Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1983-04-28
1985-01-29
Schenkman, Leonard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514863, 514561, 514563, 514566, 514567, 514551, 514533, 514534, 514547, 514550, A61K 31195
Patent
active
044965885
ABSTRACT:
A novel method of treating psoriasis which comprises administering a halomethyl derivative of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .gamma.-guanidinopropyl or R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy; a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; and the lactams thereof when Z is R.sub.a HN(CH.sub.2).sub.n -- and each of R.sub.a and R.sub.b is hydrogen; with the proviso that when Z is .gamma.-guanidinopropyl Y is FCH.sub.2 --, F.sub.2 CH-- or F.sub.3 C-- and R.sub.1 is hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof.
REFERENCES:
patent: 2662915 (1953-12-01), Lontz et al.
Rando, "Chemistry & Enzymology of k.sub.G2 T Inhibitors" Science, vol. 5, pp. 320-324 (Jul. 26, 1974).
J. of Medicinal Chemistry, vol. 17, No. 4, pp. 447-451 (1974) and vol. 18 No. 6, pp. 600-604 (1975).
Burger, Medicinal Chemistry, 3rd Ed., Part I, Pub. Wiley Interscience, pp. 65, 7/2, 72 (1970).
Bey Philippe
Jung Michel
McDonald Raymond A.
Merrell Toraude et Compagnie
Schenkman Leonard
Stein William J.
Street Gary D.
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