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US 8,476,404 B1Granted
Selectively functionalized polyhydric compounds
OwnerBhalchandra Shripad Leleinventor
Life of this patent
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Abstract
This invention relates to polyhydric compounds containing primary and secondary hydroxyl groups selectively conjugated with linkers, polymers, and/or bioactive agents.
Claims3
Conjugates of water soluble polymers with compounds of formula (I) wherein water soluble polymers are covalently attached via linker L1 or L2
- n(L1-O—CH2—)—R—(—CH—O-L2)m (I)
- wherein R is hydrocarbon in polyhydric alcohols containing at least one primary hydroxyl group and at least one secondary hydroxyl group selected from group of alcohols comprising
- 1,2,6-hexanetriol, 1,2,4-butanetriol, glycerol, triglycerol, tetraglycerol, pentaglycerol, hexaglycerol, polyglycerol, 2,2,6,6-tetrakis(hydroxymethyl)cyclohexanol, 3-Bromo-1,2-propanediol, 3-Chloro-1,2-propanediol, 1,3-butanediol, 1,2-butanediol, 2-hydroxymethyl-1,3-propanediol, DL-threitol, 1,2-pentanediol, 1,4-pentanediol, 3-Methyl-1,3-butanediol, 1,2-hexanediol, 1,5-hexanediol, 1,2,6-hexanetriol, α,α′-diglycerol, 3-tert-butoxy-1,2-propanediol, 1-phenyl-1,2-ethanediol, 1-phenyl-1,2-ethanediol, 1,2-octanediol, 2-ethyl-1,3-hexanediol, 1,2,7,8-octanetetrol, 1-(4-nitrophenoxy)-2,3-propanediol, 4-hydroxy-3-methoxyphenylglycol, 3-benzyloxy-1,2-propanediol, mephenesin, 1,2-dodecanediol, 1,2-hexadecanediol, 1-O-palmityl-glycerol, batyl alcohol and the likes;
- L1 and L2 are linkers conjugated to hydroxyl groups in polyhydric alcohols and capable of undergoing further conjugation selected from group of linkers comprising
- N-hydroxysuccininimidyl esters, maleimidoalkanoic acids, succinic acid, succinic anhydride, p-nitrophenylchloroformate, formyl benzoic acid, isocyanates, diisocyanates, isothiocyanates, diisothiocyantes, aminoalkanoic acids, thioalkanoic acids, acetals, ketals, sulfones acrylates, methacrylates, alkyl chlorides, acyl chlorides, aldehydes and the likes
- and n and m are integers from 1 to 12.
3 more elements
Dependencies are inferred from the claim text.