公开(公告)号：US08987303B2

公开(公告)日：2015-03-24

申请号：US13801030

申请日：2013-03-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Donald Payan ,  Rajinder Singh ,  Simon Shaw ,  David Carroll ,  Yasumichi Hitoshi

IPC: A61K31/4427 ,  C07D401/14 ,  C07D487/04 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D495/04 ,  C07D405/12 ,  C07D213/81 ,  C07D213/56

CPC classification number: C07D401/14 ,  C07B2200/07 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, 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: 公开了取代的吡啶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E，J，T，由“B”，T，R3，R4，w和x表示的环系统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：US08980921B2

公开(公告)日：2015-03-17

申请号：US13801064

申请日：2013-03-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Donald Payan ,  Rajinder Singh ,  Simon Shaw ,  David Carroll ,  Yasumichi Hitoshi

IPC: A61K31/4427 ,  C07D401/14 ,  C07D487/04 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D495/04 ,  C07D405/12 ,  C07D213/81 ,  C07D213/56

CPC classification number: C07D401/14 ,  C07B2200/07 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, 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：US20140330007A1

公开(公告)日：2014-11-06

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: C07D498/04 ,  C07D405/14 ,  C07D403/14 ,  C07D413/14 ,  C07D409/14 ,  C07F5/02 ,  C07D417/12 ,  C07D413/12 ,  C07D403/12 ,  C07D409/12 ,  C07D495/04 ,  C07D239/48 ,  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.

Abstract translation: 本发明提供了抑制导致释放化学介质，中间体和合成化合物的方法的IgE和/或IgG受体信号级联的2,4-嘧啶二胺化合物和在多种情况下使用化合物的方法，包括 在治疗和预防以IgE和/或IgG受体信号传导级联的活化作用通过脱颗粒和其它方法释放化学介质引起或与之相关的疾病。

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：US20140163022A1

公开(公告)日：2014-06-12

申请号：US14095893

申请日：2013-12-03

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Rao Kolluri ,  Esteban Masuda ,  Kin Tso ,  Salvador Alvarez ,  Thilo Heckrodt ,  Sacha Holland ,  Ryan Kelley ,  Matthew Duncton ,  Rajinder Singh ,  Darren McMurtrie

IPC: C07D471/04 ,  C07D498/04

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  C07D455/02 ,  C07D498/04

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 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：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：US08642593B2

公开(公告)日：2014-02-04

申请号：US13759457

申请日：2013-02-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Jeffrey Clough

IPC: A61K31/5383

CPC classification number: C07D498/04 ,  C07F9/6561

Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Abstract translation: 本公开提供式（I） - （III）的生物活性2,4-嘧啶二胺化合物及其盐，包含这些化合物的组合物，以及在各种应用中使用这些化合物的方法。

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：US20130267702A1

公开(公告)日：2013-10-10

申请号：US13801064

申请日：2013-03-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Donald Payan ,  Rajinder Singh ,  Simon Shaw ,  David Carroll ,  Yasumichi Hitoshi

IPC: C07D487/04 ,  C07D213/56 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D401/14 ,  C07B2200/07 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, 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: 公开了取代的吡啶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E，J，T，由“B”，T，R3，R4，w和x表示的环系统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。