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：USRE47396E1

公开(公告)日：2019-05-21

申请号：US14918353

申请日：2015-10-20

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/505 ,  A61K31/675 ,  C07D413/12 ,  C07F9/02 ,  C07B59/00 ,  C07D239/02 ,  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.

公开(公告)号：US10233170B2

公开(公告)日：2019-03-19

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 ,  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 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：US20180162848A1

公开(公告)日：2018-06-14

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

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：US20170342048A1

公开(公告)日：2017-11-30

申请号：US15366981

申请日：2017-07-13

Applicant: Rigel Pharmaceuticals, Inc.

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

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

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：US09611260B2

公开(公告)日：2017-04-04

申请号：US14725932

申请日：2015-05-29

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：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：US20150259332A1

公开(公告)日：2015-09-17

申请号：US14725932

申请日：2015-05-29

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

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.

Abstract translation: 公开了式I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。 还公开了制备该化合物的方法。

公开(公告)号：US09067925B2

公开(公告)日：2015-06-30

申请号：US13685433

申请日：2012-11-26

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: A61K31/505 ,  A61K31/675 ,  C07D413/12 ,  C07D239/02 ,  C07F9/02 ,  C07B59/00

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.

Abstract translation: 公开了式I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。 还公开了制备该化合物的方法。

公开(公告)号：US20140107073A1

公开(公告)日：2014-04-17

申请号：US14046834

申请日：2013-10-04

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07F9/6503 ,  C07D417/04 ,  C07D498/04 ,  C07D405/14 ,  C07D401/14 ,  C07D213/26 ,  C07D401/04 ,  C07D471/04

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.

Abstract translation: 描述了式（I）的GCF-8抑制剂及其药学上可接受的盐，其中n，R1，R2，R5，R6，X和Z如本文所定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于抑制细胞中的GDF-8的方法和用于治疗患有疾病或病症的患者的方法，其中患者将从肌肉组织的质量或强度的增加中治疗获益。