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：US20200061041A1

公开(公告)日：2020-02-27

申请号：US16289311

申请日：2019-02-28

Applicant: Zacharia Cheruvallath ,  Jason Green ,  Ben Johnson ,  Kristin Schleicher ,  Huikai Sun ,  Mingnam Tang ,  Takeda Pharmaceutical Company Limited

Inventor： Zacharia Cheruvallath ,  Jason Green ,  Ben Johnson ,  Kristin Schleicher ,  Huikai Sun ,  Mingnam Tang

IPC: A61K31/4439 ,  C07D401/12 ,  A61K31/4545 ,  C07D403/12 ,  A61K31/506 ,  C07D401/14 ,  A61K31/40 ,  C07D207/14 ,  C07D211/58 ,  A61K31/4468 ,  A61K31/501 ,  A61K31/497 ,  A61K31/4355 ,  C07D491/048 ,  A61K31/438

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6, R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 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 SSTR4.

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.

公开(公告)号：US10406157B2

公开(公告)日：2019-09-10

申请号：US16009308

申请日：2018-06-15

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 ,  A61K45/06 ,  C07D487/04 ,  A61P9/00 ,  A61P25/16

Abstract: Disclosed is a compound of Formula 1, and a pharmaceutically acceptable salt thereof. This disclosure also relates to materials and methods for preparing the compound of Formula 1, to pharmaceutical compositions which contain it, and to its use for treating diseases, disorders, and conditions associated with GPR6.

公开(公告)号：US20180360831A1

公开(公告)日：2018-12-20

申请号：US16009308

申请日：2018-06-15

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 ,  A61K45/06 ,  A61P25/16 ,  A61P9/00 ,  C07D487/04

CPC classification number: A61K31/4985 ,  A61K45/06 ,  A61P9/00 ,  A61P25/16 ,  C07D487/04

Abstract: Disclosed is a compound of Formula 1, and a pharmaceutically acceptable salt thereof. This disclosure also relates to materials and methods for preparing the compound of Formula 1, to pharmaceutical compositions which contain it, and to its use for treating diseases, disorders, and conditions associated with GPR6.

公开(公告)号：US20180346464A1

公开(公告)日：2018-12-06

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：US10125145B2

公开(公告)日：2018-11-13

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 ,  C07D451/12 ,  C07D471/04 ,  C07D519/00 ,  A61K31/19 ,  A61K31/5386 ,  C07D221/22 ,  C07D453/02 ,  C07C53/40 ,  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.

公开(公告)号：US20160185801A1

公开(公告)日：2016-06-30

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: C07D519/00 ,  C07D498/08 ,  C07D471/08 ,  C07C53/40 ,  C07D453/02

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.