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公开(公告)号：US11274096B2
公开(公告)日：2022-03-15
申请号：US16961109
申请日：2019-01-10
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Debra Jane Wallace , Fenger Zhou , Yuguang Wang , Takashi Nakai , Vishnu Vardhan Reddy Karnati , Wayne C. Schairer , William Kissel , Song Xue , Ahmad Hashash
IPC: C07D413/14 , C07D403/04 , C07D413/12
Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as simulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said simulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.
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公开(公告)号：US20220017515A1
公开(公告)日：2022-01-20
申请号：US17485858
申请日：2021-09-27
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Glen Robert Rennie , Timothy Claude Barden , Thomas Wai-Ho Lee , Rajesh R. Iyengar , Takashi Nakai , Ara Mermerian , Lei Jia , Karthik Iyer , G-Yoon Jamie Im , Paul Allan Renhowe , Joon Jung , Peter Germano , Kim Tang
IPC: C07D471/04 , C07D403/04 , C07D403/14 , C07D487/04
Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula I:
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公开(公告)号：US11180493B2
公开(公告)日：2021-11-23
申请号：US16348377
申请日：2017-11-07
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Glen Robert Rennie , Timothy Claude Barden , Thomas Wai-Ho Lee , Rajesh R. Iyengar , Takashi Nakai , Ara Mermerian , Lei Jia , Karthik Iyer , G-Yoon Jamie Im , Paul Allan Renhowe , Joon Jung , Peter Germano , Kim Tang
IPC: C07D471/04 , C07D403/04 , C07D403/14 , C07D487/04
Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula (I).
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4.发明公开
公开(公告)号：US20230339928A1
公开(公告)日：2023-10-26
申请号：US18140966
申请日：2023-04-28
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Debra Jane Wallace , Fenger Zhou , Yuguang Wang , Takashi Nakai , Vishnu Vardhan Reddy Karnati , Wayne C. Schairer , William Kissel , Song Xue , Ahmad Hashash
IPC: C07D413/14 , C07D403/04 , C07D413/12
CPC classification number: C07D413/14 , C07D403/04 , C07D413/12 , C07B2200/13
Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.
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5.发明申请
公开(公告)号：US20220024909A1
公开(公告)日：2022-01-27
申请号：US17497352
申请日：2021-10-08
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Debra Jane Wallace , Fenger Zhou , Yuguang Wang , Takashi Nakai , Vishnu Vardhan Reddy Karnati , Wayne C. Schairer , William Kissel , Song Xue , Ahmad Hashash
IPC: C07D413/14 , C07D403/04 , C07D413/12
Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.
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公开(公告)号：US11207323B2
公开(公告)日：2021-12-28
申请号：US16817830
申请日：2020-03-13
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Takashi Nakai , Joel Moore , Nicholas Robert Perl , Rajesh R. Iyengar , Ara Mermerian , G-Yoon Jamie Im , Thomas Wai-Ho Lee , Colleen Hudson , Glen Robert Rennie , Lei Jia , Paul Allan Renhowe , Timothy Claude Barden , Xiang Y. Yu , James Edward Sheppeck , Karthik Iyer , Joon Jung , George Todd Milne , Kimberly Kafadar Long , Mark G. Currie
IPC: A61K31/506 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D403/04 , C07D487/10 , C07D491/107 , C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D401/14 , C07D471/08 , C07D471/10 , A61K45/06 , C07D451/02 , A61K31/519
Abstract: Compounds of Formulae I′ and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
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公开(公告)号：US20210214364A1
公开(公告)日：2021-07-15
申请号：US17122542
申请日：2020-12-15
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Paul Allan Renhowe , James Edward Sheppeck , Takashi Nakai , Karthik Iyer , Nicholas Robert Perl , Glen Robert Rennie , Mark G. Currie , Kimberly Kafadar Long , George Todd Milne , Rajesh R. Iyengar
IPC: C07D487/04 , C07D405/14 , C07D405/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14
Abstract: The present patent application discloses at least the compounds according to Formula l shown below, or pharmaceutically acceptable salts thereof, wherein ringjB,n, JD, J,0, X, X1, J, RC, and W are as defined herein. These compounds are useful as simulators of soluble sGC.
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公开(公告)号：US20200316065A1
公开(公告)日：2020-10-08
申请号：US16817830
申请日：2020-03-13
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Takashi Nakai , Joel Moore , Nicholas Robert Perl , Rajesh R. Iyengar , Ara Mermerian , G-Yoon Jamie Im , Thomas Wai-Ho Lee , Colleen Hudson , Glen Robert Rennie , Lei Jia , Paul Allan Renhowe , Timothy Claude Barden , Xiang Y. Yu , James Edward Sheppeck , Karthik Iyer , Joon Jung , George Todd Milne , Kimberly Kafadar Long , Mark G. Currie
IPC: A61K31/506 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D403/04 , C07D487/10 , C07D491/107 , C07D498/04 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D401/14 , C07D471/08 , C07D471/10 , A61K45/06 , C07D451/02
Abstract: Compounds of Formulae I′ and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
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公开(公告)号：US20240228520A9
公开(公告)日：2024-07-11
申请号：US18241630
申请日：2023-09-01
Applicant: Cyclerion Therapeutics, Inc.
Inventor： James Edward Sheppeck , Paul Allan Renhowe , Ara Mermerian , Timothy Claude Barden , Glen Robert Rennie , Rajesh R. Iyengar , Takashi Nakai
IPC: C07F9/6558 , A61P3/00 , A61P9/10 , A61P9/12 , A61P25/28
CPC classification number: C07F9/65583 , A61P3/00 , A61P9/10 , A61P9/12 , A61P25/28 , C07F9/65586
Abstract: The present patent application discloses the compounds according to Formula I shown below, or pharmaceutically acceptable salts thereof, wherein JB, n, R1, R2, R3, R4, R5, m and X as defined herein.
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10.发明授权
公开(公告)号：US11708361B2
公开(公告)日：2023-07-25
申请号：US17497352
申请日：2021-10-08
Applicant: Cyclerion Therapeutics, Inc.
Inventor： Debra Jane Wallace , Fenger Zhou , Yuguang Wang , Takashi Nakai , Vishnu Vardhan Reddy Karnati , Wayne C. Schairer , William Kissel , Song Xue , Ahmad Hashash
IPC: C07D413/14 , C07D403/04 , C07D413/12
CPC classification number: C07D413/14 , C07D403/04 , C07D413/12 , C07B2200/13
Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.
