.alpha.-acetylenic derivatives of amines

C - Chemistry – Metallurgy – 07 – H

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260/468, 260/543

C07H 19/16 (2006.01) C07C 279/12 (2006.01)

Patent

CA 1090790

ABSTRACT OF THE DISCLOSURE Novel acetylenic derivatives of amines of the follow- ing general structure: Image wherein Z is .beta.-methylthioethyl, .beta.-benzylthioethyl, S- (5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidino- propyl, or Image wherein n is 2 or 3 and R1 is hydrogen or lower alkyl from 1 to 4 carbon atoms with the proviso that when R1 is other than hydrogen, n is 2; and each of Ra and Rb 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 Image wherein R2 is hydrogen, a straight or branched lower alkyl of from 1 to 4 carbon atoms, benzyl or ?-hydroxybenzyl; with the provisos that when Z is .beta.-benzyl- thioethyl or S-(5'-sesoxyandenosin-5'-yl)-S-methylthioethyl, Rb is hydrogen, and when Z is Image each of Ra and Rb can be the same or different; and pharmaceutically acceptable salts and individual optical isomers thereof.

304897

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