公开(公告)号：US20230012676A1

公开(公告)日：2023-01-19

申请号：US17465662

申请日：2021-09-02

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/4545 ,  C07D471/04 ,  C07D519/00 ,  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：US11524955B2

公开(公告)日：2022-12-13

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: C07D239/48 ,  C07D403/12 ,  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 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; 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.

公开(公告)号：US20210130361A1

公开(公告)日：2021-05-06

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：US20200369644A1

公开(公告)日：2020-11-26

申请号：US16991368

申请日：2020-08-12

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Jiaxin Yu ,  Beth Fernandez ,  Gary Park ,  Ihab Darwish

IPC: C07D401/04 ,  C07D257/04 ,  A61P37/02 ,  C07D249/12 ,  C07C323/60

Abstract: Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs 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 prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.

公开(公告)号：US10774066B2

公开(公告)日：2020-09-15

申请号：US16412217

申请日：2019-05-14

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Jiaxin Yu ,  Beth Fernandez ,  Gary Park ,  Ihab Darwish

IPC: C07D401/04 ,  C07D257/04 ,  A61P37/02 ,  C07D249/12 ,  C07C323/60

Abstract: Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs 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 prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.

公开(公告)号：US20200078348A1

公开(公告)日：2020-03-12

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

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：US10166216B2

公开(公告)日：2019-01-01

申请号：US15147669

申请日：2016-05-05

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/635 ,  A61K31/519 ,  A61K31/517 ,  A61K31/506 ,  A61K31/502 ,  A61K31/501 ,  A61K31/498 ,  A61K31/497 ,  A61K31/454 ,  A61K31/428 ,  A61K31/4196 ,  C07D401/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377

Abstract: 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.

公开(公告)号：US09624229B2

公开(公告)日：2017-04-18

申请号：US14243579

申请日：2014-04-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Jeffrey Clough ,  Ankush Argade ,  Rajinder Singh ,  Vadim Markovtsov ,  Pingyu Ding ,  Jiaxin Yu ,  Andy Atuegbu ,  Hui Hong ,  Ihab Darwish ,  Sambaiah Thota

IPC: C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

CPC classification number: C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

Abstract: This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, or a pharmaceutically acceptable salt.

公开(公告)号：US09353124B2

公开(公告)日：2016-05-31

申请号：US14094392

申请日：2013-12-02

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D453/06 ,  C07D409/14 ,  C07D471/18 ,  C07D495/04 ,  C07D403/12

CPC classification number: C07D495/04 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D471/18

Abstract: Bridged bicyclic aryl or 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: 公开了桥连双环芳基或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：US20160039773A1

公开(公告)日：2016-02-11

申请号：US14815589

申请日：2015-07-31

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: C07D257/04 ,  C07D401/04 ,  C07D405/04

CPC classification number: A61K31/4439 ,  A61K31/41 ,  C07D257/04 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06

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.

Abstract translation: 本公开的方面包括可用于治疗多种自身免疫性和炎性疾病和病症的化合物。 本公开的实施方案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。