Modified amino acids and compositions comprising the same for delivering active agents
First Claim
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1. A compound selected from the group consisting of ##STR11## and salts thereof.
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Abstract
The present invention provides modified amino acids for delivering active agents, and particularly biologically or chemically active agents. The preferred modified amino acids of the present invention include N-acylated or sulfonated amino acids. These modified amino acids are used as carriers to facilitate the delivery of a cargo to a target. Such modified amino acids are well suited to form non-covalent mixtures with biologically-active agents for oral administration to animals. Methods for the preparation and administration of the modified amino acids and compositions including the same are also provided.
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30 Claims
- 1. A compound selected from the group consisting of ##STR11## and salts thereof.
- 2. A poly amino acid comprising at least one residue derived from at least one compound selected from the group consisting of ##STR12## and salts thereof.
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4. A composition comprising
(a) an active agent; - and
(b) a compound selected from the group consisting of ##STR13## and salts thereof. - View Dependent Claims (7, 8, 9, 16, 22)
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5. A composition comprising
(a) an active agent; - and
(b) a poly amino acid comprising at least one residue derived from an amino acid selected from the group consisting of ##STR14## and salts thereof. - View Dependent Claims (6, 10, 11, 12, 13, 14, 15, 18, 19, 20, 21, 23, 24)
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28. A method for preparing a compound having the formula ##STR15## wherein Y is ##STR16## R1 is C3 -C24 alkyl, C2 -C20 alkenyl, C2 -C20 alkyne, cycloalkyl, or aromatic;
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R2 is hydrogen, C1 -C4 alkyl, or C2 -C4 alkenyl; and R3 is C1 -C7 alkyl, C3 -C10 cycloalkyl, aryl, thienyl, pyrrolo, or pyridyl, where R3 is optionally substituted by one or more C1 -C5 alkyl group, C2 -C4 alkenyl group, F, Cl, OH, SO2, COOH and SO3 H;
said method comprising(a) reacting in water and the presence of a base, a compound having the formula ##STR17## with a compound having the formula
space="preserve" listing-type="equation">R.sup.3 --Y--X,wherein Y, R1, R2, and R3 are as above and X is a leaving group.
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29. A composition for oral delivery of a biologically active agent, said composition comprising
(a) a biologically active agent; - and
(b) an oral delivery effective amount of at least one compound selected from the group consisting of ##STR18## a poly amino acid derived from at least one compound selected from the group consisting of compounds V, XXXI, and XXXIII, and salts thereof, wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid. - View Dependent Claims (30)
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Specification