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US 7,351,855 B2Granted
Chemically defined non-polymeric valency platform molecules and conjugates thereof
AssigneeLa Jolla Pharmaceutical Company
InventorsStephen M. Coutts, David S. Jones, Douglas Alan Livingston, Lin Yu
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Abstract
Chemically-defined, non-polymeric valency platform molecules and conjugates comprising chemically-defined valency platform molecules and biological or chemical molecules including polynucleotide duplexes of at least 20 base pairs that have significant binding activity for human lupus anti-dsDNA autoantibodies.
Claims143
A conjugate formable by the conjugation of at least one biologically active molecule and a valency platform having the formula:
- Q1-(CH2CH2O)nCH2CH2-Q1
- wherein each Q1 is a chemical moiety independently selected from the group consisting of:
- wherein each Q2 is a chemical moiety of the formula:
- wherein each Q3 is a chemical moiety independently selected from the group consisting of:
- wherein each T is a chemical moiety independently selected from the group consisting of:
- wherein:
- n is an integer from 0 to 300;
- m is in integer from 1 to 10;
- p is independently selected from an integer from 1 to 10;
- each X is independently a halogen of atomic number greater than 16 and less than 54 or other good leaving group;
- each RALK is independently a linear, branched, or cyclic alkyl group of 1 to 20 carbon atoms;
- each RSUB is independently H, a linear, branched, or cyclic alkyl group of 1 to 20 carbon atoms, an aryl group of 6 to 20 carbon atoms, or an alkaryl group of 7 to 30 carbon atoms;
- each RESTER is independently N-succinimidyl, p-nitrophenyl, pentafluorophenyl, tetrafluorophenyl, tetrachlorophenyl, 2,4,5-trichlorophenyl, 2,4-dinitrophenyl, cyanomethyl, or other activating group;
- and
- each RB is independently a chemical moiety comprising 1 to 50 atoms selected from the group consisting of C, H, N, O, Si, P, and S;
- and
- the conjugate optionally comprises a linker moiety linking the biologically active molecule to the valency platform molecule.
14 more elements
A valency platform molecule of the formula:
- Q1-(CH2CH2O)nCH2CH2-Q1
- wherein each Q1 is a chemical moiety independently selected from the group consisting of:
- wherein each Q3 is a chemical moiety independently selected from the group consisting of:
- wherein each T is a chemical moiety independently selected from the group consisting of:
- wherein:
- n is an integer from 0 to 300;
- m is in integer from 1 to 10;
- p is independently selected from an integer from 1 to 10;
- each X is independently a halogen of atomic number greater than 16 and less than 54 or other good leaving group;
- each RALK is independently a linear, branched, or cyclic alkyl group of 1 to 20 carbon atoms;
- each RSUB is independently H, a linear, branched, or cyclic alkyl group of 1 to 20 carbon atoms, an aryl group of 6 to 20 carbon atoms, or an alkaryl group of 7 to 30 carbon atoms;
- each RESTER is independently N-succinimidyl, p-nitrophenyl, pentafluorophenyl, tetrafluorophenyl, tetrachlorophenyl, 2,4,5-trichlorophenyl, 2,4-dinitrophenyl, cyanomethyl, or other activating group;
- and
- each R8 is independently a chemical moiety comprising 1 to 50 atoms selected from the group consisting of C, H, N, O, Si, P, and S.
11 more elements
Dependencies are inferred from the claim text.