Rigel Pharmaceuticals, Incorporated

Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Marina Gelman

Rajinder Paul Singh

Todd M Kinsella

Somasekhar Bhamidipati

Jeffrey Clough

Jiaxin Yu

Ihab S Darwish

Pingyu Ding

Donald G Payan

Robert Michael Borzilleri

Upender Velaparthi

Jayakumar Sankara Warrier

Hasibur Rahaman

Hui Li

Darren J McMurtrie

Sambaiah Thota

Carlos A Valdez

Hui Hong

Peiying Liu

John Yudhistir Ramphal

Andy Atuegbu

Chetan Padmakar Darne

Chetan Padmakar Dame

John Ramphal

Darren Mcmurtrie

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

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

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

Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R, R, R, R, 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.

Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

Growing community of inventors

San Francisco, CA, United States of America

Marina Gelman