Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1994-03-08
1995-11-14
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514619, 514622, 514629, A61K 31165, A61K 3116
Patent
active
054667151
ABSTRACT:
Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;
R is alkyl;
R.sup.1 is --OH;
R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; and
R.sup.3 is a lipophilic moiety selected from the group consisting of substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.16 cycloalkyl and 2,4-di-t-pentylphenyl.
REFERENCES:
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Gillis et al., Nature, 268, 154-156, 1977.
Farrar J. et al., J. Immunol, 121, 1353-1360, 1978.
Gillis et al., J. Immunol 120, 2027-2033, 1978.
Gillis et al, J. Immunol 124, 1954-1962 1980.
Gillis et al, J. Immunol 125, 2570-2578, 1980.
Gillis et al, J. Exp Med, 152, 1709-1719, 1980.
Illig Carl R.
Latimer Lee H.
Lussier Barbara B.
Washburn William N.
Balogh Imre (Jim)
Davis William J.
Goldberg Jerome D.
Sterling Winthrop Inc.
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