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：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：US09283238B2

公开(公告)日：2016-03-15

申请号：US14534784

申请日：2014-11-06

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Rajinder Singh ,  Thomas Sun ,  Esteban Masuda

IPC: A61K31/675 ,  C07D498/04 ,  C07F9/6561

CPC classification number: A61K31/675 ,  A61K9/0053 ,  C07D498/04 ,  C07F9/6561

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

公开(公告)号：US20160024116A1

公开(公告)日：2016-01-28

申请号：US14754989

申请日：2015-06-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

IPC: C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  C07D239/95 ,  C07D473/16

CPC classification number: C07D519/00 ,  A61K31/517 ,  C07D239/94 ,  C07D239/95 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D495/04 ,  C07D495/12

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Abstract translation: 本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。

公开(公告)号：US09062068B2

公开(公告)日：2015-06-23

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: C07D455/02 ,  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：US20140329842A1

公开(公告)日：2014-11-06

申请号：US14200951

申请日：2014-03-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rao Kolluri ,  Salvador Alvarez ,  Matthew Duncton ,  Rajinder Singh ,  Jing Zhang ,  Esteban Masuda

IPC: C07D401/14

CPC classification number: C07D401/14 ,  A61K31/506 ,  C12N9/12 ,  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：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：US20240382470A1

公开(公告)日：2024-11-21

申请号：US18690705

申请日：2022-08-26

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vadim Markovtsov ,  Esteban Masuda

IPC: A61K31/4439 ,  A61K31/427 ,  A61K31/5377 ,  A61K31/675 ,  A61K31/685

Abstract: Disclosed herein is method for treating and/or preventing a cytokine release-related condition associated with infection by a respiratory virus, e.g., COVID-19 or influenza. In certain embodiments, the method may comprise administering a compound that inhibits Interleukin Receptor-Associated Kinase (IRAK) to a subject experiencing, or at risk of developing, the condition. In some embodiments, the compound may have a structure according to Formulas IV or VII, or a salt, solvate, N-oxide and/or prodrug thereof.

公开(公告)号：US20220218705A1

公开(公告)日：2022-07-14

申请号：US17547819

申请日：2021-12-10

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Rajinder Singh ,  Vanessa Taylor ,  Donald G. Payan

IPC: A61K31/506 ,  A61K45/06 ,  A61P37/06

Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.