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Last Updated: April 19, 2024

Claims for Patent: 7,427,689


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Summary for Patent: 7,427,689
Title:ErbB-2 selective small molecule kinase inhibitors
Abstract: A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is \"compound B17\"=methyl-(p-nitrophenyl)-2-propynoate.
Inventor(s): Wang; Shaomeng (Saline, MI), Yang; Dajun (Rockville, MD), Enyedy; Istvan (Hamden, CT)
Assignee: Georgetown University (Washington, DC)
Application Number:10/343,267
Patent Claims:1. A compound that inhibits erbB-2 kinase activity through targeting the SER783 residue of an erbB-2 protein, wherein said compound is ##STR00003## or a pharmaceutically acceptable salt thereof.

2. The composition of claim 1, wherein said composition is able to inhibit cellular proliferation of cells overexpressing erbB-2.

3. A pharmaceutical composition comprising the composition of claim 1, and a herceptin based anti-cancer agent.

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