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：US20180339979A1

公开(公告)日：2018-11-29

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

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：US09981944B2

公开(公告)日：2018-05-29

申请号：US15043729

申请日：2016-02-15

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

Inventor： Pingyu Ding ,  Marina Gelman ,  Todd Kinsella ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Upender Velaparthi ,  Robert M. Borzilleri ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07B59/00 ,  C07C53/06 ,  C07C53/18 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07B59/002 ,  C07B2200/05 ,  C07C53/06 ,  C07C53/18 ,  C07D471/04 ,  C07D487/04

Abstract: Disclosed are 2,2′-bipyridyl 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, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.

公开(公告)号：US09834568B2

公开(公告)日：2017-12-05

申请号：US14754989

申请日：2015-06-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

IPC: C07D487/04 ,  C07D239/95 ,  A61K31/517 ,  A61P35/00 ,  C07D519/00 ,  C07D495/12 ,  C07D239/94 ,  C07D473/16 ,  C07D495/04 ,  C07D471/04

CPC classification number: C07D519/00 ,  A61K31/517 ,  C07D239/94 ,  C07D239/95 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D495/04 ,  C07D495/12

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

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：US20170096409A1

公开(公告)日：2017-04-06

申请号：US15128051

申请日：2015-04-02

Applicant: Rigel Pharmaceuticals, Inc.

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

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

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/635 ,  A61K31/695 ,  A61K39/39541 ,  A61K45/06 ,  A61K2039/505 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07F7/0812 ,  C07K16/2818

Abstract: The invention described herein comprises compounds of formula (IV) 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 (IV) inhibit signaling by a member of the TGF-β superfamily such as Nodal or Activin.

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：US09156820B2

公开(公告)日：2015-10-13

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: A61K31/502 ,  C07D237/26 ,  C07D401/14 ,  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

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：US08809347B2

公开(公告)日：2014-08-19

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: A61K31/395 ,  A61K31/519

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：US20140155386A1

公开(公告)日：2014-06-05

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: C07D495/04 ,  C07D401/14 ,  C07D453/06 ,  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。