Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-11-20
1998-10-20
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514212, 514218, 5142225, 5142282, 5142292, 5142335, 514241, 514247, 514255, 514359, 514364, 514369, 514372, 514374, 514378, 514383, 514397, 514406, 514450, A61K 31365, A61K 3155
Patent
active
058246746
ABSTRACT:
Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.
REFERENCES:
Haerri, E. et al., Chemical Abstract 59, 5726h (1963).
Banerjee, P.K. et al., Design of Prodrugs, Bundgaard, H. ed. (Elsevier Science, Amsterdam), pp. 93-96 (1985).
Kovach, I.M. et al., J. Pharm. Sci. 64:1070-1071 (1975).
Connors, T.A., Xenobiotica 16:975-988 (1986).
Kane, Jr. Charles Theodore
Malspeis Louis
Supko Jeffrey G.
Vishnuvajjala B. Rao
Raymond Richard L.
Starks Associates
The United States of America as represented by the Department of
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