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：US09255085B2

公开(公告)日：2016-02-09

申请号：US14705742

申请日：2015-05-06

Applicant: Rigel Pharmaceuticals, Inc.

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

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

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：US20150232451A1

公开(公告)日：2015-08-20

申请号：US14705742

申请日：2015-05-06

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/14 ,  C07D401/12

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：US20140179738A1

公开(公告)日：2014-06-26

申请号：US14189638

申请日：2014-02-25

Applicant: Rigel Pharmaceuticals, Inc.

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

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

CPC classification number: C07D401/12 ,  C07D211/58 ,  C07D211/96 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract translation: 本发明提供N-取代的 - 杂环烷氧基苯甲酰胺化合物，以及药物组合物和使用方法。 本发明的一个实施方案是具有其中R 1，R 2，R 3，R 4，T，n，w和x如本文所述的结构的化合物。 在本发明的某些实施方案中，本发明的化合物激活AMPK途径，并且可用于治疗与代谢相关的病症和病症。

公开(公告)号：US20180051006A1

公开(公告)日：2018-02-22

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: C07D403/04 ,  C07D235/26 ,  C07D403/14 ,  C07D403/12

CPC classification number: 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：US09181220B2

公开(公告)日：2015-11-10

申请号：US14189638

申请日：2014-02-25

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D211/58 ,  C07D211/96 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

CPC classification number: C07D401/12 ,  C07D211/58 ,  C07D211/96 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract translation: 本发明提供N-取代的 - 杂环烷氧基苯甲酰胺化合物，以及药物组合物和使用方法。 本发明的一个实施方案是具有其中R 1，R 2，R 3，R 4，T，n，w和x如本文所述的结构的化合物。 在本发明的某些实施方案中，本发明的化合物激活AMPK途径，并且可用于治疗与代谢相关的病症和病症。

公开(公告)号：US20220098175A1

公开(公告)日：2022-03-31

申请号：US17500681

申请日：2021-10-13

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: 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：US09174964B2

公开(公告)日：2015-11-03

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: A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D211/46 ,  C07D211/58 ,  C07D405/14 ,  C07D409/14 ,  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 including certain AMPK-activating piperidinylxoy-substituted 2,3-dihydro-1H-indene-1-amine compounds, as well as pharmaceutical compositions including them. One embodiment is a compound having the structure in which R1, R3,R4,R5,R14,R15,R17, G, Q, k, v, x and y 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: 公开了包括某些AMPK活化的哌啶基偶氮取代的2,3-二氢-1H-茚-1-胺化合物的甲酰胺，磺酰胺和胺化合物，以及包括它们的药物组合物。 一个实施方案是具有其中R 1，R 3，R 4，R 5，R 14，R 15，R 17，G，Q，k，v，x和y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：US09062052B2

公开(公告)日：2015-06-23

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: A61K31/437 ,  C07D471/04 ,  C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08

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。