公开(公告)号：US20170246167A1

公开(公告)日：2017-08-31

申请号：US15443145

申请日：2017-02-27

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. Rossii

IPC: A61K31/505 ,  A61K31/5377 ,  A61K31/506

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：US09732073B2

公开(公告)日：2017-08-15

申请号：US14974143

申请日：2015-12-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Sambaiah Thota ,  David Carroll ,  Ankush Argade ,  Kin Tso ,  Arvinder Sran ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Robin Cooper ,  Rajinder Singh ,  Brian Wong

IPC: C07D403/04 ,  A61K31/506 ,  C07D413/12 ,  C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/395 ,  C07D498/04 ,  C07F7/10 ,  A61K45/06 ,  C07D401/14 ,  C07D417/12 ,  C07F7/08 ,  C07D285/22

CPC classification number: C07D413/12 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/3955 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D285/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07F7/0812 ,  C07F7/10

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

公开(公告)号：US09701647B2

公开(公告)日：2017-07-11

申请号：US15233676

申请日：2016-08-10

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D257/04 ,  A61K31/41 ,  C07D403/06 ,  C07D403/14 ,  C07D401/12 ,  C07D403/12 ,  C07D401/10 ,  C07D413/10 ,  C07D501/16 ,  C07D401/14 ,  C07J43/00 ,  C07D401/04 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4184 ,  A61K31/4709 ,  A61K31/4245 ,  A61K31/546 ,  A61K31/55 ,  A61K31/496 ,  A61K31/58 ,  A61K31/506 ,  A61K31/519

CPC classification number: C07D257/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/55 ,  A61K31/58 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06 ,  C07D501/16 ,  C07D501/46 ,  C07J9/005 ,  C07J43/003

Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

公开(公告)号：US09682976B2

公开(公告)日：2017-06-20

申请号：US15056535

申请日：2016-02-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Matthew Duncton ,  Jing Zhang ,  Salvador Alvarez ,  Kin Tso ,  Sacha Holland ,  Rose Yen ,  Rao Kolluri ,  Thilo Heckrodt ,  Yan Chen ,  Esteban Masuda ,  Hui Li ,  Donald G. Payan ,  Ryan Kelley

IPC: A61K31/5383 ,  A61K31/5386 ,  A61K31/506 ,  A61K31/553 ,  A61K31/538 ,  A61K31/5377 ,  C07D519/00 ,  C07D471/04 ,  C12Q1/48 ,  C12N9/12

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  C12N9/12 ,  C12Q1/485 ,  C12Y207/11013

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：US20170152246A1

公开(公告)日：2017-06-01

申请号：US15261294

申请日：2016-09-09

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Kin Tso ,  Jing Zhang ,  Matthew Duncton ,  Salvador Alvarez ,  Rao Kolluri ,  John Ramphal ,  Sacha Holland

IPC: C07D405/14 ,  C07D401/14

CPC classification number: C07D405/14 ,  A61K31/41 ,  A61K31/506 ,  C07D401/14

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.

公开(公告)号：US20170121291A1

公开(公告)日：2017-05-04

申请号：US15290918

申请日：2016-10-11

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ankush Argade ,  Arvinder Sran ,  David Carroll ,  Jeffrey Clough ,  Kin Tso ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Rajinder Singh ,  Vanessa Taylor ,  Hui Li ,  Esteban Masuda

IPC: C07D239/48 ,  C07D403/12 ,  C07D417/12 ,  C07D401/14 ,  C07D498/04 ,  C07D413/14 ,  C07D405/12 ,  C07D401/12 ,  C07D413/12

CPC classification number: C07D239/48 ,  A61K31/505 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04

Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

公开(公告)号：US09566278B2

公开(公告)日：2017-02-14

申请号：US14849376

申请日：2015-09-09

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Matthew Duncton ,  Jing Zhang ,  Salvador Alvarez ,  Kin Tso ,  Sacha Holland ,  Rose Yen ,  Rao Kolluri ,  Thilo Heckrodt ,  Yan Chen ,  Esteban Masuda ,  Hui Li ,  Donald G. Payan

IPC: C12N9/99 ,  C07D471/04 ,  C07D498/04 ,  A61K31/506

CPC classification number: A61K31/506 ,  C07D471/04 ,  C07D498/04 ,  Y02A50/411

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：US09540334B2

公开(公告)日：2017-01-10

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: C07D239/48 ,  A61K31/505 ,  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 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D498/04 ,  C07D265/36 ,  A61K31/5395 ,  C07D495/04 ,  C07F5/02 ,  C07D498/14 ,  C07D407/14

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：US20160229838A1

公开(公告)日：2016-08-11

申请号：US14993936

申请日：2016-01-12

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  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。

公开(公告)号：US20160213648A1

公开(公告)日：2016-07-28

申请号：US15005773

申请日：2016-01-25

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: A61K31/4155 ,  C07D471/04 ,  A61K31/519 ,  A61K31/517 ,  A61K31/5383 ,  C07D401/12 ,  A61K31/4725 ,  C07D403/10 ,  C07D403/12 ,  C07D498/06

CPC classification number: C07D257/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/55 ,  A61K31/58 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06 ,  C07D501/16 ,  C07D501/46 ,  C07J9/005 ,  C07J43/003

Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Abstract translation: 本公开提供了包含活性剂的羧基的四唑酮衍生物的化合物。 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，以及制备这些化合物的方法。