A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/5513 (2006.01) A61K 47/40 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2359646
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.
L'invention concerne un complexe d'inhibiteur de la ras-farnésyltransférase, constitué d'un inhibiteur de la ras-farnésyltransférase ou d'un sel de celui-ci, acceptable au plan pharmaceutique, de formule (I), dans laquelle n vaut 0 ou 1; R1 est choisi parmi Cl, Br, phényle, pyridyle or cyano; R2 représente aralkyle; R3 est choisi parmi alkyle inférieur, aryle ou hérétocyclo ou aryle substitué; Z1 est choisi parmi CO, SO2, CO2 ou SO2NR5, R5 est choisi parmi hydrogène, alkyle inférieur ou alkyle substitué; et sulfobutyléther-7- beta -cyclodextrine ou 2-hydroxypropyl- beta -cyclodextrine. L'inhibiteur de ras-farnésyltransférase dudit complexe présente une solubilité aqueuse étonnamment élevée et ledit complexe est utile dans l'administration intraveineuse à des humains souffrant de cancer. L'invention porte également sur un procédé de formation du complexe. Les inhibiteurs de ras-farnésyltransférase sont utiles en tant qu'agents antitumoraux.
Malloy Timothy M.
Raghavan Krishnaswamy S.
Varia Sailesh A.
Bristol-Myers Squibb Company
Gowling Lafleur Henderson Llp
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