaard, Lars Østergaard Pedersen, 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: 1-[2-(2,4-dimethylphenylsulphanyl)phenyl)]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
Type:
Grant
Filed:
August 10, 2017
Date of Patent:
January 9, 2018
Assignee:
H. Lundbeck A/S
Inventors:
André Faldt, Heidi Lopez de Diego, Rene Holm
Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines 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:
June 29, 2017
Publication date:
January 4, 2018
Applicant:
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: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
Type:
Grant
Filed:
November 22, 2016
Date of Patent:
December 26, 2017
Assignee:
H. Lundbeck A/S
Inventors:
Niels Svenstrup, Klaus Bæk Simonsen, Lars Kyhn Rasmussen, Karsten Juhl, Morten Langgård, Kate Wen, Yazhou Wang
Abstract: The present invention is directed to compounds of Formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
Type:
Application
Filed:
November 9, 2015
Publication date:
November 30, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Lena Tagmose, Mauro Marigo
Abstract: A dose regimes comprising the simultaneous administration of two pharmaceutical compositions, wherein the first pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof for once daily oral administration, and the second pharmaceutical composition is a composition comprising vortioxetine or a pharmaceutically acceptable salt thereof which together with said first composition quickly achieves a steady-state plasma level of vortioxetine in said patient which steady-state plasma level is the same as the steady-state vortioxetine plasma level achieved by the administration to said patient of said first composition alone.
Abstract: The present invention relates to 5-HT6 receptor antagonists for the treatment of Alzheimer's disease with comorbid apathy comprising administering an effective dose of a 5-HT6 receptor antagonist to improve or augment the effect of an acetylcholinesterase inhibitor.
Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
Type:
Application
Filed:
November 9, 2015
Publication date:
November 9, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Lena Tagmose, Mauro Marigo
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 abnormal plasma lipid concentrations and associated diseases and/or 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.
Abstract: The present invention is directed to compounds according to Formula (I) which compounds are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for 5 which the reduction of A? deposits is beneficial such as Alzheimer's disease.
Type:
Application
Filed:
November 9, 2015
Publication date:
November 2, 2017
Applicant:
H. Lundbeck A/S
Inventors:
Karsten JUHL, Lena TAGMOSE, Mauro MARIGO