公开(公告)号：US11059798B2

公开(公告)日：2021-07-13

申请号：US16672870

申请日：2019-11-04

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: C07D295/073 ,  C07B59/00 ,  C07D241/04 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07C45/61 ,  C07C45/67

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

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：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。

公开(公告)号：US09012453B2

公开(公告)日：2015-04-21

申请号：US13924849

申请日：2013-06-24

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: A61K31/497 ,  C07D295/00 ,  C07D295/073 ,  C07B59/00 ,  C07D241/04 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554

CPC classification number: C07D295/073 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07B59/002 ,  C07B2200/05 ,  C07C45/61 ,  C07C45/67 ,  C07D241/04

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

Abstract translation: 本发明涉及在多巴胺受体D1和D2以及中枢神经系统中的5HT2受体具有活性的氘代1-哌嗪基-3-苯基 - 茚并及其盐，包括这些化合物作为活性成分的药物 的这种化合物在治疗中枢神经系统中的疾病，以及包括施用这些化合物的治疗方法。

公开(公告)号：US09095588B2

公开(公告)日：2015-08-04

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: C07D295/033 ,  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 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′, X1, 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：US09617231B2

公开(公告)日：2017-04-11

申请号：US14941800

申请日：2015-11-16

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: C07D295/073 ,  C07B59/00 ,  C07D241/04 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07C45/61 ,  C07C45/67

CPC classification number: C07D295/073 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07B59/002 ,  C07B2200/05 ,  C07C45/61 ,  C07C45/67 ,  C07D241/04

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

公开(公告)号：US20140256943A1

公开(公告)日：2014-09-11

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: C07D295/096

CPC classification number: A61K31/495 ,  A61K9/14 ,  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：US12116355B2

公开(公告)日：2024-10-15

申请号：US17340201

申请日：2021-06-07

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: C07D295/073 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07B59/00 ,  C07C45/61 ,  C07C45/67 ,  C07D241/04

CPC classification number: C07D295/073 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07B59/002 ,  C07C45/61 ,  C07C45/67 ,  C07D241/04 ,  C07B2200/05

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

公开(公告)号：US10118907B2

公开(公告)日：2018-11-06

申请号：US15435826

申请日：2017-02-17

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: C07D295/073 ,  C07B59/00 ,  C07D241/04 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07C45/61 ,  C07C45/67

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

公开(公告)号：US09216961B2

公开(公告)日：2015-12-22

申请号：US14656925

申请日：2015-03-13

Applicant: H. Lundbeck A/S

Inventor： Morten Jorgensen ,  Peter Hongaard Andersen ,  Klaus Gjervig Jensen

IPC: C07D295/073 ,  C07D241/04 ,  C07C45/67 ,  C07C45/61

CPC classification number: C07D295/073 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/519 ,  A61K31/551 ,  A61K31/554 ,  C07B59/002 ,  C07B2200/05 ,  C07C45/61 ,  C07C45/67 ,  C07D241/04

Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.