Forma Therapeutics, Inc.

University of South Florida

Yale University

Katherine J Kayser-Bricker

Kenneth W Bair

Matthew W Martin

David S Millan

Adam Charles Talbot

Shawn E R Schiller

George P Luke

Torsten Herbertz

Goss S Kauffman

Mark Joseph Tebbe

Said M Sebti

Andrew D Hamilton

Jin Q Cheng

Goss Stryker Kauffman

Mark J Tebbe

Shawn E Schiller

Shawn ER Schiller

The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R, R, R, and Rare as described herein.

Tetrahydroquinoline compositions as BET bromodomain inhibitors

The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R, R, Rand Rare defined herein.

Benzopiperazine compositions as BET bromodomain inhibitors

Tetrahydroquinoline compositions as bet bromodomain inhibitors

Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.

Substrate-mimetic AKT inhibitor

Substrate-mimetic Akt inhibitor

The present invention relates to inhibitors of bromo and extra terminal (BET) br'omodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R, R, Rand Rare defined herein.

Growing community of inventors

Branford, CT, United States of America

Katherine J Kayser-Bricker