Bristol-myers Squibb Compnay

Rigel Pharmaceuticals, Incorporated

Bristol Meyers Squibb Company

Ensemble Therapeutics Corporation

Robert Michael Borzilleri

Zhen-Wei Cai

Soong-Hoon Kim

Kyoung S Kim

Gregory D Vite

Yong Zhang

Sanjeev Gangwar

Jayakumar Sankara Warrier

James A Johnson

Ivar M McDonald

Naidu S Chowdari

Rajeev S Bhide

Upender Velaparthi

Rajinder Paul Singh

Todd M Kinsella

Brian E Fink

John S Tokarski

John T Hunt

Peiying Liu

Marina Gelman

Andrew J Tebben

Jiaxin Yu

Ihab S Darwish

Hui Hong

Xiao-Tao Chen

Lalgudi S Harikrishnan

Alicia Regueiro-Ren

Wayne D Vaccaro

David K Williams

Somasekhar Bhamidipati

Michael A Poss

Kap-Sun Yeung

Pingyu Ding

Percy H Carter

Gretchen M Schroeder

Heidi L Perez

Tram N Huynh

Hasibur Rahaman

Donna Wei

Ligang Qian

Lyndon A M Cornelius

Erik M Stang

Robert J Schmidt

Liping Zhang

Chetan Padmakar Darne

Walter Lewis Johnson

Andrew Forrest Donnell

Gerhard H&ouml;fle

Gopikishan Tonukunuru

Thomas Leibold

Balaji Seshadri

Zhong Chen

Peter Zheng

Yufen Zhao

Michael Matthew Miller

Heng Cheng

Robert F Kaltenbach, Iii

Muthoni G Kamau

Andrew W Fraley

William P Gallagher

Denis Favreau

Shankar Swaminathan

Zhenrong Guo

Ivar M Mcdonald

John E Thornton

Manjunatha Narayana Rao Kamble

Raju Mannoori

Benjamin A Seigal

Tai W Wong

Robert C Livingston

Wen Sen Li

Chetan Padmakar Dame

Benjamin Adam Seigal

Lyndon A Cornelius

Nicholas Terrett

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

The invention relates generally to compounds of formula (I) that modulate the activity of TGF&#x3b2;R-1 and TGF&#x3b2;R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. 

TGF beta receptor antagonists

The invention relates generally to compounds that modulate the activity of TGF&#x3b2;R-1 and TGF&#x3b2;R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. 

The invention relates generally to compounds that modulate the activity of TGF&#x3b2;R-1 and TGF&#x3b2; R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

TGF&#x3b2; receptor antagonist

The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

TGF-&#x3b2; inhibitors

Benzodiazepine dimers having a structure represented by wherein Ris wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Benzodiazepine dimers, conjugates thereof, and methods of making and using

Tubulysin analogs of the formula (I) where R, RR, R, R, R, R, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Tubulysin analogs and methods of making and 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

Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).

Macrocyclic benzodiazepine dimers, conjugates thereof, preparation and uses

Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; Ris and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Heteroarylene-bridged benzodiazepine dimers, conjugates thereof, and methods of making and using

There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention. 

IAP antagonists

The invention relates generally to compounds that modulate the activity of TGF&#x3b2;R-1 and TGF&#x3b2;R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

TGF&#x3b2;R antagonists

Growing community of inventors

New Hope, PA, United States of America

Robert Michael Borzilleri