公开(公告)号：US11535611B2

公开(公告)日：2022-12-27

申请号：US16955926

申请日：2018-12-19

Applicant: H. Lundbeck A/S

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

IPC: C07D401/14 ,  C07D405/14

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, 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：US20210015794A1

公开(公告)日：2021-01-21

申请号：US17060796

申请日：2020-10-01

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: A61K31/4162 ,  C07D471/04 ,  A61K31/4745 ,  C07D413/04

Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (1) 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：US20210009571A1

公开(公告)日：2021-01-14

申请号：US16955926

申请日：2018-12-19

Applicant: H. Lundbeck A/S

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

IPC: C07D405/14 ,  C07D401/14

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, 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：US20190352302A1

公开(公告)日：2019-11-21

申请号：US16424585

申请日：2019-05-29

Applicant: H. Lundbeck A/S

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

IPC: A61K31/502 ,  C07D471/04 ,  C07D519/00 ,  C07D487/04 ,  A61P25/28 ,  A61P25/00 ,  A61P25/18 ,  A61P25/16

Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, 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：US20180000786A1

公开(公告)日：2018-01-04

申请号：US15637920

申请日：2017-06-29

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: A61K31/4162 ,  C07D413/04 ,  A61K31/4745 ,  C07D401/04 ,  C07D305/06

CPC classification number: A61K31/4162 ,  A61K31/4745 ,  C07D305/06 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04

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：US09701665B2

公开(公告)日：2017-07-11

申请号：US15105647

申请日：2014-12-18

Applicant: H. Lundbeck A/S

Inventor： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

IPC: C07D405/12

CPC classification number: C07D405/12

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.

公开(公告)号：US09592230B2

公开(公告)日：2017-03-14

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: C07D487/04 ,  A61K31/4985 ,  C07D403/12 ,  C07D471/04 ,  A61K31/437 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K31/437 ,  A61K45/06 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04

Abstract: This invention is directed to phenylimidazole derivatives having the formula I: wherein HET is an optionally substituted heteroaromatic group; -L- is selected from the group consisting of —CH2—CH2—, —S—CH2—, —CH2—S— and —CH═CH—, R1 is selected from the group consisting of H, C1-C6 alkyl; C1-C6 alkyl(C3-C8)cycloalkyl; C1-C6 hydroxyalkyl, CH2CN, CH2C(O)NH2, C1-C6 arylalkyl, and C1-C6 alkyl-heterocycloalkyl, and R2, R3, R4, R5 and R6 are selected individually from the group consisting of H, C1-C6 alkoxy and halogen, or pharmaceutically acceptable acid addition salts thereof, which are PDE10A enzyme inhibitors useful in the treatment of psychiatric disorders and drug addiction.

Abstract translation: 本发明涉及苯基咪唑化合物，它们是可用于治疗神经和精神疾病的PDE10A酶抑制剂。

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：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。