公开(公告)号：US20190389836A1

公开(公告)日：2019-12-26

申请号：US16481772

申请日：2018-01-29

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Michael Dechantsreiter ,  Istvan Enyedy ,  John H. Jones ,  Edward Yin-Shiang Lin ,  Brian Stuart Lucas ,  Bin Ma

IPC: C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D215/14 ,  C07D405/14 ,  C07D471/04 ,  C07D451/02

Abstract: Provided are tetrahydroisoquinoline derivatives as Nrf2 activators.

公开(公告)号：US20240279197A1

公开(公告)日：2024-08-22

申请号：US18545312

申请日：2023-12-19

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Edward Yin Shiang Lin ,  Brian Stuart Lucas

IPC: C07D311/74

CPC classification number: C07D311/74

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, which are activators of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) and are useful to treat diseases caused by oxidative stress, such as neurodegenerative diseases or inflammation. Also provided are methods for their use and production.

公开(公告)号：US11465963B2

公开(公告)日：2022-10-11

申请号：US16765614

申请日：2018-11-20

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Edward Yin Shiang Lin ,  Brian Stuart Lucas

IPC: C07C255/47 ,  C07D317/72

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production.

公开(公告)号：US20220112216A1

公开(公告)日：2022-04-14

申请号：US17507922

申请日：2021-10-22

Applicant: The Broad Institute, Inc. ,  Biogen MA Inc.

Inventor： Florence Fevrier Wagner ,  Michel Weiwer ,  Arthur J. Campbell ,  Joshua R. Sacher ,  Edward Holson ,  Brian Stuart Lucas ,  TeYu Chen

IPC: C07D513/04 ,  C07D498/04 ,  C07D513/20

Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).

公开(公告)号：US11203601B2

公开(公告)日：2021-12-21

申请号：US16603112

申请日：2018-04-05

Applicant: The Broad Institute, Inc. ,  Biogen MA Inc.

Inventor： Florence Fevrier Wagner ,  Michel Weiwer ,  Arthur J. Campbell ,  Joshua R. Sacher ,  Edward Holson ,  Brian Stuart Lucas ,  TeYu Chen

IPC: C07D513/04 ,  C07D498/04 ,  C07D513/20 ,  A61K45/06

Abstract: The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).

公开(公告)号：US20210387960A1

公开(公告)日：2021-12-16

申请号：US17333498

申请日：2021-05-28

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Edward Yin Shiang Lin ,  Brian Stuart Lucas

IPC: C07D311/74

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, which are activators of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) and are useful to treat diseases caused by oxidative stress, such as neurodegenerative diseases or inflammation. Also provided are methods for their use and production.

公开(公告)号：US20200299230A1

公开(公告)日：2020-09-24

申请号：US16765614

申请日：2018-11-21

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Edward Yin Shiang Lin ,  Brian Stuart Lucas

IPC: C07C255/47 ,  C07D317/72

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production.

公开(公告)号：US20210340107A1

公开(公告)日：2021-11-04

申请号：US17221358

申请日：2021-04-02

Applicant: BIOGEN MA INC.

Inventor： Brian Stuart Lucas ,  Edward Yin Shiang Lin ,  Andrew George Capacci ,  Zhili Xin ,  Istvan Enyedy ,  TeYu Chen ,  John H. Jones ,  Kurt D. van Vloten

IPC: C07D217/04 ,  C07D217/08 ,  C07D217/20 ,  C07D217/22 ,  C07D223/14 ,  C07D311/74 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D498/04

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.

公开(公告)号：US10968181B2

公开(公告)日：2021-04-06

申请号：US16473667

申请日：2017-12-27

Applicant: BIOGEN MA INC.

Inventor： Brian Stuart Lucas ,  Edward Yin-Shiang Lin ,  Andrew George Capacci ,  Zhili Xin ,  Istvan Enyedy ,  TeYu Chen ,  John H. Jones ,  Kurt D. van Vloten

IPC: C07D311/76 ,  C07D217/04 ,  C07D217/08 ,  C07D223/16 ,  C07D498/14 ,  A61K31/352 ,  A61K31/47 ,  C07D217/20 ,  C07D217/22 ,  C07D223/14 ,  C07D311/74 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06 ,  C07D498/04

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.

公开(公告)号：US20190389830A1

公开(公告)日：2019-12-26

申请号：US16481743

申请日：2018-01-26

Applicant: BIOGEN MA INC.

Inventor： Andrew George Capacci ,  Edward Yin-Shiang Lin ,  Brian Stuart Lucas

IPC: C07D311/74

Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, which are activators of nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) and are useful to treat diseases caused by oxidative stress, such as neurodegenerative diseases or inflammation. Also provided are methods for their use and production.