公开(公告)号：US09321763B2

公开(公告)日：2016-04-26

申请号：US13857028

申请日：2013-04-04

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: A61K31/506 ,  A61K31/505 ,  A61K31/535 ,  A61K31/553 ,  C07D471/04 ,  C07D519/00 ,  C07D295/00

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：US20160058760A1

公开(公告)日：2016-03-03

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: 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.

公开(公告)号：US20150306100A1

公开(公告)日：2015-10-29

申请号：US14712748

申请日：2015-05-14

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: A61K31/506 ,  A61K31/5383 ,  A61K31/5377 ,  A61K31/538

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：US09169249B2

公开(公告)日：2015-10-27

申请号：US14209997

申请日：2014-03-13

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: C07D471/04 ,  C07D498/04

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：US11919890B2

公开(公告)日：2024-03-05

申请号：US17210261

申请日：2021-03-23

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vanessa Taylor ,  Jiaxin Yu ,  Esteban Masuda ,  Ihab Darwish ,  Yan Chen

IPC: C07D413/12 ,  A61K31/553 ,  A61P29/00 ,  A61P37/02 ,  C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

CPC classification number: C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20230391748A1

公开(公告)日：2023-12-07

申请号：US18204304

申请日：2023-05-31

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Esteban Masuda ,  Chrystelle Lamagna

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  G01N33/574

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  G01N33/57484 ,  G01N2333/91205

Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitor compounds and compositions comprising such compounds. The compounds may have a structure according to Formula I




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.

公开(公告)号：US11472782B2

公开(公告)日：2022-10-18

申请号：US17072862

申请日：2020-10-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Simon Shaw ,  Vanessa Taylor ,  Somasekhar Bhamidipati

IPC: C07D267/14 ,  C07D487/04 ,  C07D413/06 ,  C07D413/14 ,  C07D403/12 ,  C07D493/04 ,  C07D407/06 ,  A61P35/00 ,  C07D413/12

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US11370764B2

公开(公告)日：2022-06-28

申请号：US17023136

申请日：2020-09-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Simon Shaw ,  Vanessa Taylor ,  Somasekhar Bhamidipati

IPC: A61K31/553 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  C07D413/12 ,  C07D267/14 ,  C07D413/14 ,  C07D487/04

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：USRE48898E1

公开(公告)日：2022-01-25

申请号：US16291992

申请日：2019-03-04

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/675 ,  C07D498/04 ,  A61K9/00 ,  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：US11220496B2

公开(公告)日：2022-01-11

申请号：US16551431

申请日：2019-08-26

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/12 ,  C07F9/653 ,  A61K31/675 ,  A61K45/06 ,  A61K31/506

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.