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US 4,542,124 AGranted
Octapeptide vasopressin antagonists
AssigneeSmithKline Beckman Corporation
InventorsWilliam F. Huffman, Michael L. Moore
Life of this patent
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Abstract
Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general characterized by having an amino acid unit at position 4 which is other than valine. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-.alpha.-aminobutyric acid-8-arginine-9-desglycine]vasopressin.
Claims12
A polypeptide compound of the formula:
- ##STR34## in which:
- P is Phe or Phe(4'-Alk);
- X is D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Pba, D-Nle, D-Cha, D-Abu, D-Met, D-Chg, D-Tyr, L-Tyr, D-aIle, D-Tyr(alk) or L-Tyr(alk);
- Y is NH.sub.2, NHAlk, NHBzl or OH;
- A is Ile, Abu, Ala, Gly, Lys, Cha, Nle, Phe, Leu, Chg, Nva or, when n is 0 or 2 or W is D-Pro, Val;
- W is L-Pro, .DELTA.Pr or, when A is Val or is as defined above, D-Pro;
- Z is D-Arg, L-Arg, D-Lys or L-Lys;
- and
- n is 1 or, when A is Val or is as defined above, 0 or 2;
- or a pharmaceutically acceptable salt or prodrug derivative thereof.
7 more elements
Dependencies are inferred from the claim text.