公开(公告)号：US20130310340A1

公开(公告)日：2013-11-21

申请号：US13895152

申请日：2013-05-15

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Donald G. Payan ,  Esteban Masuda ,  Todd Kinsella

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/541 ,  A61K31/506 ,  A61K31/554

CPC classification number: A61K31/519 ,  A61K31/00 ,  A61K31/437 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553 ,  A61K31/554 ,  A61K31/675 ,  A61K45/06

Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.

Abstract translation: 公开了一种治疗肌肉退化的方法。 还公开了化合物的实施方案，以及包含该化合物的组合物，用于抑制肌肉恶化，包括萎缩，营养不良和恶病质，例如可能由通气引起。

公开(公告)号：US12116354B2

公开(公告)日：2024-10-15

申请号：US17939020

申请日：2022-09-07

Applicant: Rigel Pharmaceuticals, Inc.

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

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

CPC classification number: 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：US11370765B2

公开(公告)日：2022-06-28

申请号：US17023149

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：US11110082B2

公开(公告)日：2021-09-07

申请号：US16575852

申请日：2019-09-19

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/519 ,  A61K31/4545 ,  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：US20210238153A2

公开(公告)日：2021-08-05

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：US20200087293A1

公开(公告)日：2020-03-19

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.

公开(公告)号：US10577381B2

公开(公告)日：2020-03-03

申请号：US16203108

申请日：2018-11-28

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D498/04 ,  C07F9/6574 ,  C07F9/6561 ,  C07F9/6558 ,  A61K31/5383 ,  A61K31/675

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.

公开(公告)号：US10414758B2

公开(公告)日：2019-09-17

申请号：US15875897

申请日：2018-01-19

Applicant: Rigel Pharmaceuticals, Inc.

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

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

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.

公开(公告)号：US20190060310A1

公开(公告)日：2019-02-28

申请号：US15918929

申请日：2018-03-12

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 ,  C07D498/04 ,  C07D471/04

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 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：US20180008589A1

公开(公告)日：2018-01-11

申请号：US15645775

申请日：2017-07-10

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/4545 ,  A61K31/519

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.