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：US09062060B2

公开(公告)日：2015-06-23

申请号：US14309423

申请日：2014-06-19

Applicant: H. Lundbeck A/S

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

IPC: C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

Abstract: This invention is directed to compounds with the structure 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.

Abstract translation: 本发明涉及具有PDE10A酶抑制剂结构的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US20150025081A1

公开(公告)日：2015-01-22

申请号：US14488554

申请日：2014-09-17

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/4985 ,  C07D471/04 ,  A61K31/437

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US20140357639A1

公开(公告)日：2014-12-04

申请号：US14309423

申请日：2014-06-19

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Jacob Nielsen ,  Mauro Marigo ,  John Paul Kilburn ,  Morten Langgârd

IPC: C07D487/04 ,  A61K31/437 ,  C07D471/04 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US20130281459A1

公开(公告)日：2013-10-24

申请号：US13922371

申请日：2013-06-20

Applicant: H. Lundbeck A/S

Inventor： Ask Puschl ,  Jacob Nielsen ,  Jan Kehler ,  John Paul Kilburn ,  Mauro Marigo ,  Morton Langgard

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04

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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US20230144725A1

公开(公告)日：2023-05-11

申请号：US18049802

申请日：2022-10-26

Applicant: H. Lundbeck A/S ,  Vernalis (R&D) Limited

Inventor： Thomas Jensen ,  Mikkel Jessing ,  Wanwan YU ,  David Rodriguez Diaz ,  Jacob Nielsen ,  Christopher Richard Jones ,  Thomas Andersen ,  Mikkel Fog Jacobsen

IPC: C07D498/22

CPC classification number: C07D498/22 ,  C07B2200/05

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.

公开(公告)号：US20150190395A1

公开(公告)日：2015-07-09

申请号：US14663706

申请日：2015-03-20

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: A61K31/4985 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US09018217B2

公开(公告)日：2015-04-28

申请号：US14488554

申请日：2014-09-17

Applicant: H. Lundbeck A/S

Inventor： Andreas Ritzen ,  Morten Langgard ,  Jan Kehler ,  Jacob Nielsen ,  John Paul Kilburn ,  Mohamed M. Farah

IPC: C07D239/42 ,  C07D231/10 ,  C07D487/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US08927738B2

公开(公告)日：2015-01-06

申请号：US13924712

申请日：2013-06-24

Applicant: H. Lundbeck A/S

Inventor： Ask Puschl ,  Jacob Nielsen ,  Jan Kehler ,  John Paul Kilburn ,  Mauro Marigo ,  Morton Langgard

IPC: C07D233/64 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: This invention is directed to compounds of formula I having the structure 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.

Abstract translation: 本发明涉及具有PDE10A酶抑制剂结构的式I化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。

公开(公告)号：US20140005201A1

公开(公告)日：2014-01-02

申请号：US14016685

申请日：2013-09-03

Applicant: H. Lundbeck A/S

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

IPC: C07D471/04 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

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.

Abstract translation: 本发明涉及PDE10A酶抑制剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了制备式I化合物的方法。本发明还提供了治疗患有神经变性疾病的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明 本发明还提供了治疗患有药物成瘾症的受试者的方法，其包括向受试者施用治疗有效量的式I化合物。本发明还提供了治疗患有精神病障碍患者的方法，包括给予 治疗有效量的式I化合物。