Bombesin analogs

Details Bombesin analogs Bombesin analogs

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01)

Patent

CA 2144264

The invention features linear therapeutic peptides of the following formula: R1 A1-A-A3-A4-A5-A6-A7-A8-A9-R3, R2 in which A1 is a D-.alpha.-aromatic amino acid or a D-.alpha.- tethered amino acid; A 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 .beta.-Ala; 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-l0 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.

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