Patent ID: 6034135
Filing Date: 2000-03-07
Classification: A61K,C07C,C07K,C12N

Abstract:
A compound of the formulaZ-S-S-Zwherein Z is ##STR5## wherein (a) n is 0, 1 or 2;(b) R.sub.1 is hydroxy, a glyceryl moiety or a lipophilic moiety;(c) R.sub.2 is(i) --NH-[alk.sub.1 --NH].sub.n1 -- wherein n1 is an integer from 0 to 2 and alk.sub.1, is an alkylene group of 2 to 6 carbon atoms;(ii) --[W.sub.1 ].sub.n2 - wherein n.sub.2 is an integer from 0 to 3 and each W.sub.1 is an independently selected amino acid residue;(iii) --N(R.sub.4) (alk.sub.2 -) wherein R.sub.4 is hydrogen, alkyl of 1 to 18 carbon atoms optionally mono-, di- or tri-substituted with Y.sub.1, Y.sub.2 and/or Y.sub.3 ; alkenyl of 2 to about 12 carbon atoms, aryl of about 6 to 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms and alk.sub.2 is a straight chained or branched chain alkylene group of 1 to 18 carbon atoms optionally mono-, di- or tri-substituted with Y.sub.1, Y.sub.2 and/or Y.sub.3 where Y.sub.1, Y.sub.2 and Y.sub.3 are independently selected from the group consisting of arylamine of 5 to about 10 carbon atoms, aralkylamine of 5 to about 10 carbon atoms, heterocylic amine, fluorine, a guanidinium moiety, an amidinium moiety, --NH.sub.2, --NHR.sub.10, --NR.sub.10 R.sub.11, and --N(R.sub.10 R.sub.11 R.sub.12) wherein R.sub.10, R.sub.11 and R.sub.12 are as defined hereinbelow;(d) R, is(i) --NH-[alk.sub.3 ].sub.n3 -H wherein n3 is an integer from 0 to 4 and alk.sub.3 is an alkylene group of 2 to 6 carbon atoms;(ii) --[W.sub.2 ].sub.n4 H wherein n4 is an integer from 0 to 3 and each W.sub.2 is an independently selected amino acid residue;(iii) a negatively charged group selected from the group consisting of -alk.sub.4 C(O)O.sup.- ; -alk.sub.4 -S(O.sub.2)O.sup.- ; -alk.sub.4 P(O)(O.sup.-)O.sup.- and -alk.sub.4 OP(O)(O.sup.-)(O.sup.-) wherein alk.sub.4 is an alkylene group of 1 to 6 carbon atoms;(iv) heterocyclo of 4 to about 10 ring atoms with the ring atoms selected from carbon and heteroatoms, wherein the heteroatoms are selected from the group consisting of oxygen, nitrogen and S(O).sub.i wherein i is 0, 1 or 2;(v) alkyl of 1 to about 12 carbon atoms optionally substituted with a substituent selected from fluoro, a guanidinium moiety, an amidinium moiety, --NH.sub.2, --NHR.sub.10, --NR.sub.10 R.sub.11 or NR.sub.10 R.sub.11 R.sub.12 wherein each of R.sub.10, R.sub.11 and R.sub.12 is independently selected from alkyl of 1 to about 12 carbon atoms, alkyl of 1 to about 12 carbon atoms substituted with 1 to about 25 fluorine atoms and alkenyl of 2 to about 12 carbon atoms; or(vi) W-(CH.sub.2).sub.t --NH--(CH.sub.2).sub.q -- wherein t and q are independently selected integers from 2 to 6 and W is a guanidinium moiety, an amidinium moiety, --NH.sub.2, --NHR.sub.10, --NR.sub.10 R.sub.11, or --NR.sub.10 R.sub.11 R.sub.12 wherein R.sub.10, R.sub.11 and R.sub.12 are as defined herein above, and pharmaceutically acceptable salts thereof.