公开(公告)号：US10696693B2

公开(公告)日：2020-06-30

申请号：US15527908

申请日：2015-11-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Todd Kinsella ,  Jiaxin Yu ,  Marina Gelman ,  Ihab S. Darwish

IPC: C07D498/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/424 ,  A61K31/428 ,  A61K31/498 ,  A61P19/02 ,  A61K31/416 ,  A61K31/4188 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a 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：US10434096B2

公开(公告)日：2019-10-08

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

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：US20180086764A1

公开(公告)日：2018-03-29

申请号：US15563075

申请日：2015-04-01

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04

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：US09475781B2

公开(公告)日：2016-10-25

申请号：US14815589

申请日：2015-07-31

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: A61K31/41 ,  C07D257/04 ,  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.

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。

公开(公告)号：US20160257690A1

公开(公告)日：2016-09-08

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

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.

Abstract translation: 公开了咪唑和噻唑化合物，以及药物组合物及其使用方法。 一个实施方案是具有其结构和药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物）的化合物，其中X，A，Z，R 1和R'如本文所述。 在某些实施方案中，本文公开的化合物抑制TGF-β，并且可用于通过阻断TGF-β信号传导治疗疾病。

公开(公告)号：US20160243085A1

公开(公告)日：2016-08-25

申请号：US15147669

申请日：2016-05-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Jing Zhang ,  Catherine Sylvain ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding

IPC: A61K31/4196 ,  A61K31/519 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/635 ,  A61K31/498 ,  A61K31/4545 ,  A61K31/428 ,  A61K31/501 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/502 ,  A61K31/4355 ,  A61K31/517

CPC classification number: A61K31/4196 ,  A61K31/428 ,  A61K31/4355 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/635 ,  C07D249/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

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。

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.