The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Mar. 20, 1984
Filed:
Jun. 25, 1982
Philippe Bey, Strasbourg, FR;
Michel Jung, Illkirch-Graffenstaden, FR;
Merrell Toraude et Compagnie, Strasbourg, FR;
Abstract
Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: wherein Y is ClCH.sub.2, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR1## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; 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 .rho.-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 .rho.-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 provisos that when Z is .gamma.-guanidinopropyl or .beta.-methylthioethyl, Y is FCH.sub.2 --, F.sub.2 CH-- or F.sub.3 C--; when Z is .gamma.-guanidinopropyl, R.sub.1 is hydroxy; and when Z is .beta.-thioethyl, .beta.-benzylthioethyl, S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl ##STR4## Y and Y.sub.2 are FCH.sub.2 --, F.sub.2 CH--, or F.sub.3 C-- and are the same, each of R.sub.a and R.sub.b is hydrogen and R.sub.1 is hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof.