Modified amino acids for drug delivery
First Claim
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1. A composition comprising:
- (A) at least one biologically active agent, and(B) (a) at least one acylated amino acid;
(b) at least one peptide comprising at least one acylated amino acid;
or (c) a combination of (a) and (b);
wherein said acylated amino acid is acylated by(i) a C3 -C10 cycloalkyl acylating agent, substituted with C1 -C7 alkyl, C2 -C7 alkenyl, C1 -C7 alkoxy, hydroxy, phenyl, phenoxy, or --CO2 R, wherein R is hydrogen, C1 -C4 alkyl or C2 -C4 alkenyl;
(ii) an unsubstituted C3 -C10 cycloalkyl;
or(iii) a C1 -C6 alkyl acylating agent substituted with C3 -C10 cycloalkyl.
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Abstract
Compositions are provided which include (A) at least one biologically active agent, and (B) (a) at least one acylated amino acid; (b) at least one peptide comprising at least one acylated amino acid; or (c) a combination of (a) and (b); wherein said acylated amino acid is acylated by (I) a C3 -C10 cycloalkyl acylating agent substituted with C1 -C7 alkyl, C2 -C7 alkenyl, C1 -C7 alkoxy, hydroxy, phenyl, phenoxy, or --CO2 R, wherein R is hydrogen, C1 -C4 alkyl or C2 -C4 alkenyl; (ii) an unsubstituted C3 -C10 cycloalkyl acylating agent; or (iii) a C1 -C6 alkyl acylating agent substituted with C3 -C10 cycloalkyl.
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Citations
29 Claims
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1. A composition comprising:
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(A) at least one biologically active agent, and (B) (a) at least one acylated amino acid; (b) at least one peptide comprising at least one acylated amino acid;
or(c) a combination of (a) and (b); wherein said acylated amino acid is acylated by (i) a C3 -C10 cycloalkyl acylating agent, substituted with C1 -C7 alkyl, C2 -C7 alkenyl, C1 -C7 alkoxy, hydroxy, phenyl, phenoxy, or --CO2 R, wherein R is hydrogen, C1 -C4 alkyl or C2 -C4 alkenyl; (ii) an unsubstituted C3 -C10 cycloalkyl;
or(iii) a C1 -C6 alkyl acylating agent substituted with C3 -C10 cycloalkyl. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)
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27. A method for preparing a composition, said method comprising mixing:
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(A) at least one biologically-active agent; (B) (a) at least one acylated amino acid; (b) at least one peptide comprising at least one acylated amino acid;
or(c) a combination of (a) and (b); wherein said acylated amino acid is acylated by (i) a C3 -C10 cycloalkyl acylating agent substituted with C1 -C7 alkyl, C2 -C7 alkenyl, C1 -C7 alkoxy, hydroxy, phenyl, phenoxy, or --CO2 R, wherein R is hydrogen, C1 -C4 alkyl or C2 -C4 alkenyl; (ii) an unsubsituted C3 -C10 cyckloalkyl acylating agent;
or(iii) a C1 -C6 alkyl acylating agent substituted with C10 -C cycloalkyl; and (C) optionally a dosing vehicle. - View Dependent Claims (28, 29)
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Specification