公开(公告)号：US08754217B2

公开(公告)日：2014-06-17

申请号：US13926427

申请日：2013-06-25

Applicant: H. Lundbeck A/S ,  Biotie Therapies Corp.

Inventor： Heidi Lopez de Diego ,  Carla De Faveri ,  Florian Anton Martin Huber

IPC: C07D489/08

CPC classification number: C07D489/08

Abstract: The present invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment comprising administering Nalmefene hydrochloride dihydrate.

Abstract translation: 本发明涉及盐酸纳美芬二氢盐，盐酸纳美芬酸二水合物的制备方法，包含盐酸纳美芬二水合物的药物组合物和包括给予盐酸纳美芬二水合物的方法。

公开(公告)号：US11332478B2

公开(公告)日：2022-05-17

申请号：US16828141

申请日：2020-03-24

Applicant: H. Lundbeck A/S

Inventor： Carla De Faveri ,  Florian Anton Martin Huber

IPC: C07D498/04 ,  C07D491/113 ,  C07D211/78 ,  C07C269/04 ,  C07C227/22 ,  C07C227/18 ,  C07C249/02 ,  C07C271/22 ,  C07C229/08

Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.

公开(公告)号：US09975850B2

公开(公告)日：2018-05-22

申请号：US15480647

申请日：2017-04-06

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Florian Anton Martin Huber

IPC: C07D209/14 ,  B01D3/36

CPC classification number: C07D209/14 ,  B01D3/36 ,  C07D209/16

Abstract: The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof:

公开(公告)号：US20210147366A1

公开(公告)日：2021-05-20

申请号：US17045045

申请日：2019-04-05

Applicant: H. Lundbeck A/S

Inventor： Carla De Faveri ,  Florian Anton Martin Huber ,  Mariano Stivanello

IPC: C07D241/04 ,  B01J23/44

Abstract: This invention relates to a novel chemical process for the synthesis of 2,2-dimethylpiperazine and the further transformation of 2,2-dimethylpiperazine into ferf-butyl-3,3-dimethylpiperazine-1-carboxylate-hemi-DL-tartrate.

公开(公告)号：US20200223865A1

公开(公告)日：2020-07-16

申请号：US16828141

申请日：2020-03-24

Applicant: H. Lundbeck A/S

Inventor： Carla De Faveri ,  Florian Anton Martin Huber

IPC: C07D498/04 ,  C07C269/04 ,  C07C271/22 ,  C07C227/22 ,  C07D211/78 ,  C07C227/18 ,  C07C249/02 ,  C07C229/08 ,  C07D491/113

Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.

公开(公告)号：US20180065984A1

公开(公告)日：2018-03-08

申请号：US15559630

申请日：2016-03-22

Applicant: H. Lundbeck A/S

Inventor： Carla De Faveri ,  Florian Anton Martin Huber

IPC: C07D498/04 ,  C07D211/78 ,  C07D491/113 ,  C07C227/18 ,  C07C227/22 ,  C07C249/02 ,  C07C269/04 ,  C07C271/22

CPC classification number: C07D498/04 ,  C07C227/18 ,  C07C227/22 ,  C07C229/08 ,  C07C249/02 ,  C07C269/04 ,  C07C271/22 ,  C07D211/78 ,  C07D491/113 ,  C07C251/04 ,  C07C229/16

Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.

公开(公告)号：US20170291874A1

公开(公告)日：2017-10-12

申请号：US15480647

申请日：2017-04-06

Applicant: H. Lundbeck A/S

Inventor： Mikkel Fog Jacobsen ,  Florian Anton Martin Huber

IPC: C07D209/14

CPC classification number: C07D209/14 ,  B01D3/36 ,  C07D209/16

Abstract: The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof: