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：US10822337B2

公开(公告)日：2020-11-03

申请号：US15563075

申请日：2016-03-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 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：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：US20210276982A1

公开(公告)日：2021-09-09

申请号：US17324320

申请日：2021-05-19

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D403/12 ,  A61P35/02 ,  C07D401/12 ,  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 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：US20210130361A1

公开(公告)日：2021-05-06

申请号：US17087459

申请日：2020-11-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 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：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：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：US20130310340A1

公开(公告)日：2013-11-21

申请号：US13895152

申请日：2013-05-15

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Donald G. Payan ,  Esteban Masuda ,  Todd Kinsella

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/541 ,  A61K31/506 ,  A61K31/554

CPC classification number: A61K31/519 ,  A61K31/00 ,  A61K31/437 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553 ,  A61K31/554 ,  A61K31/675 ,  A61K45/06

Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.

Abstract translation: 公开了一种治疗肌肉退化的方法。 还公开了化合物的实施方案，以及包含该化合物的组合物，用于抑制肌肉恶化，包括萎缩，营养不良和恶病质，例如可能由通气引起。