Title:
【発明の名称】ステロイド誘導体、それらを含む薬剤組成物、及びそれらの薬剤学的用途
Document Type and Number:
Japanese Patent JPH09509959
Kind Code:
A
Abstract:
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 alpha -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(R)(R) where p and q are each independently 3 or 4, and R and R 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.
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Inventors:
Free Lee L.
Zaslov Michael A.
Kinney William A.
Moriarty Robert
Collins Delwood Sea.
Zaslov Michael A.
Kinney William A.
Moriarty Robert
Collins Delwood Sea.
Application Number:
JP52342995A
Publication Date:
October 07, 1997
Filing Date:
September 13, 1994
Export Citation:
Assignee:
Magainin Pharmaceuticals, Inc.
International Classes:
A61P31/04; C07J9/00; C07J17/00; C07J31/00; A61K31/56; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): C07J41/00; A61K31/56; C07J43/00; C07J51/00
Attorney, Agent or Firm:
Shimizu Hatsushi