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：US09156820B2

公开(公告)日：2015-10-13

申请号：US14261094

申请日：2014-04-24

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: A61K31/502 ,  C07D237/26 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

Abstract: Polycyclic heteroaryl 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.

Abstract translation: 公开了多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

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：US08809347B2

公开(公告)日：2014-08-19

申请号：US13918697

申请日：2013-06-14

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/395 ,  A61K31/519

CPC classification number: A61K31/519 ,  A61K31/395 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D495/04

Abstract: Bicyclic aryl substituted triazoles or heteroaryl 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.

Abstract translation: 公开了双环芳基取代的三唑或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

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：US20140155386A1

公开(公告)日：2014-06-05

申请号：US14094392

申请日：2013-12-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Joane Litvak

IPC: C07D495/04 ,  C07D401/14 ,  C07D453/06 ,  C07D403/12

CPC classification number: C07D495/04 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D471/18

Abstract: Bridged bicyclic aryl or heteroaryl 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.

Abstract translation: 公开了桥连双环芳基或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20130281468A1

公开(公告)日：2013-10-24

申请号：US13918697

申请日：2013-06-14

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D495/04

CPC classification number: A61K31/519 ,  A61K31/395 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D495/04

Abstract: Bicyclic aryl substituted triazoles or heteroaryl 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.

Abstract translation: 公开了双环芳基取代的三唑或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20130090330A1

公开(公告)日：2013-04-11

申请号：US13644738

申请日：2012-10-04

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: C07D495/04 ,  C07D403/14 ,  C07D407/14 ,  C07D413/14

CPC classification number: C07D495/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl 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.

Abstract translation: 公开了N 3 - 杂芳基取代的三唑和N 5 - 杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。