公开(公告)号：US08815914B2

公开(公告)日：2014-08-26

申请号：US13934277

申请日：2013-07-03

Applicant: H. Lundbeck A/S

Inventor： Anette Graven Sams ,  Jorgen Eskildsen ,  Ask Püschl

IPC: C07D213/647 ,  C07D405/12 ,  A61K31/44

CPC classification number: A61K31/44 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/505 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D239/34 ,  C07D405/12 ,  C07D491/056

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 α7 receptor.

公开(公告)号：US20220220077A1

公开(公告)日：2022-07-14

申请号：US17606303

申请日：2020-05-19

Applicant: H. Lundbeck A/S

Inventor： Morten Jørgensen ,  Erhad Ascic ,  Martin Juhl ,  Klaus Gjervig Jensen ,  Ask Püschl ,  Benny Bang-Andersen

IPC: C07D221/08 ,  C07F9/576

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.

公开(公告)号：US20160303120A1

公开(公告)日：2016-10-20

申请号：US14940272

申请日：2015-11-13

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Jacob Nielsen ,  Ask Püschl ,  John Paul Kilburn ,  Morten Langgård

IPC: A61K31/4985 ,  A61K31/4709 ,  A61K31/519

CPC classification number: A61K31/4985 ,  A61K31/4709 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04

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.

公开(公告)号：US20150376186A1

公开(公告)日：2015-12-31

申请号：US14305736

申请日：2012-12-21

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Jacob Nielsen ,  Ask Püschl ,  John Paul Kilburn ,  Morten Langgård

IPC: C07D487/04 ,  C07D471/04

CPC classification number: A61K31/4985 ,  A61K31/4709 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04

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 PDE10 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.

公开(公告)号：US09050327B2

公开(公告)日：2015-06-09

申请号：US14054941

申请日：2013-10-16

Applicant: H. Lundbeck A/S

Inventor： Jørgen Eskildsen ,  Anette Graven Sams ,  Ask Püschl

IPC: C07D213/71 ,  C07D239/34 ,  C07D405/12 ,  A61K31/4355 ,  A61K31/44 ,  A61K31/505 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D491/056 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  A61K31/443 ,  A61K31/4433 ,  A61K45/06 ,  A61K31/4427 ,  A61K31/436

CPC classification number: A61K31/44 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/505 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D239/34 ,  C07D405/12 ,  C07D491/056

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 α7 receptor.

公开(公告)号：US09801878B2

公开(公告)日：2017-10-31

申请号：US14940272

申请日：2015-11-13

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Jacob Nielsen ,  Ask Püschl ,  John Paul Kilburn ,  Morten Langgård

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/4709 ,  A61K31/519

CPC classification number: A61K31/4985 ,  A61K31/4709 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04

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.

公开(公告)号：US09669029B2

公开(公告)日：2017-06-06

申请号：US14749754

申请日：2015-06-25

Applicant: H. Lundbeck A/S

Inventor： Ask Püschl ,  Jacob Nielsen ,  Jan Kehler ,  John Paul Kilburn ,  Mauro Marigo ,  Morten Langgård

IPC: A61K31/4985 ,  C07D487/04 ,  C07D471/04 ,  A61K45/06 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28 ,  A61P25/22

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention is directed to compounds, which are PDE10A 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 also provides a method of treating a subject suffering from a drug addiction 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.

公开(公告)号：US09216986B1

公开(公告)日：2015-12-22

申请号：US14305736

申请日：2012-12-21

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Jacob Nielsen ,  Ask Püschl ,  John Paul Kilburn ,  Morten Langgård

IPC: C07D487/04 ,  C07D471/04

CPC classification number: A61K31/4985 ,  A61K31/4709 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04

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 PDE10 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.

Abstract translation: 本发明提供了作为PDE10A酶抑制剂的式I的喹啉衍生物，因此可用于治疗神经变性和精神疾病。 特别地，本发明提供对PDE10比其它PDE亚型具有高度选择性的化合物。 本发明还提供包含本发明化合物的药物组合物和使用本发明化合物治疗病症的方法。

公开(公告)号：US20140044806A1

公开(公告)日：2014-02-13

申请号：US14054941

申请日：2013-10-16

Applicant: H. Lundbeck A/S

Inventor： Jørgen Eskildsen ,  Anette Graven Sams ,  Ask Püschl

IPC: C07D405/12 ,  A61K31/44 ,  C07D213/647 ,  C07D213/84 ,  A61K45/06 ,  C07D491/056 ,  A61K31/4355 ,  A61K31/436 ,  C07D239/34 ,  A61K31/505 ,  C07D213/40 ,  A61K31/443

CPC classification number: A61K31/44 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/505 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D239/34 ,  C07D405/12 ,  C07D491/056

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 α7 receptor.

Abstract translation: 本发明涉及可用于治疗的化合物，包含所述化合物的组合物，以及治疗疾病的方法，包括施用所述化合物。 所提及的化合物是烟碱乙酰胆碱α7受体的正变构调节剂（PAM）。

公开(公告)号：US20150315130A1

公开(公告)日：2015-11-05

申请号：US14650633

申请日：2013-12-09

Applicant: H. LUNDBECK A/S

Inventor： Jørgen Eskildsen ,  Anette Graven Sams ,  Ask Püschl

IPC: C07C233/60 ,  C07C233/59

CPC classification number: C07C233/60 ,  C07C233/58 ,  C07C233/59 ,  C07C2601/02

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 α7 receptor.

Abstract translation: 本发明涉及可用于治疗的化合物，包含所述化合物的组合物，以及治疗疾病的方法，包括施用所述化合物。 所提及的化合物是烟碱乙酰胆碱α7受体的正变构调节剂（PAM）。