公开(公告)号：US20210379064A1

公开(公告)日：2021-12-09

申请号：US17351996

申请日：2021-06-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yasumichi Hitoshi ,  Sacha Holland ,  Donald G. Payan

IPC: A61K31/502 ,  A61K45/06 ,  A61K31/4196 ,  A61K33/243 ,  C07D403/04 ,  C07D403/14

Abstract: This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents.

公开(公告)号：US10851093B2

公开(公告)日：2020-12-01

申请号：US16424619

申请日：2019-05-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ihab Darwish ,  Jiaxin Yu ,  Rao Kolluri ,  Sacha Holland

IPC: C07D215/00 ,  C07D413/14 ,  C07D417/14 ,  C07D491/107 ,  C07D453/00

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 R1, X, Y1, Y2, Y3 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：US10434096B2

公开(公告)日：2019-10-08

申请号：US16151959

申请日：2018-10-04

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D519/00 ,  A61K31/4545 ,  A61K31/519 ,  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：US10005777B2

公开(公告)日：2018-06-26

申请号：US15588410

申请日：2017-05-05

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 ,  Ryan Kelley

IPC: C07D471/04 ,  C12Q1/48 ,  A61K31/506 ,  A61K31/538 ,  C12N9/12 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  C12N9/12 ,  C12Q1/485 ,  C12Y207/11013

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：US20160243085A1

公开(公告)日：2016-08-25

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: A61K31/4196 ,  A61K31/519 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/635 ,  A61K31/498 ,  A61K31/4545 ,  A61K31/428 ,  A61K31/501 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/502 ,  A61K31/4355 ,  A61K31/517

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.

公开(公告)号：US09206161B2

公开(公告)日：2015-12-08

申请号：US14593981

申请日：2015-01-09

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/502 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D471/18 ,  C07D221/22 ,  C07D237/26 ,  C07D237/34

CPC classification number: C07D403/04 ,  A61K31/502 ,  C07D221/22 ,  C07D237/26 ,  C07D237/34 ,  C07D401/14 ,  C07D403/14 ,  C07D471/18

Abstract: Bridged bicyclic 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：US09181222B2

公开(公告)日：2015-11-10

申请号：US14200951

申请日：2014-03-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rao Kolluri ,  Salvador Alvarez ,  Matthew Duncton ,  Rajinder Singh ,  Jing Zhang ,  Esteban Masuda

IPC: C07D401/14 ,  A61K31/506 ,  C12N9/12

CPC classification number: C07D401/14 ,  A61K31/506 ,  C12N9/12 ,  C12Y207/11013

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：US20140128400A1

公开(公告)日：2014-05-08

申请号：US14150401

申请日：2014-01-08

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D471/18 ,  C07D237/26 ,  C07D221/22

CPC classification number: C07D403/04 ,  A61K31/502 ,  C07D221/22 ,  C07D237/26 ,  C07D237/34 ,  C07D401/14 ,  C07D403/14 ,  C07D471/18

Abstract: Bridged bicyclic 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：US20130338161A1

公开(公告)日：2013-12-19

申请号：US13908874

申请日：2013-06-03

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yasumichi Hitoshi ,  Sacha Holland ,  Donald G. Payan

IPC: A61K31/502 ,  A61K45/06 ,  C07D403/14 ,  C07D403/04

CPC classification number: A61K31/502 ,  A61K31/4196 ,  A61K33/24 ,  A61K45/06 ,  C07D403/04 ,  C07D403/14 ,  A61K2300/00

Abstract: This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents.

Abstract translation: 本发明涉及在患者体内预防，治疗或控制癌症，优选转移性癌症的方法。 所述方法包括与施用有效量的一种或多种化学治疗剂组合施用有效量的Axl抑制剂。

公开(公告)号：US20130331374A1

公开(公告)日：2013-12-12

申请号：US13857028

申请日：2013-04-04

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: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  C12N9/12 ,  C12Q1/485 ,  C12Y207/11013

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.