C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/31 (2006.01) A61K 38/16 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2331888
The present invention provides a cyclic peptide comprising structure (I) wherein X is selected from the group consisting of an amino acid, an amino acid analog, a peptidomimetic and a non-amide isostere, Z is selected from the group consisting of a synthetic amino acid and a biosynthetic amino acid, R is selected from the group consisting of oxygen, nitrogen and carbon, n is 0 to 10 and y is 1 to 10. The present invention also provides a cyclic peptide comprising the amino acid sequence of NH2-X(n)-Z-X(y)-COOH and a cyclic bond between the Z residue and COOH other than a thioester bond, wherein X is selected from the group consisting of an amino acid, an amino acid analog, a peptidomimetic and a non-amide isostere, Z is selected from the group consisting of a synthetic amino acid and a biosynthetic amino acid, n is 0 to 10 and y is 1 to 10. Methods of preparation including a cyclization protocol, and methods of use of the cyclic peptides of the invention are also disclosed.
L'invention porte sur un peptide cyclique de structure (I) dans laquelle X est choisi parmi un acide aminé, un analogue d'acide aminé, un peptidomimétique, et un isostère non amidique, Z est choisi parmi un acide aminé de synthèse et un acide aminé de biosynthèse, R est choisi parmi O, N, et C, n étant 0 à 10, et y étant 0 à 10. L'invention porte également sur un peptide cyclique comportant la séquence d'acides aminés NH¿2?-X¿(n)?-Z-X¿(y)?-COOH et une liaison cyclique entre le résidu Z et COOH autre qu'une liaison thioester, X étant choisi parmi un acide aminé, un analogue d'acide aminé, un peptidomimétique, et un isostère non amidique, Z étant choisi parmi un acide aminé de synthèse et un acide aminé de biosynthèse, et n étant 0 à 10 et y étant 0 à 10. L'invention porte également sur leurs procédés de préparation comportant un protocole de cyclisation et sur les méthodes d'utilisation desdits peptides cycliques.
Beavis Ronald
Ji Guangyong
Mayville Patricia
Muir Tom W.
Novick Richard P.
New York University
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
The Rockefeller University
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