| 摘要 |
The invention features linear therapeutic peptides of the following formula: <IMAGE> in which A1 is a D- alpha -aromatic amino acid or a D- alpha -tethered amino acid; A2 is Gln, His, 1-methyl-His, or 3-methyl-His; A3 is the D- or L-isomer selected from Nal, Trp, Phe, and p-X-Phe, where X is F, Cl, Br, NO2, OH or CH3; A4 is Ala, Val, Leu, Ile, Nle, or alpha -aminobutyric acid; A5 is Val, Ala, Leu, Ile, Nle, Thr, or alpha -aminobutyric acid; A6 is Gly, Sar, beta -Ala, or the D-isomer selected from Ala, N-methyl-Ala, Trp, and Nal; A7 is His, 1-methyl-His, 3-methyl-His, Lys, or epsilon -alkyl-Lys; A8 is Leu, Ile, Val, Nle, alpha -aminobutyric acid, Trp, Pro, Nal, Chx-Ala, Phe, or p-X-Phe, where X is F, Cl, Br, NO2, OH or CH3; A9 is Met, Met-oxide, Leu, Ile, Nle, alpha -aminobutyric acid, or Cys; each R1 and R2, independently, is H, C1-12 alkyl, C7-10 phenylalkyl, or COE1, where E1 is C1-20 alkyl, C3-20 alkenyl, C3-20 alkynyl, phenyl, 3,4-dihydroxyphenylalkyl, naphthyl, or C7-10 phenylalkyl; provided that when either R1 or R2 is COE1, the other must be H; and R3 is OH, NH2, C1-12 alkoxy, C7-10 phenylalkoxy, C11-20 naphthylalkoxy, C1-12 alkylamino, C7-10 phenylalkylamino, C11-20 naphthylalkylamino; or a pharmaceutically acceptable salt of such peptides.
|
