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Lipophilic drug derivatives for use in liposomes

  • US 5,534,499 A
  • Filed: 05/19/1994
  • Issued: 07/09/1996
  • Est. Priority Date: 05/19/1994
  • Status: Expired due to Fees
First Claim
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1. A pharmaceutical compound for use in liposome and micellar formulations, said compound being a member selected from the group consisting of compounds of formula I and compounds of formula II:

  • ##STR21## wherein, A is a member selected from the group consisting of a serine radical, an ethanolamine radical, a choline radical, a phosphocholine radical, a phosphoserine radical, a phosphoethanolamine radical, a glycerol radical, a phosphoglycerol radical, an inositol radical, a phosphoinositol radical, --NR1 R2, --OCOR3, --OH, --O--glucose, --O--galactose and --O--oligosaccharide;

    wherein,R1 and R2 are each members independently selected from the group consisting of H and lower alkyl; and

    R3 is a member selected from the group consisting of alkyl radicals and unsaturated alkyl radicals;

    X1 and X2 are each members independently selected from the group consisting of alkyl, unsaturated alkyl, alkyl linking group, and unsaturated alkyl linking group;

    Y1 and Y2 are each members independently selected from the group consisting of --S--, --NH--, --NHCO--, --CO(CH2)p CO2 --, --O--, ═

    NNHCO--, --CO-- and --CO(CH2)p CONH--, wherein p is an integer of from 0 to 8;

    Z1 and Z2 are each independently a therapeutic agent; and

    m and n are each independently an integer of from 0 to 1, with the proviso that n+m is at least 1; and

    with the further provisos that when m is 0, X1 is not a linking group, and when n is 0 that X2 is not a linking group.

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