公开(公告)号：US11667643B2

公开(公告)日：2023-06-06

申请号：US17358698

申请日：2021-06-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Simon Shaw ,  Ihab Darwish ,  Jiaxin Yu ,  Rao Kolluri ,  Vanessa Taylor ,  Esteban Masuda ,  Mark Irving

IPC: A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D498/14 ,  C07D498/22 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/22 ,  C07D513/14 ,  C07D519/00

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：US11667611B2

公开(公告)日：2023-06-06

申请号：US16404481

申请日：2019-05-06

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: C07D239/42 ,  C07D239/48 ,  A61K31/505 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07D405/12 ,  C07D413/14 ,  C07D498/04

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：US11332451B2

公开(公告)日：2022-05-17

申请号：US17023127

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：US20210283152A1

公开(公告)日：2021-09-16

申请号：US17323901

申请日：2021-05-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Vadim Markovtsov

IPC: A61K31/675 ,  A61K31/245 ,  A61K31/155 ,  A61K31/4706 ,  A61K31/427 ,  A61K31/573 ,  A61K31/519 ,  A61K39/42 ,  A61K31/4748 ,  A61K31/7048 ,  A61P31/14

Abstract: Provided herein are a variety of methods that involve administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having or suspected of having a COVID-19 infection. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop acute respiratory distress syndrome, acute kidney injury, and/or thrombosis. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop symptoms associated with a cytokine response. Aspects of the methods may further include identifying a patient with kidney malfunction, e.g., acute kidney injury, and/or thrombosis.

公开(公告)号：US20210009537A1

公开(公告)日：2021-01-14

申请号：US17023138

申请日：2020-09-16

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D267/14 ,  A61P35/00 ,  C07D413/12 ,  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：US20200377518A1

公开(公告)日：2020-12-03

申请号：US16888430

申请日：2020-05-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda

IPC: C07D498/04 ,  A61P7/02

Abstract: A method of preventing or treating thrombosis in a patent is disclose, wherein the method comprises administering to the patient an amount of fostamatinib or a form or metabolite thereof effective to prevent or treat the thrombosis, respectively.

公开(公告)号：US20190099411A1

公开(公告)日：2019-04-04

申请号：US16151959

申请日：2018-10-04

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Pingyu Ding ,  Rao Kolluri ,  Ihab Darwish ,  Esteban Masuda ,  Jiaxin Yu

IPC: A61K31/4545 ,  C07D519/00 ,  A61K31/519 ,  C07D471/04

CPC classification number: A61K31/4545 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.

公开(公告)号：US09913843B2

公开(公告)日：2018-03-13

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 ,  C07D498/04 ,  C07D455/02 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383

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.

公开(公告)号：US20180030050A1

公开(公告)日：2018-02-01

申请号：US15588410

申请日：2017-05-05

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

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：US20160367575A1

公开(公告)日：2016-12-22

申请号：US15005771

申请日：2016-01-25

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/675 ,  A61K9/00

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.