公开(公告)号：US20180327421A1

公开(公告)日：2018-11-15

申请号：US16041875

申请日：2018-07-23

Applicant: Takeda Pharmaceutical Company Limited

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

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

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：US10077266B2

公开(公告)日：2018-09-18

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: A61K31/4985 ,  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：US20180258073A1

公开(公告)日：2018-09-13

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: A61K31/551 ,  C07D401/04 ,  C07D401/14 ,  C07D241/28

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：US20180072758A1

公开(公告)日：2018-03-15

申请号：US15610382

申请日：2017-05-31

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D498/08 ,  C07D471/08 ,  C07D453/02 ,  C07C53/40 ,  C07C53/18 ,  A61K31/19 ,  A61K31/5386 ,  C07D519/00 ,  C07D471/04 ,  C07D451/12 ,  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 5-HT3 receptor antagonists and are therefore 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：US20170348319A1

公开(公告)日：2017-12-07

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: A61K31/53 ,  C07D253/08

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：US09770452B2

公开(公告)日：2017-09-26

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: A61K31/53 ,  A61K31/5377 ,  C07D241/44 ,  C07D471/04 ,  C07D487/04 ,  C07D405/12 ,  A61K31/197 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  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.

公开(公告)号：US09670229B2

公开(公告)日：2017-06-06

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: C07D519/00 ,  C07D498/08 ,  C07D471/04 ,  C07D451/12 ,  C07D221/22 ,  A61K31/19 ,  A61K31/5386 ,  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 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：US09181249B2

公开(公告)日：2015-11-10

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: A61K31/4965 ,  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，以及用于制备化合物及其中间体的方法。

公开(公告)号：US11426397B2

公开(公告)日：2022-08-30

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

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：US10407443B2

公开(公告)日：2019-09-10

申请号：US16041875

申请日：2018-07-23

Applicant: Takeda Pharmaceutical Company Limited

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

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

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.