Synthetic peptide amides

A synthetic peptide amide having the formula:

• or a pharmaceutically acceptable salt, hydrate, or acid salt hydrate thereof;
• wherein
• Xaa1 is (A)(A′)D-Phe, wherein each (A) and each (A′) are phenyl ring substituents independently selected from the group consisting of —H, —F, —Cl, —NO2, —CH3, —CF3, —CN, and —CONH2;
• Xaa2 is (A)(A′)D-Phe;
• Xaa3 is 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;
• Xaa4 is ε-(B)D-Lys, wherein each (B) is independently selected from the group consisting of H and C1-C4 alkyl;
• W is
• Null;
• the moiety
• is an optionally substituted 4 to 8-membered heterocyclic ring moiety wherein Y is N and Z is C;
• provided that when such ring moiety is a six, seven or eight-membered ring, such ring moiety is non-aromatic;
• V is C1-C6 alkyl, and e is zero or 1, wherein when e is zero, then V is null and R1 and R2 are directly bonded to the same or different ring atoms;
• wherein (i) R1 is selected from the group consisting of —H, —OH, halo, —CF3, —NH2, —COOH, C1-C6 alkyl, C1-C6 alkoxy, amidino, C1-C6 alkyl-substituted amidino, aryl, optionally substituted heterocyclyl, Pro-amide, Pro, Gly, Ala, Val, Leu, Ile, Lys, Arg, Orn, Ser, Thr, —CN, —CONH2, —COR′, —SO2R′, —CONR′R″, —NHCOR′, OR′ and SO2NR′R″;
• wherein said optionally substituted heterocyclyl is optionally singly or doubly substituted with substituents independently selected from the group consisting of C1-C6 alkyl, C1-C6 alkoxy, oxo, —OH, —Cl, —F, —NH2, —NO2, —CN, —COOH, and amidino;
• wherein R′ and R″ are each independently —H, C1-C8 alkyl, aryl, or heterocyclyl or R′ and R″ are combined to form a 4- to 8-membered ring, which ring is optionally singly or doubly substituted with substituents independently selected from the group consisting of C1-C6 alkyl, —C1-C6 alkoxy, —OH, —Cl, —F, —NH2, —NO2, —CN, —COOH and amidino;
• and R2 is selected from the group consisting of —H, amidino, singly or doubly C1-C6 alkyl-substituted amidino, —CN, —CONH2, —CONR′R″, —NHCOR′, —SO2NR′R″ and —COOH;
• or
• (ii) R1 and R2 taken together can form an optionally substituted 4- to 9-membered heterocyclic monocyclic or bicyclic ring moiety which is bonded to a single ring atom of the Y and Z-containing ring moiety;
• or
• (iii) R1 and R2 taken together with a single ring atom of the Y and Z-containing ring moiety can form an optionally substituted 4- to 8-membered heterocyclic ring moiety to form a spiro structure;
• or
• (iv) R1 and R2 taken together with two or more adjacent ring atoms of the Y and Z-containing ring moiety can form an optionally substituted 4- to 9-membered heterocyclic monocyclic or bicyclic ring moiety fused to the Y and Z-containing ring moiety;
• wherein each of said optionally substituted 4-, 5-, 6,-, 7-, 8- and 9-membered heterocyclic ring moieties comprising R1 and R2 is optionally singly or doubly substituted with substituents independently selected from the group consisting of C1-C6 alkyl, C1-C6 alkoxy, optionally substituted phenyl, oxo, —OH, —Cl, —F, —NH2, —NO2, —CN, —COOH, and amidino;
• provided that when the Y and Z-containing ring moiety is a six or seven membered ring and e is zero, then R1 is not —OH, and R1 and R2 are not both —H.