公开(公告)号：US20140051673A1

公开(公告)日：2014-02-20

申请号：US14053325

申请日：2013-10-14

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/14 ,  C07D409/14 ,  C07D405/14 ,  C07D401/12 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D211/46 ,  C07D211/58 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

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, E, T, n 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，E，T，n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：US11672791B2

公开(公告)日：2023-06-13

申请号：US17465662

申请日：2021-09-02

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D471/04 ,  A61K31/4545 ,  C07D519/00 ,  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：US11667643B2

公开(公告)日：2023-06-06

申请号：US17358698

申请日：2021-06-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Simon Shaw ,  Ihab Darwish ,  Jiaxin Yu ,  Rao Kolluri ,  Vanessa Taylor ,  Esteban Masuda ,  Mark Irving

IPC: A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/22 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/22 ,  C07D513/14 ,  C07D519/00

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 treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US11407736B2

公开(公告)日：2022-08-09

申请号：US17012779

申请日：2020-09-04

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/5517 ,  A61K31/54 ,  C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  A61K31/553 ,  C07D267/02 ,  C07D413/12 ,  C07D413/14 ,  C07D493/04

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 treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20210078990A1

公开(公告)日：2021-03-18

申请号：US17105334

申请日：2020-11-25

Applicant: Rigel Pharmaceuticals, Inc.

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

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

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.

公开(公告)号：US10889562B2

公开(公告)日：2021-01-12

申请号：US16991368

申请日：2020-08-12

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Jiaxin Yu ,  Beth Fernandez ,  Gary Park ,  Ihab Darwish

IPC: C07D401/04 ,  C07D257/04 ,  C07C323/60 ,  C07D249/12 ,  A61P37/02

Abstract: Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.

公开(公告)号：US10822337B2

公开(公告)日：2020-11-03

申请号：US15563075

申请日：2016-03-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US20190099411A1

公开(公告)日：2019-04-04

申请号：US16151959

申请日：2018-10-04

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/4545 ,  C07D519/00 ,  A61K31/519 ,  C07D471/04

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：US09801866B2

公开(公告)日：2017-10-31

申请号：US15269233

申请日：2016-09-19

Applicant: RIGEL PHARMACEUTICALS, INC.

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

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

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

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：US20170065569A1

公开(公告)日：2017-03-09

申请号：US15269233

申请日：2016-09-19

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: A61K31/4439 ,  A61K31/41

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

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.

Abstract translation: 本公开的方面包括可用于治疗多种自身免疫性和炎性疾病和病症的化合物。 本公开的实施方案还涉及包括这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。