公开(公告)号：US10512632B2

公开(公告)日：2019-12-24

申请号：US16033395

申请日：2018-07-12

申请人： H. Lundbeck A/S

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

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

摘要： 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：US10005764B2

公开(公告)日：2018-06-26

申请号：US15301210

申请日：2015-03-27

申请人： H. Lundbeck A/S

发明人： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

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

CPC分类号： C07D405/12 ,  C07D403/12 ,  C07D491/048

摘要： 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.

公开(公告)号：US09993477B2

公开(公告)日：2018-06-12

申请号：US15452827

申请日：2017-03-08

申请人： H. LUNDBECK A/S

发明人： Niels Svenstrup ,  Klaus Bæk Simonsen ,  Lars Kyhn Rasmussen ,  Karsten Juhl ,  Morten Langgård ,  Kate Wen ,  Yazhou Wang

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/506

CPC分类号： A61K31/506 ,  C07D487/04

摘要： This invention is directed to compounds, which are PDE9 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 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：US09850249B2

公开(公告)日：2017-12-26

申请号：US15358168

申请日：2016-11-22

申请人： H. Lundbeck A/S

发明人： Niels Svenstrup ,  Klaus Bæk Simonsen ,  Lars Kyhn Rasmussen ,  Karsten Juhl ,  Morten Langgård ,  Kate Wen ,  Yazhou Wang

IPC分类号： C07D487/04 ,  A61K31/53

CPC分类号： C07D487/04 ,  A61K31/53

摘要： This invention is directed to compounds, which are PDE9 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 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：US20170291901A1

公开(公告)日：2017-10-12

申请号：US15481083

申请日：2017-04-06

申请人： H. Lundbeck A/S

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

IPC分类号： C07D487/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  C07D471/04

摘要： 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：US09718832B2

公开(公告)日：2017-08-01

申请号：US15116743

申请日：2015-02-06

申请人： H. Lundbeck A/S

发明人： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

IPC分类号： C07D491/048 ,  C07D403/04 ,  C07D405/04 ,  C07D519/00

CPC分类号： C07D491/048 ,  C07D403/04 ,  C07D405/04 ,  C07D519/00

摘要： The present invention provides hexahydrofuropyrroles 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：US20170173018A1

公开(公告)日：2017-06-22

申请号：US15452827

申请日：2017-03-08

申请人： H. LUNDBECK A/S

发明人： Niels Svenstrup ,  Klaus Bæk Simonsen ,  Lars Kyhn Rasmussen ,  Karsten Juhl ,  Morten Langgård ,  Kate Wen ,  Yazhou Wang

IPC分类号： A61K31/506

CPC分类号： A61K31/506 ,  C07D487/04

摘要： This invention is directed to compounds, which are PDE9 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 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：US09643970B2

公开(公告)日：2017-05-09

申请号：US14434308

申请日：2012-10-09

申请人： H Lundbeck A/S

发明人： Niels Svenstrup ,  Klaus Baek Simonsen ,  Lars Kyhn Rasmussen ,  Karsten Juhl ,  Morten Langgard ,  Kate Wen ,  Yazhou Wang

IPC分类号： A61K31/4985 ,  C07D487/04

CPC分类号： A61K31/506 ,  C07D487/04

摘要： This invention is directed to compounds, which are PDE9 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 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：US20170022186A1

公开(公告)日：2017-01-26

申请号：US15301210

申请日：2015-03-27

申请人： H. Lundbeck A/S

发明人： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

IPC分类号： C07D405/12 ,  C07D491/048

CPC分类号： C07D405/12 ,  C07D403/12 ,  C07D491/048

摘要： 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.

摘要翻译： 本发明提供作为PDE1抑制剂的卤代喹唑啉-THF-胺及其作为药物的用途，特别是用于治疗神经退行性疾病和精神障碍。

公开(公告)号：US20160347759A1

公开(公告)日：2016-12-01

申请号：US15116743

申请日：2015-02-06

申请人： H. LUNDBECK A/S

发明人： Jan Kehler ,  Lars Kyhn Rasmussen ,  Morten Langgård

IPC分类号： C07D491/048

CPC分类号： C07D491/048 ,  C07D403/04 ,  C07D405/04 ,  C07D519/00

摘要： The present invention provides hexahydrofuropyrroles as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

摘要翻译： 本发明提供作为PDE1抑制剂的六氢呋喃并吡喃酮及其作为药物的用途，特别是用于治疗神经退行性疾病和精神疾病。