University of Texas System

Baylor College of Medicine

Navire Pharma, Inc.

Pijus K Mandal

Philip Jones

Jason Cross

Christopher Lawrence Carroll

John S McMurray

Kang Le

Michael J Soth

Barbara Czako

Timothy Joseph McAfoos

Pietro Morlacchi

Morgan Knight

David B Corry

Fredika Robertson

Zhiyong Ren

Warren S Liao

Xiaomin Chen

Ramesh Rajaopal

The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

Imidazopiperazine inhibitors of transcription activating proteins

The present invention relates to compounds which are useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

PTPN11 inhibitors

The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.

STAT6 inhibitors

Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.

Inhibitors of STAT3 and uses thereof

Growing community of inventors

Houston, TX, United States of America

Pijus K Mandal