公开(公告)号：US20180071271A1

公开(公告)日：2018-03-15

申请号：US15711754

申请日：2017-09-21

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Somasekhar Bhamidipati ,  Jiaxin Yu ,  Ihab Darwish ,  Rajinder Singh

IPC: A61K31/4439 ,  A61K31/41 ,  C07D405/06 ,  C07D403/12 ,  C07D401/04 ,  C07D257/04 ,  C07D405/04

CPC classification number: A61K31/4439 ,  A61K31/41 ,  C07D257/04 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  Y02A50/411 ,  Y02A50/414

Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

公开(公告)号：US20180008589A1

公开(公告)日：2018-01-11

申请号：US15645775

申请日：2017-07-10

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Pingyu Ding ,  Rao Kolluri ,  Ihab Darwish ,  Esteban Masuda ,  Jiaxin Yu

IPC: A61K31/4545 ,  A61K31/519

CPC classification number: A61K31/4545 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.

公开(公告)号：US20160122321A1

公开(公告)日：2016-05-05

申请号：US14993948

申请日：2016-01-12

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Jiaxin Yu ,  Hui Hong ,  Ihab S. Darwish ,  Xiang Xu ,  Rajinder Singh

IPC: C07D401/14

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08

Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

公开(公告)号：US08895578B2

公开(公告)日：2014-11-25

申请号：US14053328

申请日：2013-10-14

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ihab S. Darwish ,  Jiaxin Yu ,  Hui Hong ,  Rajinder Singh ,  Sambaiah Thota ,  Xiang Xu

IPC: A61K31/454 ,  A61K31/437 ,  C07D471/04 ,  C07D401/06 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract translation: 公开了羧酰胺，磺酰胺和胺化合物，以及药物组合物和使用方法。 一个实施方案是具有其中R 1，R 2，R 4，D，E，J，T，p，q和x如本文所述的结构的化合物。 在某些实施方案中，本文公开的化合物激活AMPK途径，并且可用于治疗与代谢有关的病症和病症。

公开(公告)号：US11919890B2

公开(公告)日：2024-03-05

申请号：US17210261

申请日：2021-03-23

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vanessa Taylor ,  Jiaxin Yu ,  Esteban Masuda ,  Ihab Darwish ,  Yan Chen

IPC: C07D413/12 ,  A61K31/553 ,  A61P29/00 ,  A61P37/02 ,  C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

CPC classification number: C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US11578078B2

公开(公告)日：2023-02-14

申请号：US17091270

申请日：2020-11-06

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Jiaxin Yu ,  Simon Shaw ,  Ihab Darwish ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  Zhushou Luo ,  Rao Kolluri

IPC: C07D223/16 ,  A61K31/55 ,  C07D491/107 ,  A61P39/00 ,  C07D401/14 ,  C07D403/14 ,  C07D471/08 ,  C07D471/10

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula I The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20210214347A1

公开(公告)日：2021-07-15

申请号：US17210261

申请日：2021-03-23

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vanessa Taylor ,  Jiaxin Yu ,  Esteban Masuda ,  Ihab Darwish ,  Yan Chen

IPC: C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20210139494A1

公开(公告)日：2021-05-13

申请号：US17091270

申请日：2020-11-06

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Jiaxin Yu ,  Simon Shaw ,  Ihab Darwish ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  Zhushou Luo ,  Rao Kolluri

IPC: C07D491/107 ,  A61P39/00 ,  C07D471/10 ,  C07D471/08 ,  C07D403/14 ,  C07D401/14

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula I The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US10975064B2

公开(公告)日：2021-04-13

申请号：US16402103

申请日：2019-05-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vanessa Taylor ,  Jiaxin Yu ,  Esteban Masuda ,  Ihab Darwish ,  Yan Chen

IPC: A61K31/553 ,  C07D413/12 ,  C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US10851093B2

公开(公告)日：2020-12-01

申请号：US16424619

申请日：2019-05-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ihab Darwish ,  Jiaxin Yu ,  Rao Kolluri ,  Sacha Holland

IPC: C07D215/00 ,  C07D413/14 ,  C07D417/14 ,  C07D491/107 ,  C07D453/00

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, X, Y1, Y2, Y3 and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.