公开(公告)号：US11352360B2

公开(公告)日：2022-06-07

申请号：US16360162

申请日：2019-03-21

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Dame ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  A61P35/00 ,  C07D417/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US09884868B2

公开(公告)日：2018-02-06

申请号：US15054895

申请日：2016-02-26

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

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：US20200031832A1

公开(公告)日：2020-01-30

申请号：US16360162

申请日：2019-03-21

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US10287295B2

公开(公告)日：2019-05-14

申请号：US15860379

申请日：2018-01-02

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US20180127426A1

公开(公告)日：2018-05-10

申请号：US15860379

申请日：2018-01-02

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

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：US09624229B2

公开(公告)日：2017-04-18

申请号：US14243579

申请日：2014-04-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Jeffrey Clough ,  Ankush Argade ,  Rajinder Singh ,  Vadim Markovtsov ,  Pingyu Ding ,  Jiaxin Yu ,  Andy Atuegbu ,  Hui Hong ,  Ihab Darwish ,  Sambaiah Thota

IPC: C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

CPC classification number: C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

Abstract: This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, or a pharmaceutically acceptable salt.

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.