公开(公告)号：US11173161B2

公开(公告)日：2021-11-16

申请号：US16732536

申请日：2020-01-02

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard

IPC: A61K31/53 ,  A61P25/18 ,  C07D253/08

Abstract: The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

公开(公告)号：US10738046B2

公开(公告)日：2020-08-11

申请号：US16057350

申请日：2018-08-07

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Jason W. Brown ,  Stephen Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Holger Monenschein ,  Holly Reichard ,  Kristin Schleicher ,  Huikai Sun ,  Todd Macklin

IPC: C07D471/04

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

公开(公告)号：US10273225B2

公开(公告)日：2019-04-30

申请号：US15979069

申请日：2018-05-14

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Mark E. Adams ,  Jason W. Brown ,  Stephen Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun

IPC: C07D401/04 ,  C07D401/14 ,  C07D241/26 ,  C07D241/28 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

公开(公告)号：US10179783B2

公开(公告)日：2019-01-15

申请号：US15118447

申请日：2015-02-13

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Todd Macklin

IPC: C07D471/04

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

公开(公告)号：US09695195B2

公开(公告)日：2017-07-04

申请号：US15064407

申请日：2016-03-08

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: C07D471/04 ,  C07D519/00 ,  C07D498/04 ,  A61K31/537 ,  C07D498/08 ,  C07D451/12 ,  A61K31/19 ,  A61K31/5386 ,  C07D221/22 ,  C07C53/40 ,  C07D453/02 ,  C07D471/08 ,  C07C53/18

CPC classification number: C07D498/08 ,  A61K31/19 ,  A61K31/5386 ,  C07C53/18 ,  C07C53/40 ,  C07D221/22 ,  C07D451/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00

Abstract: The present invention provides compounds of the formula: that are 5HT3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20170095480A1

公开(公告)日：2017-04-06

申请号：US15382490

申请日：2016-12-16

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard

IPC: A61K31/53

CPC classification number: A61K31/53 ,  C07D253/08

Abstract: The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

公开(公告)号：US20170035775A1

公开(公告)日：2017-02-09

申请号：US15334198

申请日：2016-10-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: A61K31/5377 ,  A61K31/5025 ,  A61K31/197 ,  A61K31/4985 ,  A61K31/498 ,  A61K45/06

CPC classification number: A61K31/5377 ,  A61K31/197 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06 ,  C07D241/44 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): that are GPR6 modulators and are therefore useful for the treatment of diseases treatable by modulation of GPR6, in particular treating Parkinson disease, levodopa induced dyskinesias, Huntington's disease, other dyskinesias, akinesias, and motor disorders involving dysfunction of the striatum, schizophrenia and drug addiction. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 这是GPR6调节剂，因此可用于治疗通过调节GPR6可治疗的疾病，特别是治疗帕金森病，左旋多巴诱导的运动障碍，亨廷顿病，其他运动障碍，运动障碍和涉及纹状体功能障碍的运动障碍，精神分裂症和药物成瘾 。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。

公开(公告)号：US20160251373A1

公开(公告)日：2016-09-01

申请号：US15150013

申请日：2016-05-09

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: C07D498/08 ,  C07C53/18

CPC classification number: C07D498/08 ,  A61K31/19 ,  A61K31/5386 ,  C07C53/18 ,  C07C53/40 ,  C07D221/22 ,  C07D451/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00

Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 本发明提供式（I）的5-HT 3受体拮抗剂：其可用于治疗通过抑制5-HT 3受体如呕吐，疼痛，药物成瘾，神经变性和精神疾病以及GI障碍而可治疗的疾病。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。

公开(公告)号：US10561662B2

公开(公告)日：2020-02-18

申请号：US16179709

申请日：2018-11-02

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard

IPC: C07D253/08 ,  A61K31/53 ,  A61P25/18

Abstract: The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

公开(公告)号：US20190070187A1

公开(公告)日：2019-03-07

申请号：US16179709

申请日：2018-11-02

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Betty Lam ,  Holger Monenschein ,  Holly Reichard

IPC: A61K31/53 ,  C07D253/08

Abstract: The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.