Forma Therapeutics, Inc.

Aileron Therapeutics, Inc.

Hoffmann-la Roche Inc.

Bradford Graves

Anna M Ericsson

Steven Gregory Mischke

Shawn E R Schiller

Hongbin Li

Angela V West

Torsten Herbertz

Jennifer R Downing

Huw M Nash

Tomi K Sawyer

Vincent Guerlavais

Eric Feyfant

Carl Elkin

Qingjie Ding

Sung-Sau So

Peter Michael Wovkulich

Zhuming Zhang

Jin-Jun Liu

Allen John Lovey

Binh Vu

Giacomo Pizzolato

Xin-Jie Chu

Norman Kong

Jing Zhang

Nan Jiang

David Joseph Bartkovitz

John Lawson Roberts

Shawn ER Schiller

The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.

Inhibiting CREB binding protein (CBP)

The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains (e.g., certain forms of cancer), and methods of synthesis of these compounds.

Inhibiting cyclic AMP-responsive element-binding protein (CREB)

Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors

Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.

Peptidomimetic macrocycles

There are provided compounds of the formula wherein X, Y and Rto Rare described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

Spiroindolinone pyrrolidines

There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereofwherein X, X, R, R, R, R, Rand Rare herein described. The compounds exhibit activity as anticancer agents.

4,4,5,5, tetrasubstituted imidazolines

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Nutley, NJ, United States of America

Bradford Graves