Patent ID: 7842662

Claim:
A synthetic peptide amide dimer having the formula: or a stereoisomer, mixture of stereoisomers, pharmaceutically acceptable salt, hydrate, acid salt hydrate, or N-oxide thereof, wherein each Xaa 1 is independently selected from the group consisting of (A)(A′)D-Phe, (A)(A′)(α-Me)D-Phe, D-Tyr, D-Tic, D-tert-leucine, D-neopentylglycine, D-phenylglycine, D-homophenylalanine, and β-(E)D-Ala, wherein each (A) and each (A′) are phenyl ring substituents independently selected from the group consisting of —H, —F, —Cl, —NO 2 , —CH 3 , —CF 3 , —CN, —CONH 2 , and wherein each (E) is independently selected from the group consisting of cyclobutyl, cyclopentyl, cyclohexyl, pyridyl, thienyl and thiazolyl; each Xaa 2 is independently selected from the group consisting of (A)(A′)D-Phe, (A)(A′)(α-Me)D-Phe, D-1NaI, D-2NaI, D-Tyr, (E)D-Ala, and D-Trp; each Xaa 3 is independently selected from the group consisting of D-Nle, D-Phe, (E)D-Ala, D-Leu, (α-Me)D-Leu, D-Hle, D-Val, and D-Met; each Xaa 4 is independently selected from the group consisting of (B) 2 D-Arg, (B) 2 D-Nar, (B) 2 D-Har, ζ-Dap, ε-(B)D-Lys, ε-(B) 2 -D-Lys, D-Amf, amidino-D-Amf, γ-(B) 2 D-Dbu, δ-(B) 2 α-(B′)D-Orn, D-2-amino-3(4-piperidyl)propionic acid, D-2-amino-3(2-aminopyrrolidyl)propionic acid, D-α-amino-β-amidino-propionic acid, α-amino-4-piperidineacetic acid, cis-α,4-diaminocyclohexane acetic acid, trans-α,4-diaminocyclohexaneacetic acid, cis-α-amino-4-methyl-aminocyclo-hexane acetic acid, trans-α-amino-4-methylaminocyclohexane acetic acid, α-amino-1-amidino-4-piperidineacetic acid, cis-α-amino-4-guanidino-cyclohexane acetic acid, and trans-α-amino-4-guanidinocyclohexane acetic acid, wherein each (B) is independently selected from the group consisting of —H and C 1 -C 4 alkyl, and (B′) is —H or (α-Me), and p is zero or 1; q is zero or 1; r is zero or 1; s is zero or 1; p and t are each independently zero or 1, provided that at least one of q, r, s and t is 1; and wherein either A. (i) L is a linker selected from the group consisting of ε-D-Lys, ε-Lys, δ-D-Orn, δ-Orn, γ-aminobutyric acid, 8-aminooctanoic acid, 11-amino-undecanoic acid, 8-amino-3,6-dioxaoctanoic acid, 4-amino-4-carboxylic piperidine, and (D-Lys-Gly lactam) 2 , and (ii) the moieties Xaa 1 -Xaa 2 -Xaa 3 -(Xaa 4 ) p and (Xaa 1 ) q -(Xaa 1 ) r -(Xaa 3 ) s -(Xaa 4 ) t are different from one another; or B. L is a linker selected from the group consisting of γ-aminobutyric acid, 8-aminooctanoic acid, 11-amino-undecanoic acid, 8-amino-3,6-dioxaoctanoic acid, 4-amino-4-carboxylic piperidine, and (D-Lys-Gly lactam) 2 .