公开(公告)号：US20130281468A1

公开(公告)日：2013-10-24

申请号：US13918697

申请日：2013-06-14

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D495/04

CPC classification number: A61K31/519 ,  A61K31/395 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D495/04

Abstract: Bicyclic aryl substituted triazoles 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: 公开了双环芳基取代的三唑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：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：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：US20190284155A1

公开(公告)日：2019-09-19

申请号：US16249458

申请日：2019-01-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Pingyu Ding ,  Donald Payan ,  Marina Gelman ,  Todd Kinsella

IPC: C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  A61K45/06 ,  A61K39/395 ,  C07D405/14 ,  C07F7/08 ,  C07K16/28 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/695 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14 ,  C07D417/04

Abstract: The invention described herein comprises compounds and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin

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：US09353126B2

公开(公告)日：2016-05-31

申请号：US14540323

申请日：2014-11-13

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 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D495/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D417/04 ,  C07D491/048

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

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.

Abstract translation: 公开了含有这些化合物的取代的三唑和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：US20140323490A1

公开(公告)日：2014-10-30

申请号：US14261094

申请日：2014-04-24

Applicant: RIGEL PHARMACEUTICALS, INC.

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

IPC: C07D401/14

CPC classification number: C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

Abstract: Polycyclic 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: 公开了多环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：US08796259B2

公开(公告)日：2014-08-05

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

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：US11672791B2

公开(公告)日：2023-06-13

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

公开(公告)号：US20220024907A1

公开(公告)日：2022-01-27

申请号：US17494370

申请日：2021-10-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo J. Heckrodt ,  Yan Chen ,  Darren John McMurtrie ,  Vanessa Taylor ,  Rajinder Singh ,  Pingyu Ding ,  Rose Yen

IPC: C07D413/12 ,  C07B59/00 ,  C07F9/6558

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.