公开(公告)号：US08853397B2

公开(公告)日：2014-10-07

申请号：US13759835

申请日：2013-02-05

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 ,  C07D413/12 ,  C07D401/12 ,  A61K31/551 ,  C07D409/12 ,  C07D409/14 ,  A61K31/538 ,  C07D417/12 ,  A61K31/519 ,  C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D265/36 ,  A61K31/5383 ,  A61K31/505 ,  A61K45/06 ,  C07D413/10 ,  C07D413/14 ,  A61K31/5377 ,  C07D498/04 ,  C07D405/12 ,  C07D417/14 ,  C07D403/12

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：US08822685B2

公开(公告)日：2014-09-02

申请号：US13961780

申请日：2013-08-07

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 ,  C07D405/14 ,  A61K31/551 ,  C07D403/12 ,  C07D409/14 ,  A61K31/5383 ,  C07D413/14 ,  C07D413/10 ,  A61K31/5377 ,  C07D405/12 ,  C07D265/36 ,  C07D401/14 ,  C07D498/04 ,  C07D409/12 ,  A61K31/519 ,  C07D401/12 ,  C07D417/14 ,  C07D403/14 ,  C07D413/12 ,  A61K31/506 ,  A61K31/538 ,  C07D417/12 ,  A61K45/06

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：US08748597B2

公开(公告)日：2014-06-10

申请号：US13909830

申请日：2013-06-04

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Ankush Argade ,  Catherine Sylvain

IPC: C07D265/36

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：US20140011770A1

公开(公告)日：2014-01-09

申请号：US14023158

申请日：2013-09-10

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

IPC: C07D413/12 ,  A61K45/06 ,  C07D403/12 ,  C07D471/08 ,  A61K31/5377 ,  C07F9/6558 ,  A61K31/675 ,  C07D487/08 ,  A61K31/551 ,  C07D471/04 ,  C07D413/14 ,  A61K31/541 ,  C07D491/08 ,  C07D487/04 ,  C07D487/10 ,  A61K31/54 ,  C07D419/14 ,  A61K31/55 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/538 ,  A61K31/506

CPC classification number: C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

Abstract translation: 公开了式I的化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。

公开(公告)号：US20130338357A1

公开(公告)日：2013-12-19

申请号：US13909858

申请日：2013-06-04

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

IPC: C07F9/6558 ,  C07D498/04

CPC classification number: C07D498/04 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65742

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

Abstract translation: 本公开提供了生物活性2,4-嘧啶二胺化合物的前药，包含前体药物的组合物，用于合成前药的中间体和方法以及在各种应用中使用前药的方法。

公开(公告)号：US20130309228A1

公开(公告)日：2013-11-21

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: A61K31/5383 ,  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.

公开(公告)号：US20130267701A1

公开(公告)日：2013-10-10

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: C07D487/04 ,  C07D213/81 ,  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.

公开(公告)号：US20130142807A1

公开(公告)日：2013-06-06

申请号：US13750632

申请日：2013-01-25

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: A61K31/506 ,  A61K31/505 ,  C07F7/10 ,  A61K31/695 ,  C07D403/12 ,  C07D401/12 ,  A61K31/5377 ,  C07D413/12 ,  C07D413/14 ,  A61K31/541 ,  A61K31/538 ,  C07D498/04 ,  A61K31/5383 ,  A61K39/395 ,  A61K38/13 ,  A61K31/436 ,  A61K31/343 ,  C07D239/48

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：US20130109695A1

公开(公告)日：2013-05-02

申请号：US13725407

申请日：2012-12-21

Applicant: RIGEL PHARMACEUTICALS, INC.

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

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

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.

公开(公告)号：US11993594B2

公开(公告)日：2024-05-28

申请号：US17953570

申请日：2022-09-27

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC: C07D413/14 ,  A61P29/00

CPC classification number: C07D413/14 ,  A61P29/00

Abstract: Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.