Rigel Pharmaceuticals, Incorporated

Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Torch Therapeutics

Rigel Pharmacauticals, Inc.

Todd M Kinsella

Mark K Bennett

Rajinder Paul Singh

Marina Gelman

Esteban Masuda

David C Anderson

Justin E Warner

Somasekhar Bhamidipati

Taisei Kinoshita

Donald G Payan

Jiaxin Yu

Ihab S Darwish

Pingyu Ding

Jeffrey Clough

Robert Michael Borzilleri

Upender Velaparthi

Jayakumar Sankara Warrier

Yasumichi Hitoshi

Hasibur Rahaman

Hui Hong

Peiying Liu

Ramesh Bhatt

James Bradley Lorens

Todd R Pray

Chetan Padmakar Darne

Kristen Baltgalvis

Wei Ey Li

Mary Shen

James B Lorens

X Charlene Liao

Simon Yu

Peter Chu

Denise Pearsall

Annabelle Freiro

Chetan Padmakar Dame

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 Rare 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.

TGF-β inhibitors

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 Rare as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-&#x3b2; superfamily, and can be used to treat disease by blocking such activity.

TGF-&#x3b2; inhibitors

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, Rand R' are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-&#x3b2;, and can be used to treat disease by blocking TGF-&#x3b2; signaling.

TGF-beta inhibitors

This invention describes the design of bispecific antibodies that function as conditionally effective therapeutics by binding to a functionally silent epitope on one component of a targeted signaling complex and simultaneously binding to a second protein, whose expression or accessibility is cell- or disease environment-specific, and whose antibody-driven proximity to the signaling complex leads to an alteration of signal transduction.

Method of using a bispecific antibody to conditionally inhibit a receptor signaling complex

The present disclosure provides antibodies that specifically bind to and block signaling by ACVR2A, i.e., ACVR2A but not ACVR2B, as well as methods for using the same. The antibodies may be used for the treatment of a number of conditions associated with muscle atrophy, as well as other conditions.

ACVR2A-specific antibody and method of treatment of muscle atrophy

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-&#x3b2; superfamily, and can be used to treat disease by blocking such activity. 

TGF-&#xdf; inhibitors

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-&#x3b2; superfamily such as Nodal or Activin.

2,3-Disubstituted pyridine compounds as TGF-&#x3b2; inhibitors and methods of use

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 Rare as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-&#x3b2; superfamily, and can be used to treat disease by blocking such activity. 

TGF-&#x3b2; inhibitorC

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

Antigen binding molecules to TIGIT

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, R, Rm, p and a are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-&#x3b2;, and can be used to treat disease by blocking TGF-&#x3b2; signaling. 

Fused imidazole derivatives as TGF-beta inhibitors

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-&#x3b2; superfamily such as Nodal or Activin. 

2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use

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 R, 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.

GDF-8 inhibitors

A construct system for expressing a reporter protein, as well as a transgenic animal and a screening method employing the same, are provided. In certain embodiments, the construct system is a three component system in which expression of a reporter protein from a reporter construct is induced by a transcription factor that is produced using two other constructs, each producing a different part of the transcription factor. The parts of the transcription factor are ligated together. Expression of the reporter only occurs in tissues in which both of the parts of the transcription factor are produced.

In vivo reporter system

Growing community of inventors

Fayetteville, NC, United States of America

Todd M Kinsella