Ras-farnesyltransferase esulfobutylether-7-ß-cyclodextrin or 2-hydroxypropyl-ß-cyclodextrin inhibitor complex and process

摘要

"RAS-FARNESILTRANSFERASEE SULFOBUTYLÉTER-7- 225 -CYCLODEXTRIN OU2-HYDROXYPROPIL- 225 CYCLODEXTRIN AND PROCESS INHIBITOR COMPLEX". a ras-farnesyltransferase inhibitor complex formed from a ras-farnesyltransferase inhibitor or a pharmacologically acceptable salt thereof, of formula (I), where n is 0 or 1; R ~ 1 ~ is selected from Cl, Br, phenyl, pyridyl or cyano; R ~ 2 ~ is aralkyl; R ~ 3 ~ is selected from lower alkyl, aryl, substituted aryl or heterocycle; Z ~ 1 ~ is selected from CO, S0 ~ 2 ~, CO ~ 2 ~, SO ~ 2 ~ NR ~ 5 ~ R ~ 5 ~ is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7- 225 -cyclodextrin or 2-hydroxypropyl- 225 -cyclodextrin. The complex unexpectedly has high aqueous solubility of the deras-farnesyltransferase inhibitor and is useful for its intravenous release to human beings with cancer. A process for forming the complex is also provided. Ras-farnesyltransferase inhibitors are useful as anti-tumor agents.