Therapeutic decapeptides

Abstract

Abstract A decapeptide of the formula: N-Ac-A 1 -A 2 -A 3 -Ser-A 4 -A 5 -A 6 -A 7 -A 8 -A 9 , wherein each A 1 , A 2 , and A 3 , independently, is D-β-Nal, D-p-X-Phe (where X is halogen, H, NH 2 , NO 2 , OH, or C 1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A 4 is p-X-Phe (where X is halogen, H, NH 2 , NO 2 , or C 1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A 5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-β-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH 2 , NO 2 , or C 1-3 alkyl), or D-Lys-ε-NH-R (where R is H, a branched or straight chain C 1 -C 10 alkyl group, or an aryl group); A 6 is Leu, β-Nal, p-X-Phe (where X is halogen, H, NH 2 , NO 2 , OH, C 2 F 5 , C 1-3 alkyl), or Trp; A 7 is Arg, Lys, or Lys ε-NH-R (where R is H, a branched or straight chain C 1 -C 6 alkyl group, or an aryl group); A 8 is Pro; and A 9 is D-Ala, D-Ala-NH 2 , Ala-NH 2 , aminoisobutyric acid amide, or Gly-NH 2 ; provided that at least one of A 2 or A 3 must be D-Phe or D-Tyr, and provided further that when A 4 is Lys or Arg, A 5 must not be D-Arg, D-Lys, D-homo-Arg, D-diethyl-homo-Arg, or D-Lys-ε-NH-R, or a pharmaceutically acceptable salt thereof. The invention also features a method of treating T-cell-deficient patients, e.g., those suffering from Acquired Immune Deficiency Syndrome, by administering a therapeutically effective amount of an LH-RH antagonist.

Inventors

• 👤 David H. Coy
• 👤 Jacques-Pierre Moreau

Bibliographic Details