公开(公告)号：US12227508B2

公开(公告)日：2025-02-18

申请号：US17962305

申请日：2022-10-07

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：US11466018B2

公开(公告)日：2022-10-11

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：US11352360B2

公开(公告)日：2022-06-07

申请号：US16360162

申请日：2019-03-21

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

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Dame ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  A61P35/00 ,  C07D417/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US11021468B2

公开(公告)日：2021-06-01

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: A61P35/02 ,  C07D401/12 ,  C07D403/12 ,  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 (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：US10759855B2

公开(公告)日：2020-09-01

申请号：US15829422

申请日：2017-12-01

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ramesh R. Bhatt ,  Todd Kinsella ,  Wei Li

IPC: C07K16/28 ,  A61K39/395 ,  A61P17/06 ,  A61P19/02 ,  A61P31/18 ,  A61P1/00 ,  A61P35/00

Abstract: Provided herein are antigen binding molecules that bind to TIGIT, include antibodies and antigen binding fragments thereof.

公开(公告)号：US20190284155A1

公开(公告)日：2019-09-19

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

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：US09884868B2

公开(公告)日：2018-02-06

申请号：US15054895

申请日：2016-02-26

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

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US20200339678A1

公开(公告)日：2020-10-29

申请号：US16925818

申请日：2020-07-10

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ramesh R. Bhatt ,  Todd Kinsella ,  Wei Li

IPC: C07K16/28 ,  A61P17/06 ,  A61P19/02 ,  A61P31/18 ,  A61P1/00 ,  A61P35/00

Abstract: Provided herein are antigen binding molecules that bind to TIGIT, including antibodies and antigen binding fragments thereof.

公开(公告)号：US10696693B2

公开(公告)日：2020-06-30

申请号：US15527908

申请日：2015-11-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Todd Kinsella ,  Jiaxin Yu ,  Marina Gelman ,  Ihab S. Darwish

IPC: C07D498/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/424 ,  A61K31/428 ,  A61K31/498 ,  A61P19/02 ,  A61K31/416 ,  A61K31/4188 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

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.