公开(公告)号：US09346797B1

公开(公告)日：2016-05-24

申请号：US14933301

申请日：2015-11-05

Applicant: H. Lundbeck A/S

Inventor： Karsten Juhl ,  Lena Tagmose ,  Mauro Marigo

IPC: C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/44

CPC classification number: A61K31/4439 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to novel 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 Aβ deposits is beneficial such as Alzheimer's disease.

Abstract translation: 本发明涉及BACE1酶的新型抑制剂。 本发明的单独方面涉及包含所述化合物的药物组合物和该化合物用于治疗A和Bgr的减少的病症的用途; 沉积物是有益的，例如阿尔茨海默氏病。

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：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：US11466027B2

公开(公告)日：2022-10-11

申请号：US16916769

申请日：2020-06-30

Applicant: H. Lundbeck A/S

Inventor： John Paul Kilburn ,  Erhad Ascic ,  Mauro Marigo ,  Laurent David

IPC: C07D495/04

Abstract: The present invention is directed to novel modulators of the NMDA receptor. Separate aspects of the inventions are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat neurological disorders or neuropsychiatric disorders such as depression.

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：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：US20190105302A1

公开(公告)日：2019-04-11

申请号：US16033395

申请日：2018-07-12

Applicant: H. Lundbeck A/S

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

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

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.