Indiana University

Purdue Research Foundation

University of Florida Research Foundation, Incorporated

Wisconsin Alumni Research Foundation

Zhong-Yin Zhang

Li-Fan Zeng

Sheng Zhang

Mingji Dai

Dexter Cameron Davis

Rongjun He

Maria Kontaridis

Alexander Adibekian

Dominic Gregor Hoch

Jianxun Wang

Ben Shen

Yantao He

Kasi Viswanatharaju Ruddraraju

Jianping Lin

The present disclosure relates to novel sesquiterpenoid compounds as SHP2 and/or POLE3 inhibitors for potential treatment for cancers, and to methods of making and using the sesquiterpenoid compounds. The present invention therefore provides a method of using the disclosed compounds as chemosensitizations agent to a DNA damaging drugs for cancers.

Sesquiterpenoid analogs

The present disclosure relates to novel lymphoid-specific tyrosine phosphatase (LYP, encoded by the PTPN22 gene) inhibitors, and to methods of making and using the novel LYP inhibitors. Thus, the compounds according to the disclosure may be used for treating diseases or disorders associated with PTPN22 genetic polymorphism, including type 1 diabetes, rheumatoid arthritis, systemic lupus erythematosis, Graves' disease, Addison's disease, vitiligo, juvenile arthritis, Hashimoto thyroiditis, and other rarer diseases. Furthermore, these LYP inhibitors may be served for a novel class of cancer immunotherapy. The compounds can be injected or orally administered.

Lymphoid-specific tyrosine phosphatase (LYP) inhibitors

The present disclosure relates to novel N-aryl oxamic acid based inhibitors forprotein tyrosine phosphatase B (mPTPB), and to the method of making and using the novel N-aryl oxamic acid based inhibitors. More specifically, compounds provided in this disclosure can be used to inhibitprotein tyrosine phosphatase B (mPTPB) and to treat a patient having a Tuberculosis disease.

N-aryl oxamic acids

Small molecule compounds derived from &#x3b1;-sulfophenylacetic amide (SPAA) are provided as novel sulfonic acid based pTyr mimetics. These compounds effectively inhibit a variety of protein tyrosine phosphatases (PTPs), such as mPTPA, mPTPB, LMWPTP, and Laforin. Use of these compounds as pharmaceutical agents for treating diseases associated with abnormal protein tyrosine phosphatase activity is also provided.

Small molecule inhibitors of protein tyrosine phosphatases and uses thereof

Protein tyrosine phosphatases or SHP2 inhibitors and uses thereof

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

Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.

Inhibitors of protein tyrosine phosphatases

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.

[object Object]

Novel protein tyrosine phosphatase (PTP) inhibitor compounds synthesized from phosphonodifluoromethyl phenylalanine (F2Pmp) are provided. Use of these compounds for inhibiting a PTP enzyme (such as PTP-MEG2), as well as treating a disease, disorder, or condition associated with inappropriate activity of a PTP (such as type 2 diabetes), is also provided.

The present invention relates to tautomycetin (TTN) and analogs thereof. Also provided are methods of using TTN and analogs thereof in the treatment of various diseases relating to SHP2 function.

Growing community of inventors

Carmel, IN, United States of America

Zhong-Yin Zhang