Erbb-2 selective small molecule kinase inhibitors
AssigneeGeorgetown University
InventorsShaomeng Wang, Dajun Yang, Istvan Enyedy
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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-(posa-notrophenyl)-2-propynoate.
Claims15
A method of therapy which results in the inhibition of erbB-2 kinase in a subject in need of such inhibition which comprises administering a therapeutically effective amount of at least one compound having one of generic formulae (I) to (V) or a pharmaceutically acceptable salt thereof:
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- wherein R1 is a substituted monocyclic or bicyclic aryl or heteroaryl and R2 is selected from hydrogen, alkyl, and heteroaryl.
The method of 10, wherein the amount of said compound more preferably ranges from 5 mg to 50 mg/kg of the weight of said subject.
Dependencies are inferred from the claim text.