公开(公告)号：US10858335B2

公开(公告)日：2020-12-08

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 ,  A61K31/519 ,  A61K45/06 ,  A61K31/4439 ,  C07D405/14 ,  C07F7/08 ,  C07K16/28 ,  A61K31/444 ,  A61K31/517 ,  A61K31/695 ,  A61K31/5377 ,  A61K31/635 ,  A61K39/395 ,  C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14 ,  C07D417/04 ,  A61K39/00

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：US10479783B2

公开(公告)日：2019-11-19

申请号：US15892224

申请日：2018-02-08

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 ,  C07F9/6558 ,  C07B59/00

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.

公开(公告)号：US20190099411A1

公开(公告)日：2019-04-04

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

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：US09920041B2

公开(公告)日：2018-03-20

申请号：US15439705

申请日：2017-02-22

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

CPC classification number: C07D413/12 ,  C07B59/002 ,  C07B2200/05 ,  C07F9/65583

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.

公开(公告)号：US20170158683A1

公开(公告)日：2017-06-08

申请号：US15439705

申请日：2017-02-22

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

CPC classification number: C07D413/12 ,  C07B59/002 ,  C07B2200/05 ,  C07F9/65583

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.

公开(公告)号：US09518040B2

公开(公告)日：2016-12-13

申请号：US14833689

申请日：2015-08-24

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D405/04 ,  C07D487/04 ,  C07D453/02 ,  C07D417/14 ,  C07D401/04 ,  C07F9/6503 ,  C07D417/04 ,  C07D471/04 ,  C07D405/14 ,  C07D401/14 ,  C07D213/26 ,  C07D498/04 ,  C07D413/04 ,  C07D513/04

CPC classification number: C07D401/04 ,  C07D213/26 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/65038

Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

公开(公告)号：US20160264553A1

公开(公告)日：2016-09-15

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

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.

Abstract translation: 和其药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物），其中R1，Z和n如本文所述。 在某些实施方案中，本文公开的化合物抑制GDF8，并且可以用于通过阻断GDF8信号传导来治疗疾病。

公开(公告)号：US09084795B2

公开(公告)日：2015-07-21

申请号：US13943599

申请日：2013-07-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Vanessa Taylor ,  Rajinder Singh ,  Pingyu Ding ,  Rose Yen

IPC: A61K31/5377 ,  A61K31/551 ,  A61K31/541 ,  A61K31/54 ,  A61K31/5383 ,  C07D487/04 ,  C07D419/14 ,  C07D413/04 ,  C07D491/08 ,  A61K31/5415 ,  C07D401/14 ,  C07D403/12 ,  C07D487/08 ,  A61K31/506 ,  A61K45/06 ,  C07D413/12 ,  C07D471/08 ,  A61K31/538 ,  A61K31/55 ,  A61K31/675 ,  C07D413/14 ,  C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07F9/6558

CPC classification number: C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

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.

Abstract translation: 公开了式I的化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。

公开(公告)号：US20150072959A1

公开(公告)日：2015-03-12

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: C07D495/04 ,  C07D401/04 ,  C07D471/04 ,  C07D417/04 ,  C07D403/14 ,  C07D491/048 ,  C07D249/14 ,  C07D403/04

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：US20140213585A1

公开(公告)日：2014-07-31

申请号：US14243579

申请日：2014-04-02

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D487/08

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.

Abstract translation: 本发明涉及在哺乳动物中治疗与JAK2活性相关的疾病或病症的方法，包括施用式（I）化合物：其中n，m，Y，R 1，R 2，R 3，R 4和R 5在本文中公开， 或药学上可接受的盐。