Patent ID: 6310042
Filing Date: 2001-10-30
Classification: A61P,C07H

Abstract:
A pharmaceutical composition comprising as a pharmaceutically active ingredient a compound according to formula I ##STR22##and a pharmaceutically acceptable carrier, excipient or additive thereof;where R.sub.21, R.sub.31 and R.sub.42 are ##STR23##where R.sub.7 and R.sub.8 independently are(1) hydrogen;(2) a cation selected from the group consisting of sodium, potassiumn and calcium; or in the case where the cation is Ca.sup.+2, R.sub.7 and R.sub.8 jointly represent the cation;(3) a lower alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, pentyl; were R.sub.22, R.sub.32, R.sub.41, R.sub.61 and R.sub.62 are hydrogenwhere one of R.sub.11 and R.sub.12 is hydrogen, and the other is selected from(1) --OR.sub.9 ; ##STR24##or(3) --NR.sub.13 R.sub.14and where R.sub.63 is(1) OR.sub.9 ; ##STR25##or(3) --NR.sub.13 R.sub.14,where R.sub.9 is(a) straight or branched alkyl with 1 to 24 carbon atoms;(b) cycloalkyl with 3 to 16 carbon atoms;(c) alkenyl with 2 to 24 carbon atoms;(d) cycloalkenyl with 4 to 16 carbon atoms;(e) aryl with 6 to 24 carbon atoms;(f) aralkyl;(g) alkaryl;(h) aralkenyl;(i) alkenylaryl;(j) a heterocyclic group with at least one atom of oxygen, nitrogen or sulfur;(k) a glycosyl residue;(l) a glyropeptide;(m) a glycoprotein;(n) a glycolipid;(o) carboxy, sulfonyl or phosphonyl;(p) silyl or substituted silyl; or(q) hydrogen;wherein the above groups (a) to (n) are unsubstituted or substituted with hydroxy, oxo, alkoxy, aryloxy, halocyano, isocyanato, carboxy, esterifed carboxy, amino, substituted amino, formyl, acyl, acyloxo, acylamino, sulfinyl, sulfonyl, phosphino, phosphinyl, phosphonyl, mercapto, alkylthio, arylthio, silyl, silyloxy, silylthio, nitro or azido;where R.sub.10 is(a) straight or branched alkyl with 1 to 24 carbon atoms;(b) cycloalkyl with 3 to 16 carbon atoms;(c) alkenyl with 2 to 24 carbon atoms;(d) cycloalkenyl with 4 to 16 carbon atoms;(e) aryl with 6 to 24 carbon atoms;(f) aralkyl;(g) alkaryl;(h) aralkenyl;(i) alkenylaryl;(j) a heterocyclic group with at least one atom of oxygen, nitrogen or sulfur;(k) carboxy or esterified carboxy;(l) amino or substituted amino; or(m) hydrogen,wherein the above groups (a) to (i) are unsubstituted or substituted with hydroxy, oxo, alkoxy, aryloxy, halocyano, isocyanato, carboxy, esterfied carboxy, amino, substituted amino, formyl, acyl, acyloxo, acylamino, sulfinyl, sulfonyl, phosphino, phospinyl, phosphonyl, mercapto, alkylthio, arylthio, silyl, silyloxy, silylthio, nilro or azido;and where R.sub.13 and R.sub.14 are(a) hydrogen;(b) hydroxyl;(c) lower acyl selected from the group consisting of formyl, acetyl, propionyl, butyryl, valeryl, pivaloyl; or(d) lower alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, pentyl or hexyl.