STEROID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR PHARMACEUTICAL USES

摘要

Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of formula (III), preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z5 is a-H; one Z7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z12 are hydrogen; X' is a polyamine side chain of the formula -NH(CH2)p-NH(CH2)q-N(R11)(R111) where p and q are each independently 3 or 4, and R II and R III are each independently hydrogen or methyl; R' is methyl; and Y' is (C1-C10)-alkyl substituted with a group such as -CO2H or -SO3H. Such compounds, as well as squalamine itself, have antiangiogenic activity and Na+/K+-- ATPase-inhibiting activity.