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：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：US12005054B2

公开(公告)日：2024-06-11

申请号：US17320574

申请日：2021-05-14

Applicant: Takeda Pharmaceutical Company Limited

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

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

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

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：US11045457B2

公开(公告)日：2021-06-29

申请号：US16289311

申请日：2019-02-28

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

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

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

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：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：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.