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：US08796304B2

公开(公告)日：2014-08-05

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: A61K31/437 ,  C07D471/06 ,  C07D487/06

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

Abstract: The 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：US10905688B2

公开(公告)日：2021-02-02

申请号：US16345136

申请日：2017-10-26

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård ,  Mikkel Jessing ,  Paulo Jorge Vieira Vital ,  Karsten Juhl

IPC: A61K31/4985 ,  C07D487/04 ,  A61P25/28 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  A61K31/55

Abstract: The present invention provides combination treatments comprising compounds of Formula (I): that are PDE1 enzyme inhibitors and other compounds useful in the treatment of psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of psychiatric and/or cognitive disorders.

公开(公告)号：US10806718B2

公开(公告)日：2020-10-20

申请号：US16670408

申请日：2019-10-31

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Karsten Juhl ,  Mauro Marigo ,  Paulo Jorge Vieira Vital ,  Mikkel Jessing ,  Morten Langgård ,  Lars Kyhn Rasmussen ,  Carl Martin Sebastian Clementson

IPC: C07D401/14 ,  A61K31/437 ,  A61K31/4162 ,  C07D471/04 ,  A61K31/4745 ,  C07D413/04 ,  C07D305/06 ,  C07D401/04

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.

公开(公告)号：US20190308968A1

公开(公告)日：2019-10-10

申请号：US16340429

申请日：2017-10-17

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård ,  Mikkel Jessing ,  Paulo Jorge Vieira Vital ,  Karsten Juhl

IPC: C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds according to formula (I) below that are PDE1 enzyme inhibitors and their use as medicaments, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. 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：US20190194204A1

公开(公告)日：2019-06-27

申请号：US16051612

申请日：2018-08-01

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mikkel Jessing ,  Morten Langgård ,  Paulo Jorge Vieira Vital ,  Mauro Marigo ,  Jan Kehler ,  Lars Kyhn Rasmussen

IPC: C07D487/04 ,  A61K31/519 ,  C07D471/04 ,  A61K31/437

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.

公开(公告)号：US20190194189A1

公开(公告)日：2019-06-27

申请号：US16218019

申请日：2018-12-12

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mikkel Jessing ,  Morten Langgård ,  Paulo Jorge Vieira Vital ,  Jan Kehler ,  Lars Kyhn Rasmussen ,  Carl Martin Sebastian Clementson ,  Mauro Marigo

IPC: C07D471/04 ,  A61P25/28 ,  A61P25/22 ,  A61P25/24 ,  A61P25/18

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US20190185489A1

公开(公告)日：2019-06-20

申请号：US16217754

申请日：2018-12-12

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Mikkel Jessing ,  Morten Langgård ,  Paulo Jorge Vieira Vital ,  Jan Kehler ,  Lars Kyhn Rasmussen ,  Carl Martin Sebastian Clementson ,  Mauro Marigo

IPC: C07D498/22 ,  A61K31/4375

CPC classification number: C07D498/22 ,  A61K31/4375

Abstract: The present invention provides macrocycles of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

公开(公告)号：US20190144434A1

公开(公告)日：2019-05-16

申请号：US16007561

申请日：2018-06-13

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

IPC: C07D405/12 ,  C07D403/12 ,  C07D491/048

Abstract: The present invention provides halogenated quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.