Millennium Pharmaceuticals Limited

Zhigen Hu

Steven P Langston

He Xu

Hirotake Mizutani

Matthew O Duffey

Dylan Bradley England

Charles McIntyre

Koji Ono

Brian Scott Freeze

Zhan Shi

Stepan Vyskocil

Yongbo Hu

Masaaki Hirose

Hong Myung Lee

Tianlin Xu

Charles Mcintyre

Mitsuhiro Ito

Scott Freeze

Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, R, R', R, R, X, X, X, R, Z, and Zhave the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Heteroaryl compounds useful as inhibitors of SUMO activating enzyme

Heteroaryl compounds useful as inhibitors of sumo activating enzyme

Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, R, R, R, R, X, X, X, R, Z, and Zhave the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Disclosed are compounds of formula (I); or a pharmaceutically acceptable salt thereof; wherein Y, R, R, R, R, X, R, R, R, R, m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders. 

Heteroaryl inhibitors of sumo activating enzyme

This invention provides compounds of formula IA or IB: wherein HY, R, R, G, W, n, and A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders. 

Heteroaryls and uses thereof

This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R, R, G, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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Newton Center, MA, United States of America

Zhigen Hu