公开(公告)号：US20210040053A1

公开(公告)日：2021-02-11

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 ,  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：US20210002237A1

公开(公告)日：2021-01-07

申请号：US17023149

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：US20210002236A1

公开(公告)日：2021-01-07

申请号：US17023136

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：US20200016179A1

公开(公告)日：2020-01-16

申请号：US16438972

申请日：2019-06-12

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/675 ,  C07D498/04 ,  C07F9/6561 ,  A61K9/00

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：US20190292197A1

公开(公告)日：2019-09-26

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 ,  C07F9/6558 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/6561 ,  C07F9/6574

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：US10130623B2

公开(公告)日：2018-11-20

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: A61K31/506 ,  A61K31/4545 ,  A61K31/519

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：US20180141938A1

公开(公告)日：2018-05-24

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

CPC classification number: C07D413/12 ,  A61K31/506 ,  A61K31/675 ,  A61K45/06 ,  C07F9/65324 ,  Y10T436/141111 ,  A61K2300/00

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：US09890144B2

公开(公告)日：2018-02-13

申请号：US14750794

申请日：2015-06-25

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

CPC classification number: C07D413/12 ,  A61K31/506 ,  A61K31/675 ,  A61K45/06 ,  C07F9/65324 ,  Y10T436/141111 ,  A61K2300/00

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：US20170360786A1

公开(公告)日：2017-12-21

申请号：US15395606

申请日：2016-12-30

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

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：US09481654B2

公开(公告)日：2016-11-01

申请号：US14624301

申请日：2015-02-17

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Ankush Argade ,  Kin Tso ,  Sambaiah Thota ,  David Carroll ,  Arvinder Sran ,  Robin Cooper ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Esteban Masuda

IPC: C07D239/48 ,  A61K31/505 ,  C07D239/50 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/506 ,  A61K45/06

CPC classification number: C07D239/50 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

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.