公开(公告)号：US20130150349A1

公开(公告)日：2013-06-13

申请号：US13759835

申请日：2013-02-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald G. Payan ,  Susan Molineaux ,  Sacha J. Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander B. Rossi

IPC: C07D239/48 ,  A61K45/06 ,  C07D405/12 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/12 ,  C07D413/12 ,  A61K31/538 ,  C07D401/12 ,  C07D409/12 ,  C07D413/14 ,  C07D498/04 ,  A61K31/5383 ,  C07D417/12 ,  A61K31/551 ,  C07D403/14 ,  A61K31/505

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5395 ,  A61K31/551 ,  A61K45/06 ,  C07D239/48 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D498/04 ,  C07D498/14 ,  C07F5/027

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

公开(公告)号：US20130090330A1

公开(公告)日：2013-04-11

申请号：US13644738

申请日：2012-10-04

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Pingyu Ding ,  Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Joane Litvak

IPC: C07D495/04 ,  C07D403/14 ,  C07D407/14 ,  C07D413/14

CPC classification number: C07D495/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract translation: 公开了N 3 - 杂芳基取代的三唑和N 5 - 杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US12227508B2

公开(公告)日：2025-02-18

申请号：US17962305

申请日：2022-10-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US11466018B2

公开(公告)日：2022-10-11

申请号：US17087459

申请日：2020-11-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

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.

公开(公告)号：US11352360B2

公开(公告)日：2022-06-07

申请号：US16360162

申请日：2019-03-21

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Dame ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  A61P35/00 ,  C07D417/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US11279686B2

公开(公告)日：2022-03-22

申请号：US17075152

申请日：2020-10-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/04 ,  C07D249/12 ,  C07D255/02 ,  C07D257/04

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate 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：US11129819B2

公开(公告)日：2021-09-28

申请号：US16600873

申请日：2019-10-14

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Somasekhar Bhamidipati ,  Jiaxin Yu ,  Ihab Darwish ,  Rajinder Singh

IPC: A61K31/41 ,  A61K31/4439 ,  C07D403/12 ,  C07D405/06 ,  C07D257/04 ,  C07D401/04 ,  C07D405/04

Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate 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：US11021468B2

公开(公告)日：2021-06-01

申请号：US15563056

申请日：2016-03-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Pingyu Ding ,  Todd Kinsella ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Jeffrey Clough

IPC: A61P35/02 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04

Abstract: Disclosed are aryl pyrimidine compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, R and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US20200299276A1

公开(公告)日：2020-09-24

申请号：US16893981

申请日：2020-06-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

IPC: C07D403/12 ,  C07D239/48 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 M; a TAK1 IC50 of from 0.008 μM to 132 M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.