Monovalent and polyvalent synthetic polysaccharide antigens for immunological intervention in disease

A synthetic polysaccharide antigen, wherein the SPA is a polymer comprising the sequence:

• X1—[-MO—]W—X2
• wherein
• X1 and X2 are independently H or a terminator;
• W represents the number of monomeric units (MO) in the polymer, and may be an integer in the range of from about 2 to about 375;
• each MO is a monomeric unit selected from the group comprising unsubstituted repeat units (UR), one or more than one species of Th epitope repeat units (ThR), one or more than one species of target epitope repeat units (TR), one or more than one species of combined Th/target epitope repeat unit (Th/TR), and a combination thereof,
• or a pharmaceutically acceptable salt thereof.

A pro-inflammatory synthetic polysaccharide antigen (SPA) comprising from about 10 to about 375 monomeric units, the monomeric units independantly selected from

• and pharmaceutically acceptable salts thereof,
• wherein
• R are independently selected from H or lower allyl;
• STEM PEPTIDE are independantly selected, and comprise about 2 to about 5 amino acids, wherein the amino acids are independantly joined at the α or γ carboxyl groups, and at the α or ε amino groups, or any combination thereof, provided that a pendant carboxylate or carboxamide group is present;
• LINKER 1 and LINKER2 are independantly selected, and comprise about 1 to about 6 segments, each segment selected from —CH2—, —CHR—, ═CH—, and ≡CH—, —O—, —NH—, —NR—, —S—, —SO—, and —SO2—, provided that there are no contiguous heteroatom segments and that the heteroatom segments are not in segments 1 and 2, where R is a lower alkyl;
• SPACER1 is a peptide of about 1 to about 10 amino acids in length;
• SPACER2 is 0 to about 10 amino acids in length;
• (target epitope)n is a is a number n of different target epitopes, each target epitope is independantly selected and is peptide sequence or carbohydrate moiety that is an immunogen to CD8+ T cells or to B cells;
• and
• (Th epitope)n is a number n of different Th epitopes, each Th epitope is independantly selected and comprises a generic T helper epitope.

A pro-inflammatory synthetic polysaccharide antigen (SPA) comprising from about 10 to about 375 monomeric units, the monomeric units independantly selected from

• and pharmaceutically acceptable salts thereof,
• wherein
• R are independantly selected from H or lower alkyl;
• STEM PEPTIDE are independently selected, and comprise about 2 to about 5 amino acids, wherein the amino acids are independantly joined at the α or γ carboxyl groups, and at the α or ε amino groups, or any combination thereof, provided that a pendant carboxylate or carboxamide group is present;
• LINKER 1 and LINKER2 are independantly selected, and comprise about 1 to about 6 segments, each segment selected from —CH2—, —CHR—, ═CH—, and ≡CH—, —O—, —NH—, —NR—, —S—, —SO—, and —SO2—, provided that there are no contiguous heteroatom segments and that the heteroatom segments are not in segments 1 and 2, where R is a lower alkyl;
• SPACER1 is a peptide of about 1 to about 10 amino acids in length;
• SPACER2 is 0 to about 10 amino acids in length;
• (target epitope)n is a number n of different target epitopes, each target epitope is independantly selected and is peptide sequence or carbohydrate moiety that is an immunogen to CD8+ T cells or to B cells;
• and
• (Th epitope)n is a number n of different Th epitopes, each Th epitope is independantly selected and comprises a generic T helper epitope.

A suppressive synthetic polysaccharide antigen (SPA) comprising from about 10 to about 375 monomeric units, the monomeric units independantly selected from

• and pharmaceutically acceptable salts thereof,
• wherein
• R are independantly selected from H or lower alkyl;
• STEM PEPTIDE are independantly selected, and comprise about 2 to about 5 amino acids, wherein the amino acids are independantly joined at the α or γ carboxyl groups, and at the α or ε amino groups, or any combination thereof, provided there is no pendant carboxylate or carboxamide group;
• LINKER 1 and LINKER2 are independently selected, and comprise about 1 to about 6 segments, each segment selected from —CH2—, —CHR—, ═CH—, and ≡CH—, —O—, —NH—, —NR—, —S—, —SO—, and —SO2—, provided that there are no contiguous heteroatom segments and that the heteroatom segments are not in segments 1 and 2, where R is a lower alkyl;
• SPACER1 is a peptide of about 1 to about 10 amino acids in length;
• and
• (target epitope)n is a number n of different target epitopes, each target epitope is independantly selected and is peptide sequence or carbohydrate moiety.