公开(公告)号：US08871770B2

公开(公告)日：2014-10-28

申请号：US14171624

申请日：2014-02-03

Applicant: Rigel Pharmaceuticals Inc.

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

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

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.

Abstract translation: 公开了羧酰胺化合物，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 3，R 4，D，J，Z，T，p，q，w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：US08785449B2

公开(公告)日：2014-07-22

申请号：US13622078

申请日：2012-09-18

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/497 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/454 ,  C07D401/14 ,  C07D471/04 ,  C07D401/12 ,  C07D413/14 ,  C07D487/04

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：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：US11174246B2

公开(公告)日：2021-11-16

申请号：US15677809

申请日：2017-08-15

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Simon Shaw ,  Xiang Xu ,  Sarkiz Issakani ,  Rajinder Singh ,  Yasumichi Hitoshi ,  Matthew Duncton ,  Nan Lin

IPC: C07D403/10 ,  A61K31/4184 ,  C07D403/04 ,  C07D235/26 ,  C07D403/12 ,  C07D403/14

Abstract: Disclosed are benzimidazole 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, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.

公开(公告)号：US09353111B2

公开(公告)日：2016-05-31

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

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：US20150011582A1

公开(公告)日：2015-01-08

申请号：US14493050

申请日：2014-09-22

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D471/04

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：US20140148467A1

公开(公告)日：2014-05-29

申请号：US14171624

申请日：2014-02-03

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/14 ,  C07D401/12 ,  C07D471/04 ,  C07D401/14 ,  C07D487/08 ,  C07D417/14

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.

Abstract translation: 公开了羧酰胺化合物，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 3，R 4，D，J，Z，T，p，q，w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：US20140045882A1

公开(公告)日：2014-02-13

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: C07D471/04

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。