Complex of ras-farnesyltransferase inhibitor and sulfobutylether-7-.beta.-cyclodextrin or 2-hydroxypropyl-.beta.-cyclodextrin and method
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United States of America Patent
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Apr 17, 2001
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N/A
app pub date -
Jan 17, 2000
filing date -
Jan 21, 1999
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Abstract
A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of the formula I ##STR1## wherein n is 0 or 1; R.sub.1 is selected from Cl, Br, phenyl, pyridyl or cyano; R.sub.2 is aralkyl; R.sub.3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z.sub.1 is selected from CO, SO.sub.2, CO.sub.2, or SO.sub.2 NR.sub.5, R.sub.5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7-.beta.-cyclodextrin or 2-hydroxypropyl-.beta.-cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.
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