COMPLEX OF RAS-FARNESYLTRANSFERASE INHIBITOR AND SULFOBUTYLETHER-7-.BETA.-CYCLODEXTRIN OR 2-HYDROXYPROPYL-.BETA.-CYCLODEXTRIN AND METHOD

A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of formula (I), wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl o...

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Bibliographische Detailangaben
Hauptverfasser:	VARIA, SAILESH A, RAGHAVAN, KRISHNASWAMY S, MALLOY, TIMOTHY M
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of formula (I), wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2 or SO2NR5, R5 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.