Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1992-11-05
1996-02-06
Brust, Joseph Paul
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514 90, 514 91, 544148, 548517, 549221, A61K 3121, A61K 31665, A61K 3140, C07D31912
Patent
active
054895804
ABSTRACT:
Novel compounds and use therefor in treating neoplastic and immune system disorders are disclosed. The compound of the present invention comprises a substituted lysophospholipid, which includes a C12 to C20 alkyl ether, a C12 to C20 thioether, or a substituted C3 to C6 heterocycle containing at least two ring heteroatoms, selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof; and also includes a choline group or a C4 to C7 heterocycle containing heteroatoms selected from the group consisting of nitrogen, oxygen, sulfur and combinations thereof.
The method for treating neoplastic or immune system disorders includes administering an effective dose of a compound of the present invention in a therapeutic manner. Effective doses of these compounds result in cytotoxic effects upon various leukemic cell lines.
The compounds of this invention have the advantage that these compounds possess antineoplastic and immunomodulatory characteristics. Thus, these compound are suited for use, for example, as a drug for the therapeutic treatment of cancers, leukemias and immune system diseases.
REFERENCES:
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K. Meyer et al., "In Vitro Evaluation of Phosphocholine and Quaternary Ammonium Containing Lipids as Novel Anti-HIV Agents", J. Med. Chem. 34:1377-1383 (1991).
Duclos, et al.; J. Org. Chem., 57(23), pp. 6156-6163, (1992); "Synthesis of All Four Stereoisomers which are Conformationally Constrained 1,4-Dioxanyl Analogs of the Antineoplastic Ether Lipid ET-18-OCH.sub.3 ".
Duclos, Jr. Richard I.
Fournier Donna J.
Makriyannis Alexandros
Brust Joseph Paul
University of Connecticut
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