公开(公告)号：US20180155283A1

公开(公告)日：2018-06-07

申请号：US15537741

申请日：2015-12-18

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Luka Dordevic ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D207/12 ,  C07D211/18 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  A61P25/16 ,  A61P25/18

CPC分类号： C07D207/12 ,  A61P25/16 ,  A61P25/18 ,  C07D211/18 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07K14/70571

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and/or on the cAMP pathway.

公开(公告)号：US20230143552A1

公开(公告)日：2023-05-11

申请号：US17962346

申请日：2022-10-07

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Luka Dordevic ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D207/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D211/18 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D211/22 ,  A61P25/18 ,  A61P25/16

CPC分类号： C07D207/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D211/18 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D211/22 ,  A61P25/18 ,  A61P25/16 ,  C07K14/70571

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

公开(公告)号：US20210147355A1

公开(公告)日：2021-05-20

申请号：US16826028

申请日：2020-03-20

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Luka Dordevic ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D207/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D211/18 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D211/22 ,  A61P25/18 ,  A61P25/16

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

公开(公告)号：US20190023656A1

公开(公告)日：2019-01-24

申请号：US15537738

申请日：2015-12-18

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D211/26 ,  A61P25/00 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

公开(公告)号：US11498896B2

公开(公告)日：2022-11-15

申请号：US16826028

申请日：2020-03-20

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Luka Dordevic ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D405/06 ,  A61K31/453 ,  C07D207/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/06 ,  C07D471/10 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D211/18 ,  C07D211/38 ,  C07D211/42 ,  C07D211/48 ,  C07D211/58 ,  C07D211/62 ,  C07D211/70 ,  C07D211/22 ,  A61P25/18 ,  A61P25/16 ,  C07K14/705

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

公开(公告)号：US20220211658A1

公开(公告)日：2022-07-07

申请号：US17610130

申请日：2020-05-08

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Zhanyan Fu ,  Jennifer Q. Pan ,  Ayan Ghoshal ,  Guoping Feng ,  Edward Scolnick

IPC分类号： A61K31/343 ,  A61K31/381 ,  A61K45/06 ,  A61P25/20

摘要： Provided herein are methods for treating a disorder associated with a sleep spindle deficit using a group II metabotropic glutamate receptor modulator.

公开(公告)号：US10752588B2

公开(公告)日：2020-08-25

申请号：US15537738

申请日：2015-12-18

申请人： The Broad Institute, Inc. ,  Massachusetts Institute of Technology

发明人： Edward Holson ,  Florence Fevrier ,  Michel Weiwer ,  Edward Scolnick ,  Michelle Palmer ,  Michael C. Lewis ,  Jennifer Q. Pan ,  Yan-Ling Zhang ,  Qihong Xu

IPC分类号： C07D211/26 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D471/10 ,  C07D211/62 ,  A61P25/00

摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.

公开(公告)号：US11052080B2

公开(公告)日：2021-07-06

申请号：US16198589

申请日：2018-11-21

申请人： The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc. ,  The General Hospital Corporation

发明人： Florence Fevrier Wagner ,  Jennifer Q. Pan ,  Sivaraman Dandapani ,  Andrew Germain ,  Edward Holson ,  Benito Munoz ,  Partha P. Nag ,  Michael C. Lewis ,  Stephen J. Haggarty ,  Joshua A. Bishop ,  Kimberly Stegmaier ,  Michel Weiwer ,  Versha Banerji

IPC分类号： C07D471/04 ,  C07D471/10 ,  A61K31/4745 ,  A61K31/4747

摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.

公开(公告)号：US20220160702A1

公开(公告)日：2022-05-26

申请号：US17344830

申请日：2021-06-10

申请人： The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc. ,  The General Hospital Corporation d/b/a Massachusetts General Hospital

发明人： Florence Fevrier Wagner ,  Jennifer Q. Pan ,  Sivaraman Dandapani ,  Andrew Germain ,  Edward Holson ,  Benito Munoz ,  Partha P. Nag ,  Michael C. Lewis ,  Stephen J. Haggarty ,  Joshua A. Bishop ,  Kimberly Stegmaier ,  Michel Weiwer ,  Versha Banerji

IPC分类号： A61K31/4745 ,  C07D471/04 ,  C07D471/10 ,  A61K31/4747

摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.

公开(公告)号：US20190175584A1

公开(公告)日：2019-06-13

申请号：US16198589

申请日：2018-11-21

申请人： The Broad Institute, Inc. ,  Dana-Farber Cancer Institute, Inc. ,  The General Hospital Corporation d/b/a Massachusetts General Hospital

发明人： Florence Fevrier Wagner ,  Jennifer Q. Pan ,  Sivaraman Dandapani ,  Andrew Germain ,  Edward Holson ,  Benito Munoz ,  Partha P. Nag ,  Michael C. Lewis ,  Stephen J. Haggarty ,  Joshua A. Bishop ,  Kimberly Stegmaier ,  Michel Weiwer ,  Versha Banerji

IPC分类号： A61K31/4745 ,  C07D471/04 ,  A61K31/4747 ,  C07D471/10

摘要： The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3α or GSK3β) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.