Solid support matricles containing a toxin binding oligosaccharide
AssigneeSynsorb Biotech, Inc.
InventorsOle Hindsgaul, Ulf J. Nilsson
Life of this patent
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Abstract
Disclosed are novel solid support matrices having a toxin-binding oligosaccharide covalently attached to a solid support through a linking arm which has at least 8 atoms separating the oligosaccharide from the solid support. The disclosed solid support matrices are useful for neutralizing toxins from disease-causing microrganisms.
Claims10
A solid support matrix of the formula:
- ##STR7## wherein SS is a solid support;
- R.sup.1 is selected from the group consisting of a covalent bond and a hydrocarbylene group having from 1 to about 20 carbon atoms,
- R.sup.2 is a hydrocarbylene group of from 2 to 20 carbon atoms;
- each X' is independently selected from the group consisting of --O-- and>NR.sup.4 wherein each R.sup.4 is independently selected from hydrogen, R.sup.2 NH.sub.2 or R.sup.2 NR.sup.3 Z wherein R.sup.2 is as defined above;
- R.sup.3 is selected from the group consisting of hydrogen and --C(O)R.sup.5 wherein R.sup.5 is selected from the group consisting of hydrogen and hydrocarbyl of from 1 to 20 carbon atoms;
- W is selected from oxygen or sulfur;
- X is selected from the group consisting of --NH--, --O-- and --S--;
- Y is selected from the group consisting of --NH--, --O-- and --S--,
- Z is toxin-binding oligosaccharide;
- p is an integer from 0 to 50;
- and
- n is an integer such that the matrix has a loading level of the toxin-binding oligosaccharide of from about 0.001 to about 2000 .mu.moles per gram of solid support
- wherein the total number of atoms separating the solid support from the toxin- binding oligosaccharide is at least 8.
A solid support matrix of the formula:
- ##STR8## wherein SS is a solid support;
- R.sup.1 is selected from the group consisting of a covalent bond and a hydrocarbylene group having from 1 to about 20 carbon atoms;
- R.sup.3 is selected from the group consisting of hydrogen and --C(O)R.sup.5 wherein R.sup.5 is elected from the group consisting of hydrogen and hydrocarbyl of from 1 to 20 carbon atoms;
- R.sup.6 is an alkylene group of from 4 to 10 carbon atoms.
- Z is toxin-binding oligosaccharide, and
- n is an integer such that the matrix has a loading level of the toxin-binding oligosaccharide of from about 0.001 to about 2000 .mu.moles per gram of solid support
- wherein the total number of atoms separating the solid support from the toxin- binding oligosaccharide is at least 8.
A pharmaceutical composition useful for in vivo treatment of a toxin-mediated disease in a mammal, which composition comprises a pharmaceutically acceptable carrier suitable for oral administration and a solid support matrix of the formula:
- ##STR9## wherein SS is a solid support;
- R.sup.1 is selected from the group consisting of a covalent bond and a hydrocarbylene group having from I to about 20 carbon atoms;
- R.sup.2 is a hydrocarbylene group of from 2 to 20 carbon atoms;
- each X' is independently selected from the group consisting of --O-- and>NR.sup.4 wherein each R.sup.4 is independently selected from hydrogen, R.sup.2 NH.sub.2 or R.sup.2 NR.sup.3 Z wherein R.sup.2 is as defined above;
- R.sup.3 is selected from the group consisting of hydrogen and --C(O)R.sup.5 wherein R.sup.5 is selected from the group consisting of hydrogen and hydrocarbyl of from 1 to 20 carbon atoms;
- W is selected from oxygen or sulfur;
- X is selected from the group consisting of --NH--, --O-- and --S--;
- Y is selected from the group consisting of --NH--, --O-- and --S--;
- Z is toxin-binding oligosaccharide;
- p is an integer from 0 to 50;
- and
- n is an integer such that the matrix has a loading level of the toxin-binding oligosaccharide of from about 0.001 to about 2000 .mu.moles per gram of solid support
- wherein the total number of atoms separating the solid support from the toxin-binding oligosaccharide is at least 8
- wherein the matrix is capable of being eliminated from the gastrointestinal tract.
A pharmaceutical composition useful for in vivo treatment of a toxin-mediated disease in a mammal, which composition comprises a pharmaceutically acceptable carrier suitable for oral administration and a solid support matrix of the formula ##STR10## wherein SS is a solid support;
- R.sup.1 is selected from the group consisting of a covalent bond and a hydrocarbylene group having from 1 to about 20 carbon atoms;
- R.sup.3 is selected from the group consisting of hydrogen and --C(O)R.sup.5 wherein R.sup.5 is selected from the group consisting of hydrogen and hydrocarbyl of from 1 to 20 carbon atoms;
- R.sup.6 is an alkylene group of from 4 to 10 carbon atoms.
- Z is toxin-binding oligosaccharide, and
- n is an integer such that the matrix has a loading level of the toxin-binding oligosaccharide of from about 0,001 to about 2000 .mu.moles per gram of solid support
- wherein the total number of atoms separating the solid support from the toxin-binding oligosaccharide is at least 8
- wherein the matrix is capable of being eliminated from the gastrointestinal tract.
Dependencies are inferred from the claim text.