公开(公告)号：US20150376203A1

公开(公告)日：2015-12-31

申请号：US14754415

申请日：2015-06-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Haoran Zhao ,  Rao Kolluri ,  Carlos Valdez ,  Kin Tso ,  Rajinder Singh ,  John Ramphal

IPC: C07D498/04

CPC classification number: C07D498/04 ,  A61K31/5383 ,  C07D498/14

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising 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: 本公开涉及可用作蛋白激酶C（PKC）的抑制剂的化合物，因此可用于治疗通过PKC的活性介导或维持的多种疾病和病症。 本公开还涉及包含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：US20150329532A1

公开(公告)日：2015-11-19

申请号：US14812829

申请日：2015-07-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald G. Payan ,  Susan Molineaux ,  Sacha J. Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander B. Rossi

IPC: C07D417/12 ,  C07D403/14 ,  C07D413/14 ,  C07D413/12 ,  C07D409/14 ,  C07D405/12 ,  C07D409/12 ,  C07D403/12 ,  C07D239/48 ,  C07D405/14

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5395 ,  A61K31/551 ,  A61K45/06 ,  C07D239/48 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07F5/027

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

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：US09149475B2

公开(公告)日：2015-10-06

申请号：US13718632

申请日：2012-12-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Hui Li ,  Haoran Zhao ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu ,  Carlos Valdez ,  Jing Zhang ,  Emily Stauffer ,  Matthew Duncton ,  Salvador Alvarez

IPC: A61K31/506 ,  A61K31/55 ,  A61K31/538 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising 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.

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：US20150216864A1

公开(公告)日：2015-08-06

申请号：US14688843

申请日：2015-04-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Thilo J. Heckrodt ,  Sacha Holland

IPC: A61K31/502

CPC classification number: A61K31/502 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/14

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：US09079898B2

公开(公告)日：2015-07-14

申请号：US13725407

申请日：2012-12-21

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Thilo J. Heckrodt ,  Sacha Holland

IPC: C07D237/36 ,  C07D471/04 ,  C07D403/04 ,  C07D471/14 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

CPC classification number: A61K31/502 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/14

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：US20150158823A1

公开(公告)日：2015-06-11

申请号：US14626471

申请日：2015-02-19

Applicant: Rigel Pharmaceuticals, Inc

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald G. Payan ,  Susan Molineaux ,  Sacha J. Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander B. Rossi

IPC: C07D239/48 ,  C07D401/12 ,  C07D413/12 ,  C07D403/12 ,  C07D498/14 ,  C07D413/14 ,  C07D409/12 ,  C07F5/02 ,  C07D417/12 ,  C07D405/12 ,  C07D401/14

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5395 ,  A61K31/551 ,  A61K45/06 ,  C07D239/48 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07F5/027

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

公开(公告)号：US09040550B2

公开(公告)日：2015-05-26

申请号：US14333163

申请日：2014-07-16

Applicant: Rigel Pharmaceuticals, Inc

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald G. Payan ,  Susan Molineaux ,  Sacha J. Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander B. Rossi

IPC: C07D239/48 ,  A61K31/506 ,  A61K31/5395 ,  A61K31/519 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D498/04 ,  C07D265/36 ,  C07D495/04 ,  C07F5/02

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5395 ,  A61K31/551 ,  A61K45/06 ,  C07D239/48 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07F5/027

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

公开(公告)号：US09040527B2

公开(公告)日：2015-05-26

申请号：US13948342

申请日：2013-07-23

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Andy Atuegbu ,  John Ramphal ,  Hui Li ,  Marina Gelman ,  Jeffrey Clough ,  Carlos Valdez ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Darren McMurtrie

IPC: C07D413/04 ,  C07D498/04 ,  A61K31/5415 ,  A61K31/538 ,  C07D413/14 ,  A61K31/5383 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  A61K45/06

CPC classification number: A61K31/5383 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/08 ,  C07D498/04

Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

Abstract translation: 公开的实施方案提供了可用于抑制激酶活性的嘧啶二胺化合物，包括polo样激酶1（PLK1）的活性。 还公开了包含这些化合物的药物组合物和治疗与激酶活性相关的疾病的方法，特别是增强的PLK1催化活性，例如与异常细胞增殖相关的疾病，包括肿瘤性疾病。