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

摘要

A RAS-FARNESYLTRANSFERASE INHIBITOR COMPLEX FORMED OF RAS-FARNESYLTRANSFERASE INHIBITOR OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, OF THE FORMULA I WHEREIN N IS 0 OR 1; R1 IS SELECTED FROM C1, 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 -(BETHA)- CYCLODEXTRIN OR 2-HYDROXYPROPYL-(BETHA)-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.