N-acylpeptide derivatives and their uses
OwnerRuey J. Yu, Eugene J. Van Scottinventors
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Abstract
N-acylpeptide derivatives are described. Compositions comprising N-acylpeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with tumors or cancers, immune, nervous, vascular, musculoskeletal, cutaneous system, or other tissues or systems in a subject.
Claims33
A peptide derivative having the following generic Formula (I):
- R1-AAB-(AAA)n-AAC-R2 Formula (I)
- or an isomer, free acid, base, salt, lactone, amide, hydroxylamide, hydrazide, or ester thereof, wherein R1 is an acyl radical having up to 19 carbon atoms;
- AAB is an amino-terminal amino acid residue;
- (AAA)n is a peptide having n amino acid residues, each of the amino acid residues is independently selected from any amino acid;
- n is an integer from 3-18;
- AAC is a carboxyl-terminal amino acid residue;
- R2 is OR3, NHR4 or NHNHR5;
- R3 is H, an alkyl, aralkyl or aryl radical having up to 19 carbon atoms;
- R4 or R5 is independently H, OH, an alkyl, aralkyl, aryl or acyl radical having up to 19 carbon atoms;
- a side chain of each of the AAB, AAA and AAC optionally and independently has an extra functional radical selected from the group consisting of OH, SH, NHCONH2, NHC(═NH)NH2, NH2, COOH, CONH2, imidazolyl, pyrrolidinyl, and indolyl;
- and the H or OH of the extra functional radical is optionally substituted by NH2, an acyl, alkyl, aralkyl, or aryl radical having up to 19 carbon atoms.
A composition for topical or systemic administration to a mammal comprising a pharmaceutically or cosmetically acceptable carrier and a therapeutically effective amount of a peptide derivative having the following generic Formula (I):
- R1-AAB-(AAA)n-AAC-R2 Formula (I)
- or an isomer, free acid, base, salt, lactone, amide, hydroxylamide, hydrazide, or ester thereof, wherein R1 is an acyl radical having up to 19 carbon atoms;
- AAB is an amino-terminal amino acid residue;
- (AAA)n is a peptide having n amino acid residues, each of the amino acid residues is independently selected from any amino acid;
- n is an integer from 1-18;
- AAC is a carboxyl-terminal amino acid residue;
- R2 is OR3, NHR4 or NHNHR5;
- R3 is H, an alkyl, aralkyl or aryl radical having up to 19 carbon atoms;
- R4 or R5 is independently H, OH, an alkyl, aralkyl, aryl or acyl radical having up to 19 carbon atoms;
- a side chain of each of the AAB, AAA and AAC optionally and independently has an extra functional radical selected from the group consisting of OH, SH, NHCONH2, NHC(═NH)NH2, NH2, COOH, CONH2, imidazolyl, pyrrolidinyl, and indolyl;
- and the H or OH of the extra functional radical is optionally substituted by NH2, an acyl, alkyl, aralkyl, or aryl radical having up to 19 carbon atoms.
A method of treating a disorder, disease, symptom or syndrome associated with a tumor, cancer, immune, nervous, vascular, musculoskeletal or cutaneous system, or other tissues or systems in a subject, comprising systemically or topically administering to the subject a composition comprising a pharmaceutically or cosmetically acceptable carrier and a therapeutically effective amount of a peptide derivative having the following generic Formula (I):
- R1-AAB-(AAA)n-AAC-R2 Formula (I)
- or an isomer, free acid, base, salt, lactone, amide, hydroxylamide, hydrazide, or ester thereof, wherein R1 is an acyl radical having up to 19 carbon atoms;
- AAB is an amino-terminal amino acid residue;
- (AAA)n is a peptide having n amino acid residues, each of the amino acid residues is independently selected from any amino acid;
- n is an integer from 1-18;
- AAC is a carboxyl-terminal amino acid residue;
- R2 is OR3, NHR4 or NHNHR5;
- R3 is H, an alkyl, aralkyl or aryl radical having up to 19 carbon atoms;
- R4 or R5 is independently H, OH, an alkyl, aralkyl, aryl or acyl radical having up to 19 carbon atoms;
- a side chain of each of the AAB, AAA and AAC optionally and independently has an extra functional radical selected from the group consisting of OH, SH, NHCONH2, NHC(═NH)NH2, NH2, COOH, CONH2, imidazolyl, pyrrolidinyl, and indolyl;
- and the H or OH of the extra functional radical is optionally substituted by NH2, an acyl, alkyl, aralkyl, or aryl radical having up to 19 carbon atoms.
Dependencies are inferred from the claim text.