Syros Pharmaceuticals, Inc.

Dana-farber-cancer Institute Inc.

University of Massachusetts

Whitehead Institute for Biomedical Research

Michael Robert McKeown

Matthew Lucas Eaton

James Elliott Bradner

David A Orlando

Cindy Collins

Mei Wei Chen

Matthew G Guenther

Nan Ke

Jeremy Lopez

Jun Qi

Christopher Fiore

Christian Fritz

Emily Payton Lee

Nathanael Schiander Gray

Dennis Buckley

Jason J Marineau

Richard A Young

Kwok-kin Wong

Margaret A Shipp

Peter B Rahl

Wei Zhang

Bjoern Chapuy

Harry Hongning Fu

Shuai Liu

Zhao Chen

The present invention provides methods for treating cancer using combinations of bromodomain and extra-terminal (BET) protein inhibitors and certain chemotherapeutic drugs.

Combination therapy for cancer using bromodomain and extra-terminal (BET) protein inhibitors

The invention provides methods that define cellular populations that are sensitive to RARA agonists and identify patient subgroups that will benefit from treatment with RARA agonists. The invention also provides packaged pharmaceutical compositions that comprise a RARA agonist and instructions for determining if such agonist is suitable for use in treatment.

Methods of stratifying patients for treatment with retinoic acid receptor-alpha agonists

Described herein are methods that define cellular populations that are sensitive to RARA agonists and identify patient populations that will benefit from treatment with RARA agonists. The methods may comprise administering RARA agonists to patient populations.

Methods of stratifying patients for treatment with retinoic acid receptor-&#x3b1; agonists

The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception. 

Uses of diazepane derivatives

The present invention provides novel compounds of any one of Formulae (I) to (IV), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I) to (IV) are believed to be inhibitors of bromodomain-containing proteins (e.g., bromo and extra terminal proteins (BETs)). Also provided are methods, uses, and kits using the inventive compounds and pharmaceutical compositions for inhibiting the activity of the bromodomain-containing proteins and for treating and/or preventing in a subject in need thereof diseases associated with bromodomain-containing proteins, such as proliferative diseases. 

Inhibitors of transcription factors and uses thereof

The present invention provides compounds of any one of Formulae (I), (II-C) (e.g., Formula (II)), and (III), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I), (II-C), and (III) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception. 

Diazepane derivatives and uses thereof

The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The present invention further provides methods of using the compounds described herein for treating Myc-mediated disorders (e.g., cancer and other proliferative diseases). The present invention also provides assays for identifying Myc inhibitors. 

Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors

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Brookline, MA, United States of America

Michael Robert McKeown