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：US20160083359A1

公开(公告)日：2016-03-24

申请号：US14948775

申请日：2015-11-23

Applicant: H. Lundbeck A/S

Inventor： Benny Bang-Andersen ,  André Faldt ,  Arne Mørk ,  Heidi Lopez De Diego ,  René Holm ,  Tine Bryan Stensbøl ,  Lone Munch Ringgard ,  Michael J. Mealy ,  Michael Harold Rock ,  Jørgen Brodersen ,  Morten Jørgensen ,  Nicholas Moore

IPC: C07D295/096

CPC classification number: A61K31/495 ,  A61K9/14 ,  A61P25/22 ,  C07D295/096 ,  Y10T428/2982

Abstract: 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.

Abstract translation: 1- [2-（2,4-二甲基苯基硫烷基）苯基]哌嗪显示出对SERT，5-HT3和5-HT1A的有效活性，并且可以用于治疗认知障碍，特别是抑郁症患者。

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：US09125910B2

公开(公告)日：2015-09-08

申请号：US14481000

申请日：2014-09-09

Applicant: H. Lundbeck A/S

Inventor： Benny Bang-Andersen ,  Arne Mork ,  Tine Bryan Stensbol ,  Andre Faldt

IPC: A61K31/495 ,  C07D295/096

CPC classification number: A61K31/495 ,  A61K9/14 ,  C07D295/096 ,  Y10T428/2982

Abstract: This disclosure relates to a method of treating a disease selected from the group consisting of Alzheimer's disease, cognitive impairment, and attention deficit hyperactivity disorder (ADHD). The method includes administering a therapeutically effective amount of Compound I or a pharmaceutically acceptable salt thereof to patient in need thereof, in which Compound I is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine.

Abstract translation: 本公开涉及治疗选自阿尔茨海默氏病，认知障碍和注意缺陷多动障碍（ADHD）的疾病的方法。 该方法包括向有需要的患者施用治疗有效量的化合物I或其药学上可接受的盐，其中化合物I是1- [2-（2,4-二甲基苯基硫烷基） - 苯基]哌嗪。

公开(公告)号：US09108938B2

公开(公告)日：2015-08-18

申请号：US14050466

申请日：2013-10-10

Applicant: H. Lundbeck A/S

Inventor： John Paul Kilburn ,  Lars Kyhn Rasmussen ,  Mikkel Jessing ,  Eman Mohammed Eldemenky ,  Bin Chen ,  Yu Jiang

IPC: C07D413/06 ,  C07D295/13 ,  C07D401/06 ,  C07D403/06 ,  C07D211/38 ,  C07D213/40 ,  C07D239/26 ,  C07D267/10 ,  C07D209/52

CPC classification number: A61K31/553 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/625 ,  C07D209/52 ,  C07D211/38 ,  C07D213/40 ,  C07D239/26 ,  C07D267/10 ,  C07D295/13 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.

Abstract translation: 本发明涉及抑制P2X7受体的新型环胺。

公开(公告)号：US09101626B2

公开(公告)日：2015-08-11

申请号：US14264373

申请日：2014-04-29

Applicant: H. Lundbeck A/S

Inventor： Andre Faldt ,  Lone Munch Ringgaard ,  Michael J. Mealy ,  Michael Harold Rock ,  Jorgen Brodersen ,  Morten Jorgensen

IPC: C07D295/033 ,  A61K31/495 ,  C07D295/096

CPC classification number: A61K31/495 ,  A61K9/14 ,  C07D295/096 ,  Y10T428/2982

Abstract: This disclosure relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulfanyl) -phenyl]piperazine or a pharmaceutically acceptable salt thereof. The process includes reacting compound II with compound III and compound IV in the presence of a solvent, a base and a palladium catalyst. R, R′, Xi, and X2 in the formulas above are defined in the Specification.

Abstract translation: 本公开涉及1- [2-（2,4-二甲基苯基硫基） - 苯基]哌嗪或其药学上可接受的盐的制备方法。 该方法包括在溶剂，碱和钯催化剂存在下使化合物II与化合物III和化合物IV反应。 上述式中的R，R'，X 1和X 2在本说明书中定义。

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：US09050327B2

公开(公告)日：2015-06-09

申请号：US14054941

申请日：2013-10-16

Applicant: H. Lundbeck A/S

Inventor： Jørgen Eskildsen ,  Anette Graven Sams ,  Ask Püschl

IPC: C07D213/71 ,  C07D239/34 ,  C07D405/12 ,  A61K31/4355 ,  A61K31/44 ,  A61K31/505 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D491/056 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  A61K31/443 ,  A61K31/4433 ,  A61K45/06 ,  A61K31/4427 ,  A61K31/436

CPC classification number: A61K31/44 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/505 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D239/34 ,  C07D405/12 ,  C07D491/056

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

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：US20140371453A1

公开(公告)日：2014-12-18

申请号：US14472896

申请日：2014-08-29

Applicant: H. Lundbeck A/S

Inventor： Andre Faldt ,  Lone Munch Ringgaard ,  Michael J. Mealy ,  Michael Harold Rock ,  Jorgen Brodersen ,  Morten Jorgensen

IPC: C07D295/096

CPC classification number: A61K31/495 ,  A61K9/14 ,  C07D295/096 ,  Y10T428/2982

Abstract: This disclosure relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or a salt thereof.

Abstract translation: 本公开涉及1- [2-（2,4-二甲基苯基硫基） - 苯基]哌嗪或其盐的制备方法。