公开(公告)号：US20200375969A1

公开(公告)日：2020-12-03

申请号：US16497967

申请日：2018-03-26

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Jason Green ,  Maria Hopkins ,  Benjamin Jones ,  Andre A. Kiryanov ,  Jon Kuehler ,  Holger Monenschein ,  Sean Murphy ,  Thomas Nixey ,  Huikai Sun

IPC: A61K31/4545 ,  A61K31/198 ,  A61K31/454 ,  A61K31/451 ,  A61K31/506 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/553 ,  A61K31/4535 ,  A61K31/519 ,  A61K31/501 ,  A61K31/5365 ,  C07D401/12 ,  C07D211/52 ,  C07D401/14 ,  C07D405/12 ,  C07D498/04 ,  C07D413/12 ,  C07D409/12 ,  C07D487/04 ,  C07D417/12

Abstract: Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R4, R5, R8, R10, R11, X1, X2, X3, X9, X12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.

公开(公告)号：US20170260201A1

公开(公告)日：2017-09-14

申请号：US15599239

申请日：2017-05-18

Applicant: Takeda Pharmaceutical Company Limited

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

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

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.

公开(公告)号：US09556130B2

公开(公告)日：2017-01-31

申请号：US14946194

申请日：2015-11-19

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D253/08 ,  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.

Abstract translation: 本发明提供了使用式1化合物治疗与GPR139相关的疾病，病症或病症的方法：其为GPR139的激动剂，式1所涵盖的某些化合物，其药物组合物，制备该化合物的方法及其中间体。

公开(公告)号：US20160145218A1

公开(公告)日：2016-05-26

申请号：US14946194

申请日：2015-11-19

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D253/08 ,  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.

Abstract translation: 本发明提供了使用式1化合物治疗与GPR139相关的疾病，病症或病症的方法：其为GPR139的激动剂，式1所涵盖的某些化合物，其药物组合物，制备该化合物的方法及其中间体。

公开(公告)号：US09303045B2

公开(公告)日：2016-04-05

申请号：US14415712

申请日：2013-07-16

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D471/04 ,  C07D498/04 ,  A61K31/537 ,  C07D519/00 ,  C07D498/08 ,  C07D451/12 ,  A61K31/19 ,  A61K31/5386 ,  C07D221/22

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.

Abstract translation: 本发明提供下式的化合物：其为5HT3受体拮抗剂，因此可用于治疗通过抑制5HT3受体如呕吐，疼痛，药物成瘾，神经变性和精神病症以及胃肠疾病而可治疗的疾病。 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：US10159677B2

公开(公告)日：2018-12-25

申请号：US15683589

申请日：2017-08-22

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：US10000468B2

公开(公告)日：2018-06-19

申请号：US15118461

申请日：2015-02-13

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: C07D401/14 ,  C07D241/28 ,  C07D401/04

CPC classification number: C07D401/14 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04

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：US20170283414A1

公开(公告)日：2017-10-05

申请号：US15621761

申请日：2017-06-13

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

CPC classification number: 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：US09770450B2

公开(公告)日：2017-09-26

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 ,  C07D253/08 ,  A61P25/18

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：US20150175602A1

公开(公告)日：2015-06-25

申请号：US14577480

申请日：2014-12-19

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D471/04

CPC classification number: 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.

Abstract translation: 本发明提供式I化合物：其可用作GPR6的调节剂，其药物组合物，用于治疗与GPR6相关的病症的方法，用于制备化合物的方法及其中间体。