Indiana University

Li-Fan Zeng

Zhong-Yin Zhang

Maria Kontaridis

Jianxun Wang

Yantao He

Methods are disclosed herein for administering a oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitor for treating autoimmune and/or glomerulonephritis-associated diseases, and in particular, Systemic Lupus Erythematosus (SLE).

Methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors

SHP2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors

Inhibitors of protein tyrosine phosphatases are disclosed. The inhibitors include hydroxyindole carboxylic acids having a linker and an amine scaffold that are potent inhibitors of Src homology 2-domain containing protein tyrosine phosphatase-2.

Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors ofprotein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed inand characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.

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Indianapolis, IN, United States of America

Li-Fan Zeng