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US 6,310,042 B1Granted
Derivatives of carbohydrates and compositions containing them
OwnerLars Persson, Nicola Rehnberginventors
Life of this patent
Estimating the term…
Abstract
The present invention relates to derivatives of phosphorylated carbohydrates and pharmaceutical compositions comprising as a pharmaceutically active ingredient at least one of these compounds.
Claims7
A pharmaceutical composition comprising as a pharmaceutically active ingredient a compound according to formula I
- and a pharmaceutically acceptable carrier, excipient or additive thereof;
- where R21, R31 and R42 are
- where R7 and R8 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+2, R7 and R8 jointly represent the cation;
- (3) a lower alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, pentyl;
- were R22, R32, R41, R61 and R62 are hydrogen
- where one of R11 and R12 is hydrogen, and the other is selected from
- (1) —OR9;
- or
- (3) —NR13R14
- and where R63 is
- (1) OR9;
- or
- (3) —NR13R14,
- where R9 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 R10 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 R13 and R14 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.
55 more elements
A pharmaceutical composition comprising as a pharmaceutically active ingredient a compound according to formula I
- and a pharmaceutically acceptable carrier, excipient or additive thereof;
- where R22, R31 and R42 are
- where R7 and R8 independently are
- (1) hydrogen;
- (2) a cation selected from the group consisting of sodium, potassium and calcium;
- or in the case where the cation is Ca+2, R7 and R8 jointly represent the cation;
- where R21, R32, R41 are hydrogen;
- where R11 and R2 are different and one is hydrogen, and the other is —OR9,
- and where R63 is
- (1) hydrogen;
- (2) —OR9;
- or
- where R9 and R10 independently are
- (1) alkyl or substituted alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, isobutyl, pentyl or hexyl;
- (2) aryl or substitutted aryl selected from the group consistinng of phenyl or biphenyl;
- or
- (3) silyl or substituted silyl.
14 more elements
A pharmaceutical composition comprising as a pharmaceutically active ingredient a compound according to formula I
- and a pharmaceuticaly acceptable carrier, excipient or additive thereof;
- where R21, R32 and R42 are
- where R7 and R8 independently are
- (1) hydrogen;
- (2) a cation selected from the group consisting of sodium, potassium and calcium;
- or in the case where the cation is Ca+2, R7 and R8 jointly represcnt the cation;
- (3) a lower alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, pentyl where P22, R32, R41 are hydrogen;
- where R11 and R12 are different and one is hydrogen, and the other is —OR9
- and where R63 is
- (1) hydrogen;
- (2) —OR9;
- or
- where R9 and R10 independently are
- (1) alkyl or substituted alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, isobutyl, pentyl or hexyl;
- (2) aryl or substituted aryl selccted from the group consisting of phenyl or biphenyl or
- (3) silyl or substituted silyl.
13 more elements
A pharmaceutical composition comprising as a pharmaceutically active ingredient a compound according to formula I
- and a pharmaceutically acceptable carrier, excipicnt or additive thereof;
- where R21, R32 and R41 are
- where R7 and R8 are
- (1) hydrogen;
- (2) a cation selected from the group consisting of sodium, potassium and calcium;
- where R22,
- R31, and R42 are hydrogen;
- where R11 and R12 are different and one is hydrogen, and the other is —OR9,
- and where R63 is
- (1) hydrogen;
- (2) —OR9;
- or
- where R9 and R10 independently are
- (1) alkyl or substituted alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, isobutyl, pentyl, hexyl;
- (2) aryl or substituted aryl selected from the group consisting of phenyl or biphenyl or
- (3) silyl or substituted silyl.
13 more elements
A pharmaceutical composition comprising as a pharmaceutically active ingredient a conpound according to formula I
- and a pharmaceutically acceptable carrer, excipient or additive thereof;
- where R21, R31 and R41 are
- where R7 and R8 are
- (1) hydrogen;
- (2) a cation selected from the group consisting of sodium, potassium or calcium, where R22, R32, and R42 are hydrogen;
- where R11 and R12 are different and one is hydrogen, and the other is —OR9,
- and where R63 is
- (1) —OR9;
- or
- where R9 and R10 independently are
- (1) alkyl or substituted alkyl selected from the group consisting of methyl, ethyl, propyl, butyl, isobutyl, penityl or hexyl;
- (2) aryl or substited aryl selected from the group consisting of phenyl or biphenyl;
- or
- (3) silyl or substituted silyl.
11 more elements
Dependencies are inferred from the claim text.