发明名称 A ras-farnesyltransferase inhibitor complex that is stable and water soluble and useful as an anti-tumour agent
摘要 Described is 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. 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- tumour agents.
申请公布号 NZ511995(A) 申请公布日期 2003.11.28
申请号 NZ19990511995 申请日期 1999.12.21
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 VARIA, SAILESH A;MALLOY, TIMOTHY M;RAGHAVAN,KRISHNASWAMY S
分类号 C07D403/06;A61K9/08;A61K31/55;A61K31/5513;A61K47/12;A61K47/40;A61K47/48;A61P35/00;C07D243/14;C07D409/14;(IPC1-7):A01N43/00 主分类号 C07D403/06
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